- Simultaneous targeting of NQO1 and SOD1 eradicates breast cancer stem cells via mitochondrial futile redox cyclin
Luo M, Shen N, Shang L, Fang Z, Xin Y, Ma Y, Du M, Yuan Y, Hu C, Tang Y, Huang J, Wei W, Lee MR, Hergenrother PJ, Wicha MS
Cancer Res. 2024 published on web September 12, 2024
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- Raptinal: a powerful tool for rapid induction of apoptotic cell death
Smith AJ and Hergenrother PJ
Cell Death Discov. 2024, 10, 371
- Capturing cell morphology dynamics with high temporal resolution using single-shot quantitative phase gradient imaging
Hur SW, Kwon M, Manoharaan R, Mohammadi MH, Samuel A, Mulligan MP, Hergenrother PJ, Bhargava R
J. Biomed. Optics 2024, 29, S22712
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- Development of NR0B2 as a therapeutic target for the re-education of tumor associated myeloid cells
Gamage HEV, Albright ST, Smith AJ, Farmer R, Shahoei SH, Wang Y, Fink EC, Jacquin E, Weisser E, Bautista RO, Henn MA, Schane CP, Nelczyk AT, Ma L, Gupta AD, Bendre SV, Nguyen T, Tiwari S, Krawczynska N, He S, Tjoanda E, Chen H, Sverdlov M, Gann PH, Boidot R, Vegran F, Fanning SW, Apet L, Hergenrother PJ, Nelson ER
Cancer Letters 2024, 597, 217086.
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- NR0B2 re-educates myeloid immune cells to reduce regulatory T cell expansion and progression of breast and other solid tumors
Gamage HEV, Shahoei SH, Wang Y, Jacquin E, Weisser E, Bautista RO, Henn MA, Schane CP, Nelczyk A, Ma L, Das Gupta A, Bendre SV, Nguyen T, Tiwari S, Tjoanda E, Krawczynska N, He S, Albright ST, Farmer R, Smith AJ, Fink EC, Chen H, Sverdlov M, Gann PH, Boidot R, Vegran F, Fanning SW, Hergenrother PJ, Apetoh L, Nelson ER
Cancer Letters 2024, 597, 217042.
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- Structures of the Staphylococcus aureus ribosome inhibited by fusidic acid and fusidic acid cyclopentane
Gonzalez-Lopez A, Larsson DSD, Koripella RK, Cain BN, Sanyal S, Chavez MG, Hergenrother PJ, Sanyal S, Selmer M
Sci. Rep. 2024, 14, 14253
- A Gram-negative-selective antibiotic that spares the gut microbiome
Muñoz KA, Ulrich RJ, Vasan AK, Sinclair M, Wen P-C, Holmes JR, Lee HY, Hung C-C, Fields CJ, Tajkhorshid E, Lau GW, Hergenrother PJ
Nature 2024, 630, 429-436
- Precise readout of MEK1 proteoforms upon MAPK pathway modulation by individual ion mass spectrometry
Drown BS, Gupta R, McGee JP, Hollas MAR, Hergenrother PJ, Kafader JO, Kelleher NL
Anal. Chem. 2024, 96, 4455−4462
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- Using permeation guidelines to design new antibiotics – a PASsagE into Pseudomonas aeruginosa
Cain BN and Hergenrother PJ
Clin. Transl. Med. 2024, 4, e1600
- A catalytic process enables efficient and programmable access to precisely altered indole alkaloid scaffolds
Huang Y, Li X, Mai BK, Tonogai EJ, Smith AJ, Hergenrother PJ, Liu P, Hoveyda, AH
Nature Chem. 2024, 16, 1003-1014
- New antibiotic targets a drug-resistant bacterium
Gugger MK and Hergenrother PJ
Nature 2024, 625, 451-452 (News & Views)
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- Discovery of KRB-456, a KRAS G12D switch-I/II allosteric pocket binder that inhibits the growth of pancreatic cancer patient-derived tumors
Kazi A, Ranjan A, Kumar MVV, Agianian B, Chavez MG, Vudatha V, Wang, R, Vangipurapu R, Chen L, Kennedy P, Subramanian K, Quirke JCK, Beato F, Underwood P, Fleming JB, Trevino J, Hergenrother PJ, Gavathiotis E, Sebti S
Cancer Res. Comm. 2023, 3, 2623-2639
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- Augmented concentration of isopentyl-deoxynyboquinone in tumors selectively kills NAD(P)H quinone oxidoreductase 1-positive cancer cells through programmed necrotic and apoptotic mechanisms
Wang J, Su X, Jiang L, Boudreau MW, Chatkewitz LE, Kilgore JA, Zahid KR, Williams NS, Chen Y, Liu S, Hergenrother PJ, Huang X
Cancers 2023, 15, 5844
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- Porin-independent accumulation in Pseudomonas enables antibiotic discovery
Geddes EJ, Gugger MK, Garcia A, Chavez MG, Lee MR, Perlmutter SJ, Bieniossek C, Guasch L, Hergenrother PJ
Nature 2023, 624, 145-153
- IP-DNQ induces mitochondrial dysfunction and G2/M phase cell cycle arrest to selectively kill NQO1-positive pancreatic cancer cells
Jiang L, Liu Y, Tumbath S, Boudreau MW, Chatkewitz LE, Wang J, Su X, Rafiq, Zahid K, Li K, Chen Y, Yang K, Hergenrother PJ, Huang X
Antioxid. Redox Signal. 2024, 41, 74-92.
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- The combination of PAC-1 and entrectinib for the treatment of metastatic uveal melanoma
Boudreau MW, Tonogai EJ, Schane CP, Xi MX, Fischer JH, Vijayakumar J, Ji Y, Tarasow TM, Fan TM, Hergenrother PJ, Dudek AZ
Melanoma Res. 2023, 33, 514-524
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- Phase 1 dose escalation study of procaspase activating compound-1 (PAC-1) in combination with temozolomide in patients with recurrent high-grade astrocytomas
Holdhoff M, Nicholas KM, Peterson RA, Maraka S, Liu LC, Fischer JH, Wefel JS, Fan TM, Vannorsdall T, Russell M, Iacoboni M, Tarasow TM, Hergenrother PJ, Dudek AZ, Danciu OC
Neuro-Oncol. Adv. 2023, 5, vdad087
- Plasma Membrane Channel TRPM4 Mediates Immunogenic Therapy-Induced Necrosis
Ghosh S, Yang R, Duraki D, Zhu J, Kim JE, Jabeen M, Mao C, Dai X, Livezey MR, Boudreau MW, Park BH, Nelson ER, Hergenrother PJ, Shapiro DJ
Cancer Res. 2023, 83, 3115-3130
- A single CAR T cell treatment controls disseminated ovarian cancer in a syngeneic mouse model
Ranoa DRE, Sharma P, Shane CP, Lewis AN, Valdez E, Marada VVVR, Hager MV, Montgomery W, Wolf SP, Schreiber K, Schreiber H, Bailey K, Fan TM, Hergenrother PJ, Roy EJ, Kranz DM
J. Immunother. Cancer 2023, 11, e006509
- A fluorescence polarization assay for macrodomains facilitates the identification of potent inhibitors of SARS-CoV-2 macrodomain
Anmangandla A, Jana S, Peng K, Wallace SD, Bagde SR, Drown BS, Hergenrother PJ, Fromme JC, Lin H
ACS Chem. Biol. 2023, 18, 1200-1207
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- Phase 1 study of procaspase activating compound-1 (PAC-1) in the treatment of advanced malignancies
Danciu OC, Holdhoff M, Peterson RA, Fisher JH, Liu LC, Wang H, Venepalli NK, Chowdhery R, Nicholas MK, Russell MJ, Fan TM, Hergenrother PJ, Tarasow TM, Dudek AZ
Brit. J. Cancer 2023, 128, 783
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UIUC press release
- Computational discovery of dynobactin antibiotics
Munoz KA and Hergenrother PJ
Nature Microbiology 2022, 7, 1512-1513 (News and Views).
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- An iterative approach guides discovery of the FabI inhibitor fabimycin, a late-stage antibiotic candidate with in vivo efficacy against drug-resistant gram-negative infections
†Parker EN, †Cain BN, Hajian B, Ulrich RJ, Geddes EJ, Barkho S, Lee HY, Williams JD, Rynor M, Caridha D, Zaino A, Rodhe JM, Zak M, Shekhar M, Muñoz KA, Rzasa KM, Temple ER, Hunt D, Jin X, Vuong C, Pannone K, Kelly AM, Mulligan MP, Lee KK, Lau GW, Hung DT, Hergenrother PJ
ACS Cent. Sci. 2022, 8, 1145-1158
- Target-agnostic P-glycoprotein assessment yields strategies to evade efflux, leading to a BRAF inhibitor with intracranial efficacy
Kelly, A.M.; Berry, M.R.; Tasker, S.Z.; McKee, S.A.; Fan, T.M.; Hergenrother, P.J.
J. Am. Chem. Soc. 2022, 144, 12367-12380
- Mitigation of SARS-CoV-2 transmission at a large public university
Ranoa, D.R.E.; Holland, R.L.; Alnaji, F.G.; Green, K.J.; . . . Sullivan, W.C.; Smith, R.L.; Goldenfeld, N.D.; Fan, T.M.; Hergenrother, P.J, Burke, M.D.
Nature Comm. 2022, 13, 3207
- Evolution of 3-(4-hydroxyphenyl)indoline-2-one as a scaffold for potent and selective anticancer activity
Boudreau, M.W. and Hergenrother, P.J.
RSC Med. Chem. 2022, 13, 711-725
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- Role of internal loop dynamics in antibiotic permeability of outer membrane porins
Vasan, A.K.; Haloi, N.; Ulrich, R.J.; Metcalf, M.E.; Wen, P.C.; Metcalf, W.W.; Hergenrother, P.J.; Shukla, D.; Tajkhorshid, E.
Proc. Natl. Acad. Sci. 2022, 119, e2117009119
- Novel imidazotetrazine evades known resistance mechanisms and is effective against temozolomide-resistant brain cancer in cell culture
Svec, R.L; McKee, S.A.; Berry, M.R.; Kelly, A.M.; Fan, T.M.; Hergenrother, P.J.
ACS Chem. Biol. 2022, 17, 299-313
- Activators of the anticipatory unfolded protein response with enhanced selectivity for estrogen receptor positive breast cancer
Boudreau, M.W.; Mulligan, M.P.; Shapiro, D.J.; Fan, T.M.; Hergenrother, P.J.
J. Med. Chem. 2022, 65, 3894-3912
- Plasticity of extrachromosomal and intrachromosomal BRAF amplifications in overcoming targeted therapy dosage challenges
Song, K.; Minami J.K.; Huang, A.; Dehkordi, S.R.; Lomeli, S.H.; Luebeck, J.; Goodman, M.H.; Moriceau, G.; Krijgsman, O.; Dharanipragada, P.; Ridgley, T.; Crosson, W.P.; Salazar, J.; Pazol, E.; Karin, G.; Jayaraman, R.; Balanis, N.G.; Alhani, S.; Sheu, K.; Ten Hoeve, J.; Palermo, A.; Motika, S.E.; Senaratne, T.N.; Paraiso, K.H.; Hergenrother, P.J.; Rao, P.N.; Multani, A.S.; Peeper, D.S.; Bafna, V.; Lo, R.S.; Graeber, T.G.
Cancer Discov. 2022, 12, 1046-1069
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- Rationalizing generation of broad spectrum antibiotics with the addition of a positive charge
Haloi, N.; Vasan, A.K.; Geddes, E.; Prasanna, A.; Wen, P.-C.; Metcalf, W.W.; Hergenrother, P.J.; Tajkhorshid, E.
Chem. Sci. 2021, 12, 15028
- A LC-MS/MS assay and complementary web-based tool to quantify and predict compound accumulation in E. coli
Geddes, E.J; Li, Z.; Hergenrother, P.J.
Nature Protocols 2021, 16, 4833-4854.
- A small molecule activator of the unfolded protein response eradicates human breast tumors in mice
Boudreau, MW; Duraki, D; Wang, L.; Mao, C.; Kim, J.E.; Tang, B.; Fanning, S.W.; Kiefer, J.; Tarasow, T.M.; Bruckheimer, E.M.; Moreno, R.; Mousses, S.; Greene, G.L.; Roy, E.J.; Park, B.H.; Fan, T.M.; Nelson, E.R.; Hergenrother, P.J.; Shapiro, D.J.
Science Transl. Med. 2021, 13, eabf1383
- Dysfunction of the key ferroptosis-surveilling systems hypersensitizes mice to tubular necrosis during acute kidney injury
Tonnus, W; Meyer, C; Steinebach, C; Belavgeni, A; von Mässenhausen, A; Zamora Gonzalez, N; Maremonti, F; Gembardt, F; Himmerkus, N; Latk, M; Locke, S; Marschner, J; Li, W; Short, S; Doll, S; Ingold, I; Proneth, B; Daniel, C; Kabgani, N; Kramann, R; Hergenrother, PJ; Bornstein, S; Hugo, C; Becker, J; Amann, K; Anders, H-J; Kreisel, D; Pratt, D; Gütschow, M; Conrad, M; Motika, S; Linkermann A.
Nature Comm. 2021, 12, 4402
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- Evaluation of a procaspase-3 activator with hydroxyureas or temozolomide against high-grade meningioma in cell culture and canine cancer patients
Tonogai, E.; Huang, S.; Botham, R.; Berry, M.; Joslyn, S.; Daniel, G.; Chen, Z.; Rao, J.; Zhang, X.; Basuli, F.; Rossmisl, J.; Riggins, G.; LeBlanc, A.; Fan, T.; Hergenrother, P.J.
Neuro-Oncology 2021, 23, 1723-1735.
- Utilizing feline oral squamous cell carcinoma patients to develop a targeted therapy with potential for human head-and-neck cancer
Lundberg, A.P.; Boudreau, M.W.; Selting, K.A.; Chatkewitz, L.E.; Samuelson, J.; Francis, J.M.; Parkinson, E.I.; Barger, A.M.; Hergenrother, P.J.; Fan, T.F.
Neoplasia 2021, 8, 811-822.
- Limonin as a Starting Point for the Construction of Compounds with High Scaffold Diversity
Furiassi, L; Tonogai, E.J.; Hergenrother, P.J.
Angew. Chem. Int. Ed. 2021, 60, 16119-16128.
- Facilitating compound entry as a means to discover antibiotics for Gram-negative bacteria
Munoz, K.A. and Hergenrother, P.J.
Acc. Chem. Res. 2021, 54, 1322-1333.
- A phosphonate natural product made by Pantoea ananatis is necessary and sufficient for the hallmark lesion of onion center rot
Polidore, A.L.A.; Furiassi, L.; Hergenrother, P.J.; Metcalf, W.M.
mBio, 2021, 12, e3402-3420.
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- Synthesis of fusidic acid derivatives yields a potent antibiotic with an improved resistance profile
Garcia Chavez, M.; Garcia, A.; Lee, H.Y.; Lau, G.W.; Parker, E.N.; Komnick, K.E.; Hergenrother, P.J.
ACS Infect. Dis. 2021, 7, 493-505.
- Synthetic studies on selective, proapoptotic isomalabaricane triterpenoids aided by computational techniques
Boyko, Y.D.; Huck, C.J.; Ning, S.; Shved, A.S.; Yang, C.; Chu, F.; Tonogai, E.J.; Hergenrother, P.J.; Sarlah, D.
J. Am. Chem. Soc. 2021, 143, 2138-2155.
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- Compound uptake into E. coli can be facilitated by N-alkyl guanidiniums and pyridinium
Perlmutter, S.J.; Geddes, E.J.; Drown, B.S.; Motika, S.E.; Lee, M.R.; Hergenrother, P.J.
ACS Infect. Dis., 2021, 7, 162-173.
- Re-engineering natural products to engage new biological targets
Motika, S. E. and Hergenrother, P. J.
Nat. Prod. Rep. 2020, 37, 1395-1403.
- Saliva-based molecular testing for SARS-CoV-2 that bypasses RNA extraction
Ranoa, D.R.E.; Holland, R.L.; Alnaji, F.G.; Green, K.J.; Wang, L.; Brooke, C.B.; Burke, M.D.; Fan, T.M.; Hergenrother, P. J.
BioRxiv. June 18, 2020, doi.org/10.1101/2020.06.18.159434
- A gram-negative antibiotic active through inhibition of an essential riboswitch
Motika, S. E.; Ulrich, R. J.; Geddes, E. J.; Lee, H. Y.; Lau, G. W.; Hergenrother, P. J.
J. Am. Chem. Soc. 2020, 142, 10856-10862.
- Imidazotetrazines as weighable diazomethane surrogates for esterifications and cyclopropanations
Svec, R.L. and Hergenrother, P.J.
Angew. Chem. Int. Ed. 2020, 59, 1857-1862.
- Implementation of permeation rules leads to a FabI inhibitor with activity against Gram-negative pathogens
Parker, E. N.; Drown, B. S.; Geddes, E. J.; Lee, H.-Y.; Ismail, N.; Lau, G. W. and Hergenrother, P. J.
Nature Microbiology 2020, 5, 67-75.
- Epigenetic loss of RNA-methyltransferase NSUN5 in glioma targets ribosomes to drive a stress adaptive translational program
Janin M.; Ortiz-Barahona V.; Boudreau M.W.; Hergenrother P.J.; Esteller M. and others
Acta Neuropathol. 2019, 138, 1053-1074.
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- Procaspase-3 overexpression in cancer: A paradoxical observation with therapeutic potential
Boudreau, M. W.; Peh, J.; Hergenrother, P. J.
ACS Chem. Biol. 2019, 14, 2335-2348.
- Diverse compounds from pleuromutilin lead to a thioredoxin inhibitor and inducer of ferroptosis
Llabani, E.; Hicklin, R. W.; Lee, H.-Y.; Motika, S. E.; Crawford, L. A.; Weerapana, E., Hergenrother, P. J.
Nature Chem. 2019, 11, 521
- Structural analyses of NudT16–ADP-ribose complexes direct rational design of mutants with improved processing of poly(ADP-ribosyl)ated proteins
Thirawatananond, P.; McPherson, R. L.; Malhi, J.; Nathan, S.; Lambrecht, M.J.; Brichacek, M.; Hergenrother, P.J.; Leung, A.K.L.; Gabelli, S.B.
Sci. Reports, 2019, 9, 5940
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- Immunohistochemical characterization of procaspase-3 overexpression as a druggable target with PAC-1, a procaspase-3 activator, in canine and human brain cancers
Schlein, L. J.; Fadl-Alla, B.; Pondenis, H. C.; Lezmi, S.; Eberhart, C. G.; LeBlanc, A. K.; Dickinson, P. J.; Hergenrother, P. J.; Fan, T. M.
Front. Oncol. 2019, 9, 96
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- Enantioselective synthesis of isocarbostyril alkaloids and analogs using catalytic dearomative functionalization of benzene
Bingham, T. W.; Hernandez, L. W.; Olson, D. G.; Svec, R. L.; Hergenrother, P. J.; Sarlah, D
J. Am. Chem. Soc. 2019, 141, 657-670.
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- The challenge of converting Gram-positive-only compounds into broad-spectrum antibiotics
Richter, M. F. and Hergenrother, P. J.
Ann NY Acad Sci. 2019, 1435, 18-38.
- (ADP-ribosyl) hydrolases: Structural basis for differential substrate recognition and inhibition
Rack, J.G.M.; Ariza, A.; Drown, B. S.; Henfrey, C.; Shirai, T.; Hergenrother, P. J.; Ahel, I.
Cell Chem. Biol. 2018, 25, 1533-1546.
- Oxygen starvation unmasks a killer
Svec, R. L. and Hergenrother, P. J.
Cell Chem. Biol. 2018, 25, 1313-1314.
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- Monitoring poly(ADP-ribosyl)glycohydrolase activity with a continuous fluorescent substrate
Drown, B. S.; Shirai, T.; Rack, J.G.M.; Ahel, I.; Hergenrother, P. J.
Cell Chem. Biol. 2018, 25, 1562-1570.
- Tunable stability of imidazotetrazines leads to a potent compound for glioblastoma
Svec, R. L.; Furiassi, L.; Skibinski, C. G.; Fan, T. M.; Riggins, G. J.; Hergenrother, P. J.
ACS Chem. Biol. 2018,13, 3206-3216.
- Preparation of structurally diverse compounds from the natural product lycorine
Tasker, S. Z.; Cowfer, A. E.; Hergenrother P. J.
Org. Lett. 2018, 20, 5894-5898.
- Overcoming resistance to targeted anticancer therapies through small-molecule mediated MEK degradation
Peh, J.; Boudreau, M. W.; Smith, H. M.; and Hergenrother, P. J.
Cell Chem. Biol. 2018, 25, 996-1005.
- Strong and sustained activation of the anticipatory unfolded protein response induces necrotic cell death
Livezey, M.; Huang, R.;Hergenrother, P. J.; Shapiro, D.S.
Cell Death Differ. 2018, 25, 1796-1807.
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- Going on offense against the Gram-negative defense
Drown, B.S. and Hergenrother, P. J.
Proc Natl. Acad. Sci. 2018, 115, 6530-6532.
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- How many human proteoforms are there?
Aebersold, R; Agar, J.N.; Amster, I.J.; Baker, M.S.; Bertozzi, C.R.; Boja, E.S.; Costello, C.E.; Cravatt, B.F.; Fenselau, C., Garcia, B.A.; Ge, Y.; Gunawardena, J.; Hendrickson, R.C.; Hergenrother, P.J.; Huber, C.G.; Ivanov, A.R.; Jensen, O.N.; Jewett, M.C.; Kelleher, N.L.; Kiessling, L.L.; Krogan, N.J.; Larsen, M.R.; Loo, J.A.; Ogorzalek Loo, R.R.; Lundberg, E.; MacCoss, M.J.; Mallick, P.; Mootha, V.K.; Mrksich, M.; Muir, T.W.; Patrie, S.M.; Pesavento, J.J.; Pitteri, S.J.; Rodriguez, H.; Saghatelian, A.; Sandoval, W.; Schlüter, H.; Sechi, S.; Slavoff, S.A.; Smith, L.M.; Snyder, M.P.; Thomas, P.M.; Uhlén, M.; Van Eyk, J.E.; Vidal, M.; Walt, D.R.; White, F.M.; Williams, E.R.; Wohlschlager, T.; Wysocki, V.H.; Yates, N.A.; Young, N.L.; Zhang, B.
Nature Chem. Biol. 2018, 14, 206-214.
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- Single-cell analysis of early antiviral gene expression reveals a determinant of stochastic IFNBI expression
Doganay, S.; Lee, M. Y.; Baum, A.; Peh, J.; Hwang, S. Y.; Yoo, J. Y.; Hergenrother, P. J.; Garcia-Sastre, A.; Myong, S.; Ha, T.
Integr. Biol. 2017, 9, 857-867.
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- Broad-Spectrum Antibiotics, a Call for Chemists
Richter, M. F.; Hergenrother, P. J.
Chem 2017, 3, 10-13 (essay).
- Synergistic and targeted therapy with a procaspase-3 activator and temozolomide extends survival in glioma rodent models and is feasible for the treatment of canine malignant glioma patients
Joshi, A. D.; Botham, R. C.; Schlein, L. J.; Roth, H. S.; Mangraviti, A.; Borodovsky, A.; Tyler, B.; Joslyn, S.; Looper, J. S.; Podell, M.; Fan, T. F.; Hergenrother, P. J.; Riggins, G. J.
Oncotarget 2017, 8, 80124-80138.
- Characterization of the Saffron Derivative Crocetin as an Inhibitor of Human Lactate Dehydrogenase 5 in the Antiglycolytic Approach against Cancer
Granchi, C.; Fortunato, S.; Meni, S.; Rizzolio, F.; Caligiuri, I.; Tuccinardi, T.; Lee, H.-Y.; Hergenrother, P. J.; Minutolo, F.
J. Agric. Food Chem. 2017, 65, 5639-5649.
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- Predictive Compound Accumulation Rules Yield a Broad-Spectrum Antibiotic
Richter, M. F.; Drown, B. S.; Riley, A. P.; Garcia, A.; Shirai, T.; Svec, R. L.; Hergenrother, P. J.
Nature 2017, 545, 299-304.
- Taming Reactive Benzynes
Tasker, S. Z.; Hergenrother, P. J.
Nature Chem. 2017, 9, 504-506 (News & Views).
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- Reactive Oxygen Species Synergize to Potently and Selectively Induce Cancer Cell Death
Lee, H.-Y.; Parkinson, E. I.; Granchi, C.; Paterni, I.; Panigrahy, D.; Seth, P.; Minutolo, F.; Hergenrother, P. J.
ACS Chem. Biol. 2017, 12, 1416-1424.
- Pharmacokinetics and Derivation of an Anticancer Dosing Regimen for the Novel Anti-Cancer Agent Isobutyl-Deoxynyboquinone (IB-DNQ), a NQO1 Bioactivatable Molecule, in the Domestic Felid Species
Lundberg, A. P.; Francis, J. M.; Pajak, M.; Parkinson, E. I.; Wycislo, K. L.; Rosol, T. J.; Brown, M. E.; London, C. A.; Dirikolu, L.; Hergenrother, P. J.; Fan. T. M.
Invest New Drugs 2017, 35, 134-144.
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- Access to a Structurally Complex Compound Collection via Ring Distortion of the Alkaloid Sinomenine
Garcia, A.; Drown, B. S.; Hergenrother, P. J.
Org. Lett. 2016, 18, 4852-4855.
- Porous Photonic Crystal External Cavity Laser Biosensor
Huang, Q.; Peh, J.; Hergenrother, P. J.; Cunningham, B. T.
Appl. Phys. Lett. 2016, 109, 071103.
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- Small-Molecule Procaspase-3 Activation Sensitizes Cancer to Treatment with Diverse Chemotherapeutics
Botham, R. C.; Roth, H. S.; Book, A. P.; Roady, P. J.; Fan, T. M.; Hergenrother, P. J.
ACS Central Science 2016, 2, 545-559.
- Targeting Multidrug-resistant Ovarian Cancer Through Estrogen Receptor α Dependent ATP Depletion Caused by Hyperactivation of the Unfolded Protein Response
Zheng, Z.; Andruska, N. D.; Lambrecht, M. L.; Sisi, H.; Hergenrother, P. J.; Nelson, E.; Shapiro, D. J.
Oncotarget 2016, 9, 14741-14753.
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- The Combination of Vemurafenib and Procaspase-3 Activation is Synergistic in Mutant BRAF Melanomas
Peh, J.; Fan, T. M.; Wycislo, K. L.; Roth, H. S.; Hergenrother, P. J.
Mol. Cancer Ther. 2016, 15, 1859-1869.
- A Potent Inhibitor of Protein Sequestration by Expanded Triplet (CUG) Repeats that Shows Phenotypic Improvements in a Drosophila Model of Myotonic Dystrophy
Luu, L. M.; Nguyen, L.; Peng, S.; Lee, J.; Lee, H. Y.; Wong, C. H.; Hergenrother, P. J.; Chan, H. Y.; Zimmerman, S. C.
ChemMedChem 2016, 11, 1428-1435.
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- Derivatives of Procaspase-Activating Compound 1 (PAC-1) and Their Anticancer Activities
Roth, H. S.; Hergenrother, P. J.
Curr. Med. Chem. 2016, 23, 201-241 (review).
- A Small Molecule that Induces Intrinsic Pathway Apoptosis with Unparalleled Speed
Palchaudhuri, R.; Lambrecht, M. J.; Botham, R. C.; Partlow, K. C.; Van Ham, T. J.; Putt, K. S.; Nguyen, L. T.; Kim, S.-H.; Peterson, R. T.; Fan, T. M.; Hergenrother, P. J.
Cell Reports 2015, 13, 2027-2036.
- Deoxynyboquinones as NQO1-Activated Cancer Therapeutics
Parkinson, E. I.; Hergenrother, P. J.
Acc. Chem. Res. 2015, 48, 2715-2733.
- Salicylketoximes that Target Glucose Transporter 1 Restrict Energy Supply to Lung Cancer Cells
Granchi, C.; Qian, Y.; Lee, H. Y.; Paterni, I.; Pasero, C.; Iegre, J.; Carlson, K. E.; Tuccinardi, T.; Chen, X.; Katzenellenbogen, J. A.; Hergenrother, P. J.; Minutolo, F.
ChemMedChem 2015, 10, 1892-1900.
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- Deoxynybomycins Inhibit Mutant DNA Gyrase and Rescue Mice Infected with Fluoroquinolone-Resistant Bacteria
Parkinson, E. I.; Bair, J. S.; Nakamura, B.; Lee, H. Y.; Kuttab, H. I.; Southgate, E. H.; Lezmi, S.; Lau, G. W.; Hergenrother, P. J.
Nat. Commun. 2015, 6, 6947
- Removal of Metabolic Liabilities Enables Development of Derivatives of Procaspase-Activating Compound 1 (PAC-1) with Improved Pharmacokinetics
Roth, H. S.; Botham, R. C.; Schmid, S. C.; Fan, T. M.; Dirikolu, L.; Hergenrother, P. J.
J. Med. Chem. 2015, 58, 4046-4065.
- Synthesis and Biological Evaluation of Non-Glucose Glycoconjugated N-Hydroyxindole Class LDH Inhibitors as Anticancer Agents
DiBussolo, V.; Calvaresi, E. C.; Granchi, C.; DelBino, L.; Frau, I.; Lang, M.; Tuccinardi, T.; Macchia, M.; Matinelli, A.; Hergenrother, P. J.; Minutolo, F.
RSC Adv. 2015, 5, 19944-19954.
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- Synthesis of Dimeric ADP-Ribose and Its Structure with Human Poly(ADP-Ribose) Glycohydrolase
Lambrecht, M. J.; Brichacek, M.; Barkauskaite, E.; Ariza, A.; Ahel, I.; Hergenrother, P. J.
J. Am. Chem. Soc. 2015, 137, 3558-3564.
- Synthesis of Bridged Oxafenestranes from Pleuromutilin
Hicklin, R. W.; López Silva, T. L.; Hergenrother, P. J.
Angew. Chem. Int. Ed. 2014, 53, 9880-9883.
- Detection of Protein-Small Molecule Binding Using a Self-Referencing External Cavity Laser Biosensor
Zhang, M.; Peh, J.; Hergenrother, P. J.; Cunningham, B. T.
J. Am. Chem. Soc. 2014, 136, 5840-5843.
- Targeting Toxic RNAs that Cause Myotonic Dystrophy Type 1 (DM1) with a Bisamidinium Inhibitor
Wong, C.-H.; Nguyen, L.; Peh, J.; Luu, L. M.; Sanchez, J. S.; Richardson, S. L.; Tuccinardi, T.; Tsoi, H.; Chan, W. Y.; Chan, H. Y. E.; Baranger, A. M.; Hergenrother, P. J.; Zimmerman, S. C.
J. Am. Chem. Soc. 2014, 136, 6355-6361.
- Dual Small-Molecule Targeting of Procaspase-3 Dramatically Enhances Zymogen Activation and Anticancer Activity.
Botham, R. C.; Fan, T. M.; Im, I.; Borst, L. B.; Dirikolu, L.; Hergenrother, P. J.
J. Am. Chem. Soc. 2014, 136, 1312-1319.
- Light Activation of Staphylococcus aureus Toxin YoeBSa1 Reveals Guanosine-Specific Endoribonuclease Activity
Larson, A. S.; Hergenrother, P. J.
Biochemistry 2014, 53, 188-201.
- Synthesis of Complex and Diverse Compounds through Ring Distortion of Abietic Acid
Rafferty, R. J.; Hicklin, R. W.; Maloof, K. A.; Hergenrother, P. J.
Angew. Chem. Int. Ed. 2014, 53, 220-224.
- Total Synthesis, Stereochemical Assignment, and Biological Activity of All Known (–)-Trigonoliimines
Han, S.; Morrison, K. C.; Hergenrother, P. J.; Movassaghi, M.
J. Org. Chem. 2014, 79, 473-486.
- Natural Products as Starting Points for the Synthesis of Complex and Diverse Compounds
Morrison, K. C.; Hergenrother, P. J.
Nat. Prod. Rep. 2014, 31, 6-14.
- Dual Targeting of the Warburg Effect with a Glucose-Conjugated Lactate Dehydrogenase Inhibitor
Calvaresi, E. C.; Granchi, C.; Tuccinardi, T.; DiBussolo, V.; Huigens, R. W.; Lee, H.-Y.; Palchaudhuri, R.; Macchia, M.; Martinelli, A.; Minutolo, F.; Hergenrother, P. J.
ChemBioChem 2013, 14, 2263-2267.
- Synthesis and Anticancer Activity of All Known (–)-Agelastatin Alkaloids
Han, S.; Siegel, D. S.; Morrison, K. C.; Hergenrother, P. J.; Movassaghi, M.
J. Org. Chem. 2013, 78, 11970-11984.
- Detection of Endogenous MazF Enzymatic Activity in Staphylococcus aureus
van Rensburg, J. J.; Hergenrother, P. J.
Anal. Biochem. 2013, 443, 81-87.
- Synthesis of (+/-)-Actinophyllic Acid and Analogs: Applications of Cascade Reactions and Diverted Total Synthesis
Granger, B. A.; Jewett, I. T.; Butler, J. D.; Hua, B.; Knezevic, C. E.; Parkinson, E. I.; Hergenrother, P. J.; Martin, S. F.
J. Am. Chem. Soc. 2013, 135,12984-12986.
- Efficient NQO1 Substrates are Potent and Selective Anticancer Agents
Parkinson, E. I.; Bair, J. S.; Cismesia, M.; Hergenrother, P. J.
ACS Chem. Biol. 2013, 8, 2173-2183.
- Assessing the Differential Action on Cancer Cells of LDH-A Inhibitors based on the N-Hydroxyindole-2-Carboxylate (NHI) and Malonic (Mal) Scaffolds
Granchi, C.; Calvaresi, E. C.; Tuccinardi, T.; Paterni, I.; Macchia, M.; Martinelli, A.; Hergenrother, P. J.; Minutolo, F.
Org. Biomol. Chem. 2013, 11, 6588-6596.
- Glucose conjugation for the specific targeting and treatment of cancer
Calvaresi, E. C.; Hergenrother, P. J.
Chem. Sci. 2013, 4, 2319-2333.
- External Cavity Laser Biosensor
Ge, C.; Lu, M.; George, S.; Flood, T. A.; Wagner, C.; Zheng, J.; Pokhriyal, A.; Eden, J. G.; Hergenrother, P. J.; Cunningham, B. T.
Lab Chip 2013, 13, 1247-1256.
- Synthesis and Anticancer Activity of Epipolythiodiketopiperazine Alkaloids
Boyer, N.; Morrison, K. C.; Kim, J.; Hergenrother, P. J.; Movassaghi, M.
Chem. Sci. 2013, 4, 1646-1657.
- A Ring Distortion Strategy to Construct Stereochemically Complex and Structurally Diverse Compounds from Natural Products
Huigens, R. W.; Morrison, K. C.; Hicklin, R. W.; Flood, T. A.; Richter, M. F.; Hergenrother, P. J.
Nature Chem. 2013, 5, 195-202.
- Structure and Mechanism of a Canonical Poly(ADP-Ribose) Glycohydrolase
Dunstan, M. S.; Barkauskaite, E.; Lafite, P.; Knezevic, C. E.; Brassington, A.; Ahel, M.; Hergenrother, P. J.; Leys, D.; Ahel, I.
Nat. Commun. 2012, 3, 878.
- An NQO1 Substrate with Potent Anti-Tumor Activity that Selectively Kills by PARP-1-Induced Programmed Necrosis
Huang, X.; Dong, Y.; Bey, E. A.; Kilgore, J. A.; Bair, J. S.; Li, L.-S.; Patel, M.; Parkinson, E. I.; Wang, Y.; Williams, N. S.; Gao, J.; Hergenrother, P. J.; Boothman, D. A.
Cancer Res. 2012, 72, 3038-3047.
- Differential effects of procaspase-3 activating compounds in the induction of cancer cell death
West, D. C.; Qin, Y.; Peterson, Q. P.; Thomas, D. L.; Palchaudhuri, R. P.; Morrison, K. C.; Lucas, P. W.; Palmer, A. E.; Fan, T. M; Hergenrother, P. J.
Mol. Pharmaceutics 2012, 9, 1425-1434.
- Artificial Activation of Toxin-Antitoxin Systems as an Antibacterial Strategy
Williams, J. J.; Hergenrother, P. J.
Trends Microbiol. 2012, 20, 291-298.
- Identification of a Novel Protein Synthesis Inhibitor Active Against Gram-Positive Bacteria
Eibergen, N. R.; Im, I.; Patel, N. Y.; Hergenrother, P. J.
ChemBioChem 2012, 13, 574-583.
- Selective Small Molecule Inhibition of Poly(ADP-Ribose) Glycohydrolase (PARG)
Finch, K. E.; Knezevic, C. E.; Nottbohm, A. C.; Partlow, K. C.; Hergenrother, P. J.
ACS Chem. Biol. 2012, 7, 563-570.
- Whole Cell Microtubule Analysis by Flow Cytometry
Morrison, K.C.; Hergenrother, P. J.
Anal. Biochem. 2012, 420, 26-32.
- Parallel Synthesis and Biological Evaluation of 837 Analogues of Procaspase-Activating Compound 1 (PAC-1)
Hsu, D. C.; Roth, H. S.; West, D. C.; Botham, R. C.; Novotny, C. J.; Schmid, S. C.; Hergenrother, P. J.
ACS Comb. Sci. 2012, 14, 44-50.
- Runaway ROS as a Selective Anticancer Strategy
Parkinson, E. I.; Hergenrother, P. J.
ChemMedChem 2011, 6, 1957-1959.
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- Toxin-Antitoxin (TA) Systems are Prevalent and Transcribed in Clinical Isolates of Pseudomonas aeruginosa and Methicillin-Resistant Staphylococcus aureus
Williams, J. J.; Halvorsen, E. M.; Dwyer, E. M.; DiFazio, R. M.; Hergenrother, P. J.
FEMS Microbiol. Lett. 2011, 322, 41-50.
- Triphenylmethyl Derivatives Enhances the Anticancer Effect of Immunotoxins
Risberg, K.; Guldvik, I. J.; Palchaudhuri, R.; Xi, Y.; Ju, J.; Fodstad, O.; Hergenrother, P. J.; Andersson, Y.
J. Immunother. 2011, 34, 438-447.
- Discovery of N-Hydroxyindole-Based Inhibitors of Human Lactate Dehydrogenase Isoform A (LDH-A) as Starvation Agents Against Cancer Cells
Granchi, C.; Roy, S.; Giacomelli, C.; Macchia, M.; Tuccinardi, T.; Martinelli, A.; Lanza, M.; Betti, L.; Giannaccini, G.; Lucacchini, A.; Funel, N.; Leon, L. G.; Giovannetti, E.; Peters, G. J.; Palchaudhuri, R.; Calvaresi, E. C.; Hergenrother, P. J.; Minutolo, F.
J. Med. Chem. 2011, 54, 1599-1612.
- Txe, an Endoribonuclease of the Enterococcal Axe-Txe Toxin-Antitoxin System, cleaves mRNA and inhibits protein synthesis
Halvorsen, E. M.; Williams, J. J.; Bhimani, A. J.; Billings, E. A.; Hergenrother, P. J.
Microbiology 2011, 157, 387-397.
- Transcript Profiling and RNA Interference as Tools to Identify Small Molecule Mechanisms and Therapeutic Potential
Palchaudhuri, R.; Hergenrother, P. J.
ACS Chem. Biol. 2011, 6, 21-33.
- Cribostatin 6 Induces Death in Cancer Cells Through a Reactive Oxygen Species (ROS)-Mediated Mechanism
Hoyt, M.T.; Palchaudhuri, R.; Hergenrother, P. J.
Invest. New Drugs 2011, 29, 562-573.
- High-Throughput Screening for Modulators of Protein-Protein Interactions: Use of Photonic Crystal Biosensors and Complementary Technologies
Heeres, J. T.; Hergenrother, P. J.
Chem. Soc. Rev. 2011, 40, 4398-4410.
- Pharmacokinetics and Derivation of an Anticancer Dosing Regimen for PAC-1, a Preferential Small Molecule Activator of Procaspase-3, in Healthy Dogs
Lucas, P. W.; Schmit, J. M.; Peterson, Q. P.; West, D. C.; Hsu, D. C.; Novotny, C. J.; Dirikoul, L.; Deorge, D. R.; Garrett, L. D.; Hergenrother, P. J.; Fan, T. M.
Invest. New Drugs 2011, 29, 901-911.
- A Noncompetitive Small Molecule Inhibitor of Estrogen-regulated Gene Expression and Breast Cancer Cell Growth that Enhances Proteasome-dependent Degradation of Estrogen Receptor α
Cherian, M. T.; Mao, C.; Aninye, I. O.; Reynolds, P. D.; Schiff, R.; Hergenrother, P. J.; Nordeen, S. K.; Wilson, E. M.; Shapiro, D. J.
J. Biol. Chem. 2010, 285, 41863-41873.
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- Discovery and Canine Preclinical Assessment of a Nontoxic Procaspase-3-Activating Compound
Peterson, Q. P.; Hsu, D. C.; Novotny, C. J.; West, D. C.; Kim, D.; Schmit, J. M.; Dirikolu, L.; Hergenrother, P. J.; Fan, T. M.
Cancer Res. 2010, 70, 7232-7241.
- Identification of Novel Synthetic Toll-Like Receptor 2 Agonists by High-Throughput Screening
Guan, Y.; Omueti-Ayoade, K.; Mutha, S. K.; Hergenrother, P. J.; Tapping, R. I.
J. Biol. Chem. 2010, 285, 23755-23763.
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- Phenylcinnamides as Novel Antimitotic Agents
Leslie, B. J.; Holaday, C. R.; Nguyen, T.; Hergenrother, P. J.
J. Med. Chem. 2010, 53, 3964-3972.
- N-((1-Benzyl-1H-1,2,3-triazol-4-yl)methyl)arylamide as a New Scaffold that Provides Rapid Access to Antimicrotubule Agents: Synthesis and Evaluation of Antiproliferative Activity Against Select Cancer Cell Lines
Stefely, J. A.; Palchaudhuri, R.; Miller, P. A.; Peterson, R. J.; Moraski, G. C.; Hergenrother, P. J.; Miller, M. J.
J. Med. Chem. 2010, 53, 3389-3395.
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- Chemistry and Biology of Deoxynyboquinone, a Potent Inducer of Cancer Cell Death
Bair, J. S.; Palchaudhuri, R.; Hergenrother, P. J.
J. Am. Chem. Soc. 2010, 132, 5469-5478.
- Preparation of the Caspase-3/7 Substrate Ac-DEVD-pNA by Solution-Phase Peptide Synthesis
Peterson, Q. P.; Goode, D. R.; West, D. C.; Botham, R. C.; Hergenrother, P. J.
Nature Protocols 2010, 5, 294-302.
- Identifying Modulators of Protein-Protein Interactions Using Photonic Crystal Biosensors
Heeres, J. T.; Kim, S.-H.; Leslie, B. J.; Lidstone, E. A.; Cunningham, B. T.; Hergenrother, P. J.
J. Am. Chem. Soc. 2009, 131, 18202-18203.
- A Method for Identifying Small Molecule Aggregators Using Photonic Crystal Biosensor Microplates
Chan, L. L; Lidstone, E. A.; Finch, K. E.; Heeres, J. T.; Hergenrother, P. J.; Cunningham, B. T.
J. Lab. Autom. 2009, 14, 348-359.
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- Procaspase-3 Activation as an Anti-Cancer Strategy: Structure-Activity Relationship of Procaspase-Activating Compound 1 (PAC-1) and Its Cellular Co-Localization with Caspase-3
Peterson, Q. P.; Hsu, D. C.; Goode, D. R.; Novotny, C. J.; Totten, R. K.; Hergenrother, P. J.
J. Med. Chem. 2009, 52, 5721-5731.
- Small Molecule Ligands for Bulged RNA Secondary Structures
Meyer, S. T.; Hergenrother, P. J.
Org. Lett. 2009, 11, 4052-4055.
- PAC-1 Activates Procaspase-3 in vitro Through Relief of Zinc-Mediated Inhibition
Peterson, Q. P.; Goode, D. R.; West, D. C.; Ramsey, K. N.; Lee, J. J.; Hergenrother, P. J.
J. Mol. Biol. 2009, 388, 144-158.
- Malaria-Infected Mice Are Cured by a Single Oral Dose of New Dimeric Trioxane Sulfones Having Also Selective and Powerful Anticancer Activity
Rosenthal, A. S.; Chen, X.; Liu, J.; West, D. C.; Hergenrother, P. J.; Shapiro, T. A; Posner, G. H.
J. Med. Chem. 2009, 52, 1198-1203.
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- The Total Synthesis and Cytoprotective Properties of Dykellic Acid
Thompson, C. M.; Quinn, C. A.; Hergenrother, P. J.
J. Med. Chem. 2009, 52, 117-125.
- Phosphate Mimics: Cyclic Compounds
Nottbohm, A. C.; Hergenrother, P. J.
Wiley Encyclopedia of Chemical Biology 2008, 1-15.
- Triphenylmethylamides (TPMAs): Structure-activity relationship of compounds that induce apoptosis in melanoma cells
Palchaudhuri, R.; Hergenrother, P. J.
Bioorg. Med. Chem. Lett. 2008, 18, 5888-5891.
- Exposing Plasmids as the Achilles’ Heel of Drug-Resistant Bacteria
Williams, J. J.; Hergenrother, P. J.
Curr. Opin. Chem. Biol. 2008, 12, 389-399.
- The Complex Role of the Triphenylmethyl Motif in Anticancer Compounds
Palchaudhuri, R.; Nesterenko, V.; Hergenrother, P. J.
J. Am. Chem. Soc. 2008, 130, 10274-10274.
- A General Method for Discovering Inhibitors of Protein-DNA Interactions Using Photonic Crystal Biosensors
Chan, L. C.; Pineda, M.; Heeres, J. T.; Hergenrother, P. J.; Cunningham, B. T.
ACS Chem. Biol. 2008, 3, 437-448.
- Identification of the Cellular Targets of Bioactive Small Organic Molecules Using Affinity Reagents
Leslie, B. J.; Hergenrother, P. J.
Chem. Soc. Rev. 2008, 37, 1347-1360.
- Identification of Promiscuous Small Molecule Activators in High-Throughput Enzyme Activation Screens
Goode, D. R.; Totten, R. K.; Heeres, J. T.; Hergenrother, P. J.
J. Med. Chem. 2008, 51, 2346-2349.
- A Small Molecule, Identified as an Inhibitor of the Binding of Estrogen Receptor a to Estrogen Response Elements Blocks the Estrogen-dependent Growth of Cancer Cells
Mao, C.; Patterson, N.; Cherian, M.; Aninye, I.; Zhang, C.; Patterson, N.; Cheng, J.; Putt, K. S.; Hergenrother, P. J.; Wilson, E.; Nordeen, S. K.; Shapiro, D. J.
J. Biol. Chem. 2008, 283, 12819-12830.
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- Targeting RNA with Small Molecules
Thomas, J. R.; Hergenrother, P. J.
Chem. Rev. 2008, 108, 1171-1224.
- Chelated Iron Sources are Inhibitors of Psudomonas aeruginosa Biofilms and Distribute Efficiently in an in vitro Model of Drug Delivery to the Human Lung
Musk, D. J.; Hergenrother, P. J.
J. Appl. Microbiol. 2008, 105, 380-388.
- DNA as a Target for Anti-Cancer Compounds: Methods to Determine the Mode of Binding and the Mechanism of Action
Palchaudhuri, R.; Hergenrother, P. J.
Curr. Opin. Biotechnol. 2007, 18, 497-503.
- Poly(ADP-Ribose) Makes a Date with Death
Heeres, J. T.; Hergenrother, P. J.
Curr. Opin. Chem. Biol. 2007, 11, 644-653.
- A Continuous Fluorometric Assay for the Assessment of MazF Ribonuclease Activity
Wang, N. R.; Hergenrother, P. J.
Anal. Biochem. 2007, 371, 173-183.
- Increased Poly(ADP-ribose) Polymerase Activity During Porcine Hemorrhagic Shock is Transient and Predictive of Mortality
Skarda, D. E.; Putt, K. S.; Hergenrother, P. J.; Mulier, K. E.; Beilman, G. J.
Resuscitation 2007, 75, 135-144.
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- Multiplex Targeting, Tracking and Imaging of Apoptosis by Fluorescent Surface Enhanced Raman Spectroscopic Dots
Yu, K. N.; Lee, S.-M.; Han, J. Y.; Park, H.; Woo, M.-A.; Noh, M. S.; Hwang, S.-K.; Kwon, J.-T.; Jin, H.; Kim, Y.-K.; Hergenrother, P. J.; Jeong, D. H.; Lee, Y.-S.; Cho, M.-H.
Bioconjugate Chem. 2007, 18, 1155-1162.
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- A Novel Colorimetric Substrate for Poly(ADP-Ribose) Polymerase-1 (PARP-1), VPARP, and Tankyrase-1
Nottbohm, A. C.; Dothager, R. S.; Putt, K. S.; Hoyt, M. T.; Hergenrother, P. J.
Angew. Chem. Int. Ed. 2007, 46, 2066-2069.
- The Promises and Pitfalls of Small-Molecule Inhibition of Poly(ADP-Ribose) Glycohydrolase (PARG)
Nottbohm, A. C.; Hergenrother, P. J.
Drug Discovery Research: New Frontiers in the Post-Genomic Era 2007, 163-185.
- A Novel Synthetic Analogue of a Constituent of Isodon excisus Inhibits Transcription of CYP1A1, -1A2, and -1B1 by Preventing Activation of the Aryl Hydrocarbon Receptor
Sienkiewicz, P.; Ciolino, H.; Leslie, B. J.; Hergenrother, P. J.; Singletary, K.; Yeh, G. C.
Carcinogenesis 2007, 28, 1052-1057.
- Toxin-Antitoxin System are Ubiquitous and Plasmid-Encoded in Vancomycin Resistant Enterococci (VRE)
Moritz, E. M.; Hergenrother, P. J.
Proc. Natl. Acad. Sci. 2007, 104, 311-316.
- The Prevalence of Plasmids and Other Mobile Genetic Elements in Clinically Important Drug-Resistant Bacteria
Moritz, E. M.; Hergenrother, P. J.
Antimicrobial Resistance in Bacteria 2007, 25-53.
- Small-Molecule Activation of Procaspase-3 to Caspase-3 as a Personalized Anticancer Strategy
Putt, K. S.; Chen, G. W.; Pearson, J. M.; Sandhorst, J. S.; Hoagland, M. S.; Kwon, J.-T.; Hwang, S.-K.; Jin, H.; Churchwell, M. I.; Cho, M.-H.; Doerge, D. R.; Helferich, W. G.; Hergenrother, P. J.
Nat. Chem. Biol. 2006, 2, 543-50.
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BBC News Highlight – #1 Most emailed story on website worldwide on Monday, August 28, 3:20 pm
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Nature Podcast – September 7, 2006; description of our work starts ~19 minutes in
Nature Chemical Biology News Highlight
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- The Compound 13-D Selectively Induces Apoptosis in White Blood Cancers Versus Other Cancer Cell Types
Putt, K. S.; Nesterenko, V.; Dothager, R. S.; Hergenrother, P. J.
ChemBioChem 2006, 7, 1916-1922.
- Biochemical and Thermodynamic Characterization of Compounds that Bind to RNA Hairpin Loops: Toward an Understanding of Selectivity
Thomas, J. R.; Liu, X.; Hergenrother, P. J.
Biochemistry 2006, 45, 10928-10938.
- Chemical Countermeasures for the Control of Bacterial Biofilms: Effective Compounds and Promising Targets
Musk, D. J.; Hergenrother, P. J.
Curr. Med. Chem. 2006, 13, 2163-2177 (review).
- Obtaining and screening compound collections: A user’s guide and a call to chemists
Hergenrother, P. J.
Curr. Opin. Chem. Biol. 2006, 10, 213-218.
- Tools for Molecular Diversification and Their Applications to Chemical Biology
Silverman, S. K.; Hergenrother, P. J.
Curr. Opin. Chem. Biol. 2006, 10, 185-187.
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- DNA Binders and Related Subjects. Topics in Current Chemistry 253 (Book Review)
Hergenrother, P. J.
J. Am. Chem. Soc. 2006, 128, 3469-3470.
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- Size-Specific Ligands for RNA Hairpin Loops
Thomas, J. R.; Liu, X.; Hergenrother, P. J.
J. Am. Chem. Soc. 2005, 127, 12434-12435.
- Using Peptidic Inhibitors to Systematically Probe the S1′ Site of Caspase-3 and Caspase-7
Goode, D. R.; Sharma, A. K.; Hergenrother, P. J.
Org. Lett. 2005, 7, 3529-3532.
- Iron Salts Perturb Biofilm Formation and Disrupt Existing Biofilms of Pseudomonas aeruginosa
Musk, D. J.; Banko, D. A.; Hergenrother, P. J.
Chem. Biol. 2005, 12, 789-796.
- Synthesis and Identification of Small Molecules that Potently Induce Apoptosis in Melanoma Cell Through G1 Cell Cycle Arrest
Dothager, R. S.; Putt, K. S.; Allen, B. J.; Leslie, B. J.; Nesterenko, V.; Hergenrother, P. J.
J. Am. Chem. Soc. 2005, 127, 8686-8696.
- The Relationship Between Aminoglycosides’ RNA Binding Proclivity and Their Antiplasmid Effect on an IncB Plasmid
Thomas, J. R.; DeNap, J. C. B.; Wong, M.; Hergenrother, P. J.
Biochemistry 2005, 44, 6800-6808.
- Structure-based Design and In-Silico Virtual Screening of Combinatorial Libraries. A Combined Chemical/Computational Laboratory Assignment
Baudry, J.; Hergenrother, P. J.
J. Chem. Educ. 2005, 82, 890-894.
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- Bacterial Death comes Full Circle: Targeting Plasmid Replication in Drug-Resistant Bacteria
DeNap, J. C. B.; Hergenrother, P. J.
Org. Biomol. Chem. 2005, 3, 959-966.
- Direct Quantitation of Poly(ADP-Ribose) Polymerase (PARP) Activity as a Method to Distinguish Necrotic and Apoptotic Death in Cell and Tissue Samples
Putt, K. S.; Beilman, G. J.; Hergenrother, P. J.
ChemBioChem 2005, 6, 53-55.
- Combating Drug-Resistant Bacteria: Small Molecule Mimics of Plasmid Incompatibility as Antiplasmid Compounds
DeNap, J. B.; Thomas, J. R.; Musk, D. J.; Hergenrother, P. J.
J. Am. Chem. Soc. 2004, 126, 15402-15404.
- Deoxystreptamine Dimers bind to RNA Hairpin Loops
Liu, X.; Thomas, J. R.; Hergenrother, P. J.
J. Am. Chem. Soc. 2004, 126, 9196-9197.
- Medicinal Chemistry – An Introduction
Hergenrother, P. J.
Synthesis 2004, 13, 2248.
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- A non-radiometric, high-throughput assay for poly(ADP-ribose) glycohydrolase (PARG): Application to inhibitor identification and evaluation
Putt, K. S.; Hergenrother, P. J.
Anal. Biochem. 2004, 333, 256-264.
- An Enzymatic Assay for Poly(ADP-Ribose) Polymerase (PARP-1) via the Chemical Quantitation of NAD+: Application to the High-Throughput Screening of Small Molecules as Potential Inhibitors
Putt, K. S.; Hergenrother, P. J.
Anal. Biochem. 2004, 326, 78-86.
- Identification from a Combinatorial Library of a Small Molecule that Selectively Induces Apoptosis in Cancer Cells
Nesterenko, V.; Putt, K. S.; Hergenrother, P. J.
J. Am. Chem. Soc. 2003, 125, 14672-14673.
- Efficient Synthesis of Enantiopure β-Amino-γ-Keto Acids from ʟ-Homoserine
Sharma, A. K.; Hergenrother, P. J.
Org. Lett. 2003, 5, 2107-2109.
- The Use of pH to Influence Regio- and Chemoselectivity in the Asymmetric Aminohydroxylation of Styrenes
Nesterenko, V.; Byers, J. T.; Hergenrother, P. J.
Org. Lett. 2003, 5, 281-284.
FROM HARVARD
- Dissecting Glucose Signaling with Diversity-Oriented Synthesis and Small Molecule Microarrays
Kuruvilla, F. G.; Shamji, A. F.; Sternson, S. M.; Hergenrother, P. J.; Schreiber, S. L.
Nature 2002, 416, 653-657.
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- Small-Molecule Microarrays: Covalent Attachment and Screening of Alcohol Containing Small Molecules on Glass Slides
Hergenrother, P. J.; Depew, K. M.; Schreiber, S. L.
J. Am. Chem. Soc. 2000, 122, 7849-7850.
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FROM TEXAS
- Total Synthesis of Erythromycin B
Breton, P.; Hergenrother, P. J.; Hida, T.; Hodgson, A.; Judd, A. S.; Kraynack, E.; Kym, P. R.; Lee, W.-C.; Loft, M. S.; Yamashita, M.; Martin, S. F.
Tetrahedron 2007, 63, 5709-5729.
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- An Abiotic Strategy for the Enantioselective Synthesis of Erythromycin B
Hergenrother, P. J.; Hodgson, A.; Judd, A. S.; Lee, W.-C.; Martin, S. F.
Angew. Chem. Int. Ed. 2003, 42, 3278-3281.
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- Altering Substrate Specificity of Phosphatidylcholine-Preferring Phospholipase C of Bacillus cereus by Random Mutagenesis of the Headgroup Binding Site
Antikainen, N. M.; Hergenrother, P. J.; Harris, M. M.; Corbett, B.; Martin, S. F.
Biochemistry 2003, 42, 1603-1610.
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- Characterization of Erythromycin Analogs by Collisional Activated Dissociation and Infrared Multiphoton Dissociation in a Quadrupole Ion Trap
Crowe, M. C.; Brodbelt, J. S.; Goolsby, B. J.; Hergenrother, P. J.
J. Am. Soc. Mass. Spectrom. 2002, 13, 630-649.
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- Phosphatidylcholine-Preferring Phospholipase C from B. cereus. Function, Structure, and Mechanism.
Hergenrother, P. J.; Martin, S. F.
Top. Curr. Chem. 2000, 211, 131-167.
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- A Novel Class of Zinc Binding Inhibitors for the Phosphatidylcholine-Preferring Phospholipase C from Bacillus cereus
Martin, S. F.; Follows, B. C.; Hergenrother, P. J.; Franklin, C. L.
J. Org. Chem. 2000, 65, 4509-4514.
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- The Choline Binding site of Phospholipase C (Bacillus cereus): Insights into Substrate Specificity
Martin, S. F.; Follows, B. C.; Hergenrother, P. J.; Trotter, B. K.
Biochemistry 2000, 39, 3410-3415.
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- Determination of the Substrate Specificity of the Phospholipase D from Streptomyces chromofuscus via an Inorganic Phosphate Quantitation Assay
Martin, S. F.; DeBlanc, R. L.; Hergenrother, P. J.
Anal. Biochem. 2000, 278, 106-110.
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- Catalytic Cycle of the Phosphatidylcholine-Preferring Phospholipase C from Bacillus cereus. Solvent Viscosity, Deuterium Isotope Effects, and Proton Inventory Studies
Martin, S. F., Hergenrother, P. J.
Biochemistry 1999, 38, 4403-4408.
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- General Base Catalysis by the Phosphatidylchloine-Preferring Phospholipase C from Bacillus cereus: the Role of Glu4 and Asp55
Martin, S. F.; Hergenrother, P. J.
Biochemistry 1998, 37, 5755-5760.
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- Enzymatic Synthesis of a Modified Phospholipid and its Evaluation as a Substrate for B. cereus Phospholipase C
Martin, S. F.; Hergenrother, P. J.
Bioorg. Med. Chem. Lett. 1998, 8, 593-596.
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- Determination of the Kinetic Parameters for Phospholipase C (Bacillus cereus) on Different Phospholipid Substrates Using a Chromogenic Assay Based on the Quantitation of Inorganic Phosphate
Hergenrother, P. J.; Martin, S. F.
Anal. Biochem. 1997, 251, 45-49.
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- Chromogenic Assay for Phospholipase D from Streptomyces chromofuscus: Application to the Evaluation of Substrate Analogues
Hergenrother, P. J.; Martin, S. F.; Haas, M. K.
Lipids 1997, 32, 783-788.
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- Expression and Site-Directed Mutagenesis of the Phosphatidylcholine-Preferring Phospholipase C from Bacillus cereus: Probing the Role of Active Site Glu146
Martin, S. F.; Spaller, M. R.; Hergenrother, P. J.
Biochemistry 1996, 35, 12970-12977.
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- Chromogenic Assay for Phospholipase C from Bacillus cereus
Hergenrother, P. J.; Spaller, M. R.; Haas, M. K.; Martin, S. F.
Anal. Biochem. 1995, 229, 313-316.
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