Paul Hergenrother

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Research Output

2020

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., Jun 17 2020, In : Journal of the American Chemical Society. 142, 24, p. 10856-10862 7 p.

Research output: Contribution to journalArticle

Imidazotetrazines as Weighable Diazomethane Surrogates for Esterifications and Cyclopropanations

Svec, R. L. & Hergenrother, P. J., Jan 27 2020, In : Angewandte Chemie - International Edition. 59, 5, p. 1857-1862 6 p.

Research output: Contribution to journalArticle

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., Fan, T. M. & Hergenrother, P., Jun 18 2020, (In preparation) Cold Spring Harbor Laboratory Press, 35 p. (bioRxiv).

Research output: Working paper

2019

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., Jun 1 2019, In : Nature Chemistry. 11, 6, p. 521-532 12 p.

Research output: Contribution to journalArticle

Editorial overview: From the iceman to modern medicine

Aye, Y. & Hergenrother, P., Jun 2019, In : Current Opinion in Chemical Biology. 50, p. A1-A2

Research output: Contribution to journalEditorial

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., Jan 9 2019, In : Journal of the American Chemical Society. 141, 1, p. 657-670 14 p.

Research output: Contribution to journalArticle

Epigenetic loss of RNA-methyltransferase NSUN5 in glioma targets ribosomes to drive a stress adaptive translational program

Janin, M., Ortiz-Barahona, V., de Moura, M. C., Martínez-Cardús, A., Llinàs-Arias, P., Soler, M., Nachmani, D., Pelletier, J., Schumann, U., Calleja-Cervantes, M. E., Moran, S., Guil, S., Bueno-Costa, A., Piñeyro, D., Perez-Salvia, M., Rosselló-Tortella, M., Piqué, L., Bech-Serra, J. J., De La Torre, C., Vidal, A. & 36 others, Martínez-Iniesta, M., Martín-Tejera, J. F., Villanueva, A., Arias, A., Cuartas, I., Aransay, A. M., La Madrid, A. M., Carcaboso, A. M., Santa-Maria, V., Mora, J., Fernandez, A. F., Fraga, M. F., Aldecoa, I., Pedrosa, L., Graus, F., Vidal, N., Martínez-Soler, F., Tortosa, A., Carrato, C., Balañá, C., Boudreau, M. W., Hergenrother, P. J., Kötter, P., Entian, K. D., Hench, J., Frank, S., Mansouri, S., Zadeh, G., Dans, P. D., Orozco, M., Thomas, G., Blanco, S., Seoane, J., Preiss, T., Pandolfi, P. P. & Esteller, M., Dec 1 2019, In : Acta Neuropathologica. 138, 6, p. 1053-1074 22 p.

Research output: Contribution to journalArticle

Open Access

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., Jan 1 2019, In : Frontiers in Oncology. 9, FEB, 96.

Research output: Contribution to journalArticle

Open Access

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. & Hergenrother, P. J., Nov 18 2019, In : Nature Microbiology.

Research output: Contribution to journalLetter

Procaspase-3 Overexpression in Cancer: A Paradoxical Observation with Therapeutic Potential

Boudreau, M. W., Peh, J. & Hergenrother, P. J., Nov 15 2019, In : ACS chemical biology. 14, 11, p. 2335-2348 14 p.

Research output: Contribution to journalReview article

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., Dec 1 2019, In : Scientific reports. 9, 1, 5940.

Research output: Contribution to journalArticle

Open Access

The challenge of converting gram-positive-only compounds into broad-spectrum antibiotics

Richter, M. F. & Hergenrother, P. J., Jan 1 2019, In : Annals of the New York Academy of Sciences. 1435, 1, p. 18-38 21 p.

Research output: Contribution to journalReview article

2018

(ADP-ribosyl)hydrolases: Structural Basis for Differential Substrate Recognition and Inhibition

Rack, J. G. M., Ariza, A., Drown, B. S., Henfrey, C., Bartlett, E., Shirai, T., Hergenrother, P. J. & Ahel, I., Dec 20 2018, In : Cell chemical biology. 25, 12, p. 1533-1546.e12

Research output: Contribution to journalArticle

Going on offense against the gram-negative defense

Drown, B. S. & Hergenrother, P. J., Jun 26 2018, In : Proceedings of the National Academy of Sciences of the United States of America. 115, 26, p. 6530-6532 3 p.

Research output: Contribution to journalComment/debate

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. & 33 others, 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., Feb 14 2018, In : Nature chemical biology. 14, 3, p. 206-214 9 p.

Research output: Contribution to journalReview article

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., Dec 20 2018, In : Cell chemical biology. 25, 12, p. 1562-1570.e19

Research output: Contribution to journalArticle

Overcoming Resistance to Targeted Anticancer Therapies through Small-Molecule-Mediated MEK Degradation

Peh, J., Boudreau, M. W., Smith, H. M. & Hergenrother, P. J., Aug 16 2018, In : Cell chemical biology. 25, 8, p. 996-1005.e4

Research output: Contribution to journalArticle

Oxygen Starvation Unmasks a Killer

Svec, R. L. & Hergenrother, P., Nov 15 2018, In : Cell chemical biology. 25, 11, p. 1313-1314 2 p.

Research output: Contribution to journalShort survey

Preparation of Structurally Diverse Compounds from the Natural Product Lycorine

Tasker, S. Z., Cowfer, A. E. & Hergenrother, P. J., Sep 21 2018, In : Organic Letters. 20, 18, p. 5894-5898 5 p.

Research output: Contribution to journalArticle

Strong and sustained activation of the anticipatory unfolded protein response induces necrotic cell death

Livezey, M., Huang, R., Hergenrother, P. J. & Shapiro, D. J., Oct 2018, In : Cell Death and Differentiation. 25, 10, p. 1796-1807 12 p.

Research output: Contribution to journalArticle

Targeting multidrug-resistant ovarian cancer through estrogen receptor a dependent ATP depletion caused by hyperactivation of the unfolded protein response

Zheng, X., Andruska, N., Lambrecht, M. J., He, S., Parissenti, A., Hergenrother, P. J., Nelson, E. R. & Shapiro, D. J., Jan 1 2018, In : Oncotarget. 9, 19, p. 14741-14753 13 p.

Research output: Contribution to journalArticle

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., Nov 16 2018, In : ACS chemical biology. 13, 11, p. 3206-3216 11 p.

Research output: Contribution to journalArticle

2017

Characterization of the Saffron Derivative Crocetin as an Inhibitor of Human Lactate Dehydrogenase 5 in the Antiglycolytic Approach against Cancer

Granchi, C., Fortunato, S., Meini, S., Rizzolio, F., Caligiuri, I., Tuccinardi, T., Lee, H. Y., Hergenrother, P. J. & Minutolo, F., Jul 19 2017, In : Journal of Agricultural and Food Chemistry. 65, 28, p. 5639-5649 11 p.

Research output: Contribution to journalArticle

Natural products: Taming reactive benzynes

Tasker, S. Z. & Hergenrother, P. J., May 24 2017, In : Nature Chemistry. 9, 6, p. 504-506 3 p.

Research output: Contribution to journalShort survey

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., Apr 1 2017, In : Investigational New Drugs. 35, 2, p. 134-144 11 p.

Research output: Contribution to journalArticle

Porous photonic crystal external cavity laser biosensor for drug screening

Huang, Q., Peh, J., Hergenrother, P. J. & Cunningham, B. T., Jan 5 2017, IEEE Sensors, SENSORS 2016 - Proceedings. Institute of Electrical and Electronics Engineers Inc., 7808619. (Proceedings of IEEE Sensors).

Research output: Chapter in Book/Report/Conference proceedingConference contribution

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., May 18 2017, In : Nature. 545, 7654, p. 299-304 6 p.

Research output: Contribution to journalArticle

Reaction: Broad-Spectrum Antibiotics, a Call for Chemists

Richter, M. F. & Hergenrother, P. J., Jul 13 2017, In : Chem. 3, 1, p. 10-13 4 p.

Research output: Contribution to journalComment/debate

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., May 19 2017, In : ACS chemical biology. 12, 5, p. 1416-1424 9 p.

Research output: Contribution to journalArticle

Single-cell analysis of early antiviral gene expression reveals a determinant of stochastic: IFNB1 expression

Doǧanay, S., Lee, M. Y., Baum, A., Peh, J., Hwang, S. Y., Yoo, J. Y., Hergenrother, P. J., García-Sastre, A., Myong, S. & Ha, T., Nov 2017, In : Integrative Biology (United Kingdom). 9, 11, p. 857-867 11 p.

Research output: Contribution to journalArticle

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. M., Hergenrother, P. J. & Riggins, G. J., Jan 1 2017, In : Oncotarget. 8, 46, p. 80124-80138 15 p.

Research output: Contribution to journalArticle

2016

Access to a Structurally Complex Compound Collection via Ring Distortion of the Alkaloid Sinomenine

Garcia, A., Drown, B. S. & Hergenrother, P. J., Oct 7 2016, In : Organic Letters. 18, 19, p. 4852-4855 4 p.

Research output: Contribution to journalArticle

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. Y., Lee, H. Y., Wong, C. H., Hergenrother, P. J., Chan, H. Y. E. & Zimmerman, S. C., Jan 1 2016, In : ChemMedChem. 11, 13, p. 1428-1435 8 p.

Research output: Contribution to journalArticle

Derivatives of procaspase-activating compound 1 (PAC-1) and their anticancer activities

Roth, H. S. & Hergenrother, P. J., Jan 1 2016, In : Current Medicinal Chemistry. 23, 3, p. 201-241 41 p.

Research output: Contribution to journalArticle

Porous photonic crystal external cavity laser biosensor

Huang, Q., Peh, J., Hergenrother, P. J. & Cunningham, B. T., Aug 15 2016, In : Applied Physics Letters. 109, 7, 071103.

Research output: Contribution to journalArticle

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., Aug 24 2016, In : ACS Central Science. 2, 8, p. 545-559 15 p.

Research output: Contribution to journalArticle

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., Aug 2016, In : Molecular Cancer Therapeutics. 15, 8, p. 1859-1869 11 p.

Research output: Contribution to journalArticle

2015

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., Dec 1 2015, In : Cell Reports. 13, 9, p. 2027-2036 10 p.

Research output: Contribution to journalArticle

Deoxynybomycins inhibit mutant DNA gyrase and rescue mice infected with fluoroquinolone-resistant bacteria

Parkinson, E. I., Bair, J. S., Nakamura, B. A., Lee, H. Y., Kuttab, H. I., Southgate, E. H., Lezmi, S., Lau, G. W. & Hergenrother, P. J., Apr 22 2015, In : Nature communications. 6, 6947.

Research output: Contribution to journalArticle

Deoxynyboquinones as NQO1-Activated Cancer Therapeutics

Parkinson, E. I. & Hergenrother, P., Oct 20 2015, In : Accounts of chemical research. 48, 10, p. 2715-2723 9 p.

Research output: Contribution to journalArticle

Molecular medicine and cancer

Wallace, H. M., Hergenrother, P. J. & Sadler, P. J., Dec 21 2015, In : Chemical Society Reviews. 44, 24, p. 8771-8772 2 p.

Research output: Contribution to journalEditorial

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., May 14 2015, In : Journal of Medicinal Chemistry. 58, 9, p. 4046-4065 20 p.

Research output: Contribution to journalArticle

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., Nov 1 2015, In : ChemMedChem. 10, 11, p. 1892-1900 9 p.

Research output: Contribution to journalArticle

Synthesis and biological evaluation of non-glucose glycoconjugated N-hydroyxindole class LDH inhibitors as anticancer agents

Di Bussolo, V., Calvaresi, E. C., Granchi, C., Del Bino, L., Frau, I., Dasso Lang, M. C., Tuccinardi, T., Macchia, M., Martinelli, A., Hergenrother, P. J. & Minutolo, F., 2015, In : RSC Advances. 5, 26, p. 19944-19954 11 p.

Research output: Contribution to journalArticle

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., Mar 18 2015, In : Journal of the American Chemical Society. 137, 10, p. 3558-3564 7 p.

Research output: Contribution to journalArticle

2014

Detection of protein-small molecule binding using a self-referencing external cavity laser biosensor

Zhang, M., Peh, J., Hergenrother, P. J. & Cunningham, B. T., Apr 23 2014, In : Journal of the American Chemical Society. 136, 16, p. 5840-5843 4 p.

Research output: Contribution to journalArticle

Detection of protein-small molecule binding using a self-referencing external cavity laser biosensor

Zhang, M., Peh, J., Hergenrother, P. & Cunningham, B. T., Nov 2 2014, 2014 36th Annual International Conference of the IEEE Engineering in Medicine and Biology Society, EMBC 2014. Institute of Electrical and Electronics Engineers Inc., p. 2073-2076 4 p. 6944024. (2014 36th Annual International Conference of the IEEE Engineering in Medicine and Biology Society, EMBC 2014).

Research output: Chapter in Book/Report/Conference proceedingConference contribution

Detection of protein-small molecule binding using a self-referencing external cavity laser biosensor

Zhang, M., Peh, J., Hergenrother, P. J. & Cunningham, B. T., Nov 2 2014, 2014 36th Annual International Conference of the IEEE Engineering in Medicine and Biology Society, EMBC 2014. Institute of Electrical and Electronics Engineers Inc., p. 2073-2076 4 p. 6944024. (2014 36th Annual International Conference of the IEEE Engineering in Medicine and Biology Society, EMBC 2014).

Research output: Chapter in Book/Report/Conference proceedingConference contribution

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., Jan 29 2014, In : Journal of the American Chemical Society. 136, 4, p. 1312-1319 8 p.

Research output: Contribution to journalArticle

Light activation of staphylococcus aureus toxin YoeBSa 1 reveals guanosine-specific endoribonuclease activity

Larson, A. S. & Hergenrother, P. J., Jan 14 2014, In : Biochemistry. 53, 1, p. 188-201 14 p.

Research output: Contribution to journalArticle