Paul Hergenrother

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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. J., 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

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

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

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
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

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

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

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

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

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

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

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

Natural products as starting points for the synthesis of complex and diverse compounds

Morrison, K. C. & Hergenrother, P. J., Jan 1 2014, In : Natural Product Reports. 31, 1, p. 6-14 9 p.

Research output: Contribution to journalArticle

Synthesis of bridged oxafenestranes from pleuromutilin

Hicklin, R. W., Lõpez Silva, T. L. & Hergenrother, P. J., Sep 8 2014, In : Angewandte Chemie - International Edition. 53, 37, p. 9880-9883 4 p.

Research output: Contribution to journalArticle

Synthesis of complex and diverse compounds through ring distortion of abietic acid

Rafferty, R. J., Hicklin, R. W., Maloof, K. A. & Hergenrother, P. J., Jan 3 2014, In : Angewandte Chemie - International Edition. 53, 1, p. 220-224 5 p.

Research output: Contribution to journalArticle

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., Apr 30 2014, In : Journal of the American Chemical Society. 136, 17, p. 6355-6361 7 p.

Research output: Contribution to journalArticle

Total synthesis, stereochemical assignment, and biological activity of all known (-)-trigonoliimines

Han, S., Morrison, K. C., Hergenrother, P. J. & Movassaghi, M., Jan 17 2014, In : Journal of Organic Chemistry. 79, 2, p. 473-486 14 p.

Research output: Contribution to journalArticle

2013

A ring-distortion strategy to construct stereochemically complex and structurally diverse compounds from natural products

Huigens, R. W., Morrison, K. C., Hicklin, R. W., Timothy, T. A., Richter, M. F. & Hergenrother, P. J., Mar 1 2013, In : Nature Chemistry. 5, 3, p. 195-202 8 p.

Research output: Contribution to journalArticle

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., Oct 14 2013, In : Organic and Biomolecular Chemistry. 11, 38, p. 6588-6596 9 p.

Research output: Contribution to journalArticle

Detection of endogenous MazF enzymatic activity in Staphylococcus aureus

Van Rensburg, J. J. & Hergenrother, P. J., Jan 1 2013, In : Analytical Biochemistry. 443, 1, p. 81-87 7 p.

Research output: Contribution to journalArticle

Dual targeting of the warburg effect with a glucose-conjugated lactate dehydrogenase inhibitor

Calvaresi, E. C., Granchi, C., Tuccinardi, T., Di Bussolo, V., Huigens, R. W., Lee, H. Y., Palchaudhuri, R., Macchia, M., Martinelli, A., Minutolo, F. & Hergenrother, P. J., Nov 25 2013, In : ChemBioChem. 14, 17, p. 2263-2267 5 p.

Research output: Contribution to journalArticle

Efficient NQO1 substrates are potent and selective anticancer agents

Parkinson, E. I., Bair, J. S., Cismesia, M. & Hergenrother, P. J., Oct 18 2013, In : ACS chemical biology. 8, 10, p. 2173-2183 11 p.

Research output: Contribution to journalArticle

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., Apr 7 2013, In : Lab on a chip. 13, 7, p. 1247-1256 10 p.

Research output: Contribution to journalArticle

Glucose conjugation for the specific targeting and treatment of cancer

Calvaresi, E. C. & Hergenrother, P. J., May 7 2013, In : Chemical Science. 4, 6, p. 2319-2333 15 p.

Research output: Contribution to journalArticle

Synthesis and anticancer activity of all known (-)-agelastatin alkaloids

Han, S., Siegel, D. S., Morrison, K. C., Hergenrother, P. J. & Movassaghi, M., Dec 6 2013, In : Journal of Organic Chemistry. 78, 23, p. 11970-11984 15 p.

Research output: Contribution to journalArticle

Synthesis and anticancer activity of epipolythiodiketopiperazine alkaloids

Boyer, N., Morrison, K. C., Kim, J., Hergenrother, P. J. & Movassaghi, M., Mar 4 2013, In : Chemical Science. 4, 4, p. 1646-1657 12 p.

Research output: Contribution to journalArticle