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Imidazotetrazines as Weighable Diazomethane Surrogates for Esterifications and Cyclopropanations.

Svec RL, Hergenrother PJ.

Angew Chem Int Ed Engl. 2019 Dec 2. doi: 10.1002/anie.201911896. [Epub ahead of print] Review.


Implementation of permeation rules leads to a FabI inhibitor with activity against Gram-negative pathogens.

Parker EN, Drown BS, Geddes EJ, Lee HY, Ismail N, Lau GW, Hergenrother PJ.

Nat Microbiol. 2020 Jan;5(1):67-75. doi: 10.1038/s41564-019-0604-5. Epub 2019 Nov 18.


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

Janin M, Ortiz-Barahona V, de Moura MC, Martínez-Cardús A, Llinàs-Arias P, Soler M, Nachmani D, Pelletier J, Schumann U, Calleja-Cervantes ME, Moran S, Guil S, Bueno-Costa A, Piñeyro D, Perez-Salvia M, Rosselló-Tortella M, Piqué L, Bech-Serra JJ, De La Torre C, Vidal A, Martínez-Iniesta M, Martín-Tejera JF, Villanueva A, Arias A, Cuartas I, Aransay AM, La Madrid AM, Carcaboso AM, Santa-Maria V, Mora J, Fernandez AF, Fraga MF, Aldecoa I, Pedrosa L, Graus F, Vidal N, Martínez-Soler F, Tortosa A, Carrato C, Balañá C, Boudreau MW, Hergenrother PJ, Kötter P, Entian KD, Hench J, Frank S, Mansouri S, Zadeh G, Dans PD, Orozco M, Thomas G, Blanco S, Seoane J, Preiss T, Pandolfi PP, Esteller M.

Acta Neuropathol. 2019 Dec;138(6):1053-1074. doi: 10.1007/s00401-019-02062-4. Epub 2019 Aug 19.


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

Boudreau MW, Peh J, Hergenrother PJ.

ACS Chem Biol. 2019 Nov 15;14(11):2335-2348. doi: 10.1021/acschembio.9b00338. Epub 2019 Jul 16.


Editorial overview: From the iceman to modern medicine.

Aye Y, Hergenrother PJ.

Curr Opin Chem Biol. 2019 Jun;50:A1-A2. doi: 10.1016/j.cbpa.2019.04.021. Epub 2019 Jun 6. No abstract available.


Diverse compounds from pleuromutilin lead to a thioredoxin inhibitor and inducer of ferroptosis.

Llabani E, Hicklin RW, Lee HY, Motika SE, Crawford LA, Weerapana E, Hergenrother PJ.

Nat Chem. 2019 Jun;11(6):521-532. doi: 10.1038/s41557-019-0261-6. Epub 2019 May 13.


Structural analyses of NudT16-ADP-ribose complexes direct rational design of mutants with improved processing of poly(ADP-ribosyl)ated proteins.

Thirawatananond P, McPherson RL, Malhi J, Nathan S, Lambrecht MJ, Brichacek M, Hergenrother PJ, Leung AKL, Gabelli SB.

Sci Rep. 2019 Apr 11;9(1):5940. doi: 10.1038/s41598-019-39491-w.


Immunohistochemical Characterization of Procaspase-3 Overexpression as a Druggable Target With PAC-1, a Procaspase-3 Activator, in Canine and Human Brain Cancers.

Schlein LJ, Fadl-Alla B, Pondenis HC, Lezmi S, Eberhart CG, LeBlanc AK, Dickinson PJ, Hergenrother PJ, Fan TM.

Front Oncol. 2019 Feb 25;9:96. doi: 10.3389/fonc.2019.00096. eCollection 2019.


Enantioselective Synthesis of Isocarbostyril Alkaloids and Analogs Using Catalytic Dearomative Functionalization of Benzene.

Bingham TW, Hernandez LW, Olson DG, Svec RL, Hergenrother PJ, Sarlah D.

J Am Chem Soc. 2019 Jan 9;141(1):657-670. doi: 10.1021/jacs.8b12123. Epub 2018 Dec 20.


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

Rack JGM, Ariza A, Drown BS, Henfrey C, Bartlett E, Shirai T, Hergenrother PJ, Ahel I.

Cell Chem Biol. 2018 Dec 20;25(12):1533-1546.e12. doi: 10.1016/j.chembiol.2018.11.001. Epub 2018 Nov 21.


Oxygen Starvation Unmasks a Killer.

Svec RL, Hergenrother PJ.

Cell Chem Biol. 2018 Nov 15;25(11):1313-1314. doi: 10.1016/j.chembiol.2018.10.028.


Monitoring Poly(ADP-ribosyl)glycohydrolase Activity with a Continuous Fluorescent Substrate.

Drown BS, Shirai T, Rack JGM, Ahel I, Hergenrother PJ.

Cell Chem Biol. 2018 Dec 20;25(12):1562-1570.e19. doi: 10.1016/j.chembiol.2018.09.008. Epub 2018 Oct 11.


Tunable Stability of Imidazotetrazines Leads to a Potent Compound for Glioblastoma.

Svec RL, Furiassi L, Skibinski CG, Fan TM, Riggins GJ, Hergenrother PJ.

ACS Chem Biol. 2018 Nov 16;13(11):3206-3216. doi: 10.1021/acschembio.8b00864. Epub 2018 Nov 8.


Preparation of Structurally Diverse Compounds from the Natural Product Lycorine.

Tasker SZ, Cowfer AE, Hergenrother PJ.

Org Lett. 2018 Sep 21;20(18):5894-5898. doi: 10.1021/acs.orglett.8b02562. Epub 2018 Sep 11.


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

Peh J, Boudreau MW, Smith HM, Hergenrother PJ.

Cell Chem Biol. 2018 Aug 16;25(8):996-1005.e4. doi: 10.1016/j.chembiol.2018.05.008. Epub 2018 Jun 14.


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

Livezey M, Huang R, Hergenrother PJ, Shapiro DJ.

Cell Death Differ. 2018 Oct;25(10):1796-1807. doi: 10.1038/s41418-018-0143-2. Epub 2018 Jun 13.


Going on offense against the gram-negative defense.

Drown BS, Hergenrother PJ.

Proc Natl Acad Sci U S A. 2018 Jun 26;115(26):6530-6532. doi: 10.1073/pnas.1807278115. Epub 2018 May 25. No abstract available.


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

Richter MF, Hergenrother PJ.

Ann N Y Acad Sci. 2019 Jan;1435(1):18-38. doi: 10.1111/nyas.13598. Epub 2018 Feb 15. Review.


How many human proteoforms are there?

Aebersold R, Agar JN, Amster IJ, Baker MS, Bertozzi CR, Boja ES, Costello CE, Cravatt BF, Fenselau C, Garcia BA, Ge Y, Gunawardena J, Hendrickson RC, Hergenrother PJ, Huber CG, Ivanov AR, Jensen ON, Jewett MC, Kelleher NL, Kiessling LL, Krogan NJ, Larsen MR, Loo JA, Ogorzalek Loo RR, Lundberg E, MacCoss MJ, Mallick P, Mootha VK, Mrksich M, Muir TW, Patrie SM, Pesavento JJ, Pitteri SJ, Rodriguez H, Saghatelian A, Sandoval W, Schlüter H, Sechi S, Slavoff SA, Smith LM, Snyder MP, Thomas PM, Uhlén M, Van Eyk JE, Vidal M, Walt DR, White FM, Williams ER, Wohlschlager T, Wysocki VH, Yates NA, Young NL, Zhang B.

Nat Chem Biol. 2018 Feb 14;14(3):206-214. doi: 10.1038/nchembio.2576.


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 AD, Botham RC, Schlein LJ, Roth HS, Mangraviti A, Borodovsky A, Tyler B, Joslyn S, Looper JS, Podell M, Fan TM, Hergenrother PJ, Riggins GJ.

Oncotarget. 2017 Jul 7;8(46):80124-80138. doi: 10.18632/oncotarget.19085. eCollection 2017 Oct 6.


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

Doğanay S, Lee MY, Baum A, Peh J, Hwang SY, Yoo JY, Hergenrother PJ, García-Sastre A, Myong S, Ha T.

Integr Biol (Camb). 2017 Nov 13;9(11):857-867. doi: 10.1039/c7ib00146k.


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 HY, Hergenrother PJ, Minutolo F.

J Agric Food Chem. 2017 Jul 19;65(28):5639-5649. doi: 10.1021/acs.jafc.7b01668. Epub 2017 Jul 7.


Natural products: Taming reactive benzynes.

Tasker SZ, Hergenrother PJ.

Nat Chem. 2017 May 24;9(6):504-506. doi: 10.1038/nchem.2786. No abstract available.


Predictive compound accumulation rules yield a broad-spectrum antibiotic.

Richter MF, Drown BS, Riley AP, Garcia A, Shirai T, Svec RL, Hergenrother PJ.

Nature. 2017 May 18;545(7654):299-304. doi: 10.1038/nature22308. Epub 2017 May 10.


Reactive Oxygen Species Synergize To Potently and Selectively Induce Cancer Cell Death.

Lee HY, Parkinson EI, Granchi C, Paterni I, Panigrahy D, Seth P, Minutolo F, Hergenrother PJ.

ACS Chem Biol. 2017 May 19;12(5):1416-1424. doi: 10.1021/acschembio.7b00015. Epub 2017 Apr 7.


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 AP, Francis JM, Pajak M, Parkinson EI, Wycislo KL, Rosol TJ, Brown ME, London CA, Dirikolu L, Hergenrother PJ, Fan TM.

Invest New Drugs. 2017 Apr;35(2):134-144. doi: 10.1007/s10637-016-0414-z. Epub 2016 Dec 14.


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

Garcia A, Drown BS, Hergenrother PJ.

Org Lett. 2016 Oct 7;18(19):4852-4855. Epub 2016 Sep 21.


Porous photonic crystal external cavity laser biosensor.

Huang Q, Peh J, Hergenrother PJ, Cunningham BT.

Appl Phys Lett. 2016 Aug 15;109(7):071103.


Small-Molecule Procaspase-3 Activation Sensitizes Cancer to Treatment with Diverse Chemotherapeutics.

Botham RC, Roth HS, Book AP, Roady PJ, Fan TM, Hergenrother PJ.

ACS Cent Sci. 2016 Aug 24;2(8):545-59. doi: 10.1021/acscentsci.6b00165. Epub 2016 Jul 25.


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

Zheng X, Andruska N, Lambrecht MJ, He S, Parissenti A, Hergenrother PJ, Nelson ER, Shapiro DJ.

Oncotarget. 2016 Jul 24;9(19):14741-14753. doi: 10.18632/oncotarget.10819. eCollection 2018 Mar 13.


The Combination of Vemurafenib and Procaspase-3 Activation Is Synergistic in Mutant BRAF Melanomas.

Peh J, Fan TM, Wycislo KL, Roth HS, Hergenrother PJ.

Mol Cancer Ther. 2016 Aug;15(8):1859-69. doi: 10.1158/1535-7163.MCT-16-0025. Epub 2016 Jun 13.


A Potent Inhibitor of Protein Sequestration by Expanded Triplet (CUG) Repeats that Shows Phenotypic Improvements in a Drosophila Model of Myotonic Dystrophy.

Luu LM, Nguyen L, Peng S, Lee J, Lee HY, Wong CH, Hergenrother PJ, Chan HY, Zimmerman SC.

ChemMedChem. 2016 Jul 5;11(13):1428-35. doi: 10.1002/cmdc.201600081. Epub 2016 Jun 1.


A Small Molecule that Induces Intrinsic Pathway Apoptosis with Unparalleled Speed.

Palchaudhuri R, Lambrecht MJ, Botham RC, Partlow KC, van Ham TJ, Putt KS, Nguyen LT, Kim SH, Peterson RT, Fan TM, Hergenrother PJ.

Cell Rep. 2015 Dec 1;13(9):2027-36. doi: 10.1016/j.celrep.2015.10.042. Epub 2015 Nov 19.


Molecular medicine and cancer.

Wallace HM, Hergenrother PJ, Sadler PJ.

Chem Soc Rev. 2015 Dec 21;44(24):8771-2. doi: 10.1039/c5cs90123e. Epub 2015 Nov 23. No abstract available.


Deoxynyboquinones as NQO1-Activated Cancer Therapeutics.

Parkinson EI, Hergenrother PJ.

Acc Chem Res. 2015 Oct 20;48(10):2715-23. doi: 10.1021/acs.accounts.5b00365. Epub 2015 Oct 7.


Salicylketoximes That Target Glucose Transporter 1 Restrict Energy Supply to Lung Cancer Cells.

Granchi C, Qian Y, Lee HY, Paterni I, Pasero C, Iegre J, Carlson KE, Tuccinardi T, Chen X, Katzenellenbogen JA, Hergenrother PJ, Minutolo F.

ChemMedChem. 2015 Nov;10(11):1892-900. doi: 10.1002/cmdc.201500320. Epub 2015 Sep 1.


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

Di Bussolo V, Calvaresi EC, Granchi C, Del Bino L, Frau I, Lang MC, Tuccinardi T, Macchia M, Martinelli A, Hergenrother PJ, Minutolo F.

RSC Adv. 2015;5(26):19944-19954.


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

Parkinson EI, Bair JS, Nakamura BA, Lee HY, Kuttab HI, Southgate EH, Lezmi S, Lau GW, Hergenrother PJ.

Nat Commun. 2015 Apr 24;6:6947. doi: 10.1038/ncomms7947.


Removal of Metabolic Liabilities Enables Development of Derivatives of Procaspase-Activating Compound 1 (PAC-1) with Improved Pharmacokinetics.

Roth HS, Botham RC, Schmid SC, Fan TM, Dirikolu L, Hergenrother PJ.

J Med Chem. 2015 May 14;58(9):4046-65. doi: 10.1021/acs.jmedchem.5b00413. Epub 2015 Apr 20.


Synthesis of dimeric ADP-ribose and its structure with human poly(ADP-ribose) glycohydrolase.

Lambrecht MJ, Brichacek M, Barkauskaite E, Ariza A, Ahel I, Hergenrother PJ.

J Am Chem Soc. 2015 Mar 18;137(10):3558-64. doi: 10.1021/ja512528p. Epub 2015 Mar 4.


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

Meng Zhang, Peh J, Hergenrother PJ, Cunningham BT.

Conf Proc IEEE Eng Med Biol Soc. 2014;2014:2073-6. doi: 10.1109/EMBC.2014.6944024.


Synthesis of bridged oxafenestranes from pleuromutilin.

Hicklin RW, López Silva TL, Hergenrother PJ.

Angew Chem Int Ed Engl. 2014 Sep 8;53(37):9880-3. doi: 10.1002/anie.201404765. Epub 2014 Jul 17.


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

Zhang M, Peh J, Hergenrother PJ, Cunningham BT.

J Am Chem Soc. 2014 Apr 23;136(16):5840-3. doi: 10.1021/ja500636p. Epub 2014 Apr 10.


Targeting toxic RNAs that cause myotonic dystrophy type 1 (DM1) with a bisamidinium inhibitor.

Wong CH, Nguyen L, Peh J, Luu LM, Sanchez JS, Richardson SL, Tuccinardi T, Tsoi H, Chan WY, Chan HY, Baranger AM, Hergenrother PJ, Zimmerman SC.

J Am Chem Soc. 2014 Apr 30;136(17):6355-61. doi: 10.1021/ja5012146. Epub 2014 Apr 22.


Dual small-molecule targeting of procaspase-3 dramatically enhances zymogen activation and anticancer activity.

Botham RC, Fan TM, Im I, Borst LB, Dirikolu L, Hergenrother PJ.

J Am Chem Soc. 2014 Jan 29;136(4):1312-9. doi: 10.1021/ja4124303. Epub 2014 Jan 16.


Light activation of Staphylococcus aureus toxin YoeBSa1 reveals guanosine-specific endoribonuclease activity.

Larson AS, Hergenrother PJ.

Biochemistry. 2014 Jan 14;53(1):188-201. doi: 10.1021/bi4008098. Epub 2013 Dec 23.


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

Rafferty RJ, Hicklin RW, Maloof KA, Hergenrother PJ.

Angew Chem Int Ed Engl. 2014 Jan 3;53(1):220-4. doi: 10.1002/anie.201308743. Epub 2013 Nov 24.


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

Morrison KC, Hergenrother PJ.

Nat Prod Rep. 2014 Jan;31(1):6-14. doi: 10.1039/c3np70063a. Review.


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

Calvaresi EC, Granchi C, Tuccinardi T, Di Bussolo V, Huigens RW 3rd, Lee HY, Palchaudhuri R, Macchia M, Martinelli A, Minutolo F, Hergenrother PJ.

Chembiochem. 2013 Nov 25;14(17):2263-7. doi: 10.1002/cbic.201300562. Epub 2013 Oct 31.

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