Publications

Huang, W.; Li, H.; Kiselar, J.; Fink, S. P.; Regmi, S.; Day, A.; Yuan, Y.; Chance, M.; Ready, J. M.; Markowitz, S. D.; Taylor, D. J. Small molecule inhibitors of 15-PGDH exploit a physiologic induced-fit closing system. Nature Commun. 2023, 14.

Imlay, L. S.; Lawong, A. K.; Gahalawat, S.; Kumar, A.; Xing, C.; Mittal, N.; Wittlin, S.; Churchyard, A.; Niederstrasser, H.; Crespo-Fernandez, B.; Posner, B. A.; Gamo, F.-J.; Baum, J.; Winzeler, E. A.; Laleu, B.; Ready, J. M.; Phillips, M. A. Fast-killing tyrosine amide ((S)-SW228703) with blood- and liver-stage antimalarial activity associated with the cyclic amine resistance locus (PfCARL). ACS Infectious Diseases 2023. PMID: 36763526.

Hu, B.; Toda, K.; Wang, X.; Antczak, M. I.; Smith, J.; Geboers, S.; Nishikawa, G.; Li, H.; Dawson, D.; Fink, S.; Desai, A. B.; Williams, N. S.; Markowitz, S. D.; Ready, J. M. Orally bioavailable quinoxaline inhibitors of 15-prostaglandin dehydrogenase (15-PGDH) promote tissue repair and regeneration. J. Med. Chem. 2022, 65, 15327-15343. PMID: 36322935. NIHMSID: 1860950.

Chen, R.; Wang, J.; Gradinaru, I.; Vu, H. S.; Geboers, S.; Naidoo, J.; Ready, J.M.; Williams, N.S.; DeBerardinis, R.J.; Ross, E.M.; Collins, J.J. A male-derived non-ribosomal peptide pheromone controls female schistosome development. Cell, 2022, 185, 1506-1520. PMID: 35385687

Jia, Y.; Li, L.; Lin, Y.-H.; Gopal, P.; Shen, S.; Zhou, K.; Yu, X.; Sharma, T.; Zhang, Y.; Siegwart, D. J.; Ready, J. M.; Zhu, H. In vivo CRISPR screening identifies BAZ2 chromatin remodelers as druggable regulators of mammalian liver regeneration. Cell Stem Cell 2022.

White, K.; Esparza, M.; Liang, J.; Bhat, P.; Naidoo, J.; McGovern, B. L.; Williams, M. A. P.; Alabi, B. R.; Shay, J.; Niederstrasser, H.; Posner, B.; García-Sastre, A.; Ready, J.; Fontoura, B. M. A. Aryl sulfonamide inhibits entry and replication of diverse influenza viruses via the hemagglutinin protein. J. Med. Chem. 2021, 64, 10951-10966.

Lawong, A.; Gahalawat, S.; Okombo, J.; Striepen, J.; Yeo, T.; Mok, S.; Deni, I.; Bridgford, J. L.; Niederstrasser, H.; Zhou, A.; Posner, B.; Wittlin, S.; Gamo, F. J.; Crespo, B.; Churchyard, A.; Baum, J.; Mittal, N.; Winzeler, E.; Laleu, B.; Palmer, M. J.; Charman, S. A.; Fidock, D. A.; Ready, J. M.; Phillips, M. A. Novel antimalarial tetrazoles and amides active against the hemoglobin degradation pathway in Plasmodium falciparum. J. Med. Chem. 2021, 64, 2739-2761. PMID: 33620219. DOI: 10.1021/acs.jmedchem.0c02022.

Smith, J. N. P.; Otegbeye, F.; Jogasuria, A. P.; Christo, K. F.; Antczak, M. I.; Ready, J. M.; Gerson, S. L.; Markowitz, S. D.; Desai, A. B. Inhibition of 15-PGDH protects mice from immune-mediated bone marrow failure. Biol. Blood Marrow Transplantation 2020, 26, 1552-1556. PMID: 32422251.

Williams, N.S.; Gonzaels, S.; Naidoo, J.; Rivera-Cancel, G.; Voruganti, S.; Mallipeddi, P.; Theodoropoulos, P.C.; Geboers, S.; Chen, H.; Ortiz, F.; Posner, B.; Nijhawan, D.; Ready, J.M. Tumor-Activated Benzothiazole Inhibitors of Stearoyl-CoA Desaturase. J. Med. Chem. 2020, 9773-9786. PMID: 32787093.

Ullah, I.; Gahalawat, S.; Booshehri, L; Niederstrasser, H.; Majumdar, S.; Leija, C.; Bradford, J. M.; Hu, B.; Ready, J. M.; Wetzel, D. M. An Antiparasitic Compound from the Medicines for Malaria Venture Pathogen Box Promotes Leishmania Tubulin Polymerization. ACS Infect. Dis. 2020, 6, 2057-2072. PMID: 32686409.

Madhusudhan, N; Hu, B.; Mishra, P.; Calva-Moreno, J. F.; Patel, K.; Boriack, R.; Ready, J. M.; Nijhawan. D. Target discovery of selective non-small-cell lung cancer toxins reveals inhibitors of mitochondrial complex I. ACS Chem. Bio., 2020, 15, 158-170. PMID: 31874028.

Esparza, M.; Mor. A.; Niederstrasser, H.; White, L.; White, A.; Zhang, K.; Gao, S.; Wang, J.; Liang, J.; Sho, S.; Sakthivel, R.; Sathe, A.; Xing, C.; Muñoz-Moreno, R.; Shay, J.; García-Sastre, S.; Ready, J.; Posner, B.; Fontoura, B. M. Chemical Intervention of Influenza Virus mRNA Nuclear Export. PLoS Pathogens, 2020, PMID: 32240278.

Luthra, P.; Naidoo, J.; Pietzsch, C.A.; De, S.; Khadka, S.; Anantpadma, M.; Williams, C.G.; Edwards, M.R.; Davey, R.A.; Bukreyev, A.; Ready, J.M.; Basler, C.F. Inhibiting pyrimidine biosynthesis impairs Ebola virus replication through depletion of nucleoside pools and activation of innate immune responses. Antiviral Res. 2018, 158, 288-302. PMID: 30144461.

Winterton, S. E.; Capota, E.; Wang, X.; Chen, H.; Mallipeddi, P. L.; Williams, N. S.; Posner, B. A.; Nijhawan, D.*; Ready, J. M.* Discovery of Cytochrome P450 4F11 Activated Inhibitors of Stearoyl Coenzyme A Desaturase. J. Med. Chem. 2018, 61, 5199-5221. PMID: 29869888.

Desai, A.; Zhang, Y.; Park, Y.; Dawson, D.M.; Larusch, G.A.; Kasturi, L.; Wald, D.; Ready, J.M.; Gerson, S.L.; Markowtiz, S.D. A second-generation 15-PGDH inhibitor promotes bone marrow transplant recovery independently of age, transplant dose, and granulocyte colony-stimulating factor support. Haematologica, 2018, 103, 1054-1064. PMID: 29472361.

Luthra, P.; Liang, J.; Pietzsch, C.A.; Khada, S.; Edwards, M.R.; Wei, S.; De, S.; Posner, B.; Bukreyev, A.; Ready, J.M.; Basler, C.F. A high throughput screen identified benzoquinoline compounds as inhibitors of Ebola virus replication. Antiviral Res. 2018, 150, 193-201. PMID: 29294299.

Kishore, A.H.; Liang, H.; Kanchwala, M.; Xing, C.; Ganesh, T.; Akgul, Y.; Posner, B.; Ready, J.M.; Markowitz, S.D.; Word, A.R. Prostaglandin dehydrogenase is a target for successful induction of cervical ripening. Proc. Natl. Acad. Sci., 2017, E4627. PMID: 28716915.

Antczak, M. I.; Zhang, Y.; Wang, C.; Doran, J.; Naidoo, J.; Voruganti, S.; Williams, N, S.; Markowitz, S.D.*; Ready, J.M.* Inhibitors of 15-Prostaglandin Dehydrogenase to Potentiate Tissue Repair. J. Med. Chem. 2017, 60, 3979-4001. PMID: 28398755.

Rujirawanich, J.; Kim, S.; Ma, A.-J.; Butler, JR.; Wang, C.; Rosen, M.; Posner, B.; Nijhawan, D.; Ready, J.M.* Synthesis and Biological Evaluation of Kibdelone C and Its Simplified Derivatives. J. Am. Chem. Soc. 2016, 138, 10561-10570. PMID: 27459345.

Theodoropoulos, P.C.; Gonzales, S.G.; Winterton, S.E.; Rodriguez-Navas, C.; McKnight, J.S.; Morlock, L.K.; Owen, A.E.; Duan, Y.; Moreno, J.R.; Hanson, J.M.; Cross, B.; Lemoff, A.; Mirzaei, H.; Posner, B.A.; Williams, N.S.; Ready*, J.M.; Nijhawan, D.* Discovery of Tumor-Specific Irreversible Inhibitors of Stearoyl CoA Desaturase. Nature Chem Biol, 2016, 12, 218-225. PMID: 26829472.

Zhang, Y.; Desai, A.; Yang, S. Y.; Bae, K. B.; Antczak, M. I.; Fink, S. P;. Tiwari, S.; Willis, J. E.; Williams, N. S.; Dawson, D. M.; Wald, D.; Chen, W.; Wang, Z.; Kasturi, L.; Larusch, G.; He, L.; Cominelli, F.; Di Martino, L.; Cjuric, Z.; Milne, G. L.; Chance, M.; Sanabria, J.; Dealwis, Ch.; Mikkola, D.; Naidoo, J.; Wei, S.; Tai, H.; Gerson, S. L.; Ready, J. M.*; Posner, B.*; Willson, J. K. V.*; Markowitz, S. D.* Inhibition of the prostaglandin- degrading enzyme 15-PGDH potentiates tissue regeneration. Science 2015, 348, aaa2340. PMID: 26068857

Jesus-Cortes, H. D.; Miller, A. D.; Britt, J. K.; DeMarco, A. J.; Jesus-Cortes, M. D.; Stubing, E.; Naidoo, J.; Vazquez-Rosa, E.; Morlock, L; Williams, N. S.; Ready, J. M.; Narayanan, N. S.; Pieper, A. A.* Protective efficacy of P7C3-S243 in the 6-hydroxydopamine model of Parkinson’s disease. NPJ Parkinson’s Disease, 2015, 15010. PMID: 27158662.

Walker, A. K.; Rivera, P. D.; Wang, Q.; Chuang, J.-C.; Tran, S.; Osborne-Lawrence, S.; Estill, S. J.; Starwalt, R.; Huntington, P.; Morlock, L.; Naidoo, J.; Williams, N.; Ready, J. M.; Eisch, A. J.; Piper, A. A.*; Zigman, J. M.* The P7C3-class of neuroprotective compounds exerts antidepressant efficacy in mice by increasing hippocampal neurogenesis. Mol. Psychiatry 2015, 20, 500-8. PMID:24751964.

Kemp, S. W. P.; Szynkaruk, M.; Stanoulis, K. N.; Wood, M. D.; Liu, E. H.; Willand, M. P.; Morlock, L.; Naidoo, J; Williams, N. S.; Ready, J. M.; Namgano, T. J.; Beggs, S.; Salter, M. W.; Gordon, T; Pieper, A. A.*; Borschel, G. H.* Pharmacologic rescue of motor and sensory neurons by the neuroprotective compound P7C3 following neonatal nerve injury. Neuroscience, 2014, 284, 202-16. PMID: 25313000.

Wang, G.; Han, T,; Nijhawan, D.; Theodoropoulos, P.; Naidoo, J.; Yadavalli, S.; Mirzaei, H.; Pieper, A.; Ready, J. M.,* McKnight, S. L.* The P7C3 Class of Neuroprotective Chemicals Function by Activating the Rate-limiting Enzyme in NAD Salvage. Cell 2014, 158, 1324-1334. PMID: 25215490.

Yin, T.C.; Britt, J.K.; De Jesus-Cortes, H.; Lu, Y.; Genova, R.M.; Khan, M.Z.; Voorhees, J.R; Shao, J.; Katzman, A.C.; Huntington, P.J.; Wassink, C.; McDaniel, L.; Newell, E.A.; Dutca, L.M.; Naidoo, J.; Cui, H.; Bassuk, A.G.; Harper, M.M.; McKnight, S.L.; Ready, J.M.; Pieper, A.A. P7C3 Neuroprotective Chemicals Block Axonal Degeneration and Preserve Function after Traumatic Brain Injury. Cell Reports 2014, 8, 1731-1740. PMID: 25220467.

Naidoo, J.; De Jesus-Cortes, H.; Huntington, P.; Estill, S; Morlock, L. K.; Starwalt, R.; Mangano, T. J.; Williams, N. S.; Pieper, A. A.*; Ready, J. M.* Discovery or a Neuroprotective Chemical, (S)-N-(3-(3,6-Dibromo-9H-carbazol-9-yl)-2-fluoropropyl)-6-methoxypyridine-2-amine [(-)-P7C3-S243], with Improved Druglike Properties. J. Med. Chem. 2014, 57, 3746. PMID: 24697290.

Pieper, A. A.; McKnight, S. L.; Ready, J. M.* P7C3 and an unbiased approach to drug discovery for neurodegenerative diseases. Chem. Soc. Rev. 2014, 43, 6716-6726. PMID:24514864.

Brown, C.S.; Lee, M.S.; Leung, D.W.; Wang, T.; Xu, W.; Luthra, P.; Anantpadma, M.; Shabman, R.S.; Melito, L.M.; MacMillan, K.S.; Borek, D.M.; Otwinowski, Z.; Ramanan, P.; Stubbs, A.J.; Peterson, D.S.; Binning, J.M.; Tonelli, M.; Olson, M.A.; Davey, R.; Ready, J.M.; Basler, C.F.; Amarasinghe, G.K.* In silico derived small molecules bind the filovirus VP35 protein and inhibit its polymerase cofactor activity, J. Mol. Biol. 2014, 2045. PMID: 24495995.

Kilgore, J. A.; Du, X.; Melito, L.; Wei, S.; Wang, C.; Chin, H. G.; Posner, B.; Pradhan, S.; Ready, J. M.; Williams, N. S.* Identification of DNMT1 Selective Antagonists Using a Novel Scintillation Proximity Assay. J. Biol. Chem. 2013, 288, 19673. PMID: 23671287.

Naidoo, J.; Bemben, C. J.; Allwein, S. R.; Liang, J.; Pieper, A. A.; Ready, J. M.* Development of a Scalable Synthesis of P7C3-A20, a Potent Neuroprotective Agent. Tetrahedron Lett. 2013, 54, 4429.

De Jesús-Cortés, H.; Xu, P.; Drawbridge, J.; Estill, S. J.; Huntington, P.; Tran, S.; Britt, J.; Tesla, R.; Morlock, L.; Naidoo, J.; Melito, L. M.; Williams, N. S.; Ready, J. M.*; McKnight, S. L.*; Pieper, A. A.* Neuroprotective Efficacy of Aminopropyl Carbazoles in a Mouse Model of Parkinson’s Disease. Proc. Natl. Acad. Sci. USA, 2012, 109, 17010. PMID: 23027934.

Tesla, R.; Wolf, H. P.; Xu, P.; Drawbridge, J.; Estill, S. J.; Huntington, P.; McDaniel, L.; Knobbe, W.; Morlock, L.; Naidoo, J.; Williams, N. S.; Ready, J. M.*; McKnight, S. L.*; Pieper, A. A.* Neuroprotective Efficacy of Aminopropyl Carbazoles in a Mouse Model of Amyotrophic Lateral Sclerosis. Proc. Natl. Acad. Sci. USA, 2012, 109, 17016. PMID: 23027932.

MacMillan, K.S.; Naidoo, J.; Liang, J.; Melito, L.; Williams, N.S.; Morlock, L.; Huntington, P.J.; Estill, S.J.; Longgood, J.;. McKnight, S.L.; Pieper, A.A.; De Brabander, J.K, Ready, J.M.* Development of Proneurogenic, Neuroprotective Small Molecules. J. Am. Chem. Soc. 2011, 133, 1428-1437. PMID: 21210688.

Pieper, A.A.; Xie, S.; Capota, E.; Estill, S.J.; Zhong, J.; Long, J.M.; Becker, G.L.; Huntington.; Goldman, S.E.; Shen, C.H.; Capota, M.; Britt, J.K.; Kotti, T.; Brat, D. J.; Williams, N.S.; MacMillan, K.S.; Naidoo, J.; Melito, L.; Hsieh, J.; De Brabander, J.; Ready, J.M.; McKnight, S.L.* Discovery of a Pro-Neurogenic, Neuroprotective Chemical. Cell 2010, 142, 39-51.

Germanas, J. P.; Wang, S.; Miner, A.; Hao, W.; Ready, J. M.* Discovery of Small-Molecule Inhibitors of Tyrosinase. Bioorg. Med. Chem. Lett. 2007, 6871-6875.