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The DHODH inhibitor PTC299 arrests SARS-CoV-2 replication and suppresses induction of inflammatory cytokines.
Luban J, Sattler RA, Mühlberger E, Graci JD, Cao L, Weetall M, Trotta C, Colacino JM, Bavari S, Strambio-De-Castillia C, Suder EL, Wang Y, Soloveva V, Cintron-Lue K, Naryshkin NA, Pykett M, Welch EM, O'Keefe K, Kong R, Goodwin E, Jacobson A, Paessler S, Peltz SW. Luban J, et al. Among authors: graci jd. Virus Res. 2021 Jan 15;292:198246. doi: 10.1016/j.virusres.2020.198246. Epub 2020 Nov 26. Virus Res. 2021. PMID: 33249060 Free PMC article.
Targeting of Hematologic Malignancies with PTC299, A Novel Potent Inhibitor of Dihydroorotate Dehydrogenase with Favorable Pharmaceutical Properties.
Cao L, Weetall M, Trotta C, Cintron K, Ma J, Kim MJ, Furia B, Romfo C, Graci JD, Li W, Du J, Sheedy J, Hedrick J, Risher N, Yeh S, Qi H, Arasu T, Hwang S, Lennox W, Kong R, Petruska J, Moon YC, Babiak J, Davis TW, Jacobson A, Almstead NG, Branstrom A, Colacino JM, Peltz SW. Cao L, et al. Among authors: graci jd. Mol Cancer Ther. 2019 Jan;18(1):3-16. doi: 10.1158/1535-7163.MCT-18-0863. Epub 2018 Oct 23. Mol Cancer Ther. 2019. PMID: 30352802 Free PMC article.
The DHODH Inhibitor PTC299 Arrests SARS-CoV-2 Replication and Suppresses Induction of Inflammatory Cytokines.
Luban J, Sattler R, Mühlberger E, Graci JD, Cao L, Weetall M, Trotta C, Colacino JM, Bavari S, Strambio-De-Castillia C, Suder EL, Wang Y, Soloveva V, Cintron-Lue K, Naryshkin NA, Pykett M, Welch EM, O'Keefe K, Kong R, Goodwin E, Jacobson A, Paessler S, Peltz S. Luban J, et al. Among authors: graci jd. bioRxiv [Preprint]. 2020 Aug 5:2020.08.05.238394. doi: 10.1101/2020.08.05.238394. bioRxiv. 2020. PMID: 32793904 Free PMC article. Updated. Preprint.
Emvododstat, a Potent Dihydroorotate Dehydrogenase Inhibitor, Is Effective in Preclinical Models of Acute Myeloid Leukemia.
Branstrom A, Cao L, Furia B, Trotta C, Santaguida M, Graci JD, Colacino JM, Ray B, Li W, Sheedy J, Mollin A, Yeh S, Kong R, Sheridan R, Baird JD, O'Keefe K, Spiegel R, Goodwin E, Keating S, Weetall M. Branstrom A, et al. Among authors: graci jd. Front Oncol. 2022 Feb 9;12:832816. doi: 10.3389/fonc.2022.832816. eCollection 2022. Front Oncol. 2022. PMID: 35223511 Free PMC article.
Identification of PTC725, an orally bioavailable small molecule that selectively targets the hepatitis C Virus NS4B protein.
Gu Z, Graci JD, Lahser FC, Breslin JJ, Jung SP, Crona JH, McMonagle P, Xia E, Liu S, Karp G, Zhu J, Huang S, Nomeir A, Weetall M, Almstead NG, Peltz SW, Tong X, Ralston R, Colacino JM. Gu Z, et al. Among authors: graci jd. Antimicrob Agents Chemother. 2013 Jul;57(7):3250-61. doi: 10.1128/AAC.00527-13. Epub 2013 Apr 29. Antimicrob Agents Chemother. 2013. PMID: 23629699 Free PMC article.
Small molecule splicing modifiers with systemic HTT-lowering activity.
Bhattacharyya A, Trotta CR, Narasimhan J, Wiedinger KJ, Li W, Effenberger KA, Woll MG, Jani MB, Risher N, Yeh S, Cheng Y, Sydorenko N, Moon YC, Karp GM, Weetall M, Dakka A, Gabbeta V, Naryshkin NA, Graci JD, Tripodi T Jr, Southwell A, Hayden M, Colacino JM, Peltz SW. Bhattacharyya A, et al. Among authors: graci jd. Nat Commun. 2021 Dec 15;12(1):7299. doi: 10.1038/s41467-021-27157-z. Nat Commun. 2021. PMID: 34911927 Free PMC article.
Discovery of novel HCV inhibitors: synthesis and biological activity of 6-(indol-2-yl)pyridine-3-sulfonamides targeting hepatitis C virus NS4B.
Zhang X, Zhang N, Chen G, Turpoff A, Ren H, Takasugi J, Morrill C, Zhu J, Li C, Lennox W, Paget S, Liu Y, Almstead N, Njoroge FG, Gu Z, Komatsu T, Clausen V, Espiritu C, Graci J, Colacino J, Lahser F, Risher N, Weetall M, Nomeir A, Karp GM. Zhang X, et al. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3947-53. doi: 10.1016/j.bmcl.2013.04.049. Epub 2013 Apr 30. Bioorg Med Chem Lett. 2013. PMID: 23683597
Structure-activity relationship (SAR) optimization of 6-(indol-2-yl)pyridine-3-sulfonamides: identification of potent, selective, and orally bioavailable small molecules targeting hepatitis C (HCV) NS4B.
Zhang N, Zhang X, Zhu J, Turpoff A, Chen G, Morrill C, Huang S, Lennox W, Kakarla R, Liu R, Li C, Ren H, Almstead N, Venkatraman S, Njoroge FG, Gu Z, Clausen V, Graci J, Jung SP, Zheng Y, Colacino JM, Lahser F, Sheedy J, Mollin A, Weetall M, Nomeir A, Karp GM. Zhang N, et al. J Med Chem. 2014 Mar 13;57(5):2121-35. doi: 10.1021/jm401621g. Epub 2013 Dec 4. J Med Chem. 2014. PMID: 24266880
26 results