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Page 1
Discovery and Preclinical Evaluation of BMS-986242, a Potent, Selective Inhibitor of Indoleamine-2,3-dioxygenase 1.
Cherney EC, Zhang L, Nara S, Zhu X, Gullo-Brown J, Maley D, Lin TA, Hunt JT, Huang C, Yang Z, Darienzo C, Discenza L, Ranasinghe A, Grubb M, Ziemba T, Traeger SC, Li X, Johnston K, Kopcho L, Fereshteh M, Foster K, Stefanski K, Fargnoli J, Swanson J, Brown J, Delpy D, Seitz SP, Borzilleri R, Vite G, Balog A. Cherney EC, et al. Among authors: seitz sp. ACS Med Chem Lett. 2021 Jan 28;12(2):288-294. doi: 10.1021/acsmedchemlett.0c00668. eCollection 2021 Feb 11. ACS Med Chem Lett. 2021. PMID: 33603977 Free PMC article.
SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors.
Zimmermann K, Wittman MD, Saulnier MG, Velaparthi U, Sang X, Frennesson DB, Struzynski C, Seitz SP, He L, Carboni JM, Li A, Greer AF, Gottardis M, Attar RM, Yang Z, Balimane P, Discenza LN, Lee FY, Sinz M, Kim S, Vyas D. Zimmermann K, et al. Among authors: seitz sp. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1744-8. doi: 10.1016/j.bmcl.2010.01.087. Epub 2010 Jan 21. Bioorg Med Chem Lett. 2010. PMID: 20153189
Modulation of cofilin phosphorylation by inhibition of the Lim family kinases.
He L, Seitz SP, Trainor GL, Tortolani D, Vaccaro W, Poss M, Tarby CM, Tokarski JS, Penhallow B, Hung CY, Attar R, Lin TA. He L, et al. Among authors: seitz sp. Bioorg Med Chem Lett. 2012 Sep 15;22(18):5995-8. doi: 10.1016/j.bmcl.2012.07.002. Epub 2012 Jul 21. Bioorg Med Chem Lett. 2012. PMID: 22902653
Development of a series of novel o-phenylenediamine-based indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors.
Williams DK, Markwalder JA, Balog AJ, Chen B, Chen L, Donnell J, Haque L, Hart AC, Mandal SK, Nation A, Shan W, Vite GD, Covello K, Hunt JT, Jure-Kunkel MN, Seitz SP. Williams DK, et al. Among authors: seitz sp. Bioorg Med Chem Lett. 2018 Feb 15;28(4):732-736. doi: 10.1016/j.bmcl.2018.01.010. Epub 2018 Jan 11. Bioorg Med Chem Lett. 2018. PMID: 29398543
Immune-modulating enzyme indoleamine 2,3-dioxygenase is effectively inhibited by targeting its apo-form.
Nelp MT, Kates PA, Hunt JT, Newitt JA, Balog A, Maley D, Zhu X, Abell L, Allentoff A, Borzilleri R, Lewis HA, Lin Z, Seitz SP, Yan C, Groves JT. Nelp MT, et al. Among authors: seitz sp. Proc Natl Acad Sci U S A. 2018 Mar 27;115(13):3249-3254. doi: 10.1073/pnas.1719190115. Epub 2018 Mar 12. Proc Natl Acad Sci U S A. 2018. PMID: 29531094 Free PMC article.
Conformational-Analysis-Guided Discovery of 2,3-Disubstituted Pyridine IDO1 Inhibitors.
Cherney EC, Zhang L, Guo W, Huang A, Williams D, Seitz S, Shan W, Zhu X, Gullo-Brown J, Maley D, Lin TA, Hunt JT, Huang C, Yang Z, D'Arienzo CJ, Discenza LN, Ranasinghe A, Grubb MF, Traeger SC, Li X, Johnston KA, Kopcho L, Fereshteh M, Foster KA, Stefanski K, Delpy D, Dhar G, Anandam A, Mahankali S, Padmanabhan S, Rajanna P, Murali V, Mariappan TT, Pattasseri S, Nimje RY, Hong Z, Kempson J, Rampulla R, Mathur A, Gupta A, Borzilleri R, Vite G, Balog A. Cherney EC, et al. ACS Med Chem Lett. 2021 Jun 16;12(7):1143-1150. doi: 10.1021/acsmedchemlett.1c00236. eCollection 2021 Jul 8. ACS Med Chem Lett. 2021. PMID: 34267885 Free PMC article.
Synthesis and biological evaluation of biaryl alkyl ethers as inhibitors of IDO1.
Markwalder JA, Balog AJ, Williams DK, Nara SJ, Reddy R, Roy S, Kanyaboina Y, Li X, Johnston K, Fan Y, Lewis H, Marsilio F, Yan C, Critton D, Newitt JA, Traeger SC, Wu DR, Jure-Kunkel MN, Jayaraman L, Lin TA, Sinz MW, Hunt JT, Seitz SP. Markwalder JA, et al. Among authors: seitz sp. Bioorg Med Chem Lett. 2023 May 15;88:129280. doi: 10.1016/j.bmcl.2023.129280. Epub 2023 Apr 11. Bioorg Med Chem Lett. 2023. PMID: 37054759
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. 3. Structure activity relationships at C3(1,2).
Yue EW, Higley CA, DiMeo SV, Carini DJ, Nugiel DA, Benware C, Benfield PA, Burton CR, Cox S, Grafstrom RH, Sharp DM, Sisk LM, Boylan JF, Muckelbauer JK, Smallwood AM, Chen H, Chang CH, Seitz SP, Trainor GL. Yue EW, et al. Among authors: seitz sp. J Med Chem. 2002 Nov 21;45(24):5233-48. doi: 10.1021/jm0201722. J Med Chem. 2002. PMID: 12431051
47 results