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Discovery of N-(Indazol-3-yl)piperidine-4-carboxylic Acids as RORγt Allosteric Inhibitors for Autoimmune Diseases.
Zhang H, Lapointe BT, Anthony N, Azevedo R, Cals J, Correll CC, Daniels M, Deshmukh S, van Eenenaam H, Ferguson H, Hegde LG, Karstens WJ, Maclean J, Miller JR, Moy LY, Simov V, Nagpal S, Oubrie A, Palte RL, Parthasarathy G, Sciammetta N, van der Stelt M, Woodhouse JD, Trotter BW, Barr K. Zhang H, et al. Among authors: nagpal s. ACS Med Chem Lett. 2020 Jan 9;11(2):114-119. doi: 10.1021/acsmedchemlett.9b00431. eCollection 2020 Feb 13. ACS Med Chem Lett. 2020. PMID: 32071676 Free PMC article.
Identification of an allosteric binding site for RORγt inhibition.
Scheepstra M, Leysen S, van Almen GC, Miller JR, Piesvaux J, Kutilek V, van Eenennaam H, Zhang H, Barr K, Nagpal S, Soisson SM, Kornienko M, Wiley K, Elsen N, Sharma S, Correll CC, Trotter BW, van der Stelt M, Oubrie A, Ottmann C, Parthasarathy G, Brunsveld L. Scheepstra M, et al. Among authors: nagpal s. Nat Commun. 2015 Dec 7;6:8833. doi: 10.1038/ncomms9833. Nat Commun. 2015. PMID: 26640126 Free PMC article.
1-(2-Hydroxy-2-methyl-3-phenoxypropanoyl)indoline-4-carbonitrile derivatives as potent and tissue selective androgen receptor modulators.
Piatnitski Chekler EL, Unwalla R, Khan TA, Tangirala RS, Johnson M, St Andre M, Anderson JT, Kenney T, Chiparri S, McNally C, Kilbourne E, Thompson C, Nagpal S, Weber G, Schelling S, Owens J, Morris CA, Powell D, Verhoest PR, Gilbert AM. Piatnitski Chekler EL, et al. Among authors: nagpal s. J Med Chem. 2014 Mar 27;57(6):2462-71. doi: 10.1021/jm401625b. Epub 2014 Mar 10. J Med Chem. 2014. PMID: 24527807
Structure-Based Approach To Identify 5-[4-Hydroxyphenyl]pyrrole-2-carbonitrile Derivatives as Potent and Tissue Selective Androgen Receptor Modulators.
Unwalla R, Mousseau JJ, Fadeyi OO, Choi C, Parris K, Hu B, Kenney T, Chippari S, McNally C, Vishwanathan K, Kilbourne E, Thompson C, Nagpal S, Wrobel J, Yudt M, Morris CA, Powell D, Gilbert AM, Chekler ELP. Unwalla R, et al. Among authors: nagpal s. J Med Chem. 2017 Jul 27;60(14):6451-6457. doi: 10.1021/acs.jmedchem.7b00373. Epub 2017 Jul 11. J Med Chem. 2017. PMID: 28696695
A mouse model of androgenetic alopecia.
Crabtree JS, Kilbourne EJ, Peano BJ, Chippari S, Kenney T, McNally C, Wang W, Harris HA, Winneker RC, Nagpal S, Thompson CC. Crabtree JS, et al. Among authors: nagpal s. Endocrinology. 2010 May;151(5):2373-80. doi: 10.1210/en.2009-1474. Epub 2010 Mar 16. Endocrinology. 2010. PMID: 20233794
Discovery of a novel mechanism of steroid receptor antagonism: WAY-255348 modulates progesterone receptor cellular localization and promoter interactions.
Yudt MR, Russo LA, Berrodin TJ, Jelinsky SA, Ellis D, Cohen JC, Cooch N, Haglund E, Unwalla RJ, Fensome A, Wrobel J, Zhang Z, Nagpal S, Winneker RC. Yudt MR, et al. Among authors: nagpal s. Biochem Pharmacol. 2011 Dec 1;82(11):1709-19. doi: 10.1016/j.bcp.2011.08.006. Epub 2011 Aug 11. Biochem Pharmacol. 2011. PMID: 21854761
524 results