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Page 1
Implementation of the CYP Index for the Design of Selective Tryptophan-2,3-dioxygenase Inhibitors.
Parr BT, Pastor R, Sellers BD, Pei Z, Jaipuri FA, Castanedo GM, Gazzard L, Kumar S, Li X, Liu W, Mendonca R, Pavana RK, Potturi H, Shao C, Velvadapu V, Waldo JP, Wu G, Yuen PW, Zhang Z, Zhang Y, Harris SF, Oh AJ, DiPasquale A, Dement K, La H, Goon L, Gustafson A, VanderPorten EC, Mautino MR, Liu Y. Parr BT, et al. Among authors: mendonca r. ACS Med Chem Lett. 2020 Mar 4;11(4):541-549. doi: 10.1021/acsmedchemlett.0c00004. eCollection 2020 Apr 9. ACS Med Chem Lett. 2020. PMID: 32292562 Free PMC article.
Aminoisoxazoles as Potent Inhibitors of Tryptophan 2,3-Dioxygenase 2 (TDO2).
Pei Z, Mendonca R, Gazzard L, Pastor R, Goon L, Gustafson A, VanderPorten E, Hatzivassiliou G, Dement K, Cass R, Yuen PW, Zhang Y, Wu G, Lin X, Liu Y, Sellers BD. Pei Z, et al. Among authors: mendonca r. ACS Med Chem Lett. 2018 Apr 2;9(5):417-421. doi: 10.1021/acsmedchemlett.7b00427. eCollection 2018 May 10. ACS Med Chem Lett. 2018. PMID: 29795752 Free PMC article.
Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling.
Zak M, Hanan EJ, Lupardus P, Brown DG, Robinson C, Siu M, Lyssikatos JP, Romero FA, Zhao G, Kellar T, Mendonca R, Ray NC, Goodacre SC, Crackett PH, McLean N, Hurley CA, Yuen PW, Cheng YX, Liu X, Liimatta M, Kohli PB, Nonomiya J, Salmon G, Buckley G, Lloyd J, Gibbons P, Ghilardi N, Kenny JR, Johnson A. Zak M, et al. Among authors: mendonca r. Bioorg Med Chem Lett. 2019 Jun 15;29(12):1522-1531. doi: 10.1016/j.bmcl.2019.04.008. Epub 2019 Apr 4. Bioorg Med Chem Lett. 2019. PMID: 30981576
Identification of C-2 hydroxyethyl imidazopyrrolopyridines as potent JAK1 inhibitors with favorable physicochemical properties and high selectivity over JAK2.
Zak M, Hurley CA, Ward SI, Bergeron P, Barrett K, Balazs M, Blair WS, Bull R, Chakravarty P, Chang C, Crackett P, Deshmukh G, DeVoss J, Dragovich PS, Eigenbrot C, Ellwood C, Gaines S, Ghilardi N, Gibbons P, Gradl S, Gribling P, Hamman C, Harstad E, Hewitt P, Johnson A, Johnson T, Kenny JR, Koehler MF, Bir Kohli P, Labadie S, Lee WP, Liao J, Liimatta M, Mendonca R, Narukulla R, Pulk R, Reeve A, Savage S, Shia S, Steffek M, Ubhayakar S, van Abbema A, Aliagas I, Avitabile-Woo B, Xiao Y, Yang J, Kulagowski JJ. Zak M, et al. Among authors: mendonca r. J Med Chem. 2013 Jun 13;56(11):4764-85. doi: 10.1021/jm4004895. Epub 2013 May 31. J Med Chem. 2013. PMID: 23659214
Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.
Zak M, Mendonca R, Balazs M, Barrett K, Bergeron P, Blair WS, Chang C, Deshmukh G, Devoss J, Dragovich PS, Eigenbrot C, Ghilardi N, Gibbons P, Gradl S, Hamman C, Hanan EJ, Harstad E, Hewitt PR, Hurley CA, Jin T, Johnson A, Johnson T, Kenny JR, Koehler MF, Bir Kohli P, Kulagowski JJ, Labadie S, Liao J, Liimatta M, Lin Z, Lupardus PJ, Maxey RJ, Murray JM, Pulk R, Rodriguez M, Savage S, Shia S, Steffek M, Ubhayakar S, Ultsch M, van Abbema A, Ward SI, Xiao L, Xiao Y. Zak M, et al. Among authors: mendonca r. J Med Chem. 2012 Jul 12;55(13):6176-93. doi: 10.1021/jm300628c. Epub 2012 Jun 28. J Med Chem. 2012. PMID: 22698084
Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.
Palmer JT, Bryant C, Wang DX, Davis DE, Setti EL, Rydzewski RM, Venkatraman S, Tian ZQ, Burrill LC, Mendonca RV, Springman E, McCarter J, Chung T, Cheung H, Janc JW, McGrath M, Somoza JR, Enriquez P, Yu ZW, Strickley RM, Liu L, Venuti MC, Percival MD, Falgueyret JP, Prasit P, Oballa R, Riendeau D, Young RN, Wesolowski G, Rodan SB, Johnson C, Kimmel DB, Rodan G. Palmer JT, et al. Among authors: mendonca rv. J Med Chem. 2005 Dec 1;48(24):7520-34. doi: 10.1021/jm058198r. J Med Chem. 2005. PMID: 16302794
Structure-based discovery of C-2 substituted imidazo-pyrrolopyridine JAK1 inhibitors with improved selectivity over JAK2.
Labadie S, Dragovich PS, Barrett K, Blair WS, Bergeron P, Chang C, Deshmukh G, Eigenbrot C, Ghilardi N, Gibbons P, Hurley CA, Johnson A, Kenny JR, Kohli PB, Kulagowski JJ, Liimatta M, Lupardus PJ, Mendonca R, Murray JM, Pulk R, Shia S, Steffek M, Ubhayakar S, Ultsch M, van Abbema A, Ward S, Zak M. Labadie S, et al. Among authors: mendonca r. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7627-33. doi: 10.1016/j.bmcl.2012.10.008. Epub 2012 Oct 11. Bioorg Med Chem Lett. 2012. PMID: 23107482
Optimization of subsite binding to the beta5 subunit of the human 20S proteasome using vinyl sulfones and 2-keto-1,3,4-oxadiazoles: syntheses and cellular properties of potent, selective proteasome inhibitors.
Rydzewski RM, Burrill L, Mendonca R, Palmer JT, Rice M, Tahilramani R, Bass KE, Leung L, Gjerstad E, Janc JW, Pan L. Rydzewski RM, et al. Among authors: mendonca r. J Med Chem. 2006 May 18;49(10):2953-68. doi: 10.1021/jm058289o. J Med Chem. 2006. PMID: 16686537
Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors.
Palmer JT, Rydzewski RM, Mendonca RV, Sperandio D, Spencer JR, Hirschbein BL, Lohman J, Beltman J, Nguyen M, Liu L. Palmer JT, et al. Among authors: mendonca rv. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3434-9. doi: 10.1016/j.bmcl.2006.04.013. Epub 2006 Apr 27. Bioorg Med Chem Lett. 2006. PMID: 16644215
Novel, potent, selective, and orally bioavailable human betaII-tryptase inhibitors.
Sperandio D, Tai VW, Lohman J, Hirschbein B, Mendonca R, Lee CS, Spencer JR, Janc J, Nguyen M, Beltman J, Sprengeler P, Scheerens H, Lin T, Liu L, Gadre A, Kellogg A, Green MJ, McGrath ME. Sperandio D, et al. Among authors: mendonca r. Bioorg Med Chem Lett. 2006 Aug 1;16(15):4085-9. doi: 10.1016/j.bmcl.2006.04.088. Epub 2006 May 24. Bioorg Med Chem Lett. 2006. PMID: 16725321
471 results