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Page 1
Inhibiting NF-κB-inducing kinase (NIK): discovery, structure-based design, synthesis, structure-activity relationship, and co-crystal structures.
Li K, McGee LR, Fisher B, Sudom A, Liu J, Rubenstein SM, Anwer MK, Cushing TD, Shin Y, Ayres M, Lee F, Eksterowicz J, Faulder P, Waszkowycz B, Plotnikova O, Farrelly E, Xiao SH, Chen G, Wang Z. Li K, et al. Among authors: cushing td. Bioorg Med Chem Lett. 2013 Mar 1;23(5):1238-44. doi: 10.1016/j.bmcl.2013.01.012. Epub 2013 Jan 11. Bioorg Med Chem Lett. 2013. PMID: 23374866
Synthesis and SAR study of potent and selective PI3Kδ inhibitors.
Bui M, Hao X, Shin Y, Cardozo M, He X, Henne K, Suchomel J, McCarter J, McGee LR, San Miguel T, Medina JC, Mohn D, Tran T, Wannberg S, Wong J, Wong S, Zalameda L, Metz D, Cushing TD. Bui M, et al. Among authors: cushing td. Bioorg Med Chem Lett. 2015 Mar 1;25(5):1104-9. doi: 10.1016/j.bmcl.2015.01.001. Epub 2015 Jan 17. Bioorg Med Chem Lett. 2015. PMID: 25666823
Discovery and in vivo evaluation of dual PI3Kβ/δ inhibitors.
Gonzalez-Lopez de Turiso F, Shin Y, Brown M, Cardozo M, Chen Y, Fong D, Hao X, He X, Henne K, Hu YL, Johnson MG, Kohn T, Lohman J, McBride HJ, McGee LR, Medina JC, Metz D, Miner K, Mohn D, Pattaropong V, Seganish J, Simard JL, Wannberg S, Whittington DA, Yu G, Cushing TD. Gonzalez-Lopez de Turiso F, et al. Among authors: cushing td. J Med Chem. 2012 Sep 13;55(17):7667-85. doi: 10.1021/jm300679u. Epub 2012 Aug 29. J Med Chem. 2012. PMID: 22876881
Discovery of INT131: a selective PPARγ modulator that enhances insulin sensitivity.
Taygerly JP, McGee LR, Rubenstein SM, Houze JB, Cushing TD, Li Y, Motani A, Chen JL, Frankmoelle W, Ye G, Learned MR, Jaen J, Miao S, Timmermans PB, Thoolen M, Kearney P, Flygare J, Beckmann H, Weiszmann J, Lindstrom M, Walker N, Liu J, Biermann D, Wang Z, Hagiwara A, Iida T, Aramaki H, Kitao Y, Shinkai H, Furukawa N, Nishiu J, Nakamura M. Taygerly JP, et al. Among authors: cushing td. Bioorg Med Chem. 2013 Feb 15;21(4):979-92. doi: 10.1016/j.bmc.2012.11.058. Epub 2012 Dec 10. Bioorg Med Chem. 2013. PMID: 23294830
Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease.
Cushing TD, Hao X, Shin Y, Andrews K, Brown M, Cardozo M, Chen Y, Duquette J, Fisher B, Gonzalez-Lopez de Turiso F, He X, Henne KR, Hu YL, Hungate R, Johnson MG, Kelly RC, Lucas B, McCarter JD, McGee LR, Medina JC, San Miguel T, Mohn D, Pattaropong V, Pettus LH, Reichelt A, Rzasa RM, Seganish J, Tasker AS, Wahl RC, Wannberg S, Whittington DA, Whoriskey J, Yu G, Zalameda L, Zhang D, Metz DP. Cushing TD, et al. J Med Chem. 2015 Jan 8;58(1):480-511. doi: 10.1021/jm501624r. Epub 2014 Dec 3. J Med Chem. 2015. PMID: 25469863
Discovery, Optimization, and in Vivo Evaluation of Benzimidazole Derivatives AM-8508 and AM-9635 as Potent and Selective PI3Kδ Inhibitors.
Shin Y, Suchomel J, Cardozo M, Duquette J, He X, Henne K, Hu YL, Kelly RC, McCarter J, McGee LR, Medina JC, Metz D, San Miguel T, Mohn D, Tran T, Vissinga C, Wong S, Wannberg S, Whittington DA, Whoriskey J, Yu G, Zalameda L, Zhang X, Cushing TD. Shin Y, et al. Among authors: cushing td. J Med Chem. 2016 Jan 14;59(1):431-47. doi: 10.1021/acs.jmedchem.5b01651. Epub 2015 Dec 21. J Med Chem. 2016. PMID: 26652588
Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-5-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-1430).
Gonzalez-Lopez de Turiso F, Hao X, Shin Y, Bui M, Campuzano ID, Cardozo M, Dunn MC, Duquette J, Fisher B, Foti RS, Henne K, He X, Hu YL, Kelly RC, Johnson MG, Lucas BS, McCarter J, McGee LR, Medina JC, Metz D, San Miguel T, Mohn D, Tran T, Vissinga C, Wannberg S, Whittington DA, Whoriskey J, Yu G, Zalameda L, Zhang X, Cushing TD. Gonzalez-Lopez de Turiso F, et al. Among authors: cushing td. J Med Chem. 2016 Aug 11;59(15):7252-67. doi: 10.1021/acs.jmedchem.6b00827. Epub 2016 Jul 25. J Med Chem. 2016. PMID: 27411843
A novel series of IKKβ inhibitors part II: description of a potent and pharmacologically active series of analogs.
Cushing TD, Baichwal V, Berry K, Billedeau R, Bordunov V, Broka C, Browner MF, Cardozo M, Cheng P, Clark D, Dalrymple S, DeGraffenreid M, Gill A, Hao X, Hawley RC, He X, Labadie SS, Labelle M, Lehel C, Lu PP, McIntosh J, Miao S, Parast C, Shin Y, Sjogren EB, Smith ML, Talamas FX, Tonn G, Walker KM, Walker NP, Wesche H, Whitehead C, Wright M, Jaen JC. Cushing TD, et al. Bioorg Med Chem Lett. 2011 Jan 1;21(1):423-6. doi: 10.1016/j.bmcl.2010.10.125. Epub 2010 Oct 29. Bioorg Med Chem Lett. 2011. PMID: 21074992
A novel series of IKKβ inhibitors part I: Initial SAR studies of a HTS hit.
Cushing TD, Baichwal V, Berry K, Billedeau R, Bordunov V, Broka C, Cardozo M, Cheng P, Clark D, Dalrymple S, DeGraffenreid M, Gill A, Hao X, Hawley RC, He X, Jaen JC, Labadie SS, Labelle M, Lehel C, Lu PP, McIntosh J, Miao S, Parast C, Shin Y, Sjogren EB, Smith ML, Talamas FX, Tonn G, Walker KM, Walker NP, Wesche H, Whitehead C, Wright M, Browner MF. Cushing TD, et al. Bioorg Med Chem Lett. 2011 Jan 1;21(1):417-22. doi: 10.1016/j.bmcl.2010.10.126. Epub 2010 Oct 29. Bioorg Med Chem Lett. 2011. PMID: 21074993
13 results