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Page 1
Discovery of an Atropisomeric PI3Kβ Selective Inhibitor through Optimization of the Hinge Binding Motif.
Perreault S, Arjmand F, Chandrasekhar J, Hao J, Keegan KS, Koditek D, Lepist EI, Matson CK, McGrath ME, Patel L, Sedillo K, Therrien J, Till NA, Tomkinson A, Treiberg J, Zherebina Y, Phillips G. Perreault S, et al. Among authors: keegan ks. ACS Med Chem Lett. 2020 Apr 13;11(6):1236-1243. doi: 10.1021/acsmedchemlett.0c00095. eCollection 2020 Jun 11. ACS Med Chem Lett. 2020. PMID: 32551006 Free PMC article.
Discovery of a Phosphoinositide 3-Kinase (PI3K) β/δ Inhibitor for the Treatment of Phosphatase and Tensin Homolog (PTEN) Deficient Tumors: Building PI3Kβ Potency in a PI3Kδ-Selective Template by Targeting Nonconserved Asp856.
Perreault S, Chandrasekhar J, Cui ZH, Evarts J, Hao J, Kaplan JA, Kashishian A, Keegan KS, Kenney T, Koditek D, Lad L, Lepist EI, McGrath ME, Patel L, Phillips B, Therrien J, Treiberg J, Yahiaoui A, Phillips G. Perreault S, et al. Among authors: keegan ks. J Med Chem. 2017 Feb 23;60(4):1555-1567. doi: 10.1021/acs.jmedchem.6b01821. Epub 2017 Feb 7. J Med Chem. 2017. PMID: 28106991
Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3.
Li Z, Wang X, Eksterowicz J, Gribble MW Jr, Alba GQ, Ayres M, Carlson TJ, Chen A, Chen X, Cho R, Connors RV, DeGraffenreid M, Deignan JT, Duquette J, Fan P, Fisher B, Fu J, Huard JN, Kaizerman J, Keegan KS, Li C, Li K, Li Y, Liang L, Liu W, Lively SE, Lo MC, Ma J, McMinn DL, Mihalic JT, Modi K, Ngo R, Pattabiraman K, Piper DE, Queva C, Ragains ML, Suchomel J, Thibault S, Walker N, Wang X, Wang Z, Wanska M, Wehn PM, Weidner MF, Zhang AJ, Zhao X, Kamb A, Wickramasinghe D, Dai K, McGee LR, Medina JC. Li Z, et al. Among authors: keegan ks. J Med Chem. 2014 Apr 24;57(8):3430-49. doi: 10.1021/jm500118j. Epub 2014 Apr 2. J Med Chem. 2014. PMID: 24641103
Biochemical characterization of tirabrutinib and other irreversible inhibitors of Bruton's tyrosine kinase reveals differences in on - and off - target inhibition.
Liclican A, Serafini L, Xing W, Czerwieniec G, Steiner B, Wang T, Brendza KM, Lutz JD, Keegan KS, Ray AS, Schultz BE, Sakowicz R, Feng JY. Liclican A, et al. Among authors: keegan ks. Biochim Biophys Acta Gen Subj. 2020 Apr;1864(4):129531. doi: 10.1016/j.bbagen.2020.129531. Epub 2020 Jan 15. Biochim Biophys Acta Gen Subj. 2020. PMID: 31953125 Free article.
Preclinical evaluation of AMG 925, a FLT3/CDK4 dual kinase inhibitor for treating acute myeloid leukemia.
Keegan K, Li C, Li Z, Ma J, Ragains M, Coberly S, Hollenback D, Eksterowicz J, Liang L, Weidner M, Huard J, Wang X, Alba G, Orf J, Lo MC, Zhao S, Ngo R, Chen A, Liu L, Carlson T, Quéva C, McGee LR, Medina J, Kamb A, Wickramasinghe D, Dai K. Keegan K, et al. Mol Cancer Ther. 2014 Apr;13(4):880-9. doi: 10.1158/1535-7163.MCT-13-0858. Epub 2014 Feb 13. Mol Cancer Ther. 2014. PMID: 24526162
AMG 176, a Selective MCL1 Inhibitor, Is Effective in Hematologic Cancer Models Alone and in Combination with Established Therapies.
Caenepeel S, Brown SP, Belmontes B, Moody G, Keegan KS, Chui D, Whittington DA, Huang X, Poppe L, Cheng AC, Cardozo M, Houze J, Li Y, Lucas B, Paras NA, Wang X, Taygerly JP, Vimolratana M, Zancanella M, Zhu L, Cajulis E, Osgood T, Sun J, Damon L, Egan RK, Greninger P, McClanaghan JD, Gong J, Moujalled D, Pomilio G, Beltran P, Benes CH, Roberts AW, Huang DC, Wei A, Canon J, Coxon A, Hughes PE. Caenepeel S, et al. Among authors: keegan ks. Cancer Discov. 2018 Dec;8(12):1582-1597. doi: 10.1158/2159-8290.CD-18-0387. Epub 2018 Sep 25. Cancer Discov. 2018. PMID: 30254093
14 results