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Discovery of an Atropisomeric PI3Kβ Selective Inhibitor through Optimization of the Hinge Binding Motif.

Autor: Perreault S; Gilead Sciences, Inc., 199 East Blaine Street, Seattle, Washington 98102, United States., Arjmand F; Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404, United States., Chandrasekhar J; Gilead Sciences, Inc., 199 East Blaine Street, Seattle, Washington 98102, United States., Hao J; Gilead Sciences, Inc., 199 East Blaine Street, Seattle, Washington 98102, United States., Keegan KS; Gilead Sciences, Inc., 199 East Blaine Street, Seattle, Washington 98102, United States., Koditek D; Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404, United States., Lepist EI; Gilead Sciences, Inc., 199 East Blaine Street, Seattle, Washington 98102, United States., Matson CK; Gilead Sciences, Inc., 199 East Blaine Street, Seattle, Washington 98102, United States., McGrath ME; Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404, United States., Patel L; Gilead Sciences, Inc., 199 East Blaine Street, Seattle, Washington 98102, United States., Sedillo K; Gilead Sciences, Inc., 199 East Blaine Street, Seattle, Washington 98102, United States., Therrien J; Gilead Sciences, Inc., 199 East Blaine Street, Seattle, Washington 98102, United States., Till NA; Gilead Sciences, Inc., 199 East Blaine Street, Seattle, Washington 98102, United States., Tomkinson A; Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404, United States., Treiberg J; Gilead Sciences, Inc., 199 East Blaine Street, Seattle, Washington 98102, United States., Zherebina Y; Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404, United States., Phillips G; Gilead Sciences, Inc., 199 East Blaine Street, Seattle, Washington 98102, United States.

Publikováno v: ACS medicinal chemistry letters [ACS Med Chem Lett] 2020 Apr 13; Vol. 11 (6), pp. 1236-1243. Date of Electronic Publication: 2020 Apr 13 (Print Publication: 2020).

AMG 176, a Selective MCL1 Inhibitor, Is Effective in Hematologic Cancer Models Alone and in Combination with Established Therapies.

Autor: Caenepeel S; Oncology Research, Amgen Inc., Thousand Oaks, California.; Amgen Research, Amgen Inc., Thousand Oaks, California., Brown SP; Amgen Research, Amgen Inc., Thousand Oaks, California. phughes@amgen.com seanpomeroy@yahoo.com.; Medicinal Chemistry, Amgen Inc., Thousand Oaks, California., Belmontes B; Oncology Research, Amgen Inc., Thousand Oaks, California.; Amgen Research, Amgen Inc., Thousand Oaks, California., Moody G; Oncology Research, Amgen Inc., Thousand Oaks, California.; Amgen Research, Amgen Inc., Thousand Oaks, California., Keegan KS; Oncology Research, Amgen Inc., Seattle, Washington.; Amgen Research, Amgen Inc., Seattle, Washington., Chui D; Amgen Research, Amgen Inc., Thousand Oaks, California.; Genome Analysis Unit, Amgen Inc., Thousand Oaks, California., Whittington DA; Molecular Engineering, Amgen Inc., Cambridge, Massachusetts.; Amgen Research, Amgen Inc., Cambridge, Massachusetts., Huang X; Molecular Engineering, Amgen Inc., Cambridge, Massachusetts.; Amgen Research, Amgen Inc., Cambridge, Massachusetts., Poppe L; Amgen Research, Amgen Inc., Thousand Oaks, California.; Discovery Attribute Sciences, Amgen Inc., Thousand Oaks, California., Cheng AC; Molecular Engineering, Amgen Inc., South San Francisco, California.; Amgen Research, Amgen Inc., South San Francisco, California., Cardozo M; Molecular Engineering, Amgen Inc., South San Francisco, California.; Amgen Research, Amgen Inc., South San Francisco, California., Houze J; Amgen Research, Amgen Inc., Cambridge, Massachusetts.; Medicinal Chemistry, Amgen Inc., Cambridge, Massachusetts., Li Y; Amgen Research, Amgen Inc., South San Francisco, California.; Medicinal Chemistry, Amgen Inc., South San Francisco, California., Lucas B; Amgen Research, Amgen Inc., South San Francisco, California.; Medicinal Chemistry, Amgen Inc., South San Francisco, California., Paras NA; Amgen Research, Amgen Inc., South San Francisco, California.; Medicinal Chemistry, Amgen Inc., South San Francisco, California., Wang X; Amgen Research, Amgen Inc., South San Francisco, California.; Medicinal Chemistry, Amgen Inc., South San Francisco, California., Taygerly JP; Amgen Research, Amgen Inc., South San Francisco, California.; Medicinal Chemistry, Amgen Inc., South San Francisco, California., Vimolratana M; Amgen Research, Amgen Inc., South San Francisco, California.; Medicinal Chemistry, Amgen Inc., South San Francisco, California., Zancanella M; Amgen Research, Amgen Inc., South San Francisco, California.; Medicinal Chemistry, Amgen Inc., South San Francisco, California., Zhu L; Amgen Research, Amgen Inc., South San Francisco, California.; Medicinal Chemistry, Amgen Inc., South San Francisco, California., Cajulis E; Oncology Research, Amgen Inc., Thousand Oaks, California.; Amgen Research, Amgen Inc., Thousand Oaks, California., Osgood T; Oncology Research, Amgen Inc., Thousand Oaks, California.; Amgen Research, Amgen Inc., Thousand Oaks, California., Sun J; Oncology Research, Amgen Inc., Thousand Oaks, California.; Amgen Research, Amgen Inc., Thousand Oaks, California., Damon L; Department of Medicine, Massachusetts General Hospital, Boston, Massachusetts., Egan RK; Department of Medicine, Massachusetts General Hospital, Boston, Massachusetts., Greninger P; Department of Medicine, Massachusetts General Hospital, Boston, Massachusetts., McClanaghan JD; Department of Medicine, Massachusetts General Hospital, Boston, Massachusetts., Gong J; The Walter and Eliza Hall Institute of Medical Research, Melbourne, Australia.; Department of Medical Biology, University of Melbourne, Melbourne, Australia., Moujalled D; Malignant Haematology and Stem Cell Transplantation Service, Alfred Hospital, Melbourne, Australia; and Australian Centre for Blood Diseases, Monash University, Melbourne, Australia., Pomilio G; Malignant Haematology and Stem Cell Transplantation Service, Alfred Hospital, Melbourne, Australia; and Australian Centre for Blood Diseases, Monash University, Melbourne, Australia., Beltran P; Oncology Research, Amgen Inc., Thousand Oaks, California.; Amgen Research, Amgen Inc., Thousand Oaks, California., Benes CH; Department of Medicine, Massachusetts General Hospital, Boston, Massachusetts., Roberts AW; The Walter and Eliza Hall Institute of Medical Research, Melbourne, Australia.; Department of Medical Biology, University of Melbourne, Melbourne, Australia.; Department of Clinical Haematology and Bone Marrow Transplantation, The Royal Melbourne Hospital, Melbourne, Australia.; Victorian Comprehensive Cancer Centre, Parkville, Australia., Huang DC; The Walter and Eliza Hall Institute of Medical Research, Melbourne, Australia.; Department of Medical Biology, University of Melbourne, Melbourne, Australia., Wei A; Malignant Haematology and Stem Cell Transplantation Service, Alfred Hospital, Melbourne, Australia; and Australian Centre for Blood Diseases, Monash University, Melbourne, Australia., Canon J; Oncology Research, Amgen Inc., Thousand Oaks, California.; Amgen Research, Amgen Inc., Thousand Oaks, California., Coxon A; Oncology Research, Amgen Inc., Thousand Oaks, California.; Amgen Research, Amgen Inc., Thousand Oaks, California., Hughes PE; Oncology Research, Amgen Inc., Thousand Oaks, California. phughes@amgen.com seanpomeroy@yahoo.com.; Amgen Research, Amgen Inc., Thousand Oaks, California.

Publikováno v: Cancer discovery [Cancer Discov] 2018 Dec; Vol. 8 (12), pp. 1582-1597. Date of Electronic Publication: 2018 Sep 25.

PI3Kδ inhibitor idelalisib in combination with BTK inhibitor ONO/GS-4059 in diffuse large B cell lymphoma with acquired resistance to PI3Kδ and BTK inhibitors.

Autor: Yahiaoui A; Gilead Sciences, Inc., Foster City, California, United States of America., Meadows SA; Gilead Sciences, Inc., Foster City, California, United States of America., Sorensen RA; Gilead Sciences, Inc., Foster City, California, United States of America., Cui ZH; Gilead Sciences, Inc., Foster City, California, United States of America., Keegan KS; Gilead Sciences, Inc., Foster City, California, United States of America., Brockett R; Gilead Sciences, Inc., Foster City, California, United States of America., Chen G; Gilead Sciences, Inc., Foster City, California, United States of America., Quéva C; Gilead Sciences, Inc., Foster City, California, United States of America., Li L; Gilead Sciences, Inc., Foster City, California, United States of America., Tannheimer SL; Gilead Sciences, Inc., Foster City, California, United States of America.

Publikováno v: PloS one [PLoS One] 2017 Feb 08; Vol. 12 (2), pp. e0171221. Date of Electronic Publication: 2017 Feb 08 (Print Publication: 2017).