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Structure-based optimization of hydroxylactam as potent, cell-active inhibitors of lactate dehydrogenase.

Autor: Wei B; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA. Electronic address: Wei.BinQing@gene.com., Robarge K; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA., Labadie SS; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA., Chen J; WuXi AppTec, 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai, 200131, China., Corson LB; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA., DiPasquale A; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA., Dragovich PS; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA., Eigenbrot C; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA., Evangelista M; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA., Fauber BP; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA., Hitz A; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA., Hong R; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA., Lai KW; WuXi AppTec, 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai, 200131, China., Liu W; WuXi AppTec, 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai, 200131, China., Ma S; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA., Malek S; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA., O'Brien T; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA., Pang J; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA., Peterson D; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA., Salphati L; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA., Sampath D; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA., Sideris S; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA., Ultsch M; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA., Xu Z; WuXi AppTec, 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai, 200131, China., Yen I; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA., Yu D; WuXi AppTec, 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai, 200131, China., Yue Q; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA., Zhou A; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA., Purkey HE; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA. Electronic address: Purkey.Hans@gene.com.

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2022 Mar 01; Vol. 59, pp. 128576. Date of Electronic Publication: 2022 Jan 19.

GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer.

Autor: Liang J; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Zbieg JR; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Blake RA; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Chang JH; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Daly S; Charles River Discovery Research Services UK Limited, 7-9 Spire Green Center, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom., DiPasquale AG; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Friedman LS; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Gelzleichter T; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Gill M; Charles River Discovery Research Services UK Limited, 7-9 Spire Green Center, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom., Giltnane JM; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Goodacre S; Charles River Discovery Research Services UK Limited, 7-9 Spire Green Center, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom., Guan J; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Hartman SJ; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Ingalla ER; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Kategaya L; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Kiefer JR; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Kleinheinz T; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Labadie SS; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Lai T; WuXi AppTec Co., Ltd., 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, P. R. China., Li J; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Liao J; WuXi AppTec Co., Ltd., 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, P. R. China., Liu Z; WuXi AppTec Co., Ltd., 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, P. R. China., Mody V; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., McLean N; Charles River Discovery Research Services UK Limited, 7-9 Spire Green Center, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom., Metcalfe C; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Nannini MA; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Oeh J; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., O'Rourke MG; Charles River Discovery Research Services UK Limited, 7-9 Spire Green Center, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom., Ortwine DF; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Ran Y; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Ray NC; Charles River Discovery Research Services UK Limited, 7-9 Spire Green Center, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom., Roussel F; Charles River Discovery Research Services UK Limited, 7-9 Spire Green Center, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom., Sambrone A; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Sampath D; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Schutt LK; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Vinogradova M; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Wai J; WuXi AppTec Co., Ltd., 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, P. R. China., Wang T; WuXi AppTec Co., Ltd., 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, P. R. China., Wertz IE; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., White JR; Charles River Discovery Research Services UK Limited, 7-9 Spire Green Center, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom., Yeap SK; Charles River Discovery Research Services UK Limited, 7-9 Spire Green Center, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom., Young A; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Zhang B; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Zheng X; WuXi AppTec Co., Ltd., 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, P. R. China., Zhou W; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Zhong Y; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Wang X; Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2021 Aug 26; Vol. 64 (16), pp. 11841-11856. Date of Electronic Publication: 2021 Jul 12.

Structural basis for dual-mode inhibition of the ABC transporter MsbA.

Autor: Ho H; Structural Biology, Genentech Inc., San Francisco, CA, USA., Miu A; Biochemical and Cellular Pharmacology, Genentech Inc., San Francisco, CA, USA., Alexander MK; Infectious Diseases, Genentech Inc., San Francisco, CA, USA., Garcia NK; Protein Analytical Chemistry, Genentech Inc., San Francisco, CA, USA., Oh A; Structural Biology, Genentech Inc., San Francisco, CA, USA., Zilberleyb I; Biomolecular Resources, Genentech Inc., San Francisco, CA, USA., Reichelt M; Pathology, Genentech Inc., San Francisco, CA, USA., Austin CD; Pathology, Genentech Inc., San Francisco, CA, USA., Tam C; Biomolecular Resources, Genentech Inc., San Francisco, CA, USA., Shriver S; Biomolecular Resources, Genentech Inc., San Francisco, CA, USA., Hu H; Discovery Chemistry, Genentech Inc., San Francisco, CA, USA., Labadie SS; Discovery Chemistry, Genentech Inc., San Francisco, CA, USA., Liang J; Discovery Chemistry, Genentech Inc., San Francisco, CA, USA., Wang L; Discovery Chemistry, Genentech Inc., San Francisco, CA, USA., Wang J; WuXi Apptec. Co. Ltd., Shanghai, China., Lu Y; WuXi Apptec. Co. Ltd., Shanghai, China., Purkey HE; Discovery Chemistry, Genentech Inc., San Francisco, CA, USA., Quinn J; Biochemical and Cellular Pharmacology, Genentech Inc., San Francisco, CA, USA., Franke Y; Biomolecular Resources, Genentech Inc., San Francisco, CA, USA., Clark K; Biochemical and Cellular Pharmacology, Genentech Inc., San Francisco, CA, USA., Beresini MH; Biochemical and Cellular Pharmacology, Genentech Inc., San Francisco, CA, USA., Tan MW; Infectious Diseases, Genentech Inc., San Francisco, CA, USA., Sellers BD; Discovery Chemistry, Genentech Inc., San Francisco, CA, USA., Maurer T; Structural Biology, Genentech Inc., San Francisco, CA, USA., Koehler MFT; Discovery Chemistry, Genentech Inc., San Francisco, CA, USA., Wecksler AT; Protein Analytical Chemistry, Genentech Inc., San Francisco, CA, USA., Kiefer JR; Structural Biology, Genentech Inc., San Francisco, CA, USA., Verma V; Discovery Chemistry, Genentech Inc., San Francisco, CA, USA., Xu Y; Biochemical and Cellular Pharmacology, Genentech Inc., San Francisco, CA, USA., Nishiyama M; Infectious Diseases, Genentech Inc., San Francisco, CA, USA., Payandeh J; Structural Biology, Genentech Inc., San Francisco, CA, USA. payandeh.jian@gene.com.; Infectious Diseases, Genentech Inc., San Francisco, CA, USA. payandeh.jian@gene.com., Koth CM; Structural Biology, Genentech Inc., San Francisco, CA, USA. koth.christopher@gene.com.; Infectious Diseases, Genentech Inc., San Francisco, CA, USA. koth.christopher@gene.com.

Publikováno v: Nature [Nature] 2018 May; Vol. 557 (7704), pp. 196-201. Date of Electronic Publication: 2018 May 02.