An allosteric pan-TEAD inhibitor blocks oncogenic YAP/TAZ signaling and overcomes KRAS G12C inhibitor resistance.

Autor: Hagenbeek TJ; Department of Discovery Oncology, Genentech, California, CA, USA., Zbieg JR; Department of Discovery Chemistry, Genentech, California, CA, USA., Hafner M; Department of Oncology Bioinformatics, Genentech, California, CA, USA., Mroue R; Department of Discovery Oncology, Genentech, California, CA, USA., Lacap JA; Department of Translational Oncology, Genentech, California, CA, USA., Sodir NM; Department of Translational Oncology, Genentech, California, CA, USA., Noland CL; Department of Structural Biology, Genentech, California, CA, USA., Afghani S; Department of Discovery Oncology, Genentech, California, CA, USA., Kishore A; Department of Discovery Oncology, Genentech, California, CA, USA., Bhat KP; Department of Discovery Oncology, Genentech, California, CA, USA., Yao X; Department of Oncology Bioinformatics, Genentech, California, CA, USA., Schmidt S; Department of Biochemical and Cellular Pharmacology, Genentech, California, CA, USA., Clausen S; Department of Biochemical and Cellular Pharmacology, Genentech, California, CA, USA., Steffek M; Department of Biochemical and Cellular Pharmacology, Genentech, California, CA, USA., Lee W; Department of Discovery Chemistry, Genentech, California, CA, USA., Beroza P; Department of Discovery Chemistry, Genentech, California, CA, USA., Martin S; Department of Discovery Oncology, Genentech, California, CA, USA., Lin E; Department of Discovery Oncology, Genentech, California, CA, USA., Fong R; Department of Structural Biology, Genentech, California, CA, USA., Di Lello P; Department of Structural Biology, Genentech, California, CA, USA., Kubala MH; Department of Structural Biology, Genentech, California, CA, USA., Yang MN; Department of Translational Oncology, Genentech, California, CA, USA., Lau JT; Department of Translational Oncology, Genentech, California, CA, USA., Chan E; Department of Translational Oncology, Genentech, California, CA, USA., Arrazate A; Department of Translational Oncology, Genentech, California, CA, USA., An L; Department of Small Molecule Pharmaceutical Sciences, Genentech, California, CA, USA., Levy E; Department of Small Molecule Pharmaceutical Sciences, Genentech, California, CA, USA., Lorenzo MN; Department of Protein Chemistry, Genentech, California, CA, USA., Lee HJ; Department of Discovery Oncology, Genentech, California, CA, USA., Pham TH; Department of Discovery Oncology, Genentech, California, CA, USA., Modrusan Z; Department of Microchemistry, Proteomics and Lipidomics, Genentech, California, CA, USA., Zang R; Department of Drug Metabolism and Pharmacokinetics, Genentech, California, CA, USA., Chen YC; Department of Drug Metabolism and Pharmacokinetics, Genentech, California, CA, USA., Kabza M; Roche Polska, Warsaw, Poland., Ahmed M; Roche Canada, Mississauga, Ontario, Canada., Li J; Department of Oncology Bioinformatics, Genentech, California, CA, USA., Chang MT; Department of Oncology Bioinformatics, Genentech, California, CA, USA., Maddalo D; Department of Translational Oncology, Genentech, California, CA, USA., Evangelista M; Department of Discovery Oncology, Genentech, California, CA, USA. evangem2@gmail.com., Ye X; Department of Discovery Oncology, Genentech, California, CA, USA. ye.xin@gene.com., Crawford JJ; Department of Discovery Chemistry, Genentech, California, CA, USA. crawford.james@gene.com., Dey A; Department of Discovery Oncology, Genentech, California, CA, USA. dey.anwesha@gene.com.

Publikováno v: Nature cancer [Nat Cancer] 2023 Jun; Vol. 4 (6), pp. 812-828. Date of Electronic Publication: 2023 Jun 05.

Kinetic, ESI-CID-MS and Computational Studies of π-Allyliridium C,O -Benzoate-Catalyzed Allylic Amination: Understanding the Effect of Cesium Ion.

Autor: Jung WO; University of Texas at Austin, Department of Chemistry, Austin, TX 78712, USA., Mai BK; Department of Chemistry, University of Pittsburgh, Pittsburgh, PA 15260, USA., Yoo M; University of Texas at Austin, Department of Chemistry, Austin, TX 78712, USA., Shields SWJ; University of Texas at Austin, Department of Chemistry, Austin, TX 78712, USA., Zbieg JR; Discovery Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, USA., Stivala CE; Discovery Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, USA., Liu P; Department of Chemistry, University of Pittsburgh, Pittsburgh, PA 15260, USA., Krische MJ; University of Texas at Austin, Department of Chemistry, Austin, TX 78712, USA.

Publikováno v: ACS catalysis [ACS Catal] 2022 Mar 18; Vol. 12 (6), pp. 3660-3668. Date of Electronic Publication: 2022 Mar 08.

The Direct Decarboxylative N -Alkylation of Azoles, Sulfonamides, Ureas, and Carbamates with Carboxylic Acids via Photoredox Catalysis.

Autor: Li P; Discovery Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Zbieg JR; Discovery Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Terrett JA; Discovery Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.

Publikováno v: Organic letters [Org Lett] 2021 Dec 17; Vol. 23 (24), pp. 9563-9568. Date of Electronic Publication: 2021 Dec 09.

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.

Visible-Light Photocatalysis as an Enabling Technology for Drug Discovery: A Paradigm Shift for Chemical Reactivity.

Autor: Li P; Discovery Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Terrett JA; Discovery Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States., Zbieg JR; Discovery Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States.

Publikováno v: ACS medicinal chemistry letters [ACS Med Chem Lett] 2020 Sep 21; Vol. 11 (11), pp. 2120-2130. Date of Electronic Publication: 2020 Sep 21 (Print Publication: 2020).