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Small-molecule inhibition of kinesin KIF18A reveals a mitotic vulnerability enriched in chromosomally unstable cancers.

Autor: Payton M; Oncology Research, Amgen Research, Thousand Oaks, CA, USA. mpayton@amgen.com., Belmontes B; Oncology Research, Amgen Research, Thousand Oaks, CA, USA., Hanestad K; Oncology Research, Amgen Research, Thousand Oaks, CA, USA., Moriguchi J; Oncology Research, Amgen Research, Thousand Oaks, CA, USA., Chen K; Lead Discovery and Characterization, Amgen Research, Thousand Oaks, CA, USA., McCarter JD; Lead Discovery and Characterization, Amgen Research, Thousand Oaks, CA, USA., Chung G; Oncology Research, Amgen Research, Thousand Oaks, CA, USA., Ninniri MS; Oncology Research, Amgen Research, Thousand Oaks, CA, USA., Sun J; Oncology Research, Amgen Research, Thousand Oaks, CA, USA., Manoukian R; Cytometry Sciences, Amgen Research, Cambridge, MA, USA., Chambers S; Research Biomics, Amgen Research, San Francisco, CA, USA., Ho SM; Research Biomics, Amgen Research, San Francisco, CA, USA., Kurzeja RJM; Protein Technologies, Amgen Research, Thousand Oaks, CA, USA., Edson KZ; PKDM, Amgen Research, Thousand Oaks, CA, USA., Dahal UP; PKDM, Amgen Research, San Francisco, CA, USA., Wu T; Pre-Pivotal Drug Product, Amgen Process Development, Thousand Oaks, CA, USA., Wannberg S; Inflammation, Amgen Research, Thousand Oaks, CA, USA., Beltran PJ; Oncology Research, Amgen Research, Thousand Oaks, CA, USA., Canon J; Oncology Research, Amgen Research, Thousand Oaks, CA, USA., Boghossian AS; Broad Institute of MIT and Harvard, Cambridge, MA, USA., Rees MG; Broad Institute of MIT and Harvard, Cambridge, MA, USA., Ronan MM; Broad Institute of MIT and Harvard, Cambridge, MA, USA., Roth JA; Broad Institute of MIT and Harvard, Cambridge, MA, USA., Minocherhomji S; Translational Safety and Bioanalytical Sciences, Amgen Research, Thousand Oaks, CA, USA., Bourbeau MP; Medicinal Chemistry, Amgen Research, Thousand Oaks, CA, USA., Allen JR; Medicinal Chemistry, Amgen Research, Thousand Oaks, CA, USA., Coxon A; Oncology Research, Amgen Research, Thousand Oaks, CA, USA., Tamayo NA; Medicinal Chemistry, Amgen Research, Thousand Oaks, CA, USA., Hughes PE; Oncology Research, Amgen Research, Thousand Oaks, CA, USA.

Publikováno v: Nature cancer [Nat Cancer] 2024 Jan; Vol. 5 (1), pp. 66-84. Date of Electronic Publication: 2023 Dec 27.

The development of a structurally distinct series of BACE1 inhibitors via the (Z)-fluoro-olefin amide bioisosteric replacement.

Autor: Frohn M; Medicinal Chemistry, Amgen Discovery Research, Amgen Inc., Thousand Oaks, CA 91320, United States. Electronic address: mfrohn@amgen.com., Liu L; Medicinal Chemistry, Amgen Discovery Research, Amgen Inc., Thousand Oaks, CA 91320, United States., Siegmund AC; Medicinal Chemistry, Amgen Discovery Research, Amgen Inc., Thousand Oaks, CA 91320, United States., Qian W; Medicinal Chemistry, Amgen Discovery Research, Amgen Inc., Thousand Oaks, CA 91320, United States., Amegadzie A; Medicinal Chemistry, Amgen Discovery Research, Amgen Inc., Thousand Oaks, CA 91320, United States., Chen N; Medicinal Chemistry, Amgen Discovery Research, Amgen Inc., Thousand Oaks, CA 91320, United States., Tan H; Pre-Pivotal Drug Product, Amgen Discovery Research, Amgen Inc., Thousand Oaks, CA 91320, United States., Hickman D; Pharmicokinetics and Drug Metabolism, Amgen Discovery Research, Amgen Inc., Thousand Oaks, CA 91320, United States., Wood S; Neuroscience Research, Amgen Discovery Research, Amgen Inc., Thousand Oaks, CA 91320, United States., Wen PH; Neuroscience Research, Amgen Discovery Research, Amgen Inc., Thousand Oaks, CA 91320, United States., Bartberger MD; Molecular Engineering, Amgen Discovery Research, Amgen Inc., Thousand Oaks, CA 91320, United States., Whittington DA; Molecular Engineering, Amgen Discovery Research, Amgen Inc., Thousand Oaks, CA 91320, United States., Allen JR; Medicinal Chemistry, Amgen Discovery Research, Amgen Inc., Thousand Oaks, CA 91320, United States., Bourbeau MP; Medicinal Chemistry, Amgen Discovery Research, Amgen Inc., Thousand Oaks, CA 91320, United States.

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2020 Jul 15; Vol. 30 (14), pp. 127240. Date of Electronic Publication: 2020 May 04.

Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ*S-X) Interaction for Conformational Constraint.

Autor: Pennington LD; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Bartberger MD; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Croghan MD; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Andrews KL; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Ashton KS; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Bourbeau MP; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Chen J; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Chmait S; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Cupples R; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Fotsch C; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Helmering J; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Hong FT; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Hungate RW; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Jordan SR; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Kong K; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Liu L; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Michelsen K; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Moyer C; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Nishimura N; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Norman MH; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Reichelt A; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Siegmund AC; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Sivits G; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Tadesse S; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Tegley CM; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Van G; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Yang KC; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Yao G; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Zhang J; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Lloyd DJ; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., Hale C; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States., St Jean DJ Jr; Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen , One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2015 Dec 24; Vol. 58 (24), pp. 9663-79. Date of Electronic Publication: 2015 Dec 01.