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المؤلفون: Hornberger KR; Arvinas Operations, Inc., 5 Science Park, 395 Winchester Avenue, New Haven, Connecticut 06511 United States., Araujo EMV; Arvinas Operations, Inc., 5 Science Park, 395 Winchester Avenue, New Haven, Connecticut 06511 United States.

المصدر: Journal of medicinal chemistry [J Med Chem] 2023 Jun 22; Vol. 66 (12), pp. 8281-8287. Date of Electronic Publication: 2023 Jun 06.

نوع المنشور: Journal Article

بيانات الدورية: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE

مواضيع طبية MeSH: Liver*, Rats ; Mice ; Animals ; Proteolysis

المؤلفون: Chirnomas D; Arvinas Operations, Inc., New Haven, CT, USA. debbie.chirnomas@arvinas.com., Hornberger KR; Arvinas Operations, Inc., New Haven, CT, USA. keith.hornberger@arvinas.com., Crews CM; Department of Molecular, Cellular & Developmental Biology, Yale University, New Haven, CT, USA. craig.crews@yale.edu.; Department of Pharmacology, Yale University, New Haven, CT, USA. craig.crews@yale.edu.; Department of Chemistry, Yale University, New Haven, CT, USA. craig.crews@yale.edu.

المصدر: Nature reviews. Clinical oncology [Nat Rev Clin Oncol] 2023 Apr; Vol. 20 (4), pp. 265-278. Date of Electronic Publication: 2023 Feb 13.

نوع المنشور: Journal Article; Review; Research Support, N.I.H., Extramural

بيانات الدورية: Publisher: Nature Pub. Group Country of Publication: England NLM ID: 101500077 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1759-4782 (Electronic) Linking ISSN: 17594774 NLM ISO Abbreviation: Nat Rev Clin Oncol Subsets: MEDLINE

مواضيع طبية MeSH: Neoplasms*/drug therapy, Humans ; Proteins/metabolism ; Proteolysis

المؤلفون: Meyers K; Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, United States., Cogan DA; Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, United States. Electronic address: derek.cogan@bioverativ.com., Burke J; Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, United States., Arenas R; Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, United States., Balestra M; Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, United States., Brown NF; Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, United States., Chen Z; Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, United States., Cerny MA; Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, United States., Clifford HE; Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, United States., Colombo F; Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, United States., Fader L; Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, United States., Frederick KS; Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, United States., Guo X; Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, United States., Goldberg D; Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, United States., Hornberger KR; Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, United States., Kugler S; Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, United States., Lord J; Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, United States., Marshall DR; Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, United States., Moss N; Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, United States., Parmentier JH; Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, United States., Richman JR; Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, United States., Schmenk J; Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, United States., Weldon SM; Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, United States., Yu M; Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, United States., Zhang M; Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Road, Ridgefield, CT 06877, United States.

المصدر: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2018 Mar 01; Vol. 28 (5), pp. 979-984. Date of Electronic Publication: 2017 Dec 08.

نوع المنشور: Journal Article

بيانات الدورية: Publisher: Elsevier Science Ltd Country of Publication: England NLM ID: 9107377 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3405 (Electronic) Linking ISSN: 0960894X NLM ISO Abbreviation: Bioorg Med Chem Lett Subsets: MEDLINE

مواضيع طبية MeSH: Cytochrome P-450 CYP11B2/*antagonists & inhibitors , Enzyme Inhibitors/*pharmacology , Isoxazoles/*pharmacology, Cytochrome P-450 CYP11B2/metabolism ; Dose-Response Relationship, Drug ; Enzyme Inhibitors/chemical synthesis ; Enzyme Inhibitors/chemistry ; Humans ; Isoxazoles/chemical synthesis ; Isoxazoles/chemistry ; Molecular Structure ; Structure-Activity Relationship

المؤلفون: Hornberger KR; OSI Pharmaceuticals LLC, 1 Bioscience Park Drive, Farmingdale, NY 11735, USA. keith.hornberger@boehringer-ingelheim.com, Chen X, Crew AP, Kleinberg A, Ma L, Mulvihill MJ, Wang J, Wilde VL, Albertella M, Bittner M, Cooke A, Kadhim S, Kahler J, Maresca P, May E, Meyn P, Romashko D, Tokar B, Turton R

المصدر: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2013 Aug 15; Vol. 23 (16), pp. 4511-6. Date of Electronic Publication: 2013 Jun 27.

نوع المنشور: Journal Article

بيانات الدورية: Publisher: Elsevier Science Ltd Country of Publication: England NLM ID: 9107377 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3405 (Electronic) Linking ISSN: 0960894X NLM ISO Abbreviation: Bioorg Med Chem Lett Subsets: MEDLINE

مواضيع طبية MeSH: Enzyme Inhibitors*/chemical synthesis , Enzyme Inhibitors*/pharmacokinetics , Enzyme Inhibitors*/pharmacology , Pyridines*/chemical synthesis , Pyridines*/pharmacokinetics , Pyridines*/pharmacology, MAP Kinase Kinase Kinases/*antagonists & inhibitors, Amines/chemical synthesis ; Amines/chemistry ; Amines/pharmacology ; Animals ; Crystallography, X-Ray ; Enzyme Activation/drug effects ; Furans/chemical synthesis ; Furans/chemistry ; Furans/pharmacology ; Humans ; Inhibitory Concentration 50 ; MAP Kinase Kinase Kinases/metabolism ; Mice ; Molecular Structure ; Neoplasms/drug therapy ; Phosphotransferases/chemistry ; Phosphotransferases/metabolism ; Structure-Activity Relationship ; Xenograft Model Antitumor Assays

المؤلفون: Hornberger KR; OSI Pharmaceuticals LLC, 1 Bioscience Park Drive, Farmingdale, NY 11735, USA. keith.hornberger@boehringer-ingelheim.com, Berger DM, Crew AP, Dong H, Kleinberg A, Li AH, Medeiros MR, Mulvihill MJ, Siu K, Tarrant J, Wang J, Weng F, Wilde VL, Albertella M, Bittner M, Cooke A, Gray MJ, Maresca P, May E, Meyn P, Peick W Jr, Romashko D, Tanowitz M, Tokar B

المصدر: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2013 Aug 15; Vol. 23 (16), pp. 4517-22. Date of Electronic Publication: 2013 Jun 25.

نوع المنشور: Journal Article

بيانات الدورية: Publisher: Elsevier Science Ltd Country of Publication: England NLM ID: 9107377 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3405 (Electronic) Linking ISSN: 0960894X NLM ISO Abbreviation: Bioorg Med Chem Lett Subsets: MEDLINE

مواضيع طبية MeSH: Pyridines*/chemical synthesis , Pyridines*/pharmacokinetics , Pyridines*/pharmacology, MAP Kinase Kinase Kinases/*antagonists & inhibitors, Amines/chemical synthesis ; Amines/chemistry ; Amines/pharmacology ; Animals ; Crystallography, X-Ray ; Drug Design ; Enzyme Activation/drug effects ; Enzyme Inhibitors/chemical synthesis ; Enzyme Inhibitors/pharmacokinetics ; Enzyme Inhibitors/pharmacology ; Furans/chemical synthesis ; Furans/chemistry ; Furans/pharmacology ; Humans ; Inhibitory Concentration 50 ; Mice ; Molecular Structure ; Neoplasms/drug therapy ; Structure-Activity Relationship ; Xenograft Model Antitumor Assays

المؤلفون: Rheault TR; Oncology R&D Medicinal Chemistry, GlaxoSmithKline , Research Triangle Park , North Carolina 27709, United States., Stellwagen JC; Oncology R&D Medicinal Chemistry, GlaxoSmithKline , Research Triangle Park , North Carolina 27709, United States., Adjabeng GM; Oncology R&D Medicinal Chemistry, GlaxoSmithKline , Research Triangle Park , North Carolina 27709, United States., Hornberger KR; Oncology R&D Medicinal Chemistry, GlaxoSmithKline , Research Triangle Park , North Carolina 27709, United States., Petrov KG; Oncology R&D Medicinal Chemistry, GlaxoSmithKline , Research Triangle Park , North Carolina 27709, United States., Waterson AG; Oncology R&D Medicinal Chemistry, GlaxoSmithKline , Research Triangle Park , North Carolina 27709, United States., Dickerson SH; Computational and Structural Chemistry, GlaxoSmithKline , Research Triangle Park, North Carolina 27709, United States., Mook RA Jr; Oncology R&D Medicinal Chemistry, GlaxoSmithKline , Research Triangle Park , North Carolina 27709, United States., Laquerre SG; Oncology R&D Cancer Research, GlaxoSmithKline , Collegeville Road, Collegeville, Pennsylvania 19426, United States., King AJ; Oncology R&D Cancer Research, GlaxoSmithKline , Collegeville Road, Collegeville, Pennsylvania 19426, United States., Rossanese OW; Oncology R&D Cancer Research, GlaxoSmithKline , Collegeville Road, Collegeville, Pennsylvania 19426, United States., Arnone MR; Oncology R&D Cancer Research, GlaxoSmithKline , Collegeville Road, Collegeville, Pennsylvania 19426, United States., Smitheman KN; Oncology R&D Cancer Research, GlaxoSmithKline , Collegeville Road, Collegeville, Pennsylvania 19426, United States., Kane-Carson LS; Platform Technology & Science, GlaxoSmithKline , Research Triangle Park, North Carolina 27709, United States., Han C; Oncology R&D Cancer Research, GlaxoSmithKline , Collegeville Road, Collegeville, Pennsylvania 19426, United States., Moorthy GS; Oncology R&D Cancer Research, GlaxoSmithKline , Collegeville Road, Collegeville, Pennsylvania 19426, United States., Moss KG; Oncology R&D Cancer Research, GlaxoSmithKline , Collegeville Road, Collegeville, Pennsylvania 19426, United States., Uehling DE; Oncology R&D Medicinal Chemistry, GlaxoSmithKline , Research Triangle Park , North Carolina 27709, United States.

المصدر: ACS medicinal chemistry letters [ACS Med Chem Lett] 2013 Feb 07; Vol. 4 (3), pp. 358-62. Date of Electronic Publication: 2013 Feb 07 (Print Publication: 2013).

نوع المنشور: Journal Article

بيانات الدورية: Publisher: American Chemical Society Country of Publication: United States NLM ID: 101521073 Publication Model: eCollection Cited Medium: Print ISSN: 1948-5875 (Print) Linking ISSN: 19485875 NLM ISO Abbreviation: ACS Med Chem Lett Subsets: PubMed not MEDLINE

المؤلفون: Bee WT; Department of Biological Reagents and Assay Development, Molecular Discovery Research, GlaxoSmithKline, Collegeville, PA 19426-0989, USA., Xie W, Truong M, Will M, Turunen B, Zuercher WJ, McMillan L, Li H, Hornberger KR, Davenport EA, Ames RS, Kallal LA

المصدر: Journal of biomolecular screening [J Biomol Screen] 2012 Aug; Vol. 17 (7), pp. 900-11. Date of Electronic Publication: 2012 May 29.

نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't

بيانات الدورية: Publisher: Sage Publications Country of Publication: United States NLM ID: 9612112 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1552-454X (Electronic) Linking ISSN: 10870571 NLM ISO Abbreviation: J Biomol Screen Subsets: MEDLINE

مواضيع طبية MeSH: Benzamides/*metabolism , Benzimidazoles/*metabolism , Cyclohexylamines/*metabolism , Drug Evaluation, Preclinical/*methods , High-Throughput Screening Assays/*methods , Receptors, G-Protein-Coupled/*antagonists & inhibitors , Receptors, G-Protein-Coupled/*metabolism , Thiophenes/*metabolism, Algorithms ; Baculoviridae/genetics ; Benzamides/chemistry ; Benzamides/pharmacology ; Benzimidazoles/chemistry ; Benzimidazoles/pharmacology ; Cell Line ; Cyclohexylamines/chemistry ; Cyclohexylamines/pharmacology ; Fluorescent Dyes ; Genes, Reporter ; HEK293 Cells ; Humans ; Morpholines/chemistry ; Morpholines/metabolism ; Morpholines/pharmacology ; Piperazines/chemistry ; Piperazines/metabolism ; Piperazines/pharmacology ; Protein Binding ; Purines/chemistry ; Purines/metabolism ; Purines/pharmacology ; Pyrazoles/chemistry ; Pyrazoles/metabolism ; Pyrazoles/pharmacology ; Smoothened Receptor ; Thiophenes/chemistry ; Thiophenes/pharmacology