المؤلفون: Flanagan JJ; Arvinas, 5 Science Park, New Haven, CT, 06511, USA., Neklesa TK; Halda Therapeutics, 23 Business Park, Branford, CT, 06405, USA. Electronic address: taavi.neklesa@haldathera.com.

المصدر: Molecular and cellular endocrinology [Mol Cell Endocrinol] 2019 Aug 01; Vol. 493, pp. 110452. Date of Electronic Publication: 2019 May 21.

نوع المنشور: Journal Article; Review

بيانات الدورية: Publisher: North Holland Publishing Country of Publication: Ireland NLM ID: 7500844 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1872-8057 (Electronic) Linking ISSN: 03037207 NLM ISO Abbreviation: Mol Cell Endocrinol Subsets: MEDLINE

مواضيع طبية MeSH: Receptors, Cytoplasmic and Nuclear/*chemistry , Receptors, Cytoplasmic and Nuclear/*metabolism , Small Molecule Libraries/*pharmacology, Animals ; Breast Neoplasms/drug therapy ; Breast Neoplasms/metabolism ; Drug Design ; Female ; Gene Expression Regulation/drug effects ; Humans ; Ligands ; Male ; Prostatic Neoplasms/drug therapy ; Prostatic Neoplasms/metabolism ; Protein Domains ; Proteolysis ; Receptors, Cytoplasmic and Nuclear/agonists ; Receptors, Cytoplasmic and Nuclear/antagonists & inhibitors ; Small Molecule Libraries/chemical synthesis ; Small Molecule Libraries/chemistry ; Small Molecule Libraries/therapeutic use

المؤلفون: Salami J; Department of Molecular, Cellular and Developmental Biology, Yale University, New Haven, 06511, CT, USA., Alabi S; Department of Pharmacology, Yale School of Medicine, New Haven, 06510, CT, USA., Willard RR; Arvinas, LLC, 5 Science Park, New Haven, 06511, CT, USA., Vitale NJ; Arvinas, LLC, 5 Science Park, New Haven, 06511, CT, USA., Wang J; Arvinas, LLC, 5 Science Park, New Haven, 06511, CT, USA., Dong H; Arvinas, LLC, 5 Science Park, New Haven, 06511, CT, USA., Jin M; Arvinas, LLC, 5 Science Park, New Haven, 06511, CT, USA., McDonnell DP; Department of Pharmacology and Cancer Biology, Duke University School of Medicine, Durham, 27710, NC, USA., Crew AP; Arvinas, LLC, 5 Science Park, New Haven, 06511, CT, USA., Neklesa TK; Arvinas, LLC, 5 Science Park, New Haven, 06511, CT, USA., Crews CM; Department of Molecular, Cellular and Developmental Biology, Yale University, New Haven, 06511, CT, USA. craig.crews@yale.edu.; Department of Pharmacology, Yale School of Medicine, New Haven, 06510, CT, USA. craig.crews@yale.edu.; Department of Chemistry, Yale University, New Haven, 06511, CT, USA. craig.crews@yale.edu.

المصدر: Communications biology [Commun Biol] 2018 Aug 02; Vol. 1, pp. 100. Date of Electronic Publication: 2018 Aug 02 (Print Publication: 2018).

نوع المنشور: Journal Article

بيانات الدورية: Publisher: Nature Publishing Group UK Country of Publication: England NLM ID: 101719179 Publication Model: eCollection Cited Medium: Internet ISSN: 2399-3642 (Electronic) Linking ISSN: 23993642 NLM ISO Abbreviation: Commun Biol Subsets: PubMed not MEDLINE

المؤلفون: Crew AP; Arvinas LLC , 5 Science Park, New Haven, Connecticut 06511, United States., Raina K; Arvinas LLC , 5 Science Park, New Haven, Connecticut 06511, United States., Dong H; Arvinas LLC , 5 Science Park, New Haven, Connecticut 06511, United States., Qian Y; Arvinas LLC , 5 Science Park, New Haven, Connecticut 06511, United States., Wang J; Arvinas LLC , 5 Science Park, New Haven, Connecticut 06511, United States., Vigil D; Arvinas LLC , 5 Science Park, New Haven, Connecticut 06511, United States., Serebrenik YV, Hamman BD; Arvinas LLC , 5 Science Park, New Haven, Connecticut 06511, United States., Morgan A; Arvinas LLC , 5 Science Park, New Haven, Connecticut 06511, United States., Ferraro C; Arvinas LLC , 5 Science Park, New Haven, Connecticut 06511, United States., Siu K; Arvinas LLC , 5 Science Park, New Haven, Connecticut 06511, United States., Neklesa TK; Arvinas LLC , 5 Science Park, New Haven, Connecticut 06511, United States., Winkler JD; Arvinas LLC , 5 Science Park, New Haven, Connecticut 06511, United States., Coleman KG; Arvinas LLC , 5 Science Park, New Haven, Connecticut 06511, United States., Crews CM

المصدر: Journal of medicinal chemistry [J Med Chem] 2018 Jan 25; Vol. 61 (2), pp. 583-598. Date of Electronic Publication: 2017 Jul 10.

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

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: Protein Serine-Threonine Kinases/*metabolism , Proteolysis/*drug effects , Von Hippel-Lindau Tumor Suppressor Protein/*metabolism, Cell Line ; Cell Proliferation/drug effects ; Chemistry Techniques, Synthetic ; Fluorescence Polarization ; Genes, ras ; Humans ; I-kappa B Kinase/genetics ; I-kappa B Kinase/metabolism ; Molecular Structure ; Mutation ; Protein Serine-Threonine Kinases/genetics ; RNA Interference ; Structure-Activity Relationship ; Von Hippel-Lindau Tumor Suppressor Protein/chemistry ; Von Hippel-Lindau Tumor Suppressor Protein/genetics

المؤلفون: Neklesa TK; Arvinas, LLC, 5 Science Park, New Haven, CT 06511, United States. Electronic address: Taavi.Neklesa@arvinas.com., Winkler JD; Arvinas, LLC, 5 Science Park, New Haven, CT 06511, United States., Crews CM; Department of Molecular, Cellular, and Developmental Biology, Yale University, New Haven, CT 06520, United States; Department of Chemistry, Yale University, New Haven, CT 06520, United States; Department of Pharmacology, Yale University, New Haven, CT 06520, United States.

المصدر: Pharmacology & therapeutics [Pharmacol Ther] 2017 Jun; Vol. 174, pp. 138-144. Date of Electronic Publication: 2017 Feb 14.

نوع المنشور: Journal Article; Review

بيانات الدورية: Publisher: Pergamon Press Country of Publication: England NLM ID: 7905840 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1879-016X (Electronic) Linking ISSN: 01637258 NLM ISO Abbreviation: Pharmacol Ther Subsets: MEDLINE

مواضيع طبية MeSH: Molecular Targeted Therapy*, Proteins/*metabolism , Proteolysis/*drug effects, Drug Delivery Systems ; Drug Design ; Enzyme Inhibitors/pharmacology ; Humans ; Molecular Weight ; Proteasome Endopeptidase Complex/metabolism ; Ubiquitination/physiology

المؤلفون: Gustafson JL; Departments of Molecular, Cellular, and Developmental Biology, Chemistry, and Pharmacology, Yale University, New Haven, CT 065111 (USA)., Neklesa TK; Departments of Molecular, Cellular, and Developmental Biology, Chemistry, and Pharmacology, Yale University, New Haven, CT 065111 (USA)., Cox CS; Departments of Molecular, Cellular, and Developmental Biology, Chemistry, and Pharmacology, Yale University, New Haven, CT 065111 (USA)., Roth AG; Departments of Molecular, Cellular, and Developmental Biology, Chemistry, and Pharmacology, Yale University, New Haven, CT 065111 (USA)., Buckley DL; Departments of Molecular, Cellular, and Developmental Biology, Chemistry, and Pharmacology, Yale University, New Haven, CT 065111 (USA)., Tae HS; Departments of Molecular, Cellular, and Developmental Biology, Chemistry, and Pharmacology, Yale University, New Haven, CT 065111 (USA)., Sundberg TB; Departments of Molecular, Cellular, and Developmental Biology, Chemistry, and Pharmacology, Yale University, New Haven, CT 065111 (USA)., Stagg DB; Department of Pharmacology and Cancer Biology, Duke University School of Medicine, Durham, NC 27710 (USA)., Hines J; Departments of Molecular, Cellular, and Developmental Biology, Chemistry, and Pharmacology, Yale University, New Haven, CT 065111 (USA)., McDonnell DP; Department of Pharmacology and Cancer Biology, Duke University School of Medicine, Durham, NC 27710 (USA)., Norris JD; Department of Pharmacology and Cancer Biology, Duke University School of Medicine, Durham, NC 27710 (USA)., Crews CM; Departments of Molecular, Cellular, and Developmental Biology, Chemistry, and Pharmacology, Yale University, New Haven, CT 065111 (USA). craig.crews@yale.edu.

المصدر: Angewandte Chemie (International ed. in English) [Angew Chem Int Ed Engl] 2015 Aug 10; Vol. 54 (33), pp. 9659-62. Date of Electronic Publication: 2015 Jun 17.

نوع المنشور: Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.

بيانات الدورية: Publisher: Wiley-VCH Country of Publication: Germany NLM ID: 0370543 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1521-3773 (Electronic) Linking ISSN: 14337851 NLM ISO Abbreviation: Angew Chem Int Ed Engl Subsets: MEDLINE

مواضيع طبية MeSH: Androgen Receptor Antagonists/*chemistry , Androgen Receptor Antagonists/*pharmacology , Proteolysis/*drug effects , Receptors, Androgen/*metabolism , Small Molecule Libraries/*chemistry , Small Molecule Libraries/*pharmacology, Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Benzamides ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Drug Resistance, Neoplasm ; Humans ; Hydrophobic and Hydrophilic Interactions ; Male ; Nitriles ; Phenylthiohydantoin/analogs & derivatives ; Phenylthiohydantoin/chemistry ; Phenylthiohydantoin/pharmacology ; Point Mutation ; Prostate/drug effects ; Prostate/metabolism ; Prostatic Neoplasms/drug therapy ; Prostatic Neoplasms/genetics ; Prostatic Neoplasms/metabolism ; Receptors, Androgen/genetics

المؤلفون: Neklesa TK; Department of Molecular Cellular and Developmental Biology, Yale University, 219 Prospect Street, New Haven, CT 06511, USA., Noblin DJ; Department of Molecular Cellular and Developmental Biology, Yale University, 219 Prospect Street, New Haven, CT 06511, USA., Kuzin AP; Department of Biological Sciences, Northeast Structural Genomics Consortium, Columbia University, New York, NY 10027, USA., Lew S; Department of Biological Sciences, Northeast Structural Genomics Consortium, Columbia University, New York, NY 10027, USA., Seetharaman J; Department of Biological Sciences, Northeast Structural Genomics Consortium, Columbia University, New York, NY 10027, USA., Acton TB; Center for Advanced Biotechnology and Medicine, Department of Molecular Biology and Biochemistry, and Northeast Structural Genomics Consortium, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA., Kornhaber GJ; Center for Advanced Biotechnology and Medicine, Department of Molecular Biology and Biochemistry, and Northeast Structural Genomics Consortium, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA., Xiao R; Center for Advanced Biotechnology and Medicine, Department of Molecular Biology and Biochemistry, and Northeast Structural Genomics Consortium, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA., Montelione GT; Center for Advanced Biotechnology and Medicine, Department of Molecular Biology and Biochemistry, and Northeast Structural Genomics Consortium, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA.; Department of Biochemistry and Molecular Biology, Robert Wood Johnson Medical School-UMDNJ, Piscataway, NJ 08854, USA., Tong L; Department of Biological Sciences, Northeast Structural Genomics Consortium, Columbia University, New York, NY 10027, USA., Crews CM; Department of Molecular Cellular and Developmental Biology, Yale University, 219 Prospect Street, New Haven, CT 06511, USA.; Department of Chemistry, Yale University, 225 Prospect Street, New Haven, CT 06511, USA.; Department of Pharmacology, Yale University, 333 Cedar Street, New Haven, CT 06511, USA.

المصدر: ACS chemical biology [ACS Chem Biol] 2013 Oct 18; Vol. 8 (10), pp. 2293-2300. Date of Electronic Publication: 2013 Aug 26.

نوع المنشور: Journal Article; Research Support, N.I.H., Extramural; Research Support, U.S. Gov't, Non-P.H.S.

بيانات الدورية: Publisher: American Chemical Society Country of Publication: United States NLM ID: 101282906 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1554-8937 (Electronic) Linking ISSN: 15548929 NLM ISO Abbreviation: ACS Chem Biol Subsets: MEDLINE

مواضيع طبية MeSH: Recombinant Fusion Proteins/*metabolism , Small Molecule Libraries/*metabolism, Binding Sites ; Crystallography, X-Ray ; Dose-Response Relationship, Drug ; Drosophila Proteins/genetics ; HEK293 Cells ; Humans ; Models, Molecular ; Mutation ; Protein Stability ; Temperature ; Ubiquitination

المؤلفون: Neklesa TK, Crews CM

المصدر: Nature [Nature] 2012 Jul 18; Vol. 487 (7407), pp. 308-9. Date of Electronic Publication: 2012 Jul 18.

نوع المنشور: News

بيانات الدورية: Publisher: Nature Publishing Group Country of Publication: England NLM ID: 0410462 Publication Model: Electronic Cited Medium: Internet ISSN: 1476-4687 (Electronic) Linking ISSN: 00280836 NLM ISO Abbreviation: Nature Subsets: MEDLINE

مواضيع طبية MeSH: Drug Discovery* , Proteolysis*, Humans ; Hydrophobic and Hydrophilic Interactions ; Protein Transport

المؤلفون: Tae HS; Department of Molecular Cellular and Developmental Biology, Yale University, 219 Prospect Street, New Haven, CT 06511, USA., Sundberg TB, Neklesa TK, Noblin DJ, Gustafson JL, Roth AG, Raina K, Crews CM

المصدر: Chembiochem : a European journal of chemical biology [Chembiochem] 2012 Mar 05; Vol. 13 (4), pp. 538-41. Date of Electronic Publication: 2012 Jan 23.

نوع المنشور: Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.

بيانات الدورية: Publisher: Wiley-VCH Verlag Country of Publication: Germany NLM ID: 100937360 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1439-7633 (Electronic) Linking ISSN: 14394227 NLM ISO Abbreviation: Chembiochem Subsets: MEDLINE

مواضيع طبية MeSH: Recombinant Fusion Proteins/*metabolism, HEK293 Cells ; Humans ; Hydrophobic and Hydrophilic Interactions ; Molecular Structure ; Recombinant Fusion Proteins/chemistry

المؤلفون: Neklesa TK; Department of Molecular, Cellular and Developmental Biology, Yale University, New Haven, Connecticut, USA., Tae HS, Schneekloth AR, Stulberg MJ, Corson TW, Sundberg TB, Raina K, Holley SA, Crews CM

المصدر: Nature chemical biology [Nat Chem Biol] 2011 Jul 03; Vol. 7 (8), pp. 538-43. Date of Electronic Publication: 2011 Jul 03.

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

بيانات الدورية: Publisher: Nature Pub. Group Country of Publication: United States NLM ID: 101231976 Publication Model: Electronic Cited Medium: Internet ISSN: 1552-4469 (Electronic) Linking ISSN: 15524450 NLM ISO Abbreviation: Nat Chem Biol Subsets: MEDLINE

مواضيع طبية MeSH: Biosensing Techniques/*methods , Fluorescent Dyes/*chemistry, Animals ; Cell Line ; Humans ; Hydrophobic and Hydrophilic Interactions ; Luminescent Proteins/chemistry ; Mice ; Molecular Structure ; Recombinant Proteins ; Sensitivity and Specificity ; Staining and Labeling ; Zebrafish

المؤلفون: Neklesa TK; Department of Biochemistry, Stanford University, Stanford, CA, USA. taavi.neklesa@yale.edu, Davis RW

المصدر: PLoS genetics [PLoS Genet] 2009 Jun; Vol. 5 (6), pp. e1000515. Date of Electronic Publication: 2009 Jun 12.

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

بيانات الدورية: Publisher: Public Library of Science Country of Publication: United States NLM ID: 101239074 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1553-7404 (Electronic) Linking ISSN: 15537390 NLM ISO Abbreviation: PLoS Genet Subsets: MEDLINE

مواضيع طبية MeSH: Evolution, Molecular*, Amino Acids/*metabolism , Intracellular Signaling Peptides and Proteins/*metabolism , Saccharomyces cerevisiae/*genetics , Saccharomyces cerevisiae/*metabolism , Saccharomyces cerevisiae Proteins/*metabolism, Dimerization ; Gene Expression Regulation, Fungal ; HeLa Cells ; Humans ; Intracellular Signaling Peptides and Proteins/genetics ; Protein Binding ; Saccharomyces cerevisiae Proteins/genetics