دورية أكاديمية
أعرض في EDS

A road map to evaluate the proteome-wide selectivity of covalent kinase inhibitors.

التفاصيل البيبلوغرافية
العنوان: A road map to evaluate the proteome-wide selectivity of covalent kinase inhibitors.
المؤلفون: Lanning BR; The Skaggs Institute for Chemical Biology and Department of Chemical Physiology, The Scripps Research Institute, 10550 N. Torrey Pines Rd. La Jolla, CA, 92307., Whitby LR; The Skaggs Institute for Chemical Biology and Department of Chemical Physiology, The Scripps Research Institute, 10550 N. Torrey Pines Rd. La Jolla, CA, 92307., Dix MM; The Skaggs Institute for Chemical Biology and Department of Chemical Physiology, The Scripps Research Institute, 10550 N. Torrey Pines Rd. La Jolla, CA, 92307., Douhan J; Pfizer Worldwide Research and Development, 200 Cambridge Park Drive, Cambridge, MA 02140., Gilbert AM; Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT 06340., Hett EC; Pfizer Worldwide Research and Development, 200 Cambridge Park Drive, Cambridge, MA 02140., Johnson TO; Pfizer Worldwide Research and Development, 10770 Science Park Drive, San Diego, CA 92121., Joslyn C; The Skaggs Institute for Chemical Biology and Department of Chemical Physiology, The Scripps Research Institute, 10550 N. Torrey Pines Rd. La Jolla, CA, 92307., Kath JC; Pfizer Worldwide Research and Development, 10770 Science Park Drive, San Diego, CA 92121., Niessen S; Pfizer Worldwide Research and Development, 10770 Science Park Drive, San Diego, CA 92121., Roberts LR; Pfizer Worldwide Research and Development, 200 Cambridge Park Drive, Cambridge, MA 02140., Schnute ME; Pfizer Worldwide Research and Development, 200 Cambridge Park Drive, Cambridge, MA 02140., Wang C; The Skaggs Institute for Chemical Biology and Department of Chemical Physiology, The Scripps Research Institute, 10550 N. Torrey Pines Rd. La Jolla, CA, 92307., Hulce JJ; The Skaggs Institute for Chemical Biology and Department of Chemical Physiology, The Scripps Research Institute, 10550 N. Torrey Pines Rd. La Jolla, CA, 92307., Wei B; Pfizer Worldwide Research and Development, 1 Burtt Rd, Andover, MA 01810., Whiteley LO; Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT 06340., Hayward MM; Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT 06340., Cravatt BF; The Skaggs Institute for Chemical Biology and Department of Chemical Physiology, The Scripps Research Institute, 10550 N. Torrey Pines Rd. La Jolla, CA, 92307.
المصدر: Nature chemical biology [Nat Chem Biol] 2014 Sep; Vol. 10 (9), pp. 760-767. Date of Electronic Publication: 2014 Jul 13.
نوع المنشور: Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't
اللغة: English
بيانات الدورية: Publisher: Nature Pub. Group Country of Publication: United States NLM ID: 101231976 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1552-4469 (Electronic) Linking ISSN: 15524450 NLM ISO Abbreviation: Nat Chem Biol Subsets: MEDLINE
أسماء مطبوعة: Original Publication: New York, NY : Nature Pub. Group, [2005]-
مواضيع طبية MeSH: Protein Kinase Inhibitors/*pharmacology , Proteome/*genetics, Adenine/analogs & derivatives ; Agammaglobulinaemia Tyrosine Kinase ; Cell Line, Tumor ; Cell Survival/drug effects ; Cysteine/chemistry ; Genes, erbB-1/genetics ; Humans ; Kinetics ; Piperidines ; Protein Kinases/metabolism ; Protein-Tyrosine Kinases/antagonists & inhibitors ; Pyrazoles/pharmacology ; Pyrimidines/pharmacology ; Signal Transduction/drug effects ; Signal Transduction/genetics
مستخلص: Kinases are principal components of signal transduction pathways and the focus of intense basic and drug discovery research. Irreversible inhibitors that covalently modify non-catalytic cysteines in kinase active sites have emerged as valuable probes and approved drugs. Many protein classes, however, have functional cysteines, and therefore understanding the proteome-wide selectivity of covalent kinase inhibitors is imperative. Here, we accomplish this objective using activity-based protein profiling coupled with quantitative MS to globally map the targets, both specific and nonspecific, of covalent kinase inhibitors in human cells. Many of the specific off-targets represent nonkinase proteins that, notably, have conserved active site cysteines. We define windows of selectivity for covalent kinase inhibitors and show that, when these windows are exceeded, rampant proteome-wide reactivity and kinase target-independent cell death conjointly occur. Our findings, taken together, provide an experimental road map to illuminate opportunities and surmount challenges for the development of covalent kinase inhibitors.
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معلومات مُعتمدة: R01 CA087660 United States CA NCI NIH HHS; R37 CA087660 United States CA NCI NIH HHS; CA087660 United States CA NCI NIH HHS
المشرفين على المادة: 0 (Piperidines)
0 (Protein Kinase Inhibitors)
0 (Proteome)
0 (Pyrazoles)
0 (Pyrimidines)
1X70OSD4VX (ibrutinib)
EC 2.7.- (Protein Kinases)
EC 2.7.10.1 (Protein-Tyrosine Kinases)
EC 2.7.10.2 (Agammaglobulinaemia Tyrosine Kinase)
JAC85A2161 (Adenine)
K848JZ4886 (Cysteine)
تواريخ الأحداث: Date Created: 20140721 Date Completed: 20141021 Latest Revision: 20240610
رمز التحديث: 20240610
مُعرف محوري في PubMed: PMC4138289
DOI: 10.1038/nchembio.1582
PMID: 25038787
قاعدة البيانات: MEDLINE
الوصف
تدمد:1552-4469
DOI:10.1038/nchembio.1582