دورية أكاديمية
أعرض في EDS

The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study.

التفاصيل البيبلوغرافية
العنوان: The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study.
المؤلفون: Burslem GM; Department of Molecular, Cellular, and Developmental Biology, Yale University, 219 Prospect Street, New Haven, CT, USA., Smith BE; Department of Molecular, Cellular, and Developmental Biology, Yale University, 219 Prospect Street, New Haven, CT, USA., Lai AC; Department of Molecular, Cellular, and Developmental Biology, Yale University, 219 Prospect Street, New Haven, CT, USA., Jaime-Figueroa S; Department of Molecular, Cellular, and Developmental Biology, Yale University, 219 Prospect Street, New Haven, CT, USA., McQuaid DC; Department of Molecular, Cellular, and Developmental Biology, Yale University, 219 Prospect Street, New Haven, CT, USA., Bondeson DP; Department of Molecular, Cellular, and Developmental Biology, Yale University, 219 Prospect Street, New Haven, CT, USA., Toure M; Department of Molecular, Cellular, and Developmental Biology, Yale University, 219 Prospect Street, New Haven, CT, USA., Dong H; Arvinas, LLC, 5 Science Park, New Haven, CT, USA., Qian Y; Arvinas, LLC, 5 Science Park, New Haven, CT, USA., Wang J; Arvinas, LLC, 5 Science Park, New Haven, CT, USA., Crew AP; Arvinas, LLC, 5 Science Park, New Haven, CT, USA., Hines J; Department of Molecular, Cellular, and Developmental Biology, Yale University, 219 Prospect Street, New Haven, CT, USA., Crews CM; Department of Molecular, Cellular, and Developmental Biology, Yale University, 219 Prospect Street, New Haven, CT, USA; Departments of Chemistry and Pharmacology, Yale University, New Haven, CT, USA. Electronic address: craig.crews@yale.edu.
المصدر: Cell chemical biology [Cell Chem Biol] 2018 Jan 18; Vol. 25 (1), pp. 67-77.e3. Date of Electronic Publication: 2017 Nov 09.
نوع المنشور: Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't
اللغة: English
بيانات الدورية: Publisher: Cell Press Country of Publication: United States NLM ID: 101676030 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 2451-9448 (Electronic) Linking ISSN: 24519448 NLM ISO Abbreviation: Cell Chem Biol Subsets: MEDLINE
أسماء مطبوعة: Original Publication: Cambridge, MA : Cell Press, 2016-
مواضيع طبية MeSH: Enzyme Inhibitors*/chemistry , Enzyme Inhibitors*/pharmacology , Proteolysis* , Receptor Protein-Tyrosine Kinases*/antagonists & inhibitors , Receptor Protein-Tyrosine Kinases*/metabolism , Ubiquitin-Protein Ligases*/antagonists & inhibitors , Ubiquitin-Protein Ligases*/metabolism, Humans ; Ligands
مستخلص: Proteolysis targeting chimera (PROTAC) technology has emerged over the last two decades as a powerful tool for targeted degradation of endogenous proteins. Herein we describe the development of PROTACs for receptor tyrosine kinases, a protein family yet to be targeted for induced protein degradation. The use of VHL-recruiting PROTACs against this protein family reveals several advantages of degradation over inhibition alone: direct comparisons of fully functional, target-degrading PROTACs with target-inhibiting variants that contain an inactivated E3 ligase-recruiting ligand show that degradation leads to more potent inhibition of cell proliferation and a more durable and sustained downstream signaling response, and thus addresses the kinome rewiring challenge seen with many receptor tyrosine kinase inhibitors. Combined, these findings demonstrate the ability to target receptor tyrosine kinases for degradation using the PROTAC technology and outline the advantages of this degradation-based approach.
(Copyright © 2017 Elsevier Ltd. All rights reserved.)
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معلومات مُعتمدة: T32 GM007223 United States GM NIGMS NIH HHS; R50 CA211252 United States CA NCI NIH HHS; R35 CA197589 United States CA NCI NIH HHS; T32 GM007205 United States GM NIGMS NIH HHS; F99 CA212229 United States CA NCI NIH HHS; P50 CA196530 United States CA NCI NIH HHS
فهرسة مساهمة: Keywords: EGFR; HER2; PROTAC; VHL; c-Met; receptor tyrosine kinases; targeted degradation
المشرفين على المادة: 0 (Enzyme Inhibitors)
0 (Ligands)
EC 2.7.10.1 (Receptor Protein-Tyrosine Kinases)
EC 2.3.2.27 (Ubiquitin-Protein Ligases)
تواريخ الأحداث: Date Created: 20171114 Date Completed: 20181226 Latest Revision: 20240229
رمز التحديث: 20240229
مُعرف محوري في PubMed: PMC5831399
DOI: 10.1016/j.chembiol.2017.09.009
PMID: 29129716
قاعدة البيانات: MEDLINE
الوصف
تدمد:2451-9448
DOI:10.1016/j.chembiol.2017.09.009