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本文引用的文献

1
Fitting of and Values from Endpoint Pre-incubation IC Data.根据终点预孵育IC数据拟合 和 值。
ACS Med Chem Lett. 2024 Apr 4;15(5):731-738. doi: 10.1021/acsmedchemlett.4c00054. eCollection 2024 May 9.
2
Emerging and Re-emerging Warheads for Targeted Covalent Inhibitors: An Update.新兴与重现的靶向共价抑制剂弹头:更新。
J Med Chem. 2024 May 23;67(10):7668-7758. doi: 10.1021/acs.jmedchem.3c01825. Epub 2024 May 6.
3
Development of Highly Potent and Selective Covalent FGFR4 Inhibitors Based on SAr Electrophiles.基于 SAr 亲电试剂的高效和选择性 FGFR4 共价抑制剂的开发。
J Med Chem. 2024 Apr 25;67(8):6549-6569. doi: 10.1021/acs.jmedchem.3c02483. Epub 2024 Apr 11.
4
Linking ATP and allosteric sites to achieve superadditive binding with bivalent EGFR kinase inhibitors.将ATP与变构位点相连以实现与二价表皮生长因子受体激酶抑制剂的超加成结合。
Commun Chem. 2024 Feb 20;7(1):38. doi: 10.1038/s42004-024-01108-3.
5
Pitfalls and Considerations in Determining the Potency and Mutant Selectivity of Covalent Epidermal Growth Factor Receptor Inhibitors.在确定共价表皮生长因子受体抑制剂的效力和突变选择性时的陷阱和注意事项。
J Med Chem. 2024 Jan 11;67(1):2-16. doi: 10.1021/acs.jmedchem.3c01502. Epub 2023 Dec 22.
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Inhibition of a lower potency target drives the anticancer activity of a clinical p38 inhibitor.低效能靶标抑制可驱动临床 p38 抑制剂的抗癌活性。
Cell Chem Biol. 2023 Oct 19;30(10):1211-1222.e5. doi: 10.1016/j.chembiol.2023.09.013. Epub 2023 Oct 11.
7
Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448).来泽替尼(YH25448)抑制突变型表皮生长因子受体的结构基础
ACS Med Chem Lett. 2022 Nov 10;13(12):1856-1863. doi: 10.1021/acsmedchemlett.2c00213. eCollection 2022 Dec 8.
8
Advances in covalent drug discovery.共价药物发现的进展。
Nat Rev Drug Discov. 2022 Dec;21(12):881-898. doi: 10.1038/s41573-022-00542-z. Epub 2022 Aug 25.
9
A Comprehensive Guide for Assessing Covalent Inhibition in Enzymatic Assays Illustrated with Kinetic Simulations.评估酶促分析中共价抑制的综合指南——结合动力学模拟加以说明。
Curr Protoc. 2022 Jun;2(6):e419. doi: 10.1002/cpz1.419.
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The Ascension of Targeted Covalent Inhibitors.靶向共价抑制剂的崛起。
J Med Chem. 2022 Apr 28;65(8):5886-5901. doi: 10.1021/acs.jmedchem.1c02134. Epub 2022 Apr 19.

Demystifying Functional Parameters for Irreversible Enzyme Inhibitors.

作者信息

Heppner David E, Ogboo Blessing C, Urul Daniel A, May Earl W, Schaefer Erik M, Murkin Andrew S, Gehringer Matthias

机构信息

Department of Chemistry, The State University of New York at Buffalo. Buffalo, New York 14221, United States.

AssayQuant Technologies Inc., Marlboro, Massachusetts 01752, United States.

出版信息

J Med Chem. 2024 Sep 12;67(17):14693-14696. doi: 10.1021/acs.jmedchem.4c01721. Epub 2024 Aug 8.

DOI:10.1021/acs.jmedchem.4c01721
PMID:39115869
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12057623/
Abstract
摘要