药物发现中的共价结合物。

Q1 Pharmacology, Toxicology and Pharmaceutics

Progress in medicinal chemistry Pub Date : 2019-01-01 Epub Date: 2019-03-11 DOI:10.1016/bs.pmch.2018.12.002

Anil Vasudevan, Maria A Argiriadi, Aleksandra Baranczak, Michael M Friedman, Julia Gavrilyuk, Adrian D Hobson, Jonathan J Hulce, Sami Osman, Noel S Wilson

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引用次数: 24

摘要

蛋白质功能的共价调节可以有多种用途，包括治疗和探针来询问生物学。虽然由于潜在的(特异性)毒性，这一领域仍然受到怀疑，但在理解如何调整亲电性以选择性地靶向特定残基方面已经取得了重大进展。在利用共价结合物的潜力来发现新的生物学和提供作为抗体药物偶联物有效载荷的增强效用方面也取得了进展。这一观点涵盖了共价粘合剂的原理和应用。

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Covalent binders in drug discovery.

Covalent modulation of protein function can have multiple utilities including therapeutics, and probes to interrogate biology. While this field is still viewed with scepticism due to the potential for (idiosyncratic) toxicities, significant strides have been made in terms of understanding how to tune electrophilicity to selectively target specific residues. Progress has also been made in harnessing the potential of covalent binders to uncover novel biology and to provide an enhanced utility as payloads for Antibody Drug Conjugates. This perspective covers the tenets and applications of covalent binders.

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来源期刊

Progress in medicinal chemistry Pharmacology, Toxicology and Pharmaceutics-Pharmacology

CiteScore

15.60

自引率

0.00%

发文量

期刊介绍： This series has a long established reputation for excellent coverage of almost every facet of Medicinal Chemistry and is one of the most respected and instructive sources of information on the subject. The latest volume certifies to the continuing success of a unique series reflecting current progress in a broadly developing field of science.