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小分子治疗自身免疫和炎症性疾病的方法(第一部分):激酶抑制剂。

Small molecule approaches to treat autoimmune and inflammatory diseases (Part I): Kinase inhibitors.

机构信息

Department of Medicinal Chemistry, Roche Innovation Center Shanghai, Roche Pharma Research and Early Development, Shanghai 201203, China.

Department of Medicinal Chemistry, Roche Innovation Center Shanghai, Roche Pharma Research and Early Development, Shanghai 201203, China.

出版信息

Bioorg Med Chem Lett. 2021 Apr 15;38:127862. doi: 10.1016/j.bmcl.2021.127862. Epub 2021 Feb 18.

Abstract

Autoimmune and inflammatory diseases place a huge burden on the healthcare system. Small molecule (SM) therapeutics provide much needed complementary treatment options for these diseases. This digest series highlights the latest progress in the discovery and development of safe and efficacious SMs to treat autoimmune and inflammatory diseases with each part representing a class of SMs, namely: 1) protein kinases; 2) nucleic acid-sensing pathways; and 3) soluble ligands and receptors on cell surfaces. In this first part of the series, the focus is on kinase inhibitors that emerged between 2018 and 2020, and which exhibit increased target and tissue selectivity with the aim of increasing their therapeutic index.

摘要

自身免疫性和炎症性疾病给医疗保健系统带来了巨大的负担。小分子 (SM) 疗法为这些疾病提供了急需的补充治疗选择。本综述系列重点介绍了在发现和开发治疗自身免疫性和炎症性疾病的安全有效的 SM 方面的最新进展,每个部分都代表一类 SM,即:1)蛋白激酶;2)核酸感应途径;3)细胞表面的可溶性配体和受体。在该系列的第一部分中,重点是 2018 年至 2020 年间出现的激酶抑制剂,这些抑制剂表现出更高的靶标和组织选择性,旨在提高其治疗指数。

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