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治疗类风湿关节炎的临床批准的小分子药物。

Clinically approved small-molecule drugs for the treatment of rheumatoid arthritis.

机构信息

Department of Orthopedics, China-Japan Union Hospital, Jilin University, Changchun, 130033, China.

The Rogel Cancer Center, Department of Internal Medicine, University of Michigan, Ann Arbor, MI, 48109, United States; School of Pharmaceutical Sciences & Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, Zhengzhou University, Zhengzhou, 450001, China.

出版信息

Eur J Med Chem. 2023 Aug 5;256:115434. doi: 10.1016/j.ejmech.2023.115434. Epub 2023 Apr 29.

Abstract

Rheumatoid arthritis (RA) is a persistent autoimmune ailment that is typified by the development of pannus, proliferation of synovial lining cells, microvascular neogenesis, infiltration of interstitial inflammatory cells, and destruction of cartilage and bone tissue. The disease not only imposes physical pain and economic burden on patients, but also results in a significant decline in their quality of life, rendering it a leading cause of disability. General treatment and drugs are commonly employed to alleviate the condition and symptoms of RA. Cyclooxygenase (COX), janus kinase (JAK), glucocorticoid receptor (GR) et al. have been identified as the main therapeutic targets for RA. This article provides a comprehensive review of the clinical applications and synthetic routes of 26 representative drugs for the treatment of RA, with the aim of facilitating the discovery of more effective new drugs for the treatment of this debilitating disease.

摘要

类风湿性关节炎(RA)是一种持续性自身免疫性疾病,其特征为血管翳的形成、滑膜衬里细胞的增殖、微血管新生、间质炎症细胞浸润以及软骨和骨组织的破坏。这种疾病不仅给患者带来身体上的痛苦和经济负担,还导致其生活质量显著下降,是导致残疾的主要原因之一。一般治疗和药物治疗常用于缓解 RA 的病情和症状。环氧化酶(COX)、Janus 激酶(JAK)、糖皮质激素受体(GR)等已被确定为 RA 的主要治疗靶点。本文全面综述了 26 种治疗 RA 的代表性药物的临床应用和合成途径,旨在促进发现更有效的新型治疗这种致残性疾病的药物。

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