摘要
本文介绍了整合素的简化视图,重点介绍了 α4 (α4β1/VLA-4) 整合素。整联蛋白是表达在白细胞细胞表面的异二聚体蛋白,其参与多种功能,例如存活、生长、分化、迁移、炎症反应、肿瘤侵袭等。当细胞外基质降解或变形时,细胞被迫经历影响生理和病理事件重塑的响应性变化。整合素识别这些变化并触发一系列细胞反应,在细胞内部和外部之间形成物理连接。整联蛋白通过质膜的通讯发生在两个方向,从细胞外到细胞内(由外向内)和从细胞内到细胞外(由内向外)。整联蛋白是抗体和小分子拮抗剂的有效靶标。一个例子是单克隆抗体那他珠单抗,以 TYSABRIR 的名义上市,用于治疗复发性多发性硬化症,它抑制 α4 整联蛋白与其反受体的粘附。此处总结了 α4β1 整联蛋白拮抗剂,还讨论了它们作为治疗剂的用途。
关键词: 整合素、靶标、粘附分子、CD49d、VLA-4、α4、α4β1 整合素拮抗剂、细胞外基质。
Current Medicinal Chemistry
Title:An Overview of the α4β1 Integrin and the Potential Therapeutic Role of its Antagonists
Volume: 28 Issue: 29
关键词: 整合素、靶标、粘附分子、CD49d、VLA-4、α4、α4β1 整合素拮抗剂、细胞外基质。
摘要: This article presents a simplified view of integrins with emphasis on the α4 (α4β1/VLA-4) integrin. Integrins are heterodimeric proteins expressed on the cell surface of leukocytes that participate in a wide variety of functions, such as survival, growth, differentiation, migration, inflammatory responses, tumour invasion, among others. When the extracellular matrix is degraded or deformed, cells are forced to undergo responsive changes that influence remodelling during physiological and pathological events. Integrins recognize these changes and trigger a series of cellular responses, forming a physical connection between the interior and the outside of the cell. The communication of integrins through the plasma membrane occurs in both directions, from the extracellular to the intracellular (outside-in) and from the intracellular to the extracellular (inside-out). Integrins are valid targets for antibodies and small-molecule antagonists. One example is the monoclonal antibody natalizumab, marketed under the name of TYSABRI®, used in the treatment of recurrent multiple sclerosis, which inhibits the adhesion of α4 integrin to its counter-receptor. α4β1 Integrin antagonists are summarized here, and their utility as therapeutics are also discussed.
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Cite this article as:
An Overview of the α4β1 Integrin and the Potential Therapeutic Role of its Antagonists, Current Medicinal Chemistry 2021; 28 (29) . https://dx.doi.org/10.2174/0929867328666210217153609
DOI https://dx.doi.org/10.2174/0929867328666210217153609 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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