溶血磷脂酸受体亚型 5（LPAR5）在炎症性疾病和癌症中的新兴作用。
Emerging roles of lysophosphatidic acid receptor subtype 5 (LPAR5) in inflammatory diseases and cancer.
机构信息
Department of Physiology, College of Medicine, University of Tennessee Health Science Center (UTHSC), Memphis, TN, United States of America.
Department of Physiology, College of Medicine, University of Tennessee Health Science Center (UTHSC), Memphis, TN, United States of America.
出版信息
Pharmacol Ther. 2023 May;245:108414. doi: 10.1016/j.pharmthera.2023.108414. Epub 2023 Apr 13.
Abstract
Lysophosphatidic acid (LPA) is a bioactive lipid mediator that regulates a variety of cellular functions such as cell proliferation, migration, survival, calcium mobilization, cytoskeletal rearrangements, and neurite retraction. The biological actions of LPA are mediated by at least six G protein-coupled receptors known as LPAR1-6. Given that LPAR1-3 were among the first LPARs identified, the majority of research efforts have focused on understanding their biology. This review provides an in-depth discussion of LPAR5, which has recently emerged as a key player in regulating normal intestinal homeostasis and modulating pathological conditions such as pain, itch, inflammatory diseases, and cancer. We also present a chronological overview of the efforts made to develop compounds that target LPAR5 for use as tool compounds to probe or validate LPAR5 biology and therapeutic agents for the treatment of inflammatory diseases and cancer.
摘要
溶血磷脂酸（LPA）是一种生物活性脂质介质，可调节多种细胞功能，如细胞增殖、迁移、存活、钙动员、细胞骨架重排和轴突回缩。LPA 的生物学作用由至少六种 G 蛋白偶联受体（LPAR1-6）介导。鉴于 LPAR1-3 是最早鉴定的 LPAR 之一，因此大多数研究都集中在了解它们的生物学上。本综述深入讨论了 LPAR5，它最近成为调节正常肠道内稳态和调节疼痛、瘙痒、炎症性疾病和癌症等病理状况的关键因素。我们还按时间顺序介绍了为开发靶向 LPAR5 的化合物所做的努力，这些化合物可用作工具化合物来探测或验证 LPAR5 的生物学，以及用于治疗炎症性疾病和癌症的治疗剂。
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