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溶血磷脂酸(LPA)可以与多种亚型受体结合,参与诸多信号调节,产生多种病理生理反应,它与心肌肥厚、肿瘤细胞的侵袭、转移和血管生成、器官纤维化、骨关节炎、神经性疼痛、精神分裂症多种疾病相关。靶向LPA受体的激动剂和拮抗剂是目前药物化学的研究热点。本文主要介绍小分子LPA受体激动剂和拮抗剂的结构及构效关系等方面的研究进展。
Lysophosphatidic acid (LPA) binds to a variety of subtype receptors and participates in a variety of signal pathways that produce a variety of pathophysiological responses that are associated with cardiac hypertrophy, tumor cell invasion, metastasis and angiogenesis, organ fibrosis, osteoarthritis , Neuropathic pain, a variety of schizophrenia-related diseases. Targeting LPA receptor agonists and antagonists is the current research focus of medicinal chemistry. This article mainly introduces the research progress on the structure and structure-activity relationship of small molecule LPA receptor agonists and antagonists.