G protein-coupled receptors as potential drug targets for lymphangiogenesis and lymphatic vascular diseases.
G protein-coupled receptors as potential drug targets for lymphangiogenesis and lymphatic vascular diseases.
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DOI：
10.1161/atvbaha.109.185066
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发表时间：
2009-05
期刊：
影响因子：
--
通讯作者：
Caron KM
中科院分区：
文献类型：
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作者：
Dunworth WP;Caron KM
g蛋白偶联受体（gpcr）是广泛表达的细胞表面受体，已被成功地用于治疗多种人类疾病。最近对基因工程小鼠模型的研究已经鉴定出几种对淋巴血管发育和功能重要的gpcr。肾上腺髓质素受体是一种介于降钙素受体样受体和受体活性修饰蛋白2之间的低聚物，是正常淋巴血管发育所必需的，并调节小鼠淋巴毛细血管通透性。大量研究也表明溶血磷脂受体参与淋巴管和淋巴内皮细胞通透性的发育。鉴于目前淋巴血管疾病（如淋巴水肿）治疗的药理靶点缺乏，对淋巴内皮细胞中gpcr的持续识别和研究可能最终导致淋巴水肿治疗的重大突破和新的药理策略。
G-protein coupled receptors (GPCRs) are widely expressed cell surface receptors that have been successfully exploited for the treatment of a variety of human diseases. Recent studies in genetically engineered mouse models have led to the identification of several GPCRs important for lymphatic vascular development and function. The adrenomedullin receptor, which consists of an oligomer between calcitonin receptor-like receptor and receptor activity modifying protein 2, is required for normal lymphatic vascular development and regulates lymphatic capillary permeability in mice. Numerous studies also suggest that lysophospholipid receptors are involved in the development of lymphatic vessels and lymphatic endothelial cell permeability. Given our current lack of pharmacological targets for the treatment of lymphatic vascular diseases like lymphedema, the continued identification and study of GPCRs in lymphatic endothelial cells may eventually lead to major breakthroughs and new pharmacological strategies for the treatment of lymphedema.