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首页> 美国卫生研究院文献>Pharmacological Reviews >International Union of Basic and Clinical Pharmacology. CVII. Structure and Pharmacology of the Apelin Receptor with a Recommendation that Elabela/Toddler Is a Second Endogenous Peptide Ligand
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International Union of Basic and Clinical Pharmacology. CVII. Structure and Pharmacology of the Apelin Receptor with a Recommendation that Elabela/Toddler Is a Second Endogenous Peptide Ligand

机译：国际基础和临床药理学联盟。 CVII。 Apelin受体的结构和药理学建议Elabela /蹒跚学步是第二种内源肽配体

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摘要

The predicted protein encoded by the APJ gene discovered in 1993 was originally classified as a class A G protein-coupled orphan receptor but was subsequently paired with a novel peptide ligand, apelin-36 in 1998. Substantial research identified a family of shorter peptides activating the apelin receptor, including apelin-17, apelin-13, and [Pyr1]apelin-13, with the latter peptide predominating in human plasma and cardiovascular system. A range of pharmacological tools have been developed, including radiolabeled ligands, analogs with improved plasma stability, peptides, and small molecules including biased agonists and antagonists, leading to the recommendation that the APJ gene be renamed APLNR and encode the apelin receptor protein. Recently, a second endogenous ligand has been identified and called Elabela/Toddler, a 54-amino acid peptide originally identified in the genomes of fish and humans but misclassified as noncoding. This precursor is also able to be cleaved to shorter sequences (32, 21, and 11 amino acids), and all are able to activate the apelin receptor and are blocked by apelin receptor antagonists. This review summarizes the pharmacology of these ligands and the apelin receptor, highlights the emerging physiologic and pathophysiological roles in a number of diseases, and recommends that Elabela/Toddler is a second endogenous peptide ligand of the apelin receptor protein.
机译：由1993年发现的APJ基因编码的预测蛋白最初被分类为AG类蛋白偶联的孤儿受体，但随后在1998年与新型肽配体apelin-36配对。大量研究确定了激活apelin的较短肽家族受体，包括apelin-17，apelin-13和[Pyr 1 ] apelin-13，后者在人体血浆和心血管系统中占主导地位。已经开发了一系列药理学工具，包括放射性标记的配体，具有改善的血浆稳定性的类似物，肽以及包括偏向激动剂和拮抗剂的小分子，因此建议将APJ基因重命名为APLNR并编码apelin受体蛋白。最近，已经鉴定出第二种内源性配体，称为Elabela / Toddler，它是最初在鱼类和人类基因组中鉴定的54个氨基酸的肽，但被误分类为非编码。该前体还能够被切割成较短的序列（32、21和11个氨基酸），并且都能够激活apelin受体并被apelin受体拮抗剂阻断。这篇综述总结了这些配体和apelin受体的药理作用，强调了在许多疾病中新兴的生理和病理生理作用，并建议Elabela / Toddler是apelin受体蛋白的第二种内源肽配体。

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