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首页> 外文期刊>Biochemistry >Structural and functional study of the apelin-13 peptide, an endogenous ligand of the HIV-1 coreceptor, APJ.
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Structural and functional study of the apelin-13 peptide, an endogenous ligand of the HIV-1 coreceptor, APJ.

机译：apelin-13肽的结构和功能研究，该蛋白是HIV-1共同受体APJ的内源性配体。

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摘要

The APJ receptor is widely expressed in the human central nervous system (CNS). Apelin was recently identified as the endogenous peptidic ligand for human APJ. Studies with animal models suggested that APJ and apelin play an important role in the hypothalamic regulation of water intake and the endocrine axis, in the regulation of blood pressure, and in cardiac contractility. Apelin has been found to block the activity of APJ as a human immunodeficiency virus type I (HIV-1) coreceptor. In this study, we combined chemical synthetic approaches with alanine substitution to evaluate the structural requirements for interactions with the APJ receptor. We demonstrated that apelin peptides in aqueous solution adopt a random conformation, and the positive charge and hydrophobic residues of apelin-13 play important roles in interactions with the APJ receptor. We have observed an important correlation between receptor binding affinity and cell-cell fusion inhibitory activity. The elucidation of structural requirements of apelin-13 in its interaction with the APJ receptor is critical for further investigation of apelin-APJ functions in vivo and in the design of small molecular inhibitors for potential treatment of HIV-1 infection in the CNS.
机译：APJ受体在人类中枢神经系统（CNS）中广泛表达。最近鉴定出Apelin是人APJ的内源肽配体。动物模型研究表明，APJ和apelin在下丘脑调节水和内分泌轴，调节血压以及心脏收缩中起重要作用。已经发现Apelin可以阻断APJ作为人类I型免疫缺陷病毒（HIV-1）核心受体的活性。在这项研究中，我们将化学合成方法与丙氨酸取代相结合，以评估与APJ受体相互作用的结构要求。我们证明了水溶液中的apelin肽采用随机构象，并且apelin-13的正电荷和疏水残基在与APJ受体的相互作用中起重要作用。我们已经观察到受体结合亲和力与细胞间融合抑制活性之间的重要关联。阐明apelin-13与APJ受体相互作用的结构要求对于进一步研究apelin-APJ在体内的功能以及设计小分子抑制剂以潜在治疗中枢神经系统HIV-1感染至关重要。

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