Adiponectin identified as an agonist for PAQR3/RKTG using a yeast-based assay system.

Adiponectin identified as an agonist for PAQR3/RKTG using a yeast-based assay system.
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DOI:
10.1080/10799890902729456
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发表时间:
2009
期刊:
Journal of receptor and signal transduction research
影响因子:
--
通讯作者:
Lyons TJ
Lyons TJ
中科院分区:
其他
文献类型:
--
作者:
Garitaonandia I;Smith JL;Kupchak BR;Lyons TJ

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PAQR 蛋白质家族包含一组有趣的新发现的受体。尽管 11 种人类 PAQR 中的 5 种已知激动剂,但大多数都被认为是“孤儿”受体。我们开发了一种基于酵母的 PAQR 受体活性检测系统,可用于识别未知功能的 PAQR 激动剂。使用该系统,我们发现蛋白质激素脂联素作为 PAQR3 的激动剂发挥作用,PAQR3 是该家族以前未被表征的成员。这并不奇怪,因为 PAQR3 与 PAQR1 (AdipoR1) 和 PAQR2 (AdipoR2) 关系最密切,后者也感知脂联素。脂联素作为 PAQR3 激动剂的鉴定具有相当大的临床意义,因为脂联素抑制肿瘤细胞的增殖,并且据报道 PAQR3 抑制肿瘤发生。因此,PAQR3 和脂联素之间的相互作用可能有助于解释脂联素的抗增殖特性。
The PAQR family of proteins comprises an intriguing group of newly discovered receptors. Although the agonist is known for 5 of the 11 human PAQRs, most are considered “orphan” receptors. We developed a yeast-based assay system for PAQR receptor activity that can be used to identify agonists for PAQRs of unknown function. Using this system, we found that the proteinaceous hormone adiponectin functions as an agonist of PAQR3, a previously uncharacterized member of this family. This is not surprising given that PAQR3 is most closely related to PAQR1 (AdipoR1) and PAQR2 (AdipoR2), which also sense adiponectin. The identification of adiponectin as an agonist for PAQR3 is of considerable clinical relevance because adiponectin suppresses the proliferation of tumor cells and it has been reported that PAQR3 suppresses tumorigenesis. Thus, the interaction between PAQR3 and adiponectin may help explain the antiproliferative properties of adiponectin.
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