GPR133 is an adhesion G protein-coupled receptor that functions as a membrane receptor for androgens. When activated by 5α-DHT, GPR133 increases intracellular cyclic AMP (cAMP) levels in muscle cells, leading to enhanced muscle strength.

2016年10月24日 · Here, we use primary human tumor biospecimens and cultures to identify GPR133 (ADGRD1), an orphan member of the adhesion family of G-protein-coupled receptors, as a critical regulator of the...

2025年1月29日 · GPR133 is identified as a membrane receptor for the androgen subtype 5α-DHT, and the cryo-EM structures define the determinants for androgen recognition, enabling the generation of a GPR133 agonist that allows for selective modulation of muscle strength in mice.

2025年1月30日 · 研究团队筛选鉴定了雄激素5α-DHT的膜受体GPR133/ADGRD1，阐明了其在骨骼肌中的调控作用及分子机制，并发展了特异性GPR133的小分子配体，为高效安全的雄激素替代药物开发提供了全新思路。 研究团队首先通过高分辨率液相色谱串联质谱分析，测定了小鼠骨骼肌 （趾长伸肌，EDL） 中的5α-DHT水平，发现5α-DHT呈现性别、年龄和组织特异性差异，骨骼肌中5α-DHT水平显著高于血液水平。 进一步研究发现，在阻断雄激素核受体 （AR） 后，5α-DHT …

2024年12月24日 · The adhesion G-protein-coupled receptors (GPCRs), including GPR133, are membrane-bound proteins with long N termini containing multiple domains. GPCRs, or GPRs, contain 7 transmembrane domains and transduce extracellular signals through heterotrimeric G proteins (summary by Bjarnadottir et al., 2004 [PubMed 15203201]).[supplied by OMIM, Nov ...

2022年4月13日 · 在“Structural basis for the tethered peptide activation of adhesion GPCRs”研究工作中，孙金鹏教授团队以粘附类受体GPR133和GPR114作为模型进行结构分析，探究 Stachel序列介导的aGPCR激活机制（图1）。

2025年1月23日 · Androgens, such as 5α-dihydrotestosterone (5α-DHT), regulate numerous functions by binding to nuclear androgen receptors (ARs) and potential unknown membrane receptors. Here, we report that the androgen 5α-DHT activates membrane receptor GPR133 in muscle cells, thereby increasing intracellular cycli …

2016年10月24日 · Here, we use primary human tumor biospecimens and cultures to identify GPR133 (ADGRD1), an orphan member of the adhesion family of G-protein-coupled receptors, as a critical regulator of the response to hypoxia and tumor growth in GBM.

2024年5月28日 · GPR133 (ADGRD1) is an adhesion G-protein-coupled receptor that signals through Gαs/cyclic AMP (cAMP) and is required for the growth of glioblastoma (GBM), an aggressive brain malignancy. The regulation of GPR133 signaling is incompletely understood.

2011年12月9日 · Here we demonstrate that GPR133, a member of the adhesion GPCR subfamily, activates the G s protein/adenylyl cyclase pathway. The presence of the N terminus and the cleavage at the GPCR proteolysis site are not required for G protein signaling.