A Gq Biased Small Molecule Active at the TSH Receptor - PMC
In summary, we identified and characterized a novel G αq/11 agonist molecule acting at the TSHR and which showed a marked anti-proliferative ability. Hence, Gq biased activation of the …
TSH Receptor Mutations and Diseases - Endotext - NCBI Bookshelf
2017年7月24日 · The TSHR activates different G-protein subtypes and signaling pathways, of which Gs and Gq induced signaling are of highest importance in the thyroid gland. A proper …
A Gq Biased Small Molecule Active at the TSH Receptor
2020年6月26日 · By virtue of its structural property, the TSH receptor (TSHR) has a unique ability to engage different G proteins making it highly amenable to selective signaling. In this study, …
在TSH受体上有活性的Gq偏小分子。,Frontiers in Endocrinology
凭借其结构特性，tsh受体（tshr）具有与不同g蛋白结合的独特能力，使其高度适应选择性信号转导。 在这项研究中，我们描述了TSHR的新型小分子激动剂的鉴定和表征，该激动剂可诱导 …
Novel Insights on Thyroid-Stimulating Hormone Receptor Signal ...
2022年4月13日 · Within the ICL2 of the TSHR, amino acids Met527, Arg528, and Asp530 appeared to be critical for both Gs and Gq activation, whereas alanine mutations of Ile523, …
Hormone- and antibody-mediated activation of the thyrotropin
2022年8月8日 · Comparisons of the active and inactivated structures of TSHR with those of the luteinizing hormone/choriogonadotropin receptor (LHCGR) reveal a universal activation …
Identification of compound heterozygous TSHR mutations (R109Q ... - PubMed
Genetic analysis showed that he was compound heterozygous for two known missense mutations (Arg109Gln and Arg450His) in the TSHR gene. Further, the signal transduction of Arg109Gln …
Principles and determinants of G-protein coupling by the ... - PubMed
2010年3月18日 · In this study we wanted to gain insights into selectivity mechanisms between G-protein-coupled receptors (GPCR) and different subtypes of G-proteins. The thyrotropin …
A Gq Biased Small Molecule Active at the TSH Receptor
2020年6月1日 · In summary, we identified and characterized a novel Gαq/11 agonist molecule acting at the TSHR and which showed a marked anti-proliferative ability. Hence, Gq biased …
Nature｜ “push and pull”激活模型——TSH和抗体介导的TSHR激活
2022年9月27日 · tsh-tshr结构与cg-lhcgr（绒毛膜促性腺激素受体）复合物的活性结构高度相似，表明tsh和cg都通过共同机制稳定受体活性构象。有趣的是，tshr ecd相对于lhcgr结构额外旋 …