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一种偏向 Gq 的激动剂,在 AT1R-Gq 融合蛋白上的分子效率是 AT1R-βarr2 融合蛋白的 10 倍。
编号:200784
CAS号:40678-47-5
单字母:H2N-DRVYIHPG-OH
TRV120056 是一种偏向 Gq 的激动剂,在 AT1R-Gq 融合蛋白上的分子效率是 AT1R-βarr2 融合蛋白的 10 倍。
TRV120056 is a Gq-biased agonists, exhibits 10-fold larger molecular efficacies at the AT1R-Gq fusion protein compared with the AT1R-βarr2 fusion protein[1].
Rajagopal S, et, al. Quantifying ligand bias at seven-transmembrane receptors. Mol Pharmacol. 2011 Sep;80(3):367-77. : https://pubmed.ncbi.nlm.nih.gov/21610196/
Strachan RT, et, al. Divergent transducer-specific molecular efficacies generate biased agonism at a G protein-coupled receptor (GPCR). J Biol Chem. 2014 May 16; 289(20): 14211-24. : https://pubmed.ncbi.nlm.nih.gov/24668815/