G protein–coupled receptors (GPCRs) which are also known as seven-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein–linked receptors (GPLR), constitute a large protein family of receptors, that sense molecules outside the cell and activate inside signal transduction pathways and, ultimately, cellular responses. Coupling with G proteins, they are called seven-transmembrane receptors because they pass through the cell membrane seven times.
G protein–coupled receptors are found only in eukaryotes, including yeast, choanoflagellates, and animals. The ligands that bind and activate these receptors include light-sensitive compounds, odors, pheromones, hormones, and neurotransmitters, and vary in size from small molecules to peptides to large proteins. G protein–coupled receptors are involved in many diseases, and are also the target of approximately 40% of all modern medicinal drugs.
RKI-1447是ROCK1和ROCK2的抑制剂,IC50分别为15.4 nM和6.2 nM。
MoreThiazovivin是一种新型ROCK抑制剂,IC50为0.5 μM,在单细胞分离后,促进人胚胎干细胞(hESC)的存活。
MorePifithrin-α (PFTα)是一种p53抑制剂,抑制p53依赖性的p53应答基因转录。
MoreNutlin-3a是Nutlin-3的活性对映体,抑制p53/MDM2相互作用,IC50为90 nM。
MoreFasudil (HA-1077) HCl是一种有效的ROCK-II, PKA, PKG, PKC,和MLCK抑制剂, Ki分别为0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM,和36 μM。
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