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.
PhiKan 083 is a p53 stabilizing agent。
MoreNSC 146109 hydrochloride是细胞膜通透性的基因型选择性抗肿瘤试剂, 激活p53依赖型转录。
MoreMIRA-1是Restores mutant p53 activity, proapoptotic。
MoreNutlin-3是一种有效的,选择性Mdm2(p53的环指依赖性泛素蛋白连接酶)拮抗剂,无细胞试验中IC50为90 nM;可稳定p53缺陷细胞中的p73。
MoreRITA (NSC 652287)诱导DNA-蛋白质和DNA-DNA交联,检测不到DNA单链断裂,通过靶向作用于p53,也抑制MDM2-p53相互作用。
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