Kumar Amit, Jaggi Amteshwar S, Singh Nirmal
CNS and CVS Research Laboratory, Pharmacology Division, Department of Pharmaceutical Sciences and Drug Research, Faculty of Medicine, Punjabi University, Patiala, 147002, Punjab, India.
Fundam Clin Pharmacol. 2015 Apr;29(2):115-30. doi: 10.1111/fcp.12097. Epub 2015 Feb 15.
Src family kinases (SFKs), the largest family of nonreceptor tyrosine kinases, include 10 members. Src was the first gene product discovered to have intrinsic protein tyrosine kinase activity. Src is widely expressed in many cell types and can have different locations within a cell; the subcellular location of Src can affect its function. Src can associate with cellular membranes, such as the plasma membrane, the perinuclear membrane, and the endosomal membrane. SFKs actions on mammalian cells are pleiotropic and include effect on cell morphology, adhesion, migration, invasion, proliferation, differentiation, and survival. SFKs at one end have been documented to play some important physiological functions; on the other end, they have been described in the pathophysiology of some disorders. In this review article, an exhaustive attempt has been made to unearth pharmacology of SFKs and therapeutic implications of SFKs modulators.
Src家族激酶(SFKs)是最大的非受体酪氨酸激酶家族,包含10个成员。Src是首个被发现具有内在蛋白酪氨酸激酶活性的基因产物。Src在多种细胞类型中广泛表达,且在细胞内可有不同定位;Src的亚细胞定位会影响其功能。Src可与细胞膜结合,如质膜、核周膜和内体膜。SFKs对哺乳动物细胞的作用具有多效性,包括对细胞形态、黏附、迁移、侵袭、增殖、分化和存活的影响。一方面,已有文献证明SFKs发挥着一些重要的生理功能;另一方面,它们也与某些疾病的病理生理学有关。在这篇综述文章中,我们进行了详尽的尝试,以探究SFKs的药理学及其调节剂的治疗意义。