Serine/threonine protein kinase Akt and Akt targeting anticancer drug development / 中国药理学通报

ABSTRACT

Dyregulation of serine/threonine protein kinase Akt/PKB activity is a prominent feature of many human cancers.A large number of studies have demonstrated that Akt plays a key role in mediating cell growth and proliferation,promoting cell migration and invasion,stimulating neoangiogenesis,and protecting from pro-apoptotic stimuli.In view of the highly pleiotropic biologic effects of Akt signaling in multiple aspects of tumor pathophysiology,development of clinically applicable drugs specifically targeting Akt has been the subject of intense research.Up to now,a number of Akt specific inhibitors such as API2,Akt-I-1,Akt-I-2 and DCIEL have been developed and investigated in pre-clinical studies.These compounds have been shown to potently inhibit growth of tumors with aberrantly expressed or activated Akt,therefore,are likely to be developed as promising targeted anticancer drugs.