Inhibition of Akt with small molecules and biologics: historical perspective and current status of the patent landscape.

摘要: Introduction: Akt plays a pivotal role in cell survival and proliferation through number of downstream effectors; unregulated activation the PI3K/PTEN/Akt pathway is prominent feature many human cancers. considered an attractive target for cancer therapy by inhibition alone or combination with standard chemotherapeutics. Both preclinical animal studies clinical trials humans have validated as important drug discovery. Area covered: A historical perspective inhibitors, including PI analogs, ATP-competitive allosteric along other inhibitory mechanisms are reviewed this paper focus on issued patents, patent applications summary trial updates since last review 2007. Expert opinion: vast diversity inhibitors Akt, both small molecule biologic, been developed past 5 years, over dozen various phases development, several displaying...