title: Non-peptidic small molecule inhibitors against Bcl-2 for cancer therapy.
abstract: A critical regulator of the apoptotic machinery is the Bcl-2 family proteins whose over expression confers a protective effect on malignant cells against death signals of apoptosis. Cancer cells that are resistant to various anti-cancer drugs and treatment regimen are found to over express these Bcl-2 proteins such as Bcl-2, Bcl-X(L), Mcl-1, Bcl-w, and A1/Bfl1. In recent years there has been an exponential growth in the identification as well as synthesis of non-peptidic cell permeable small-molecule inhibitors (SMIs) of protein-protein interaction. The focus of this article is on inhibitors of anti-apoptotic protein Bcl-2. This review summarizes an up to date knowledge of the available SMIs, their mode of action as well as their current status in preclinical as well as clinical development.
authors.affiliation: Department of Pathology, Wayne State University School of Medicine, Detroit Michigan, USA.
authors.forename: Asfar S
authors.initials: AS
authors.lastname: Azmi
authors.forename: Ramzi M
authors.initials: RM
authors.lastname: Mohammad