Small Molecule Inhibitors of Bcl-2 Family Proteins for Pancreatic Cancer Therapy

Cancers

Ashiq Masood¹  Asfar S. Azmi² 

[1] Department of Internal Medicine/Pathology, Karmanos Cancer Institute, Wayne State University, 4100 John R, HWCRC 732, Detroit, MI 48201, USA; E-Mail:;Department of Pathology, Karmanos Cancer Institute, Wayne State University, 4100 John R, HWCRC 732, Detroit MI 48201, USA; E-Mail:

关键词: PC;    Bcl-2 family proteins;    small molecule inhibitors;    apoptosis;    cancer therapy;   

DOI  :  10.3390/cancers3021527

来源: mdpi

【 摘 要 】

Pancreatic cancer (PC) has a complex etiology and displays a wide range of cellular escape pathways that allow it to resist different treatment modalities. Crucial signaling molecules that function downstream of the survival pathways, particularly at points where several of these pathways crosstalk, provide valuable targets for the development of novel anti-cancer drugs. Bcl-2 family member proteins are anti-apoptotic molecules that are known to be overexpressed in most cancers including PC. The anti-apoptotic machinery has been linked to the observed resistance developed to chemotherapy and radiation and therefore is important from the targeted drug development point of view. Over the past ten years, our group has extensively studied a series of small molecule inhibitors of Bcl-2 against PC and provide solid preclinical platform for testing such novel drugs in the clinic. This review examines the efficacy, potency, and function of several small molecule inhibitor drugs targeted to the Bcl-2 family of proteins and their preclinical progress against PC. This article further focuses on compounds that have been studied the most and also discusses the anti-cancer potential of newer class of Bcl-2 drugs.

【 授权许可】

CC BY   
© 2011 by the authors; licensee MDPI, Basel, Switzerland.