Direct Activation of Bax Protein for Cancer Therapy.

摘要: Bax, a central cell death regulator, is an indispensable gateway to mitochondrial dysfunction and major proapoptotic member of the B-cell lymphoma 2 (Bcl-2) family proteins that control apoptosis in normal cancer cells. Dysfunction renders resistant treatment as well promotes tumorigenesis. Bax activation induces membrane permeabilization, thereby leading release apoptotic factor cytochrome c consequently death. A number drugs clinical use are known indirectly activate Bax. Intriguingly, recent efforts demonstrate can serve promising direct target for small-molecule drug discovery. Several activators have been identified hold promise therapy with advantages specificity potential overcoming chemo- radioresistance. Further investigation this new class candidates will be needed advance them into clinic novel means treat cancer.