2019年以bcl2蛋白家族为靶点的抗肿瘤药物设计.pptVIP

Obatoclax Phase II AT-101 Phase II/III 早期研发的抗凋亡蛋白小分子抑制剂基本上都是 pan-Bcl-2 antagonist 包括三联苯类， HA-14-1 及其类似物，棉酚及其衍生物， BH3I 及其衍生物等 BH3I-1 S1 DCBL55 Journal of Medicinal Chemistry,2010,53(9): 3465-3479 Nature Reviews Drug Discovery ,2008,7(12): 989-1000 31 以 BCL-2 蛋白家族为靶点的抗肿瘤药物设计 Bcl-2 Family Proteins as Therapeutic Targets for anticancer drug design Date: 2013-05-23 1 Outline ? Background ? Hallmarks of Cancer ? The Bcl-2 Protein Family ? Model of BH3 mimetic-induced apoptosis ? Structure basis for designing ligands ? Small molecule inhibitors ? Peptidomimetic appr