以BCL2蛋白家族为靶点的抗肿瘤药物设计课件.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 * ABT-199 Selectively Kills BCL-2-Dependent Tumor Cells While Sparing Platelets (A) Navitoclax (ABT-263) binds with high affinity to both BCL-2 and BCL-XL. Because many tumors, particularly lymphoid malignancies, are addicted to BCL-2 for survival,... Cancer Cell , 2013,23(2),139 - 141 ABT-199：Selective Bcl-2 inhibitor * Nature medicine,2013,19(2)