However, Bax membrane translocation was independent of caspase activity as determined using the broad-range caspase inhibitor z-VAD-fmk. High level overexpression of the anti-apoptotic protein Bcl-2 prevented Bax redistribution to the mitochondria, caspase activation and apoptosis following exposure to ...
1.包含Bcl‑2抑制剂和抗CD20单抗的组合产品在制备药物中的用途,所述Bcl‑2抑制剂 是具有下式的化合物或其药学上可接受的盐: 所述抗CD20单抗是利妥昔单抗,且 所述药物用于治疗弥漫性大B细胞淋巴瘤。 2.根据权利要求1所述的用途,所述药物还包含药学上可接受的载体、稀释剂或赋形 ...
Navitoclax, a dual antagonist of BCL-2 and BCL-XL, was the first BCL-2 inhibitor to show efficacy in cancer; however, the use of this drug was limited by the occurrence of neutropenia. The highly selective and potent BCL-2 inhibitor venetoclax was subsequently developed and is now approved...
个化合物具有较好的抗肿瘤活性,有望成为新的Bcl.2蛋白 小分子抑制剂。 目的:设计、合成活性较好的Bcl.2蛋白抑制剂。 方法:军事医学科学院毒物药物所自1998年开始研发 的Bcl.2蛋白抑制剂类抗肿瘤药物,目前已合成该系列化合 物200多个,经药理评价,得到了多个活性较好的化合物如 ...
These ‘BH3 mimetic’ drugs seem destined to become powerful new weapons in the arsenal against cancer. Successful clinical trials of venetoclax/ABT-199, a specific inhibitor of BCL-2, have led to its approval for a refractory form of chronic lymphocytic leukaemia and to scores of on-going ...
SMAC/Diablo and HtrA2/Omi antagonize inhibitor of apoptosis proteins (IAPs), relieving inhibition of caspase activity, thereby reinforcing cell death signals. Sign in to download hi-res image Figure 2. Viral modulation of the intrinsic apoptotic pathway. Viruses can inhibit cell apoptosis by ...
方法Flourescence Activated Cell Sorting (FACS) for death assays and cell cycle analysis Cells were plated in triplicate in 6-well plates or 6-cm dishes to reach ~30-40% confluency the next day. On the next day, cells were treated with the indicated drugs or no drug control.Apoptosis ...
In this work, Jac-A was identified as a new inhibitor of Bcl-2 proteins. We found that Jac-A can compete for binding to BH3 domain of Bcl-2 proteins with proapoptosis proteins in the FP-based binding experiments. This result was confirmed by the co-immunoprecipitation experiment whose ...
The current clinical availability of these drugs points to the possibility of rapid clinical translation. Dasatinib, an FDA-approved inhibitor of SRC/ABL for the treatment of chronic myelogenous leukemia, demonstrated limited activity in a Phase II trial as a single agent in the treatment of ...
antiapoptotic mechanism of BCL-2,the relationships between BCL-2 protein structure and its function and the results of antisense therapy based bcl-2 gene.The feasibility of developing small molecule inhibitor of BCL-2 protein was also studied.%BCL-2蛋白抑制细胞凋亡是肿瘤发生和产生耐药...