期刊
CANCER INVESTIGATION
卷 22, 期 2, 页码 304-311出版社
TAYLOR & FRANCIS INC
DOI: 10.1081/CNV-120030218
关键词
antineoplastic agents; boronic acids; enzyme inhibitors (administration and dose); NF-KB (antagonists and inhibitors); hematologic neoplasms (drug therapy); multienzyme complexes (antagonists and inhibitors)
类别
The dipeptide boronic acid analogue VELCADE(TM) (Bortezomib; formerly known as PS-341, LDP-341 and MLM341) is a potent and selective inhibitor of the proteasome, a multicatalytic enzyme that mediates many cellular regulatory signals by degrading regulatory proteins or their inhibitors. The proteasome, is, thus, a potential target for pharmacological agents. Bortezomib, the first proteasome inhibitor to reach clinical trials, has shown in vitro and in vivo activity against a variety of malignancies, including myeloma, chronic lymphocytic leukemia, prostate cancer, pancreatic cancer, and colon cancer. The drug is rapidly cleared from the vascular compartment, but a novel pharmacodynamic assay has shown that bortezomib-mediated proteasome blockade is dose-dependent and reversible. Based on phase I studies demonstrating that bortezomib has manageable toxicities in patients with advanced cancers, phase II trials have been initiated for both solid and hematological malignancies.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据