Journal
CANCER INVESTIGATION
Volume 22, Issue 2, Pages 304-311Publisher
TAYLOR & FRANCIS INC
DOI: 10.1081/CNV-120030218
Keywords
antineoplastic agents; boronic acids; enzyme inhibitors (administration and dose); NF-KB (antagonists and inhibitors); hematologic neoplasms (drug therapy); multienzyme complexes (antagonists and inhibitors)
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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.
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