期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 12, 页码 2617-2620出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.04.077
关键词
Carbonic anhydrase; Enzyme inhibitor; Bisphosphonate; Bone resorption inhibitor; Matrix metalloproteinase inhibitor
资金
- EU FP7 projects
A set of bisphosphonate matrix metalloproteinase (MMP) inhibitors was investigated for inhibitory activity against several carbonic anhydrase (CA, EC 4.2.1.1) isozymes, some of which are overexpressed in hypoxic tumors. Some of the bisphosphonate revealed to be very potent inhibitors (in the low nanomolar range) of the cytosolic isoform CA II and the membrane-bound CA IX, XII and XIV isozymes, a feature useful for considering them as interesting compounds for bone resorption inhibition applications. We suggest here that it is possible to develop dual enzyme inhibitors bearing bisphosphonate moieties that may target both MMPs and CAs, two families of enzymes involved in tumor formation, growth, and metastasis. (C) 2014 Elsevier Ltd. All rights reserved.
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