Pyridinylpyrimidines selectively inhibit human methionine aminopeptidase-1
نویسندگان
چکیده
منابع مشابه
High expression of methionine aminopeptidase 2 in human colorectal adenocarcinomas.
PURPOSE Several viral and eukaryotic proteins required for signal transduction and regulatory functions undergo lipophilic modification by the enzyme N-myristoyltransferase. Previously we reported that N-myristoyltransferase activity is higher in colon and gallbladder carcinoma than in the corresponding normal tissues. Methionine aminopeptidase 2 (MetAP2) is a bifunctional protein that plays a ...
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Processing of the N-terminal initiator methionine is an essential cellular process conserved from prokaryotes to eukaryotes. The enzymes that remove N-terminal methionine are known as methionine aminopeptidases (MetAPs). Human MetAP2 has been shown to be required for the proliferation of endothelial cells and angiogenesis. The physiological function of MetAP1, however, has remained elusive. In ...
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In this article we describe the application of structural biology methods to the discovery of novel potent inhibitors of methionine aminopeptidases. These enzymes are employed by the cells to cleave the N-terminal methionine from nascent peptides and proteins. As this is one of the critical steps in protein maturation, it is very likely that inhibitors of these enzymes may prove useful as novel...
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ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry
سال: 2013
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2013.02.023