Structure-Based Design of Covalent Siah Inhibitors
نویسندگان
چکیده
منابع مشابه
Bioengineered Peptides Based on α1-PDX Structure as Inhibitors of Furin: Design, Synthesis and Comparative Efficacy
Furin is a Ca 2+ <span style="color: #231f20; font-family: Times New...
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In contrast to the traditional mechanism of drug action that relies on the reversible, noncovalent interaction of a ligand with its biological target, a targeted covalent inhibitor (TCI) is designed such that the initial, reversible association is followed by the formation of a covalent bond between an electrophile on the ligand and a nucleophilic center in the protein. Although this approach o...
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furin is a ca 2+ -dependent serine protease which cleaves proprotein substrates at the arg-xaa-(lys/arg)-arg site to generate biologically active proteins. furin’s critical role in many cellular events associated with health disorders such as hiv, sars, anthrax, and influenza as well as cancer has made inhibitors of this enzyme as therapeutic targets. to this date, the most potent inhibitor ...
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ژورنال
عنوان ژورنال: Chemistry & Biology
سال: 2013
ISSN: 1074-5521
DOI: 10.1016/j.chembiol.2013.06.008