Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 12, Pages 3279-3282Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.04.080
Keywords
A431 cells; Autophosphorylation; Dimerization-arm-mimetic peptide; Dimerization inhibitor; EGF receptor
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Funding
- Ministry of Education, Culture, Sports, Science and Technology (MEXT) of Japan
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A cyclic decapeptide was chemically synthesized that mimics the loop structure of a beta-hairpin arm of the EGF receptor, which is highly involved in receptor dimerization upon activation by ligand binding. This peptide was revealed to reduce dimer formation of the receptor in a detergent-solubilized extract of epidermoid carcinoma A431 cells and to inhibit receptor autophosphorylation at less than 10 mu M in the intact cells. (C) 2009 Elsevier Ltd. All rights reserved.
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