Inhibitory effect of a dimerization-arm-mimetic peptide on EGF receptor activation

A cyclic decapeptide was chemically synthesized that mimics the loop structure of a β-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 μM in the intact cells.

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