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Without affecting the overall 3D structure, amide-to-ester backbone substitution (or ester scan) exerts a pronounced influence on the conformational equilibrium of the RGD cyclopeptide cilengitide and its derivatives (see figure; RGD=Arg-Gly-Asp). The appropriate substitution, which stabilized the receptor-complementary conformations, improved the biological activity of this integrin antagonist.
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Cupido et al. (2010) studied this question.
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