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Org Biomol Chem. 2016 Mar 28;14(12):3221-33. doi: 10.1039/c6ob00287k.

New potent αvβ3 integrin ligands based on azabicycloalkane (γ,α)-dipeptide mimics.

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Centro Interdisciplinare Studi Biomolecolari e Applicazioni Industriali, Università degli Studi di Milano, Via Fantoli 16/15, I-20138, Milano.
Istituto di Scienze e Tecnologie Molecolari, Consiglio Nazionale delle Ricerche, Via C. Golgi 19, I-20133, Milano.
Dipartimento di Chimica, Università degli Studi di Milano, Via C. Golgi 19, I-20133, Milano.


We have designed a new synthetic strategy for the preparation of a new class of cyclic RGD integrin ligands in which the azabicycloalkane scaffold can be envisaged as a (γ,α) dipeptide mimic. The synthesis and in vitro biological evaluation of these RGD derivatives, as well as the computational study of their conformational properties and binding modes to αVβ3 integrin are described. Compound has shown to be a promising candidate as αVβ3 integrin antagonist able to interfere with both cell adhesion and movement on vitronectin with no evidence of cytotoxic effects.

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