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Frontispiece: Multivalency Increases the Binding Strength of RGD Peptidomimetic‐Paclitaxel Conjugates to Integrin α V β 3
Author(s) -
Raposo Moreira Dias André,
Pina Arianna,
Dal Corso Alberto,
Arosio Daniela,
Belvisi Laura,
Pignataro Luca,
Caruso Michele,
Gennari Cesare
Publication year - 2017
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.201785863
Subject(s) - peptidomimetic , conjugate , integrin , paclitaxel , chemistry , ligand (biochemistry) , biophysics , stereochemistry , receptor , biochemistry , biology , genetics , mathematics , peptide , cancer , mathematical analysis
Multivalent binding is often used to increase the strength of ligand–receptor interactions. In oncology, the development of multimeric conjugates aims at promoting a more efficient recognition of target antigens, possibly leading to better therapeutic performance. The affinity for integrin α V β 3 of multimeric conjugates ( cyclo [DKP‐RGD]) n ‐Val‐Ala‐PTX ( n =1–4) increases with the number of cyclo [DKP‐RGD] ligands up to n =3. For more information, see the Communication by L. Pignataro, C. Gennari et al. on page 14410 ff.