01727nas a2200301   4500008004100000022001400041245012600055210006900181260000800250300001400258490000700272520069800279100002100977700003200998700002001030700002701050700002401077700002201101700001901123700002201142700001901164700002201183700002601205700002501231700002301256700001901279856012701298       2018                        eng d  a0022-262300aN-Methylation of isoDGR peptides: discovery of a selective alpha 5 beta 1-integrin ligand as a potent tumor imaging agent0 aNMethylation of isoDGR peptides discovery of a selective alpha 5  cMAR  a2490-24990 v613 a<p>Specific targeting of the integrin subtype alpha 5 beta 1 possesses high potential in cancer diagnosis and therapy. Through sequential N-methylation, we successfully converted the biselective alpha 5 beta 1/alpha v beta 6 peptide c(phg-isoDGR-k) into a potent peptidic RGD binding aSfil subtype selective ligand c(phg-isoDGR-(NMe)k). Nuclear magnetic resonance spectroscopy and molecular modeling clarified the molecular basis of its improved selectivity profile. To demonstrate its potential in vivo, c(phg-isoDGR-(NMe)k) was trimerized with the chelator TRAP and used as a positron-emission tomography tracer for monitoring alpha 5 beta 1 integrin expression in a M21 mouse xenograft.</p>1 aKapp, Tobias, G.1 aDi Leva, Francesco, Saverio1 aNotni, Johannes1 aRaeder, Andreas, F. B.1 aFottner, Maximilian1 aReichart, Florian1 aReich, Dominik1 aWurzer, Alexander1 aSteiger, Katja1 aNovellino, Ettore1 aMarelli, Udaya, Kiran1 aWester, Hans-Juergen1 aMarinelli, Luciana1 aKessler, Horst  uhttps://library.ncl.res.in/content/n-methylation-isodgr-peptides-discovery-selective-alpha-5-beta-1-integrin-ligand-potent