<?xml version="1.0" encoding="UTF-8"?><xml><records><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Weinmueller, Michael</style></author><author><style face="normal" font="default" size="100%">Rechenmacher, Florian</style></author><author><style face="normal" font="default" size="100%">Marelli, Udaya Kiran</style></author><author><style face="normal" font="default" size="100%">Reichart, Florian</style></author><author><style face="normal" font="default" size="100%">Kapp, Tobias G.</style></author><author><style face="normal" font="default" size="100%">Raeder, Andreas F. B.</style></author><author><style face="normal" font="default" size="100%">Di Leva, Francesco Saverio</style></author><author><style face="normal" font="default" size="100%">Marinelli, Luciana</style></author><author><style face="normal" font="default" size="100%">Novellino, Ettore</style></author><author><style face="normal" font="default" size="100%">Munoz-Felix, Jose M.</style></author><author><style face="normal" font="default" size="100%">Hodivala-Dilke, Kairbaan</style></author><author><style face="normal" font="default" size="100%">Schumacher, Adi</style></author><author><style face="normal" font="default" size="100%">Fanous, Joseph</style></author><author><style face="normal" font="default" size="100%">Gilon, Chaim</style></author><author><style face="normal" font="default" size="100%">Hoffman, Amnon</style></author><author><style face="normal" font="default" size="100%">Kessler, Horst</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Overcoming the lack of oral availability of cyclic hexapeptides: design of a selective and orally available ligand for the integrin alpha v beta 3</style></title><secondary-title><style face="normal" font="default" size="100%">Angewandte Chemie-International Edition</style></secondary-title></titles><dates><year><style  face="normal" font="default" size="100%">2017</style></year><pub-dates><date><style  face="normal" font="default" size="100%">DEC</style></date></pub-dates></dates><volume><style face="normal" font="default" size="100%">56</style></volume><pages><style face="normal" font="default" size="100%">16405-16409</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">Ahighly systematic approach for the development of both orally bioavailable and bioactive cyclic N-methylated hexapeptides as high affinity ligands for the integrin alpha v beta 3 is based on two concepts: a) screening of systematically designed libraries with spatial diversity and b) masking of the peptide charge with a lipophilic protecting group. The key steps of the method are 1) initial design of a combinatorial library of Nmethylated analogues of the stem peptide cyclo(d-Ala-Ala(5)); 2) selection of cyclic peptides with the highest intestinal permeability; 3) design of sublibraries with the bioactive RGD sequence in all possible positions; 4) selection of the best ligands for RGD-recognizing integrin subtypes; 5) finetuning of the affinity and selectivity by additional Ala to Xaa substitutions; 6) protection of the charged functional groups according to the prodrug concept to regain intestinal and oral permeability; 7) proof of biological effects in mice after oral administration.</style></abstract><issue><style face="normal" font="default" size="100%">51</style></issue><work-type><style face="normal" font="default" size="100%">Article</style></work-type><custom3><style face="normal" font="default" size="100%">Foreign</style></custom3><custom4><style face="normal" font="default" size="100%">11.994</style></custom4></record></records></xml>