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Increasing αvβ3 Selectivity of the Anti‐Angiogenic Drug Cilengitide by N‐Methylation
Author(s) -
MasMoruno Carlos,
Beck Johannes G.,
Doedens Lucas,
Frank Andreas O.,
Marinelli Luciana,
Cosconati Sandro,
Novellino Ettore,
Kessler Horst
Publication year - 2011
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201102971
Subject(s) - methylation , integrin , drug , selectivity , chemistry , computational biology , dna methylation , cancer research , computer science , psychology , information retrieval , combinatorial chemistry , pharmacology , medicine , biochemistry , gene , biology , receptor , gene expression , catalysis
A subtle change : Structural changes upon amide bond methylation improve the selectivity of the anti‐angiogenic drug Cilengitide, which after N‐methylation at distinct positions discriminates between the closely related pro‐angiogenic integrins αvβ3 and αvβ5 (see scheme).