Increasing αvβ3 selectivity of the anti-angiogenic drug cilengitide by N-methylation

Carlos Mas-Moruno; Johannes G. Beck; Lucas Doedens; Andreas O. Frank; Luciana Marinelli; Sandro Cosconati; Ettore Novellino; Horst Kessler

doi:10.1002/anie.201102971

Increasing αvβ3 selectivity of the anti-angiogenic drug cilengitide by N-methylation

Carlos Mas-Moruno, Johannes G. Beck, Lucas Doedens, Andreas O. Frank, Luciana Marinelli, Sandro Cosconati, Ettore Novellino, Horst Kessler

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Abstract

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).

Originalsprache	Englisch
Seiten (von - bis)	9496-9500
Seitenumfang	5
Fachzeitschrift	Angewandte Chemie International Edition in English
Jahrgang	50
Ausgabenummer	40
DOIs	https://doi.org/10.1002/anie.201102971
Publikationsstatus	Veröffentlicht - 26 Sept. 2011

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10.1002/anie.201102971

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AU - Frank, Andreas O.

AU - Marinelli, Luciana

AU - Cosconati, Sandro

AU - Novellino, Ettore

AU - Kessler, Horst

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KW - N-methylation

KW - conformational studies

KW - cyclic peptides

KW - integrin

KW - receptor selectivity

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Increasing αvβ3 selectivity of the anti-angiogenic drug cilengitide by N-methylation

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