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Multiple N-methylation of MT-II backbone amide bonds leads to melanocortin receptor subtype hMC1R selectivity; pharmacological and conformational studies

Multiple N-methylation is a novel technology to improve bioavailability of peptides and increase receptor subtype selectivity. This technique has been applied here to the superpotent but non-selective cyclic peptide MT-II. A library of all possible 31 backbone N-methylated derivatives has been synth...

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Main Authors: Doedens, Lucas, Opperer, Florian, Cai, Minying, Beck, Johannes G., Dedek, Matt, Palmer, Erin, Hruby, Victor J., Kessler, Horst
Formato: Artigo
Idioma:Inglês
Publicado: 2010
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Acceso en liña:https://ncbi.nlm.nih.gov/pmc/articles/PMC2895553/
https://ncbi.nlm.nih.gov/pubmed/20496895
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ja101428m
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