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- Mutulis, FelikssUppsala universitet,Avdelningen för farmaceutisk farmakologi,Proteochemometric group (author)
N-alkylated dipeptide amides and related structures as imitations of the melanocortins' active core
- Article/chapterEnglish2005
Publisher, publication year, extent ...
- Elsevier BV,2005
- printrdacarrier
Numbers
- LIBRIS-ID:oai:DiVA.org:uu-104278
- https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-104278URI
- https://doi.org/10.1016/j.peptides.2004.11.026DOI
- http://kipublications.ki.se/Default.aspx?queryparsed=id:111529293URI
Supplementary language notes
- Language:English
- Summary in:English
Part of subdatabase
- SwePubSwePub
Classification
Notes
- Thirty-three low molecular mass structures combining both peptide and peptoid features were prepared and tested on human melanocortin receptors MC1,3-5R. Most of them displayed low micromolar activity with preference for diamines, guanidino and 2-naphthyl derivatives compared to monoacetylated, amino and 3-indolyl counterparts. Some contained L- or D-histidine residues, but the change did not influence affinity. QSAR modelling yielded excellent models for the MC3-5 receptors explaining R2Y=0.89-0.91 and predicting Q2=0.77-0.80 of the affinity variations. One compound displayed MC1R selectivity (13-fold and more). An NMR study of showed that it exists as a mixture of four rotamers at its tertiary amide bonds. Comparisons with earlier data for melanocortin core tetrapeptide analogues indicate that the novel peptide-peptoids interact with the melanocortin receptors in a different way.
Subject headings and genre
- MEDICIN OCH HÄLSOVETENSKAP Medicinska och farmaceutiska grundvetenskaper Farmaceutiska vetenskaper hsv//swe
- MEDICAL AND HEALTH SCIENCES Basic Medicine Pharmaceutical Sciences hsv//eng
- Melanocortins
- Peptidomimetics
- Peptoid–peptide hybrids
- Solid phase organic synthesis
- Structure–activity
- QSAR
- NMR
- PHARMACY
- FARMACI
Added entries (persons, corporate bodies, meetings, titles ...)
- Mutule, IlzeUppsala universitet,Avdelningen för farmaceutisk farmakologi,Proteochemometric group (author)
- Liepinsh, Edvards (author)
- Yahorau, AlehUppsala universitet,Avdelningen för farmaceutisk farmakologi,Proteochemometric group (author)
- Lapinsh, MarisUppsala universitet,Avdelningen för farmaceutisk farmakologi,Proteochemometric group (author)
- Kopantshuk, SergeiUppsala universitet,Avdelningen för farmaceutisk farmakologi,Proteochemometric group (author)
- Veiksina, SantaUppsala universitet,Avdelningen för farmaceutisk farmakologi,Proteochemometric group (author)
- Rinken, Ago (author)
- Wikberg, Jarl E SUppsala universitet,Avdelningen för farmaceutisk farmakologi,Proteochemometric group (author)
- Uppsala universitetAvdelningen för farmaceutisk farmakologi (creator_code:org_t)
Related titles
- In:Peptides: Elsevier BV26:10, s. 1997-20160196-97811873-5169
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