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Structure-Property Model for Membrane Partitioning of Oligopeptides
Umeå universitet, Teknisk-naturvetenskapliga fakulteten, Kemiska institutionen.ORCID-id: 0000-0001-9188-5518
The Royal Danish School of Pharmacy. (Departments of Medicinal Chemistry and Pharmaceutics)
The Royal Danish School of Pharmacy. (Department of Medicinal Chemistry)
2000 (Engelska)Ingår i: Journal of Medicinal Chemistry, ISSN 0022-2623, E-ISSN 1520-4804, Vol. 43, nr 1, s. 103-113Artikel i tidskrift (Refereegranskat) Published
Abstract [en]

The aim of this study was to develop a structure-property model for membrane partitioningof oligopeptides using statistical design methods and multivariate data analysis. A set of 20tetrapeptides with optional N-methylations at residues 2 and 4 was designed by a D-optimaldesign procedure. After synthesis and purification, the membrane partitioning abilities of thepeptides were tested in two chromatographic systems with phospholipids as the stationaryphase: immobilized artificial membrane chromatography (IAM) and immobilized liposomechromatography (ILC). The relationship between these measures and three different sets ofcalculated descriptors was analyzed by partial least-squares projection to latent structures(PLS). The descriptors used were the molecular surface area, Molsurf parameters, and Volsurfparameters. All three models were of good statistical quality and supported that a largehydrogen-bonding potential and the presence of a negative charge impair membrane partitioning,whereas hydrophobic parameters promote partitioning. The findings are in accordancewith what has been found for absorption of known drugs and have implications for the designof peptide-like drugs with good oral bioavailability.

Ort, förlag, år, upplaga, sidor
American Chemical Society (ACS), 2000. Vol. 43, nr 1, s. 103-113
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Annan medicinsk grundvetenskap
Identifikatorer
URN: urn:nbn:se:umu:diva-142733DOI: DOI: 10.1021/jm9910932OAI: oai:DiVA.org:umu-142733DiVA, id: diva2:1164046
Tillgänglig från: 2017-12-08 Skapad: 2017-12-08 Senast uppdaterad: 2018-06-09

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Sandberg Hiltunen, Maria

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