6533b835fe1ef96bd129e9cf
RESEARCH PRODUCT
Synthesis and biological properties of the seven alanine-modified analogues of the marine cyclopeptide hymenamide C
Ines BrunoMiguel Payà PerisPaolo RoveroAssunta NapolitanoLuigi Gomez-palomaRut LucasRaffaele Ricciosubject
PharmacologyAlanineHuman neutrophilStereochemistryChemistryOrganic ChemistryElastaseRational designBiological activityGeneral MedicineBiochemistrySolid-phase synthesisBiochemistryStructural BiologyBiological propertyDrug DiscoveryMolecular MedicineMolecular BiologyInhibitory effectdescription
The synthesis and biological activity of the marine cyclopeptide hymenamide C(1), showing an inhibitory effect on human neutrophil elastase degranulation release, were recently described. Based on this result, it was decided to undertake a systematic structure-activity relationship study of this cyclopeptide, based on the Ala-scan technique, in order to obtain useful information for the rational design of additional analogues. The synthesis and characterization of the seven Ala modified analogues are reported and their biological and pharmacological properties are described.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2002-07-24 | Journal of Peptide Science |