title: Determination of peptide hydrophobicity parameters by reversed-phase high-performance liquid chromatography.
abstract: The log kw values of fourteen potential fibrinogen receptor antagonist peptides (RGDX) determined by reversed-phase HPLC were correlated to hydrophobic parameters of the amino acid side-chain log P in position X of the tetrapeptides. Comparing the polymer columns with LiChrosorb RP-8, the correlation coefficient using a polyethylene column is higher (0.94) than that for RP-8 (0.88), which demonstrates the importance of a homogeneous hydrophobic surface and makes this method very suitable for the determination of the overall hydrophobicity of shorter peptides. The hydrophobicity parameters log kw of the RGDX peptides (-1.15 to 2.19) were used to investigate the influence of molecular parameters of X on the potency of RGDX in inhibiting platelet aggregation. The results confirm the importance of hydrophobicity for the contribution of X to the biological activity of RGDX.
authors.affiliation: Institute of Molecular Pharmacology, Berlin Germany.
authors.forename: S
authors.initials: S
authors.lastname: Rothemund
authors.forename: E
authors.initials: E
authors.lastname: Krause
authors.forename: A
authors.initials: A
authors.lastname: Ehrlich
authors.forename: M
authors.initials: M
authors.lastname: Bienert
authors.forename: E
authors.initials: E
authors.lastname: Glusa
authors.forename: P
authors.initials: P
authors.lastname: Verhallen
mesh_terms: D000595:Amino Acid Sequence; D000596:Amino Acids / Q000737:chemistry; D002851:Chromatography, High Pressure Liquid / Q000379:methods*; D008969:Molecular Sequence Data; D009842:Oligopeptides / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D000596:Amino Acids; D009842:Oligopeptides