title: Structure and activity studies of pardaxin and analogues using model membranes of phosphatidylcholine.
abstract: Thirteen synthetic pardaxin analogues were assayed for their ability to interact with model membranes of phosphatidylcholine. The results suggested the following: An amphipathic alpha-helix from isoleucine-14 to leucine-26 is responsible for most of the membrane perturbing properties of pardaxin. A hydrophobic N-terminal region enhances the activity of the isoleucine-14 to leucine-26 alpha-helix by binding the pardaxin molecule to the lipid bilayer. A bend centered around 12Ser-13Pro appears to create overall amphipathicity for the two different helical regions of pardaxin, but this contributes only slightly to potency. The C-terminal amino acids are unimportant for membrane perturbing activity and may be present only to enhance transportation in an aqueous environment prior to membrane binding in the native system.
authors.affiliation: Suntory Institute for Bioorganic Research, Osaka, Japan.
authors.forename: C J
authors.initials: CJ
authors.lastname: Barrow
authors.forename: K
authors.initials: K
authors.lastname: Nakanishi
authors.forename: K
authors.initials: K
authors.lastname: Tachibana
mesh_terms: D000595:Amino Acid Sequence; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004563:Electrochemistry; D005397:Fish Venoms / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D007532:Isoleucine / Q000737:chemistry; D007930:Leucine / Q000737:chemistry; D008051:Lipid Bilayers / Q000378:metabolism; D008081:Liposomes / Q000378:metabolism*; D008239:Lysine / Q000737:chemistry; D009682:Magnetic Resonance Spectroscopy; D008969:Molecular Sequence Data; D010713:Phosphatidylcholines / Q000378:metabolism*; D011392:Proline / Q000737:chemistry; D017433:Protein Structure, Secondary; D012996:Solutions; D013329:Structure-Activity Relationship
chemical_list: D005397:Fish Venoms; D008051:Lipid Bilayers; D008081:Liposomes; D010713:Phosphatidylcholines; D012996:Solutions; D007532:Isoleucine; C017603:pardaxin; D011392:Proline; D007930:Leucine; D008239:Lysine