title: New active analogues of Cucurbita maxima trypsin inhibitor III (CMTI-III) modified in the non-contact region.
abstract: Four new analogues of trypsin inhibitor CMTI-III(3-28) = [desArg1,desVal2,desGly29]CMTI-III which was recently shown to be fully active, were synthesized by the solid-phase method. The introduction of glycine in position 9 (peptide 1) and Gly-Pro-Gly (peptide 2) and Gly-Pro-Asn (peptide 3) in the regions 17-19 and 23-25, respectively, did not change the antitrypsin activity of all modified peptides. All of these substitutions are presumed to be outside the trypsin-binding loop as judged from the X-ray structure of the complex between beta-trypsin and the related inhibitor CMTI-I. Also the fourth analogue which was substituted in all the positions mentioned, exhibited the full activity.
authors.affiliation: Faculty of Chemistry, University of Gdańsk, Poland.
authors.forename: J
authors.initials: J
authors.lastname: Rózycki
authors.forename: G
authors.initials: G
authors.lastname: Kupryszewski
authors.forename: K
authors.initials: K
authors.lastname: Rolka
authors.forename: U
authors.initials: U
authors.lastname: Ragnarsson
authors.forename: T
authors.initials: T
authors.lastname: Zbyryt
authors.forename: I
authors.initials: I
authors.lastname: Krokoszyńska
authors.forename: T
authors.initials: T
authors.lastname: Wilusz
mesh_terms: D000595:Amino Acid Sequence; D000596:Amino Acids / Q000032:analysis; D000818:Animals; D002417:Cattle; D018360:Crystallography, X-Ray; D008969:Molecular Sequence Data; D010940:Plant Proteins / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D014357:Trypsin / Q000378:metabolism; D014361:Trypsin Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism
chemical_list: D000596:Amino Acids; C081870:CMTI protein, Cucurbita maxima; D010940:Plant Proteins; D014361:Trypsin Inhibitors; D014357:Trypsin