title: Synthesis and evaluation of the sunflower derived trypsin inhibitor as a potent inhibitor of the type II transmembrane serine protease, matriptase.
abstract: We report here the synthesis of a 14-amino acid long bicyclic peptide, previously isolated from sunflower seeds. This peptide, termed sunflower trypsin inhibitor (SFTI-1), is one of the most potent naturally occurring small-molecule trypsin inhibitors. In addition to inhibiting trypsin, the synthetic SFTI-1 is also a very potent inhibitor, with a K(i) of 0.92nM, of the recently identified epithelial serine protease, termed 'matriptase'.
authors.affiliation: Laboratory of Medicinal Chemistry, National Cancer Institute, NIH, FCRDC, 376/208, PO Box B, Frederick, MD 21702, USA.
authors.forename: Y Q
authors.initials: YQ
authors.lastname: Long
authors.forename: S L
authors.initials: SL
authors.lastname: Lee
authors.forename: C Y
authors.initials: CY
authors.lastname: Lin
authors.forename: I J
authors.initials: IJ
authors.lastname: Enyedy
authors.forename: S
authors.initials: S
authors.lastname: Wang
authors.forename: P
authors.initials: P
authors.lastname: Li
authors.forename: R B
authors.initials: RB
authors.lastname: Dickson
authors.forename: P P
authors.initials: PP
authors.lastname: Roller
mesh_terms: D000595:Amino Acid Sequence; D001671:Biochemistry / Q000379:methods; D006368:Helianthus / Q000737:chemistry; D008958:Models, Molecular; D010456:Peptides, Cyclic / Q000737:chemistry* / Q000494:pharmacology*; D011487:Protein Conformation; D012697:Serine Endopeptidases / Q000737:chemistry / Q000187:drug effects*; D015842:Serine Proteinase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D014357:Trypsin / Q000737:chemistry / Q000187:drug effects* / Q000494:pharmacology
chemical_list: D010456:Peptides, Cyclic; C448501:SFTI-1 peptide, sunflower; D015842:Serine Proteinase Inhibitors; D012697:Serine Endopeptidases; C485595:matriptase; D014357:Trypsin