title: Design and synthesis of redox stable analogues of sunflower trypsin inhibitors (SFTI-1) on solid support, potent inhibitors of matriptase.
abstract: [structure: see text] Matriptase is a member of the emerging class of type II transmembrane serine proteases. It was found that the sunflower trypsin inhibitor (SFTI-1), isolated from sunflower seeds, inhibits matriptase with a subnanomolar Ki of 0.92 nM. On the basis of this result, we designed and synthesized its proteolytically stable analogues, SFTI-2 and SFTI-3. SFTI-3 exhibited very good binding affinity to matriptase, and it was metabolically stable.
authors.affiliation: Laboratory of Medicinal Chemistry, NCI, NIH, Frederick, Maryland 21702, USA.
authors.forename: Sheng
authors.initials: S
authors.lastname: Jiang
authors.forename: Peng
authors.initials: P
authors.lastname: Li
authors.forename: Sheau-Ling
authors.initials: SL
authors.lastname: Lee
authors.forename: Cheng Yong
authors.initials: CY
authors.lastname: Lin
authors.forename: Ya-Qiu
authors.initials: YQ
authors.lastname: Long
authors.forename: Michael D
authors.initials: MD
authors.lastname: Johnson
authors.forename: Robert B
authors.initials: RB
authors.lastname: Dickson
authors.forename: Peter P
authors.initials: PP
authors.lastname: Roller
mesh_terms: D003500:Cyclization; D015195:Drug Design; D006368:Helianthus / Q000737:chemistry*; D015394:Molecular Structure; D010084:Oxidation-Reduction; D010455:Peptides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D012697:Serine Endopeptidases / Q000378:metabolism*; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014361:Trypsin Inhibitors / Q000737:chemistry*
chemical_list: D010455:Peptides; D015842:Serine Proteinase Inhibitors; D014361:Trypsin Inhibitors; D012697:Serine Endopeptidases; C485595:matriptase