SFTI-1(81) Protein Card

General Information
Name SFTI-1
Sequence GRCTKSIPPICFPD
Class BBI-like trypsin inhibitor
Average Mass 1513.79
Monoisotopic Mass 1512.72
m/z M+H 1513.79
ProteinType Wild type
Parent
Organism Helianthus annus
Helianthus exilis
Helianthus tuberosus
Notes
Cyclic Yes

Assay
Protease inhibition
Matriptase inhibitory activity of SFTI-2 is 25-fold less potent than native, while SFTI-3 exhibits similar potency. [...]Jiang S et al. (2007) Org Lett 9:9-12
12 SFTI alanine mutants were tested for inhibitory activity against bovine trypsin. K5A mutant shows the weakest activity. [...]Daly NL et al. (2006) J Biol Chem 281:23668-75
Ki calculated for a range of SFTI-1 analogues against trypsin and chymotrypsin. [...]Descours A et al. (2002) Chembiochem 3:318-23
Bifunctional analogues of SFTI-1 found to have trypsin and chymotrypsin inhibitory activity. [...]Jaulent AM and Leatherbarrow RJ (2004) Protein Eng Des Sel 17:681-7
SFTI-1 immobilised on gold and interaction with trypsin investigated. [...]Ohtsuka K et al. (2004) Analyst 129:888-9
SFTI-1, an acyclic permutant and a [CYS-Abu]-cyclic mutant shown to possess potent trypsin inhibitory activity. [...]Zablotna E et al. (2002) Biochem Biophys Res Commun 292:855-9
SFTI-1 was found to have nano-molar inhibitory effect against matriptase and trypsin. [...]Long YQ et al. (2001) Bioorg Med Chem Lett 11:2515-9
Both SFTI-1 and acyclic SFTI-1 are potent inhibitors of bovine beta trypsin [...]Korsinczky ML et al. (2001) J Mol Biol 311:579-91
Enzymatic Digest
Bifunctional analogues of SFTI-1 found to be resistant to hydrolysis by trypsin. [...]Jaulent AM and Leatherbarrow RJ (2004) Protein Eng Des Sel 17:681-7

References
Korsinczky ML, Schirra HJ, Rosengren KJ, West J, Condie BA, Otvos L, Anderson MA, Craik DJ (2001) Solution structures by 1H NMR of the novel cyclic trypsin inhibitor SFTI-1 from sunflower seeds and an acyclic permutant. J Mol Biol 311:579-91
Long YQ, Lee SL, Lin CY, Enyedy IJ, Wang S, Li P, Dickson RB, Roller PP (2001) Synthesis and evaluation of the sunflower derived trypsin inhibitor as a potent inhibitor of the type II transmembrane serine protease, matriptase. Bioorg Med Chem Lett 11:2515-9
Zablotna E, Kazmierczak K, Jaskiewicz A, Stawikowski M, Kupryszewski G, Rolka K (2002) Chemical synthesis and kinetic study of the smallest naturally occurring trypsin inhibitor SFTI-1 isolated from sunflower seeds and its analogues. Biochem Biophys Res Commun 292:855-9
Marx UC, Korsinczky ML, Schirra HJ, Jones A, Condie B, Otvos L Jr, Craik DJ (2003) Enzymatic cyclization of a potent bowman-birk protease inhibitor, sunflower trypsin inhibitor-1, and solution structure of an acyclic precursor peptide. J Biol Chem 278:21782-9
Ohtsuka K, Kajiki R, Waki M, Nojima T, Takenaka S (2004) Immobilization of sunflower trypsin inhibitor (SFTI-1) peptide onto a gold surface and analysis of its interaction with trypsin. Analyst 129:888-9
Jaulent AM, Leatherbarrow RJ (2004) Design, synthesis and analysis of novel bicyclic and bifunctional protease inhibitors. Protein Eng Des Sel 17:681-7
Stawikowski M, Stawikowska R, Jaskiewicz A, Zablotna E, Rolka K (2005) Examples of Peptide-Peptoid Hybrid Serine Protease Inhibitors Based on the Trypsin Inhibitor SFTI-1 with Complete Protease Resistance at the P1-P1' Reactive Site. Chembiochem 6:1057-61
Korsinczky ML, Clark RJ, Craik DJ (2005) Disulfide bond mutagenesis and the structure and function of the head-to-tail macrocyclic trypsin inhibitor SFTI-1. Biochemistry 44:1145-53
Descours A, Moehle K, Renard A, Robinson JA (2002) A new family of beta-hairpin mimetics based on a trypsin inhibitor from sunflower seeds. Chembiochem 3:318-23
Luckett S, Garcia RS, Barker JJ, Konarev AV, Shewry PR, Clarke AR, Brady RL (1999) High-resolution structure of a potent, cyclic proteinase inhibitor from sunflower seeds. J Mol Biol 290:525-33
Jiang S, Li P, Lee SL, Lin CY, Long YQ, Johnson MD, Dickson RB, Roller PP (2007) Design and synthesis of redox stable analogues of sunflower trypsin inhibitors (SFTI-1) on solid support, potent inhibitors of matriptase. Org Lett 9:9-12
Cascales,L., Henriques,S.T., Kerr,M.C., Huang,Y.H., Sweet,M.J., Daly,N.L. and Craik,D.J. (2011) Identification and characterization of a new family of cell-penetrating peptides: cyclic cell-penetrating peptides. J. Biol. Chem. 286:36932-36943

Cross-references
Protein precursor(s) PawS1 - exilis
PawS1 - tuberosus
PawS1 - annuus
Nucleic acids
Structure SFTI-1
SFTI-1
SFTI-1
Crystal structure of bovine trypsin complexed with sfti-1 analog containing a peptoid residue at position p1
Crystal Structure of MT-SP1 in complex with SFTI-1
Links GenBank CAJ19097.1
SwissProt Q4GWU5

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