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1 Polish Journal of Chemistry

1 2001

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Low Molecular Mass Inhibitors of Bovine beta-Trypsin Containing Binding Loop Fragment of CMTI-III. Synthesis and Evaluation of Inhibitory Activity

Frąszczak P., Lis K., Jaśkiewicz A., Miecznikowska H., Rolka K., Kupryszewski G.

Polish Journal of Chemistry

2001

Vol. 75, nr 12

1863-1868

Three peptides with sequences related to the binding loop of Cucurbita maxima trypsin inhibitor III were obtained: [G3,GIO]CMTI-HI (1-10) (1), [A1,G3,A9,G10]MTlII (1-10) (2) and c(K-A-A-P-R-I-L-M-K-Y-A-E) (3). All peptides were synthesized by the solid-phase methodusing the Fmoc/Bu t procedure. Peptide 1 revealed a relatively high inhibitory activity (association equilibrium constant with bovine beta-trypsin Ka = 4 x 10 9 [M -1]). Significantly lower activity (Ka = 3.6x l O4 [M -1) was obtained for peptide 3. Peptide 2 appeared to be inactive.