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1 Polish Journal of Chemistry

1 2002

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New Analogues of Cucurbita maxima Trypsin Inhibitor III (CMTI-III) Substituted with D-Arg or D-Lys in Position 5 (P1)

Frąszczak P., Rolka K., Kupryszewski G.

Polish Journal of Chemistry

2002

Vol. 76 / nr 4

519-523

Two new analogues of trypsin inhibitor CMTI-III substituted with D-Arg or D-Lys in position 5 (P1) were synthesized by the solid-phase method. The first analogue ([D-Arg5] CMTI-III) displayed association equilibrium constants (Ka) with bovine -trypsin by about three orders of magnitude lower than did wild CMTI-III. The second analogue ([D-Lys5] CMTI-III) displayed Ka by about four orders of magnitude lower than [Lys5] CMTI-III. The configuration of basic amino acid residue (Arg or Lys) in the reactive site (position P1) of CMTI-III and its analogues played an important role for the stabilization of the inhibitors active structure.