Identification of Inhibitors of an 80kDa Protease from Trypanosoma cruzi through the Screening of a Combinatorial Peptide Library.

…, J SCHREVEL, P GRELLIER, J SANTANA…

文献索引：Vendeville, Sandrine; Buisine, Eric; Williard, Xavier; Schrevel, Joseph; Grellier, Philippe; Santana, Jaime; Sergheraert, Christian Chemical and Pharmaceutical Bulletin, 1999 , vol. 47, # 2 p. 194 - 198

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被引用次数: 27

摘要

Two orthogonal peptide combinatorial libraries were screened to discover inhibitors of Tc80 protease, a novel target from Trypanosoma cruzi involved in host cell invasion. These libraries were composed of 15625 structurally diversified tripeptides, partitioned in 125 mixtures. The screening led to a low micromolar inhibitor which was actually an HF cleavage by-product H-Ipe-D-Tic-D-Glu (S-paratolyl)-OH. IC 50 values of several analogous ...