Identification of inhibitors of an 80 kDa protease from Trypanosoma cruzi through the screening of a combinatorial peptide library
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, partit
Vendeville, Sandrine,Buisine, Eric,Williard, Xavier,Schrevel, Joseph,Grellier, Philippe,Santana, Jaime,Sergheraert, Christian
p. 194 - 198
(2007/10/03)
Synthesis of (R)- and (S)-(glu)Thz and the Corresponding Bisthiazole Dipeptide of Dolastatin 3
Dolastatin 3 (1) has been reported to be a cyclic pentapeptide containing two thiazole amino acids, (gly)Thz (2) and (gln)Thz (3).The syntheses of (R)- and (S)-(glu)Thz (8a,b) and (glu)Thz-(gly)Thz (11a,b) derivatives suitable for elaboration to dolastatin 3 are described.A key feature of the (glu)Thz syntheses is the selective thiation of a primary amide with Lawesson's reagent in the presence of ester and urethane functionalities.
Kelly, Robert C.,Gebhard, I.,Wicnienski, N.
p. 4590 - 4594
(2007/10/02)
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