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Selective Inhibition of Trypanosomal Triosephosphate Isomerase by a Thiopeptide

1992; Wiley; Volume: 31; Issue: 3 Linguagem: Inglês

10.1002/anie.199203281

1521-3773

Horst Kessler, Hans Matter, Armin Geyer, Hans‐Jürgen Diehl, Matthias Köck, G. Kurz, Fred R. Opperdoes, Mia Callens, Rik K. Wierenga,

Biochemical and Molecular Research

One approach to conquering sleeping sickness is the selective inhibition of trypanosomal triosephosphate isomerase, a key enzyme in the pathogen's metabolism, with cyclic hexapeptides. The thionylation of the Phe 5 ‐Phe 6 amide bond of the cyclic hexapeptide cyclo (Gly 1 ‐Pro 2 ‐Phe 3 ‐Val 4 ‐Phe 5 ‐Phe 6 ) is a minor modification, but effects a total rearrangement of the intramolecular hydrogen bonds which causes a drastic improvement of inhibitoric activity— maximum effect from minimum chemistry!