Targeting Echinococcus granulosus thioredoxin glutathione reductase using a Dynamic Combinatorial approach.

Targeting Echinococcus granulosus thioredoxin glutathione reductase using a Dynamic Combinatorial approach.

Saiz, Cecilia; Castillo, Valerie; Salinas, Gustavo; Mahler., S. Graciela

Abstract:

Dynamic Combinatorial Chemistry (DCC) is a synthetic tool that merges chemical synthesis with biological tests in one pot. The library is under thermodynamic control and introduction of a template could stabilize a compound through library redistribution via reversible bonds. This stabilization could result on an amplification of the best binder. E. granulosus is a flatworm parasite responsible for cystic hydatid disease. Its thiol redox homeostasis is dependent on an essential single enzyme: thioredoxin glutathione reductase (TGR), which is a key drug target.

Dynamic Combinatorial Chemistry (DCC) is a synthetic tool that merges chemical synthesis with biological tests in one pot. The library is under thermodynamic control and introduction of a template could stabilize a compound through library redistribution via reversible bonds. This stabilization could result on an amplification of the best binder. E. granulosus is a flatworm parasite responsible for cystic hydatid disease. Its thiol redox homeostasis is dependent on an essential single enzyme: thioredoxin glutathione reductase (TGR), which is a key drug target.

Palavras-chave:

DOI: 10.5151/chempro-15bmos-BMOS2013_2013101112832

Referências bibliográficas

• [1] 1 Otto, S.; Furlan, R.; Sanders, J.K.M. Curr. Opin. Chem. Biol. 2002, 6, 321-327.
• [2] 2 Kuntz, A.N.; Davioud-Charvet, E.; Sayed, A.A.; Califf, L.L.; Dessolin, J. et al. PLoS Med 2007 4(6): e206. doi:10.1371/journal.pmed.0040206.
• [3] 3 Saiz, C.; Castillo, V. and Mahler, S.G. Synlett 2012, 23, 1090-94.

Como citar:

Saiz, Cecilia; Castillo, Valerie; Salinas, Gustavo; Mahler., S. Graciela; "Targeting Echinococcus granulosus thioredoxin glutathione reductase using a Dynamic Combinatorial approach.", p-122-122. In: In Blucher Chemistry Proceedings, São Paulo, v. 1, n. 2, Dezembro.2013. São Paulo: Blucher, 2013.
ISSN 23184043, DOI 10.5151/chempro-15bmos-BMOS2013_2013101112832