The purine transferase from Trypanosoma cruzi as a potential target for bisphosphonate-based chemotherapeutic compounds

FERNANDEZ D; WENCK MA; CRAIG SP 3RD; DELFINO JM

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Año: 2004 vol. 14 p. 4501 - 4504

0960-894X

We identified and tested bisphosphonates as inhibitors of a protozoan molecular target. Computational modeling studies demonstrated that these compounds are mimics of the natural substrate of the enzyme. The most potent bisphosphonates in vitro are pamidronate and risedronate, which inhibit the purine transferase from Trypanosoma cruzi in the micromolar range.