Protein farnesyl and N-myristoyl transferases: piggy-back medicinal chemistry targets for the development of antitrypanosomatid and antimalarial therapeutics

Michael H Gelb, Wesley C Van Voorhis, Frederick S Buckner, Kohei Yokoyama, Richard Eastman, Elisabeth P Carpenter, Chrysoula Panethymitaki, Katherine A Brown, Deborah F Smith

Research output: Contribution to journalArticlepeer-review


To accelerate progress in the development of therapeutics for protozoan parasitic diseases, we are studying enzymes active in co- and post-translational protein modification that are already the focus of drug development in other eukaryotic systems. Inhibitors of the protein farnesyltransferases (PFT) are well-established antitumour agents of low cytotoxicity and known pharmokinetic properties, while inhibitors of N-myristoyl transferase show both selectivity and specificity in the treatment of fungal infections. Here, we summarise the current evidence that supports the targeting of these ubiquitous eukaryotic enzymes for drug development against trypanosomatid infections and malaria.

Original languageEnglish
Pages (from-to)155-63
Number of pages9
Issue number2
Publication statusPublished - Feb 2003

Bibliographical note

Copyright 2002 Elsevier Science B.V.


  • Acyltransferases
  • Alkyl and Aryl Transferases
  • Animals
  • Antimalarials
  • Chemistry, Pharmaceutical
  • Drug Design
  • Plasmodium
  • Protein Conformation
  • Trypanocidal Agents
  • Trypanosoma

Cite this