Development of Chemical Proteomics for the Folateome and Analysis of the Kinetoplastid Folateome.

ABSTRACT: The folate pathway has been extensively studied in a number of organisms, with its essentiality exploited by a number of drugs. However, there has been little success in developing drugs that target folate metabolism in the kinetoplastids. Despite compounds being identified which show significant inhibition of the parasite enzymes, this activity does not translate well into cellular and animal models of disease. Understanding to which enzymes antifolates bind under physiological conditions and how this corresponds to the phenotypic response could provide insight on how to target the folate pathway in these organisms. To facilitate this, we have adopted a chemical proteomics approach to study binding of compounds to enzymes of folate metabolism. Clinical and literature antifolate compounds

SUBMITTER: Webster LA 

PROVIDER: S-EPMC6199744 | biostudies-literature | 2018 Oct

REPOSITORIES: biostudies-literature