Use of a Fission Yeast Platform to Identify and Characterize Small Molecule PDE Inhibitors.

ABSTRACT: Cyclic nucleotide phosphodiesterases (PDEs) have been proven to be targets for which highly selective and potent drugs can be developed. Mammalian genomes possess 21 genes whose products are pharmacologically grouped into 11 families; however related genes from pathogenic organisms display sufficient divergence from the mammalian homologs such that PDE inhibitors to these enzymes could be used to treat parasitic infections without acting on the related human PDEs. We have developed a platform for expressing cloned PDEs in the fission yeast Schizosaccharomyces pombe, allowing for inexpensive, but robust screening for small molecule inhibitors that are cell permeable. Such compounds typically display the expected biological activity when tested in cell culture, including anti-inflamma

SUBMITTER: Hoffman CS 

PROVIDER: S-EPMC8802716 | biostudies-literature | 2021

REPOSITORIES: biostudies-literature