Ontology highlight
ABSTRACT:
SUBMITTER: Bachmaier S
PROVIDER: S-EPMC6440977 | biostudies-literature | 2019 Mar
REPOSITORIES: biostudies-literature
Bachmaier Sabine S Volpato Santos Yuri Y Kramer Susanne S Githure George Boniface GB Klöckner Thomas T Pepperl Julia J Baums Cordula C Schenk Robin R Schwede Frank F Genieser Hans-Gottfried HG Dupuy Jean-William JW Forné Ignasi I Imhof Axel A Basquin Jerôme J Lorentzen Esben E Boshart Michael M
Nature communications 20190329 1
Protein kinase A (PKA), the main effector of cAMP in eukaryotes, is a paradigm for the mechanisms of ligand-dependent and allosteric regulation in signalling. Here we report the orthologous but cAMP-independent PKA of the protozoan Trypanosoma and identify 7-deaza-nucleosides as potent activators (EC<sub>50</sub> ≥ 6.5 nM) and high affinity ligands (K<sub>D</sub> ≥ 8 nM). A co-crystal structure of trypanosome PKA with 7-cyano-7-deazainosine and molecular docking show how substitution of key amin ...[more]