Title : Fluorometric detection of protein-ligand engagement: The case of phosphodiesterase5.

Pub. Date : 2018 Feb 5

PMID : 29132113






3 Functional Relationships(s)
Download
Sentence
Compound Name
Protein Name
Organism
1 The new approach takes advantage of Forster Resonance Energy Transfer (FRET) between, as the donor, a fluorescein-like diarsenical probe able to covalently bind a tetracysteine motif fused to the recombinant PDE5 catalytic domain and, as the acceptor, a rhodamine probe covalently bound to the pseudosubstrate cGMPS. Cyclic GMP phosphodiesterase 5A Homo sapiens
2 The FRET efficiency decreases when a competitive ligand binds the PDE5 catalytic site and displaces the cGMPS-rhodamine conjugate. Cyclic GMP phosphodiesterase 5A Homo sapiens
3 We have structurally investigated the PDE5/cGMPS-rhodamine complex by molecular modelling and have used the FRET signal to quantitatively characterize its binding equilibrium. Cyclic GMP phosphodiesterase 5A Homo sapiens