Figure 5.
Orthosteric and positive allosteric modulation. NPs (square), such as ANP and BNP, would bind to the orthosteric site of GC-A inducing a conformational change that would lead to cGMP generation. GC-A-positive allosteric modulator (PAM), such as MCUF-651, would bind to topographically distinct site(s) on the receptor to increase the affinity and/or efficacy of orthosteric ligands to which enhances cGMP signalling.
