Searchable abstracts of presentations at key conferences in endocrinology

ea0014s3.4 | Signaling and regulation of G-protein-coupled hormone receptors | ECE2007

Ago-allosteric effects of agonist drugs on 7TM receptors and their endogenous hormones – example from the ghrelin receptor

Schwartz Thue W.

Conventionally, an allosteric modulator is neutral in respect of efficacy and binds to a receptor site distant from the orthosteric site of the endogenous agonist. However, recently compounds being ago-allosteric modulators have been described i.e. compounds acting both as agonists on their own and as enhancers for the endogenous agonists in both increasing agonist potency and often providing additive efficacy - superagonism. The additive efficacy can also be observed with ago...