Optimising Binding Kinetics Yields Insurmountable MC2 Receptor Antagonists for the Treatment of Diseases of ACTH Excess
Time: 4:00 pm
day: Conference Day Two
Details:
- Diseases such as Cushing’s and Congenital Adrenal Hyperplasia are characterised by supraphysiological levels of the hormone ACTH. MC2R antagonists should inhibit this effect, but are at risk of being out-competed by high ACTH levels, resulting in very high doses being required for efficacy
- This talk will describe the discovery and characterisation of MC2R antagonists with slow dissociation kinetics that display insurmountable antagonism
- These compounds show significantly enhanced efficacy at low doses in in vivo models of ACTH excess, and promise to be more effective in a wider patient population where ACTH levels can vary significantly
