We continue our series of posts in the Biologics campaign! Today we would like to focus on Melanocortin receptors (MCRs).
Melanocortin receptors (MCRs) are an important group of proteins that belong to the 7TM GPCR superfamily. They play a crucial role in many physiological functions that are clinically relevant. The MC1R is responsible for the pigmentation of both skin and hair, while MC2R is engaged in adrenal steroidogenesis which is important for our stress response. MC3R and MC4R help control food intake and feeling of fullness, and MC5R is responsible for regulating sebum production. Understanding the MCR's role is needed for developing new medications to treat various diseases that involve these functions.
You can find more info about MCRs functions here.
Here is a recent article that describes the discovery of a new series of orally bioavailable, small-molecule MC4R antagonists. MC4R is found in the CNS and is crucial in regulating appetite and food consumption, and accordingly plays a significant role in maintaining a healthy weight. Studies have shown that deficiencies in MC4R signaling can lead to increased body mass and hyperphagia in humans. By blocking the MC4R, it's possible to mitigate decreased appetite and weight loss in conditions like anorexia. The authors introduced a new spirocyclic clinical candidate PF-07258669 that has shown robust efficacy in the rodent model of cachexia.
More information about this research is here.
