HotSpot Therapeutics has designed the first and only Technology Platform to identify and drug regulatory hotspots systematically across the entire proteome.
Conventional therapeutics target the catalytic function or active site of an enzyme and are effective in just a fraction of known disease targets. Competition with the enzyme’s substrate minimizes their effectiveness while cross-reactivity against other proteins in the body leads to unwanted side effects. Additionally, pharmaceutical properties can be suboptimal due to the charge and greasiness of these sites.
In contrast, evolution has crafted natural control mechanisms with precisely-honed selectivity and specificity. At the heart of these regulatory regions are privileged allosteric sites called regulatory hotspots that offer attractive real estate for pharmacological drug discovery.
Hotspots in action
Problems with catalytic site:
Introducing regulatory hotspots
Targeting regulatory hotspots
has many advantages:
Regulatory hotspots in disease
Through regulatory hotspots, Nature has devised a means to selectively correct for chemical imbalances and dysregulation to restore health and proper functioning. We see this in both normal biological activity and in disease. In a select number of cases, regulatory hotspots have been successfully targeted to create important new medicines: