BOSTON, Mass. (August 23, 2019)— HotSpot Therapeutics, Inc, a biotechnology company pioneering the discovery of nature’s regulatory sites to advance allosteric drug discovery, today announced the acquisition of Macroceutics, Inc., a provider of DNA-encoded library (DEL) screening technologies. The outgrowth of a strategic collaboration, the acquisition will enhance HotSpot Therapeutics’ SpotFinder™ platform, the first drug discovery platform to systematically predict, drug and differentiate unique regulatory hotspots on proteins. DEL is a next generation screening technique that enables millions of molecules to be rapidly synthesized and screened against a protein of interest.
“In working with the Macroceutics team, we were excited by their bespoke libraries and capabilities and the potential to marry the power of DNA-encoded library synthesis with specifically designed scaffolds to target regulatory hotspots,” said Geraldine Harriman, PhD, Co-Founder and Chief Scientific Officer, HotSpot Therapeutics. “Using the rich structural information delivered by our platform, we have a roadmap for the design of customized chemical scaffolds. DEL technology allows us to translate these insights into millions of tailored scaffolds quickly, accelerating hit expansion and lead optimization efforts.”
As part of the acquisition, HotSpot will be able to leverage approximately 1 billion custom drug-like molecules, the company’s full suite of DNA-based chemistries, and a fully enabled screening platform. The Macroceutics team will join HotSpot Therapeutics, thereby establishing a new in-house DEL capability that will focus on custom library/methods development, screening of HotSpot pipeline and partnered targets and novel method development. Ken Carson, PhD, Founder and Chief Executive Officer of Macroceutics, Inc., will lead the DEL screening group as Executive Vice President, Chemical Sciences.
“It has been exciting to see how well tailored DEL design works in practice with HotSpot’s platform technology. The success of our collaboration naturally led to a strategic relationship where we can fully integrate DEL into the SpotFinder™ platform,” said Carson. “We are excited to be joining forces with the HotSpot team to develop new allosteric medicines.”
Historically, it has been challenging to rationally develop small molecules against allosteric sites because allosteric pockets are difficult to distinguish from other protein sites. New chemistry and specialized assay techniques are often required to assess the binding and function of small molecules within allosteric pockets. Core to HotSpot Therapeutic’s drug discovery strategy is a commitment to novel chemistry development that leverages the unique properties of regulatory hotspots to control protein function.
About HotSpot Therapeutics
HotSpot Therapeutics is targeting nature’s regulatory mechanisms to create allosteric medicines that exhibit high precision and potency. The company leverages its proprietary SpotFinder™ technology, the first and only platform designed to identify “regulatory hotspots,” a unique family of pockets that sit remote from the active site on a protein and are used by nature to control protein function. Using bespoke chemistry approaches, HotSpot is developing a pipeline of first-in-class small molecules for the treatment of serious autoimmune and metabolic diseases. The company has identified more than 100 regulatory hotspots across a range of proteins and pathways. HotSpot’s lead compounds include the first and only allosteric inhibitors to target PKC-theta for autoimmune diseases, and S6 kinase, an immuno-metabolic enzyme involved in the regulation of hepatic insulin sensitivity and mitochondrial function – an important new target for NASH and metabolic diseases. To learn more, visit www.hotspotthera.com.