HotSpot Therapeutics Acquires Macroceutics to Enhance Allosteric Drug Discovery with DNA-Encoded Library Technology

On August 26, 2019, VCBeat (WeChat ID: vcbeat) learned from foreign media reports that biotechnology and pharmaceutical company HotSpot Therapeutics (HotSpot) announced the acquisition of Macroceutics. No financial terms of the transaction were disclosed.

It is reported that, following the completion of this acquisition, Macroceutics’ DNA-encoded library (DEL) will be integrated into HotSpot’s drug discovery platform, SpotFinder. In addition, Dr. Ken Carson, Founder and CEO of Macroceutics, will lead the DEL screening team.

Macroceutics is a provider of DNA-encoded library (DEL) synthesis and screening technologies, primarily assisting pharmaceutical companies in new drug development. The concept of DEL synthesis and screening was first proposed by Dr. Sydney Brenner and Dr. Richard Lerner at the Scripps Research Institute in the United States. This technology combines combinatorial chemistry with molecular biology and is supported by high-throughput sequencing techniques. Currently, DEL technology enables the rapid synthesis of millions of molecules and their screening against target proteins, making the identification of lead compounds faster and more efficient.

HotSpot, founded in 2017 and headquartered in Massachusetts, USA, is a biotechnology and pharmaceutical company. Under the leadership of Dr. Geraldine Harriman, Co-Founder and Chief Scientific Officer, the company is dedicated to developing therapeutics for severe autoimmune and metabolic diseases. Furthermore, HotSpot has pioneered novel therapies that help patients restore health by modulating protein function.

HotSpot’s SpotFinder platform is primarily dedicated to the research and development of allosteric drugs with high precision and high potency. Unlike traditional drug discovery approaches that target the active sites of proteins, this platform focuses on protein functions at sites distal to the active site. HotSpot states that drugs developed using the SpotFinder platform demonstrate superior efficacy and safety profiles compared to conventional therapeutics.

HotSpot has developed targeted allosteric inhibitors of PKC-θ for autoimmune diseases, as well as S6 kinase modulators involved in regulating hepatic insulin sensitivity and mitochondrial function. Furthermore, the company is exploring novel targets for the treatment of metabolic disorders such as non-alcoholic steatohepatitis (NASH).

Allosteric protein sites are difficult to distinguish from other protein sites, making the rational development of small-molecule drugs targeting allosteric sites consistently challenging. This typically requires specialized assay techniques to evaluate the binding affinity of drug molecules to allosteric sites. HotSpot’s core mission is to develop novel technologies to address this challenge and to discover drugs by modulating protein function.

Geraldine Harriman stated, “We are delighted to collaborate with the Macroceutics team. Its leading DNA-encoded library (DEL) technology will provide HotSpot Therapeutics with rich protein molecular information, helping us accelerate the development of innovative drugs.”

Carson stated, “I am very proud to see Macroceutics’ DEL technology applied to the HotSpot drug discovery platform. We will grow together with HotSpot to develop novel allosteric drugs for patients worldwide.”

(Compiled by Xu Xiaoxue)