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Protein Chemistry Biotech Gains Collaboration, Venture Funds

DNA molecule model

(Christian Guthier, Flickr.

4 Jan. 2023. An enterprise discovering new drugs with optical light-based protein chemistry is emerging from stealth, including work with biopharmaceutical company Genentech. Belharra Therapeutics Inc. in San Mateo and San Diego, California, is also raising $50 million in its first venture funding round, to go with an initial payment of $80 million from Genentech, a division of global drug maker Roche.

Belharra Therapeutics seeks to find new treatments for diseases considered difficult to address with most small-molecule drugs, from the lack of well-defined targets in proteins responsible for the conditions. To confront this problem, the company applies activity-based processes in protein chemistry called chemoproteomics that reveal ligands, or connective molecules in proteins, as well as binding pockets usually hidden, but now more open for targeting.

Belharra says those processes use photoaffinity labeling, optical techniques where chemical components in proteins respond to light-activated probes, in this case the ligands or binding sites that are otherwise missed. The company says since starting up in 2021, it compiled a library of of these photoaffinity probes that explore interactions between proteins and ligands in their native cellular environments. Belharra says it also applies computational techniques for analyzing these interactions to identify new accessible drug targets across a range of proteins, cells, and mechanisms.

“We’ve expanded the power of traditional chemoproteomic screening approaches,” says Belharra CEO Jeff Jonker in a company statement, “and integrated them into a single drug discovery engine that enables, for the first time, the ability to target the full range of protein classes and targets.”

Candidates for cancer, autoimmune, and neurodegenerative disorders

The company’s technology is based on research by its scientific founders in labs at Scripps Research and Broad Institute, a genetics research center affiliated with Harvard University and MIT. Christopher Parker and Benjamin Cravatt are professors of chemistry at Scripps Research, studying respectively protein interactions with cells and activity-based analytics of enzymes related to disease. Joining Parker and Cravatt as Belharra Therapeutics founders are Scripps immunologist and microbiologist John Teijaro who studies infectious diseases and autoimmune mechanisms, and Broad Institute chemical and cell biologist Stuart Schreiber who studies signaling proteins for developing therapeutics.

Genentech, in San Francisco, is partnering with Belharra Therapeutics on discovery of treatment candidates for a wide range of targets covering cancer, immunotherapies for cancer, autoimmune disorders, and neurodegenerative diseases. Under the multi-year deal, Genentech is providing a series of targets for Belharra to discover new small molecules, and carry out early preclinical research. Genentech is then responsible for further preclinical and clinical development, as well as regulatory and commercialization stages.

Belharra Therapeutics is receiving an upfront payment of $80 million, and is eligible for development, commercial, and sales milestones that could exceed $2 billion if all terms of the agreement are met. For some cancer and immunology targets, Belharra has an option to develop new small molecules through early clinical trials, with the companies dividing costs and profits, as well as geographic divisions of milestone payments and royalties.

“Our collaboration with Belharra,” says James Sabry, head of pharma partnering at Roche in a Belharra statement, “gives Genentech access to a drug invention platform that allows us to interrogate important therapeutic pathways and targets that we strongly believe drive disease pathogenesis, but have proven to be inaccessible to conventional approaches.”

Belharra Therapeutics was formed in 2021 by life science investor Versant Ventures, and incubated in Versant’s Inception Discovery program that starts new biotechnology companies based on research in academic labs. Versant is staking Belharra to $50 million in its first venture round.

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