On January 4, 2023 Belharra Therapeutics, reported that it has emerged from stealth mode with a novel photoaffinity-based chemoproteomics platform capable of identifying non-covalent, small molecule drug candidates for any protein (Press release, Belharra Therapeutics, JAN 4, 2023, View Source [SID1234625854]). The company has secured $130 million in capital, including $50 million in Series A financing from founding investor Versant Ventures and a multi-year collaboration with Genentech, a member of the Roche Group, that will provide $80 million in upfront capital, also announced today. Belharra is the most recent company to emerge from Versant’s Inception Discovery Engine.
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Belharra’s integrated chemoproteomic-based drug discovery engine addresses the limitations of traditional screening approaches through a proprietary library of photoaffinity-based chemical probes that explore protein-ligand interactions in the native environment of the cell. The platform utilizes photoaffinity-based labeling to "trap" these unique non-covalent protein-ligand interactions. Coupled with its novel chemoproteomics platform and informatics capabilities, Belharra’s platform identifies probe-protein interactions on a global scale, revealing novel druggable pockets across a complete range of mechanisms, protein classes and cell types.
While first-generation platforms demonstrated the power of chemoproteomics to illuminate new chemical space, they required specific nucleophilic amino acid residues, such as cysteine, be present on a protein of interest and used probe libraries composed exclusively of electrophilic drug fragments. These are limiting because only a fraction of drug targets have ligandable cysteines and irreversible ligands often have complex development paths. The Belharra photoaffinity platform is not reliant on any specific amino acid for labeling, enabling profiling of the entire proteome. By employing photochemistry to identify probe-protein interactions, the Belharra platform’s underlying mode of binding is non-covalent, providing a much more traditional development path for a drug candidate.
Next-generation chemoproteomics platform
Belharra’s uniquely differentiated platform builds on a legacy of chemoproteomic-based drug discovery to identify functional and actionable non-covalent, small molecule drug candidates for any binding site, on any protein, in any conformational state, in any cell type. The platform enables screens to be run in a whole cell context, which enables the small molecule library to interact with proteins in their native conformations, including protein complexes, which are virtually impossible to recapitulate in traditional biochemical screens. This creates the potential to identify next-generation therapeutics for previously difficult-to-treat conditions.
"We’ve expanded the power of traditional chemoproteomic screening approaches 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," said Jeff Jonker, CEO of Belharra. "Our platform enables us to rapidly rescreen all of the previously ‘undruggable’ protein targets to identify actionable non-covalent drug-like ligands for functional binding pockets."
The Belharra platform originated in the laboratories of Christopher G. Parker, Ph.D., John Teijaro, Ph.D., and Ben Cravatt, Ph.D., at Scripps Research. There, Drs. Parker and Cravatt developed a novel photoaffinity-based chemoproteomics technology to enable screening for small molecules that bind proteins in their native context and focused it on immunology targets leveraging the expertise of Dr. Teijaro. Stuart Schreiber of the Broad Institute joined as a co-founder to refine and industrialize the platform for broad therapeutic application.
During Belharra’s formative stage, the team at Scripps worked alongside Belharra’s scientists and scientists at Versant’s San Diego-based discovery engine, Inception Therapeutics, to industrialize the technology and build a proprietary library of small molecule photoaffinity probes with superior drug-like properties. Based on targeted and phenotypic screens run by Scripps and Belharra, Belharra expects to advance internal discovery candidates for both Oncology and Immunology indications in 2023.
"Having been involved in a number of important companies in the chemical proteomics field, we have high conviction that Belharra represents a new wave of innovation in the space," said Tom Woiwode, Ph.D., Managing Director at Versant and a Belharra board member. "We are very excited to be working with Jeff, Gary and the company’s world-class scientific founders to advance medicines for previously intractable targets and diseases."