BridGene Biosciences Announces Acceptance of Two Abstracts for Poster Presentations at Cambridge Health Institute's Inaugural Drug Discovery Chemistry Conference

SAN JOSE, Calif., April 14, 2022 /PRNewswire/ -- BridGene Biosciences, Inc., a biotechnology company using a unique chemoproteomic technology to discover and develop small molecules for high value, traditionally undruggable targets, today announced that two abstracts have been accepted for poster presentation during the Cambridge Health Institute's Inaugural Drug Discovery Chemistry Conference taking place April 18-21, 2022 in San Diego, California. The posters highlight the use of the Company's proprietary IMTAC™ (Isobaric Mass-Tagged Affinity Characterization) platform in small molecule drug discovery addressing "hard-to-drug" targets and research into the identification of small molecule inhibitors of Zeta Chain of T-Cell Receptor Associated Protein Kinase 70 (ZAP70).

"We are very pleased to have the opportunity to share with colleagues and fellow researchers our new developments highlighting IMTAC, our proprietary chemoproteomic platform, in two poster presentations at the Drug Discovery Chemistry Conference," stated Ping Cao, Ph.D., Co-Founder and CEO of BridGene Biosciences. "Our work at BridGene has the potential to address multiple therapeutic areas. Overall, the posters describe our IMTAC platform and its capabilities, the discovery of novel small molecule inhibitors, and the identification of previously unknown targets for approved small molecule drugs. These include small molecule inhibitors of the ZAP70 protein, an attractive therapeutic target with implications in the treatment of autoimmune diseases and some hard-to-treat forms of leukemia where patients face poor survival rates. We look forward to further demonstrating the potential of BridGene's technology."

The abstracts are as follows:

Title: IMTAC – A Next-generation Chemoproteomic Platform to Discover Small Molecule Therapies for Hard to Drug Targets

Authors: Cindy Huang, Ph.D.; Vivian Zhang, Ph.D.; Ning Deng, Ph.D.; Henry Johnson, Ph.D.; Ping Cao, Ph.D.; and Wolf. R. Wiedemeyer, Ph.D.

• IMTAC has the potential to redefine the traditional small molecule screening process, discover new drugs for previously undruggable targets, and identify new indications of known drugs.
• The platform was developed to discover small molecule medicines for hard-to-drug targets including transcription factors, splicing factors, scaffolding proteins, and E3 ligases.
• IMTAC uses a proprietary drug-like small molecule library coupled with proteome-wide or target-focused live cell screening to discover hits that can selectively bind in transient or shallow binding pockets exclusively presented in a cellular setting.
• Additionally, leveraging the platform's proteome-wide profiling capability combined with phenotypic screening can reveal unknown targets for previously characterized ligands and drugs.

Title: Identification of Selective Covalent Small Molecule Inhibitors of ZAP70

Authors: Ning Deng, Ph.D.; Steve Luo, Ph.D.; Shirley Guo, Ph.D.; Henry Johnson, Ph.D.; Ping Cao, Ph.D.; and Wolf. R. Wiedemeyer, Ph.D.

• Mutations and aberrant expression of ZAP70 are associated with severe immunodeficiency and some B-cell malignancies, making it an attractive therapeutic target in T-cell-mediated autoimmune disease (rheumatoid arthritis) and defined subgroups of ZAP70-positive B-cell leukemias.
• Novel approaches are needed to identify selective ZAP70 inhibitors. Previous attempts to develop highly selective small-molecule ZAP70 inhibitors have failed, likely due to specific structural attributes of its kinase catalytic domain, and its similarity to a closely related family member, SYK. The clinical development of a dual ZAP70/SYK inhibitor was terminated early due to an increased risk of infection.
• Using BridGene's IMTAC technology, researchers identified BGS1949 as a specific hit against ZAP70 in the target-focused screening. The covalent modification site was revealed by mass spectrometry, and in vitro kinase assays demonstrated inhibition of ZAP70 by BGS1949 with high selectivity over SYK kinase.
• Structure activity relationship (SAR)-guided optimization of BGS1949 is now underway to further improve potency and selectivity.

About BridGene Biosciences

BridGene is a biotechnology company focused on discovering and developing innovative small molecules that drug traditionally undruggable targets, providing new paths to treat diseases. By using its proprietary chemoproteomic platform, IMTAC™, BridGene is able to screen small molecules against all proteins in live cells to discover drug candidates for high value and previously undruggable targets. For this purpose, BridGene takes advantage of its proprietary, diverse library of tagged, drug-like small molecules. The ultimate goal is to enable breakthrough small molecule drug discovery and to expand the mechanisms to treat diseases, with targets previously inaccessible to small molecules. BridGene can perform IMTAC™ screening for both covalent and non-covalent molecules and discover new targets for disease treatments by deconvoluting phenotypic screening hits, setting the company apart from its peers. The company is advancing a diversified pipeline of first-in-class drugs for targets in multiple disease areas. For more information, visit http://bridgenebio.com/.

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SOURCE BridGene Biosciences