BridGene Biosciences’ IMTAC ™ Small Molecule Discovery Platform Featured in Several Presentations at AACR-NCI-EORTC 2021 International Virtual Conference on Molecular Targets and Cancer Therapeutics


SAN JOSE, California, October 7, 2021 / PRNewswire / – BridGene Biosciences, Inc., a biotechnology company using unique chemoproteomic technology to discover and develop small molecules for high value and traditionally indestructible targets, today disclosed the research results of five presentations scientists at AACR-NCI-EORTC Virtual 2021 International Conference on Molecular Targets and Cancer Therapeutics. Presentations detail the company’s proprietary small molecule discovery platform, IMTACMT (Isobaric Mass Tagged Affinity Characterization) and its use in BridGene’s latest discovery of therapeutic candidates and the identification of new targets for approved small molecule drugs.

The conference starts today, October 7, 2021, and crosses 10 October 2021.

“We are delighted to have several poster presentations at this year’s AACR-NCI-EORTC illustrating how BridGene is bringing revolutionary capabilities to drug discovery and development,” said Ping Cao, Ph.D., co-founder and CEO of BridGene Biosciences. “This is one of the most important scientific gatherings devoted to drug discovery and molecular targets. Overall, our presentations describe our IMTAC platform technology and its capabilities, the discovery of novel small molecule inhibitors for non-drug targets, and the identification of previously unknown targets for approved targets. small molecule drugs. “

Full poster presentations are available on the AACR website at -therapeutics /. The highlights of the presentations are as follows:

Presentation: A chemoproteomics platform to identify small molecule modulators of protein-protein interactions, discover new cancer targets and reveal previously unknown targets for well-known drugs

  • IMTAC has the potential to redefine precision medicine, discover new drugs and targets, and identify new indications for known drugs.
  • Using the IMTAC platform, BridGene discovered small molecule ligands for several ‘hard to drug’ targets and oncogenic mutations, including GTPases (eg, RhoA), transcription factors (eg, TEAD), splicing factors (eg, SRSF1), epigenetic factors of modulators (eg, WDR5) and E3 ligases.
  • IMTAC’s proteome-wide profiling capability has enabled BridGene to reveal, for the first time, new targets for well-known drugs.
  • The combination of IMTAC screening and phenotypic screening has uncovered new / unknown targets that lead to certain phenotypic changes in the disease.

Presentation: Identification of previously unknown targets for approved small molecule drugs using the IMTAC â„¢ chemoproteomics platform

  • BridGene’s IMTACTM profiling is a powerful approach to generate comprehensive target maps for small molecule drugs, both covalent and non-covalent.
  • IMTACTM used on different cells leads to the identification of different sets of protein targets
  • Known target kinases and previously unknown non-kinase targets have been identified for ibrutinib and sunitinib using IMTACTM
  • A TEX264 non-kinase target of sunitinib has been identified by IMTACTM, creating a new opportunity for cancer treatments.

Presentation: Discovery and development of new covalent inhibitors of YAP-TEAD transcription activity

  • BridGene is developing covalent small molecule TEAD inhibitors to treat mesothelioma, glioblastoma, liposarcoma, pancreas and other types of cancer.
  • BridGene used the IMTAC platform to screen its unique covalent library against living cell proteomes and identified three distinct sets of results (MCS Tanimoto coefficients at ~ 0.3 between two sets) for TEAD proteins with nanomolar affinity and high proteomic selectivity.
  • New and potent multiple small molecule TEAD inhibitors have been obtained with good pharmacogability.
  • BridGene TEAD inhibitors 1) exhibited anti-proliferative properties against NF2-deficient mesothelioma cell lines (NCI-H226, NF2 – / -) with low IC50 nM; 2) demonstrated the potential to disrupt TEAD-YAP protein-protein interaction in cells in an ELISA assay, 3) showed single-digit nM power to disrupt TEAD downstream gene expression in reporter cells MCF7-TEAD1 luciferase.
  • With high potency and proteomic selectivity, BridGene believes that these TEAD inhibitors could work as single agent therapies or work in combination with other agents to treat multiple cancers.

Abstract title: Discovery of a covalent inhibitor for an oncogenic RhoA mutantY42C

  • Inhibition of the RhoA protein is believed to offer a promising approach for the treatment of diffuse gastric cancer (DGC) that harbors the CDH1 mutation / deletion. Cancer Genome Atlas (TCGA) study shows that around 1% of DGC patients harbor the oncogenic mutant RhoAY42C.
  • BridGene screened its proprietary covalent library against RhoAY42C in living cells by targeted IMTAC screening to detect covalent ligands of the RhoA mutantY42C.
  • Pilot screen successfully identified covalent RhoA ligandY42C, BGS1933. Mass spec analysis confirmed the covalent modification of Cys42 in RhoA by BGS1933.
  • BGS1933 shows inhibition of cell growth CCK-81, a cell line containing RhoAY42C mutation.
  • SAR is underway to further improve its potency and selectivity towards RhoA Y42C.
  • The discovery of a covalent RhoA inhibitorY42C could enable BridGene to validate the protein’s role in GDM and facilitate the development of novel first-class targeted therapies for the treatment of gastric cancer.

Presentation: Discovery of new small molecule inhibitors for a WDR5 epigenetic modulator

  • BridGene used the IMTAC platform to screen its unique covalent library against living cell proteomes and discovered small molecule ligands for WDR5. WDR5 is a widely expressed protein and an increasingly attractive therapeutic target for many types of cancer.
  • The preliminary characterization of the “hit” compound, BGS1989, showed that it interacts with WDR5 in a dose-dependent manner and that it has the capacity to inhibit the activity of MLL1 methyltransferase at low µM power.
  • After a cycle of chemical optimization, the researchers identified an improved inhibitor, BGS2597 with nM potency versus WDR5. Work is underway to determine which WDR5 functions are modulated by BGS2597 and to improve its activity and selectivity for WDR5.
  • The WDR5 inhibitor discovered using the IMTAC platform provides an excellent starting point for the development of new drugs targeting WDR5-dependent cancers.

About the AACR
The American Association for Cancer Research (AACR) is the first and largest cancer research organization dedicated to accelerating the conquest of cancer. Through its programs and services, the AACR promotes cancer research and related biomedical sciences; accelerates the dissemination of new research results among scientists and others dedicated to the conquest of cancer; promotes science education and training; and advances the understanding of the etiology, prevention, diagnosis and treatment of cancer worldwide.

About BridGene Biosciences
BridGene is a biotechnology company focused on the discovery and development of innovative small molecules that drug traditionally non-drug targets, offering new pathways to treat disease. Using its proprietary chemoproteomics platform, IMTAC â„¢, BridGene is able to screen small molecules against all proteins in living cells to discover drug candidates for high value, previously non-drug targets. To this end, BridGene takes advantage of its proprietary and diverse library of labeled, drug-like small molecules. The ultimate goal is to enable the revolutionary discovery of small molecule drugs and to expand disease treatment mechanisms, with targets previously inaccessible to small molecules. BridGene can perform IMTAC screening for covalent and non-covalent molecules and discover new targets for disease treatment by deconvoluting the results of the phenotypic screening, which sets the company apart from its peers. The company is developing a diverse pipeline of first-class drugs for targets in multiple disease areas. For more information, visit

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SOURCE BridGene Biosciences

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