Recently, Viva Biotech contributed to an innovative research project published in the Journal of Medicinal Chemistry. The study, titled "Discovery of TNG462: A Highly Potent and Selective MTA-Cooperative PRMT5 Inhibitor to Target Cancers with MTAP Deletion", detailed the evaluation of TNG462, a next-generation PRMT5 inhibitor. Viva Biotech leveraged its world-leading protein production and structural biology platform to provide strong technical support for this structure-based drug discovery effort.
(Image Source: ACS Publications website)
The gene encoding MTAP is one of the most commonly deleted genes in cancer, occurring in approximately 10–15% of all human cancers. The research team has previously described the discovery of TNG908, a brain-penetrant clinical-stage compound that selectively targets MTAP-deleted cancer cells by binding to and inhibiting PRMT5 cooperatively with MTA, which is present in elevated concentrations in MTAP-deleted cells. In this research, the discovery of TNG462 shows a more potent and selective MTA-cooperative PRMT5 inhibitor with improved DMPK properties, currently in Phase I/II clinical trials for MTAP-deleted cancers .
In this study, Viva Biotech's structural biology team played a critical role by leveraging its diversified recombinant protein expression platforms, including E. coli, yeast, insect cells, and mammalian cell systems, and its world-leading structure determination capabilities, such as X-ray crystallography and structure analysis platforms. The team successfully resolved several high-resolution crystal structures of PRMT5/MEP50/MTA in complex with the candidate small molecules, with the best resolution reaching 2.47 Å. These high-quality structural data have provided crucial insights for rational drug design, significantly enhancing the compounds' binding affinity, selectivity, and metabolic stability. This achievement contributes valuable insights to the field of structural biology, but also highlights Viva Biotech’s outstanding capabilities in structural biology and structure-based drug discovery.
(Source: ACS Publications website)
A world-leading protein structure research platform
Since its founding in 2008, Viva Biotech has been deeply committed to advancing the frontiers of protein structure research, continuously raising technological standards and refining platform capabilities. Over the past 16 years, the company has successfully tackled numerouschallenges in protein structure determination, earning the trust of global partners through its profound understanding of client needs and expert scientific judgment. As of December 31, 2024, Viva Biotech has delivered over 82,716 high-quality protein structures to clients worldwide, with approximately 17,681 newly delivered in 2024. In the field of drug target research, the company has studied more than 2,098 distinct drug targets, including 112 new targets added in 2024, positioning Viva Biotech at the forefront of global protein structure analysis.
To learn more about our protein expression and structural biology platforms, please visit https://www.vivabiotech.com or contact our expert team atinfo@vivabiotech.com.
For more information, please refer to the full paper: Cottrell, Kevin M., et al. “Discovery of TNG462: A Highly Potent and Selective MTA-Cooperative PRMT5 Inhibitor to Target Cancers with MTAP Deletion.” Journal of Medicinal Chemistry, 4 Mar. 2025, https://doi.org/10.1021/acs.jmedchem.4c03067. Accessed 12 Mar. 2025.
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