Structure-Based Design and Synthesis of Potent and Selective KRAS G12D Inhibitors

The KRAS G12D mutation subtype is present in over 40% of pancreatic ductal adenocarcinomas (PDAC), making this an important drug target.  WuXi AppTec scientists recently contributed to a research article in ACS Med. Chem. Letters describing the optimization of a series of potent and selective KRAS G12D inhibitors through a structure-based drug design approach.  The authors identify a lead compound, ERAS-5024, which demonstrates potent in vitro antiproliferative activities in a panel of cell lines harboring the G12D mutation and exhibits robust in vivo efficacy with regression activity in a PDAC-CDX model.

Check out our extensive panel of RAS-related assays and services by clicking HERE.



View Now
← Return to Resources

Related Content

Fragment-based drug discovery (FBDD) is one of the most well-developed approaches for projects starting from small, low-affinity compounds.  At the...


At the Covalent Drug Discovery 2023 Summit and Fragments 2024 Conference, we presented a case study on Bruton’s tyrosine kinase (BTK)...

← View all Hit-to-Lead Resources
× peptide, amino acid

Contact An Expert Today!