Design products to G12D and G12V

We develop small molecule modulators, targeted to two mutant forms of KRAS. If you are interested to collaborate with us, obtain funding, and develop new treatments, contact us. Here is a remainder about the importance of these mutants...

Cancer drug discovery is a complex and dynamic field that involves the identification and development of drugs specifically designed to target and treat cancer. One of the crucial steps in this process is understanding the genetic alterations that drive cancer development and progression. Mutations in genes called oncogenes, such as KRAS, play a significant role in many types of cancer.

KRAS is one of the most frequently mutated oncogenes, and mutations in the KRAS gene are particularly common in several cancer types, including lung, pancreatic, and colorectal cancers. Two prevalent KRAS mutations are the KRAS G12V and G12D mutations. These mutations involve a single amino acid change (glycine to valine in G12V a nd glycine to aspartic acid in G12D) within the KRAS protein.

Targeting the KRAS G12V and G12D mutations is of great interest in cancer drug discovery for several reasons:

  • Prevalence: KRAS mutations, including G12V and G12D, are found in a significant proportion of cancer patients, making them attractive targets for therapeutic interventions. The frequency of KRAS mutations underscores the potential impact of developing drugs that specifically inhibit these mutations.
  • Oncogenicity: The G12V and G12D mutations in KRAS are known to confer increased oncogenic potential, leading to uncontrolled cell growth, proliferation, and survival. Consequently, targeting these specific mutations could disrupt the signaling pathways that drive cancer development, leading to improved treatment outcomes. Lack of effective therapies: Despite the importance of KRAS mutations in cancer, developing effective drugs that directly target KRAS has been challenging. Traditional approaches to targeting proteins with small molecules have not been successful in inhibiting KRAS mutations. However, recent advancements have shown promise in developing targeted therapies against KRAS G12V and G12D mutations, making it an active area of research.
  • Therapeutic opportunities: The identification of specific vulnerabilities associated with KRAS G12V and G12D mutations opens up new therapeutic opportunities. Scientists are exploring various strategies, such as inhibiting KRAS downstream effectors or exploiting synthetic lethal interactions, to develop drugs that can selectively target cancer cells harboring these mutations while sparing normal cells.

The development of targeted therapies against KRAS mutations, including G12V and G12D, is an ongoing area of research and holds great potential for improving cancer treatment outcomes. Scientists and pharmaceutical companies are investing significant efforts in unraveling the complex biology of KRAS mutations and designing innovat ive therapeutic approaches to address the challenges associated with targeting these mutations.