Posted on Dec 8, 2011
Carmot Therapeutics wins NSF SBIR Phase II award to discover novel anticancer leads and further develop its proprietary technology, Chemotype Evolution.
San Francisco, CA – December 8, 2011.
Carmot Therapeutics announced today that it has been awarded a Phase II Small Business Innovation Research (SBIR) award from the National Science Foundation (NSF) to use its proprietary technology for discovering drugs that fight cancer. Carmot’s technology platform, Chemotype Evolution, is a powerful alternative to current lead-finding approaches and addresses unmet chemical needs in therapeutic discovery. One of the strengths of Chemotype Evolution is that it can convert peptides into smaller molecules with drug-like properties through a unique iterative screening paradigm.
This competitive award recognizes achievements made during Phase I and will be used to further develop and apply Carmot’s Chemotype Evolution toward an important anti-cancer target. The protein p53 blocks damaged cells from dividing; it is mutated to an inactive form in over half of human cancers. Cancer cells can also circumvent p53 by over-expressing the hdm2 protein. Hdm2 binds to p53, inhibiting its function and targeting it for degradation. Thus, molecules that block the p53-hdm2 interaction have the potential to inhibit tumor growth and may also serve to sensitize cancer cells to chemotherapy.
There has been a tremendous amount of effort in the pharmaceutical industry to identify small-molecule drugs that block the interaction between p53 and hdm2, but these have had only limited success. Peptide inhibitors of the p53-hdm2 interaction have been reported, but peptides are rapidly degraded within the body and their low cell permeability limits their utility as drugs. Carmot is using Chemotype Evolution to transform peptide inhibitors into small molecule equivalents with similar binding properties but more promise for drug development.