Carmot Therapeutics

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.



For more information about Chemotype Evolution, click here.

Contact information: info@carmot.us

San Francisco, CA – July 11, 2011

Carmot Therapeutics announced today that it has won an SBIR grant from The National Institute of Diabetes and Digestive and Kidney Diseases to discover molecules that selectively inhibit some lipid binding proteins without interfering with other closely related proteins. These studies could lead to new drugs for the treatment of obesity and other metabolic disorders.

The award will fund the application of Carmot’s proprietary Chemotype Evolution technology to discover small molecule inhibitors of fatty acid binding proteins (FABPs), which are important in lipid metabolism and energy storage. Chemotype Evolution is a powerful drug discovery technology that rapidly identifies new lead-like molecules (www.carmot.us). Compared to conventional high-throughput screening, Chemotype Evolution can sample a greater variety of molecular possibilities using much smaller, higher quality chemical libraries.

Specifically, the project will seek small molecules that inhibit FABP4 and FABP5 but do not inhibit other members of the class of FABPs. Animals in which either FABP4 or FABP5 have been genetically knocked out show improvements in a variety of metabolic functions, and when both proteins are eliminated the animals are remarkably resistant to obesity and type 2 diabetes. However, knocking out other members of this family of lipid binding proteins is harmful. Thus, developing selective molecules is essential.

Targeting some members of a protein family without hitting others is a difficult task using traditional methods. Chemotype Evolution is an iterative, innovative approach that is ideally suited for discovering selective next-generation therapeutics.