Posted on Oct 7, 2013
Carmot wins National Cancer Institute SBIR Phase II award to discover anticancer drugs.
San Francisco, CA – October 7, 2013.
Carmot Therapeutics announced today that it has won an SBIR Phase II grant from The National Cancer Institute to discover small molecule inhibitors of the NF-κB signaling pathway. The award will support the continuation of research funded by a Phase I grant that Carmot has successfully completed.
During the Phase I research, Carmot applied its proprietary Chemotype Evolution technology to successfully advance large peptides into more potent and smaller inhibitors of NF-κB signaling. Specifically, these molecules disrupt the interaction between NEMO and IKK, which is required for phosphorylation of IκB and activation of NF-κB. The NF-κB signaling pathway creates an inflammatory microenvironment in cancer that facilitates tumor growth and metastasis. Importantly, mutations that enhance NF-κB activation are frequently found in human tumors and are particularly prevalent in lymphomas. During the Phase II research Carmot plans to advance NEMO/IKK inhibitors through in vivo proof of concept with the goal of identifying drug candidates for future clinical development.
The work will be conducted in collaboration with Prof. Adrian Whitty’s laboratory at Boston University, which also participated in the Phase I research. Dr. Whitty is an expert in protein-protein interactions and small molecule drug discovery. The Phase II research will also be supported by the laboratories of Professors Karen Allen and Sandor Vajda, providing expert capabilities in protein engineering, structural biology, and computational chemistry.
Targeting protein-protein interactions such as NEMO/IKK presents a significant untapped opportunity in therapeutic discovery. However, traditional drug discovery methods have shown limited success for this target class. Chemotype Evolution is an innovative approach and has already demonstrated the ability to rapidly identify more potent and less peptidic inhibitors of protein-protein interactions. Thus, Chemotype Evolution presents a unique opportunity to access important biological targets that have been refractory to traditional drug discovery approaches.
For more information about Carmot and Chemotype Evolution, see www.carmot.us