Small Molecules for Cancer Therapy that Reduce the Expression of Transcription Factors KLF5 and EGR-1

Background

Colorectal cancer (CRC) represents a substantial health challenge, being the third most commonly diagnosed cancer and the third leading cause of cancer-related death in the US. Current treatment strategies are frequently employed, but they face significant drawbacks, including the production of multiple side effects and frequent ineffectiveness due to specific mutations acquired during cancer progression. While the development and progression of CRC are known to stem from impairments in critical signaling pathways, specifically targeting these pathways remains a major hurdle, as no compounds acting in this manner have successfully advanced into or through clinical trials.

Technology

Researchers at Stony Brook University and the University of Florida developed a small molecule lead that inhibits the growth of colorectal cancer cells. This compound functions by reducing the expression levels of Krüppel-like factor 5 (KLF5) and EGR1, which are involved in cancer development and progression. The novel small molecule is suitable for reducing KLF5 expression in living cells and for treating tumors in mammals that are comprised of KLF5-expressing cancer cells, specifically targeting colorectal cancer in human patients.