A targeted library of small molecules has been prepared to optimize the biological activity of BN82002, our initial lead compound, recently described as an original inhibitor of CDC25 phosphatases. Some of these compounds inhibit CDC25 in the micromolar range and therefore reinforce the interest of CDC25 as an anticancer target.
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Department of Pharmacology and Toxicology, Heersink School of Medicine, University of Alabama at Birmingham, Birmingham, AL 35294, USA.
Cell division cycle 25B (CDC25B) belongs to the CDC25 family of phosphatases that regulate cell cycle progression. CDC25B also contributes to tumor initiation and progression, but no connection between CDC25B levels and drug sensitivity in pancreatic cancer has been reported. Based on our finding that bromodomain and extraterminal domain (BET) inhibitors decrease levels of CDC25B, we aim to compare the sensitivity of models expressing contrasting levels of CDC25B to the BET inhibitor JQ1, in pancreatic cancer cell lines and in patient-derived xenograft (PDX) models of pancreatic ductal adenocarcinoma (PDAC) .
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Article Synopsis
- Triple-negative breast cancer (TNBC) is difficult to treat due to its aggressive nature and limited effective therapies, prompting the need for new treatments.
- The study developed dual inhibitors targeting CDC25 and HDACs by combining specific molecular structures, showing that one compound, 18A, was particularly effective against TNBC cells while sparing non-cancerous cells.
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