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BMP Signaling Inhibitors for the Treatment of Cancer

详细技术说明

BMP PathwayInvention Summary: Bone Morphogenetic Proteins (BMPs) are a group of signaling molecules that belongs to the Transforming Growth Factor-β (TGF-β) superfamily of proteins. BMP signaling is required for lung development and is not active in adult lungs. However, BMP signaling was found to be reactivated in lung cancer. For example, BMP-2 is overexpressed in virtually every lung cancer but not in normal lung tissue or benign lung tumors. Inhibitors of BMP signaling pathway could potentially be used to treat lung cancer and other cancers associated with BMP reactivation. This invention disclosed a set of small molecules as novel inhibitors of BMP signaling. These new compounds target BMP receptors and downregulate downstream anti-apoptotic proteins (XIAP, TAKl and Idl/ld3), which makes them particularly effective as potential anti-cancer agents. In vitro experiments showed that one compound induced significantly more cell death of lung cancer cells and is more stable than other BMP signaling inhibitors. Initial in vivo study with this compound has demonstrated tumor regression with no discernable toxic side effects.Market Applications: Small molecules as drug candidates for lung cancer.Small molecules as broad anti-cancer therapeutic agents, since aberrant BMP signaling is implicated in several cancers including lung, breast, prostate, pancreas, melanoma, and sarcomas. These molecules may possess utility for medical conditions where inhibition of BMP, XIAP, and TAK1 provides therapeutic benefit such as anemia and hyperossification syndrome.Advantage: Current small molecules targeting BMP receptors for anti-cancer treatment inhibit only one receptor type. The new inhibitor inhibits all BMP receptor classes, which is significantly more potent that other BMP inhibitors.Intellectual Property & Development Status: Pending application. Available for licensing or collaboration.

*Abstract

None

*Principal Investigation

Name: David Augeri, Director, Molecular Design & Synthesis, RTS

Department: Rutgers Translational Sciences

Name: John Langenfeld

Department:

Name: John Kerrigan, PART TIME LECTURER

Department:

国家/地区

美国