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Leptin Peptide Antagonists for cancer, endometriosis, preeclampsia and fertility regulation

Organization:Boston Biomedical Research Institute, MA, US
I.P. Brief:LPAs represent for the first time that a therapeutic agent is being developed to specifically target leptin signaling. LPAs might be useful as novel drugs for breast and other cancer types, inflammatory diseases (i.e. endometriosis and arthritis), preclampsia and diabetes.
Summary of I.P.:Based upon structural analysis of leptin binding sites and a homology-based model of the leptin/leptin receptor (Ob-R) we have produced leptin peptide antagonists (LPAs) derived from leptin binding regions. LPAs are able to bind to Ob-R without transmitting an internal signal to the cells. LPAs at very low concentrations specifically negate the leptin-induced increase of adhesion, proliferation, migration and invasion of malignant mammary and endometrial cells in vitro and in vivo in mouse models. LPAs are potent inhibitors of angiogenesis and dramatically reduce the size of mammary tumors and metastasis in mice. LPAs significantly reduce the establishment of human derived endometriotic lesions in mice. LPAs are non-toxic compounds able to inhibit embryo implantation.
Patent:Patent pending
Keywords:Inflammatory disease, endometriosis, breast cancer
Primary Industry:Pharma & Biotech
Specific Market:Endometriosis, Oncology
Market Size:Commercial parnter needed to quantify various indications available.
State of the Art:There are a variety of strategies available, but one must see the animal data from LPA\'s to see the difference.
Figures of Merit:Stunning mouse data available for review.
Tech.  Obstacles:None in our lab at this time
Market Obstacles:Need to validate in larger animal models.
Publications:Gonzalez, R. R., Leavis, P. C. (2003) A peptide derived from the human leptin molecule is a potent inhibitor of the leptin receptor function in rabbit endometrial cells. Endocrine 21(2), 185-95. Ramos, M. P., Rueda, B. R., Leavis, P. C. & R. R. Gonzalez. Leptin serves as an upstream activator of an obligatory signaling cascade in the embryo-implantation process. Endocrinology. In press.
Research Team:Ruben Gonzalez, Paul Leavis


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