Small molecule antagonists of dusp5 and methods of use
AssigneesThe Medical College of Wisconsin, Inc., Marquette University, Concordia University
InventorsRamani Ramchandran, Daniel Sem, Rajendra Rathore
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Abstract
The present invention is directed to compounds that specifically target DUSP5 and act as antagonists of that enzyme. Such compounds are useful in the treatment of various conditions including, but not limited to vascular anomalies, cancer, and macular degeneration.
Claims12
A pharmaceutical composition comprising a compound, or a pharmaceutically acceptable salt, solvate, or hydrate thereof, and a pharmaceutically acceptable carrier, wherein the compound comprises two negatively charged sulfonate groups or bioisosteric sulfonate analog groups tethered by a core scaffold of biphenyl or a planar analog of biphenyl, and wherein the core scaffold separates the negatively charged groups at a distance of about 6 to about 8 Angstroms.
A method of screening a compound for effectiveness as an antagonist of DUSP5, the method comprising:
- a) exposing a sample comprising a DUSP5 polypeptide to a compound, and b) determining if DUSP5 phosphatase activity in said sample is decreased in comparison to a control sample lacking the compound.
Use of a DUSP5 inhibitor for treating, preventing, or alleviating vascular anomalies.
Use of a DUSP5 inhibitor for the preparation of a medicament for treating, preventing, or alleviating vascular anomalies.
Dependencies are inferred from the claim text.