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US 8,025,865 B2Granted
CA IX-specific inhibitors
AssigneeInstitute of Virology of the Slovak Academy of Sciences
InventorsSilvia Pastorekova, Jaromir Pastorek
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AssigneeInstitute of Virology of the Slovak Academy of Sciences
InventorsSilvia Pastorekova, Jaromir Pastorek
Estimating the term…
Therapeutic methods for inhibiting the growth of preneoplastic/neoplastic vertebrate cells that abnormally express MN protein are disclosed. Screening assays are provided for identifying compounds, preferably organic compounds, preferably aromatic and heterocylic sulfonamides, which inhibit the enzymatic activity of MN/CA IX and that are useful for treating patients with preneoplastic/neoplastic disease. Further, the CA IX-specific inhibitors when labeled can also be used diagnostically/prognostically for preneoplastic/neoplastic disease, and for imaging use, for example, to detect hypoxic precancerous cells, tumors and/or metastases, by selectively binding to activated CA IX, preferably CA IX activated under hypoxic conditions, and not to inactive CA IX. Such detection of hypoxic conditions can be helpful in determining effective treatment options, and in predicting treatment outcome and the prognosis of disease development.
A method of selectively imaging activated MN/CA IX expressed in hypoxic tissues in a patient, comprising:
A diagnostic/prognostic method for a preneoplastic/neoplastic disease associated with abnormal MN/CA IX expression, comprising determining whether MN/CA IX is activated in a vertebrate sample, comprising:
A method that is diagnostic, or diagnostic and prognostic for precancer or cancer associated with overexpression of activated MN/CA IX comprising contacting a mammalian sample with a specific inhibitor of activated MN/CA IX, wherein said specific inhibitor of activated MN/CA IX is an MN/CA IX-specific antibody that specifically binds to the activated form of MN/CA IX's CA domain and does not bind the inactive form of MN/CA IX'S CA domain, said antibody conjugated to a label or a visualizing means, and detecting, or detecting and quantifying binding of said MN/CA IX-specific antibody to cells in said sample by detecting, or detecting and quantifying said label or said visualizing means on cells in said sample, wherein said detection, or said detection and quantitation at a level above that for a control sample is indicative of precancerous or cancerous cells that overexpress activated MN/CA IX in said sample.
Dependencies are inferred from the claim text.