San Diego State University Research Foundation

Roland Wolkowicz

Provided are compositions, e.g., multiplexed platforms or systems, to screen for molecules, e.g., small molecule active agents such as drugs, that inhibit enzymes such as proteases. Provided are cell-based or multiplexed platforms for monitoring or assay the activity of a protease. Provided are cell-based assays and multiplexed systems for the monitoring of enzyme, activity such as proteolytic cleavage on the cell surface, where optionally the protein, e.g., an enzyme, can be naturally expressed on the cell surface or engineered to be expressed on the cell's surface. Provided are cells and stable cell lines expressing an 'assay construct' and an enzyme of interest, where optionally one cell or cell line expresses both the 'assay construct' and the enzyme, or two different cells or independent cell lines are used and mixed in the assay, where one expresses the &#x201c;assay construct&#x201d; with the enzyme substrate and the second expressing the enzyme.

Compositions and methods for identifying protease inhibitors

The invention is directed to compositions, e.g., cell-based and multiplexed platforms, to screen for small molecule drugs that inhibit enzymes such as proteases, e.g., viral proteases, e.g., HIV proteases; and methods for making and using these compositions. The invention provides compositions and methods for identifying compositions, e.g., drug molecules, that can inhibit proteases, e.g., viral proteases such as HIV proteases. In alternative embodiments, the invention provides cell-based platforms or assays to screen for compositions, e.g., small molecules or drugs, that inhibit or modify the activity of enzymes such as calcium-dependent protein convertases involved in HIV envelope protein processing, including cleavage of the HIV gp160 envelope precursor, resulting in gp120 and gp41 envelope products. In one embodiment, the invention provides a cell-based or multiplexed platform for monitoring the activity of enzymes, e.g., proteases such as viral proteases.

Compositions and cell-based methods for monitoring the activity of a Dengue Virus protease

Compositions and methods for identifying enzyme and transport protein inhibitors

The invention is directed to compositions to screen for small molecule drugs that inhibit proteases, such as viral proteases, e.g., HIV proteases; and methods for making and using these compositions. The invention provides compositions and methods for identifying compositions, e.g., drug molecules, that can inhibit proteases, e.g., HIV proteases. In alternative embodiments, the invention provides cell-based assays to screen for compositions, e.g., small molecules or drugs, that inhibit or modify the activity of enzymes such as calcium-dependent protein convertases involved in HIV envelop protein processing, including cleavage of the HIV gp160 envelope precursor, resulting in gp120 and gp41 envelope products.

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San Diego, CA, United States of America

Roland Wolkowicz