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ID: ALA1140981

Journal: Bioorg Med Chem

Title: Substrate optimization for monitoring cathepsin C activity in live cells.

Authors: Li J, Petrassi HM, Tumanut C, Masick BT, Trussell C, Harris JL.

Abstract: A series of peptidic fluorogenic substrates were synthesized to develop a flow cytometry assay (FACS) to monitor the proteolytic activity of cathepsin C in live cells. Of the 16 substrates tested, (NH(2)-aminobutyric-homophenylalanine)(2)-rhodamine demonstrated the best reactivity and selectivity profile in the FACS assay using the B721 human B-lymphoblastoid cell line. The resulting FACS assay was validated through correlation of the IC(50) values with a competitive radiolabeling assay against a series of small molecule inhibitors of cathepsin C.

CiteXplore: 18313933

DOI: 10.1016/j.bmc.2008.02.002