Clickable, selective, and cell-permeable activity-based probe of human cathepsin B - Minimalistic approach for enhanced selectivity.

Autor: Bhuiyan AI; Queens College of The City University of New York, Chemistry and Biochemistry Department, 65-30 Kissena Blvd, Flushing, NY 11367, USA; Chemistry Doctoral Program, The Graduate Center of The City University of New York, 365 5th Ave, New York, NY 10016, USA., Rathod P; Laguardia Community College, 31-10 Thomson Ave, Long Island City, NY 11101, USA., Ghoshal S; Department of Biological Sc. and Geology, QCC-CUNY, Bayside, NY, USA., Dana D; Queens College of The City University of New York, Chemistry and Biochemistry Department, 65-30 Kissena Blvd, Flushing, NY 11367, USA., Das T; Queens College of The City University of New York, Chemistry and Biochemistry Department, 65-30 Kissena Blvd, Flushing, NY 11367, USA., Li G; Queens College of The City University of New York, Chemistry and Biochemistry Department, 65-30 Kissena Blvd, Flushing, NY 11367, USA., Dickson AA; Queens College of The City University of New York, Chemistry and Biochemistry Department, 65-30 Kissena Blvd, Flushing, NY 11367, USA., Rafi F; Bard High School Early College Queens, 30-20 Thomson Avenue, Long Island City, NY 11101, USA., Subramaniam GS; Queens College of The City University of New York, Chemistry and Biochemistry Department, 65-30 Kissena Blvd, Flushing, NY 11367, USA., Fath KR; Queens College of The City University of New York, Department of Biology, 65-30 Kissena Blvd, Flushing, NY 11367, USA; Biochemistry Doctoral Program, The Graduate Center of The City University of New York, 365 5th Ave, New York, NY 10016, USA., Paroly S; Bard High School Early College Queens, 30-20 Thomson Avenue, Long Island City, NY 11101, USA., Chang EJ; Biochemistry Doctoral Program, The Graduate Center of The City University of New York, 365 5th Ave, New York, NY 10016, USA; York College of the City University of New York, Department of Chemistry, 94-20 Guy R. Brewer Blvd, Jamaica, NY 11451, USA; Chemistry Doctoral Program, The Graduate Center of The City University of New York, 365 5th Ave, New York, NY 10016, USA., Pathak SK; Queens College of The City University of New York, Chemistry and Biochemistry Department, 65-30 Kissena Blvd, Flushing, NY 11367, USA; Biochemistry Doctoral Program, The Graduate Center of The City University of New York, 365 5th Ave, New York, NY 10016, USA; Chemistry Doctoral Program, The Graduate Center of The City University of New York, 365 5th Ave, New York, NY 10016, USA. Electronic address: Sanjai.Kumar@qc.cuny.edu.
Jazyk: angličtina
Zdroj: Bioorganic chemistry [Bioorg Chem] 2021 Dec; Vol. 117, pp. 105463. Date of Electronic Publication: 2021 Nov 02.
DOI: 10.1016/j.bioorg.2021.105463
Abstrakt: Human cathepsin B is a cysteine-dependent protease whose roles in both normal and diseased cellular states remain yet to be fully delineated. This is primarily due to overlapping substrate specificities and lack of unambiguously annotated physiological functions. In this work, a selective, cell-permeable, clickable and tagless small molecule cathepsin B probe, KDA-1, is developed and kinetically characterized. KDA-1 selectively targets active site Cys25 residue of cathepsin B for labeling and can detect active cellular cathepsin B in proteomes derived from live human MDA-MB-231 breast cancer cells and HEK293 cells. It is anticipated that KDA-1 probe will find suitable applications in functional proteomics involving human cathepsin B enzyme.
(Copyright © 2021 Elsevier Inc. All rights reserved.)
Databáze: MEDLINE
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