Development of a highly potent, selective, and cell-active Inhibitor of cysteine cathepsin L–A hybrid design approach

Dibyendu Dana; Shatarupa De; Pratikkumar Rathod; Anibal R. Davalos; Daniel A. Novoa; Suneeta Paroly; Viviana M. Torres; Nisar Afzal; Ravi S. Lankalapalli; Susan A. Rotenberg; Emmanuel J. Chang; Gopal Subramaniam; Sanjai Kumar

doi:10.1039/C4CC04037F

Development of a highly potent, selective, and cell-active Inhibitor of cysteine cathepsin L–A hybrid design approach†

Dibyendu Dana,^a Shatarupa De,‡^a Pratikkumar Rathod,‡^ab Anibal R. Davalos,^a Daniel A. Novoa,^a Suneeta Paroly,^c Viviana M. Torres,^a Nisar Afzal,^a Ravi S. Lankalapalli,§^a Susan A. Rotenberg,^a Emmanuel J. Chang,^b Gopal Subramaniam^a and Sanjai Kumar*^a

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^a Department of Chemistry and Biochemistry, Queens College and the Graduate Center of the City University of New York, Queens, New York 11367-1597, USA
E-mail: Sanjai.Kumar@qc.cuny.edu
Fax: +1 718 997 5531
Tel: +1 718 997 4120

^b Department of Chemistry, York College of the City University of New York, Jamaica, New York, USA

^c Bard High School Early College Queens, 30-20 Thomson Avenue, Long Island City, New York, USA

Abstract

A hybrid-design approach is undertaken to develop a highly potent and selective inhibitor of human cathepsin L. Studies involving human breast carcinoma MDA-MB-231 cells establish that this inhibitor can successfully block intracellular cathepsin L activity, and retard the cell-migratory potential of these highly metastatic cells.

Chemical Communications

Development of a highly potent, selective, and cell-active Inhibitor of cysteine cathepsin L–A hybrid design approach†

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Development of a highly potent, selective, and cell-active Inhibitor of cysteine cathepsin L–A hybrid design approach

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