A review of small molecule inhibitors and functional probes of human cathepsin L

D Dana, SK Pathak - Molecules, 2020 - mdpi.com
Human cathepsin L belongs to the cathepsin family of proteolytic enzymes with primarily an
endopeptidase activity. Although its primary functions were originally thought to be only of a …

Cysteinyl cathepsins and mast cell proteases in the pathogenesis and therapeutics of cardiovascular diseases

Y Qin, GP Shi - Pharmacology & therapeutics, 2011 - Elsevier
The initiation and progression of cardiovascular diseases involve extensive arterial wall
matrix protein degradation. Proteases are essential to these pathological events. Recent …

Identification of selective, nonpeptidic nitrile inhibitors of cathepsin S using the substrate activity screening method

AW Patterson, WJL Wood, M Hornsby… - Journal of medicinal …, 2006 - ACS Publications
The substrate activity screening method, a substrate-based fragment identification and
optimization method for the development of enzyme inhibitors, was previously applied to …

Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors

GDK Kumar, GE Chavarria, AK Charlton-Sevcik… - Bioorganic & Medicinal …, 2010 - Elsevier
A small library of 36 functionalized benzophenone thiosemicarbazone analogs has been
prepared by chemical synthesis and evaluated for their ability to inhibit the cysteine …

Dipeptidyl nitrile inhibitors of Cathepsin L

N Asaad, PA Bethel, MD Coulson, JE Dawson… - Bioorganic & Medicinal …, 2009 - Elsevier
Dipeptidyl nitrile inhibitors of Cathepsin L - ScienceDirect Skip to main contentSkip to article
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Synthesis and biochemical evaluation of benzoylbenzophenone thiosemicarbazone analogues as potent and selective inhibitors of cathepsin L

EN Parker, J Song, GDK Kumar, SO Odutola… - Bioorganic & medicinal …, 2015 - Elsevier
Upregulation of cathepsin L in a variety of tumors and its ability to promote cancer cell
invasion and migration through degradation of the extracellular matrix suggest that …

Synthesis of 3-oxooxa-and 3-oxoazacycloalk-4-enes by ring-closing metathesis. Application to the synthesis of an inhibitor of cathepsin K

C Taillier, T Hameury, V Bellosta, J Cossy - Tetrahedron, 2007 - Elsevier
Synthesis of 3-oxooxa- and 3-oxoazacycloalk-4-enes by ring-closing metathesis. Application
to the synthesis of an inhibitor of cathepsin K - ScienceDirect Skip to main contentSkip to …

Functionalized benzophenone, thiophene, pyridine, and fluorene thiosemicarbazone derivatives as inhibitors of cathepsin L

GDK Kumar, GE Chavarria, AK Charlton-Sevcik… - Bioorganic & medicinal …, 2010 - Elsevier
A series of thiosemicarbazone analogs based on the benzophenone, thiophene, pyridine,
and fluorene molecular frameworks has been prepared by chemical synthesis and …

Synthesis and biochemical evaluation of thiochromanone thiosemicarbazone analogues as inhibitors of cathepsin L

J Song, LM Jones, GDK Kumar… - ACS medicinal …, 2012 - ACS Publications
A series of 36 thiosemicarbazone analogues containing the thiochromanone molecular
scaffold functionalized primarily at the C-6 position were prepared by chemical synthesis …

An approach combining deep learning and molecule docking for drug discovery of cathepsin L

Q Li, H Wang, WL Yang, JK Yang - Expert Opinion on Drug …, 2023 - Taylor & Francis
ABSTRACT Objectives Cathepsin L (CTSL) is a promising therapeutic target for metabolic
disorders and COVID-19. However, there are still no clinically available CTSL inhibitors. Our …