[HTML][HTML] 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 …

Impact of the Warhead of Dipeptidyl Keto Michael Acceptors on the Inhibition Mechanism of Cysteine Protease Cathepsin L

A Fernández-de-la-Pradilla, S Royo… - ACS …, 2023 - ACS Publications
Cathepsin L (CatL) is a lysosomal cysteine protease whose activity has been related to
several human pathologies. However, although preclinical trials using CatL inhibitors were …

An activity-based probe for cathepsin K imaging with excellent potency and selectivity

C Lemke, J Benysek, D Brajtenbach… - Journal of Medicinal …, 2021 - ACS Publications
The cysteine protease cathepsin K is a target for the treatment of diseases associated with
high bone turnover. Cathepsin K is mainly expressed in osteoclasts and responsible for the …

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 and kinetic evaluation of ethyl acrylate and vinyl sulfone derived inhibitors for human cysteine cathepsins

C Breuer, C Lemke, J Schmitz, U Bartz… - Bioorganic & Medicinal …, 2018 - Elsevier
A series of inhibitors targeting human cathepsins have been designed and synthesized
following a combinatorial approach. The compounds bear an α, β-unsaturated phenyl vinyl …

Cell penetrable, clickable and tagless activity-based probe of human cathepsin L

D Dana, J Garcia, AI Bhuiyan, P Rathod, L Joo… - Bioorganic …, 2019 - Elsevier
Human cathepsin L is a ubiquitously expressed endopeptidase and is known to play critical
roles in a wide variety of cellular signaling events. Its overexpression has been implicated in …

HLA-DR peptide occupancy can be regulated with a wide variety of small molecules

F Blazekovic, D Odukoya, SN Butler… - Human Vaccines & …, 2016 - Taylor & Francis
abstract HLA-DR is the most commonly expressed and likely the most medically important
human MHC class II, antigen presenting protein. In a normal immune response, HLA-DR …

Cathepsin L inhibitors and probes comprising vinyl sulfonate moiety and methods of using same

S Kumar, D Dana - US Patent 9,481,876, 2016 - Google Patents
Human cathepsin L inhibitors and probes containing a vinyl sulfonate ester moiety are
described. The inhibitors are highly potent (low nM affinity), selective, and cell perme able …

Design and synthesis of small-molecule inhibitors of cathepsin L bearing the thiosemicarbazone warhead as potential anti-metastatic agents.

EN Parker - 2015 - tdl-ir.tdl.org
Mestastasis is a devastating component associated with tumor progression which claims the
majority of lives lost to cancer. Upregulation of cathepsin L, a powerful cysteine protease …

Design and Synthesis of Covalent Peptidomimetic Inhibitors for Human Cysteine Cathepsins

C Breuer - 2020 - bonndoc.ulb.uni-bonn.de
The present thesis elucidates the development of (i) a series of small molecule inhibitors
reacting in a covalent-irreversible manner with the targeted proteases and (ii) a fluorescently …