Small molecules in the treatment of COVID-19

S Lei, X Chen, J Wu, X Duan, K Men - Signal transduction and targeted …, 2022 - nature.com
The outbreak of COVID-19 has become a global crisis, and brought severe disruptions to
societies and economies. Until now, effective therapeutics against COVID-19 are in high …

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 …

Structural basis of SARS-CoV-2–and SARS-CoV–receptor binding and small-molecule blockers as potential therapeutics

H Sivaraman, SY Er, YK Choong… - Annual Review of …, 2021 - annualreviews.org
Over the past two decades, deadly coronaviruses, with the most recent being the severe
acute respiratory syndrome-related coronavirus-2 (SARS-CoV-2) 2019 pandemic, have …

Structural basis for the recognition and cleavage of histone H3 by cathepsin L

MA Adams-Cioaba, JC Krupa, C Xu, JS Mort… - Nature …, 2011 - nature.com
Proteolysis of eukaryotic histone tails has emerged as an important factor in the modulation
of cell-cycle progression and cellular differentiation. The recruitment of lysosomal cathepsin …

Toxoplasma gondii cathepsin L is the primary target of the invasion-inhibitory compound morpholinurea-leucyl-homophenyl-vinyl sulfone phenyl

ET Larson, F Parussini, MH Huynh, JD Giebel… - Journal of Biological …, 2009 - ASBMB
The protozoan parasite Toxoplasma gondii relies on post-translational modification,
including proteolysis, of proteins required for recognition and invasion of host cells. We have …

Structural Elucidation and Antiviral Activity of Covalent Cathepsin L Inhibitors

S Falke, J Lieske, A Herrmann, J Loboda… - Journal of Medicinal …, 2024 - ACS Publications
Emerging RNA viruses, including SARS-CoV-2, continue to be a major threat. Cell entry of
SARS-CoV-2 particles via the endosomal pathway involves cysteine cathepsins. Due to …

2, 5-Diaryloxadiazoles and their precursors as novel inhibitors of cathepsins B, H and L

S Garg, N Raghav - Bioorganic Chemistry, 2016 - Elsevier
High levels of cathepsins indicated in various pathological conditions like arthritis, cancer
progressions, and atherosclerosis explains the need to explore potential inhibitors of these …

Chalcones, semicarbazones and pyrazolines as inhibitors of cathepsins B, H and L

N Raghav, R Kaur - International journal of biological macromolecules, 2015 - Elsevier
Abstract Cathepsin B [EC 3.4. 22.1], cathepsin H [EC 3.4. 22.16] and cathepsin L [EC 3.4.
22.15] are the most versatile lysosomal cysteine proteases and are responsible for …

[HTML][HTML] Peptidomimetics as potent dual SARS-CoV-2 cathepsin-L and main protease inhibitors: In silico design, synthesis and pharmacological characterization

T Ciaglia, V Vestuto, V Di Sarno, S Musella… - European Journal of …, 2024 - Elsevier
In this paper we present the design, synthesis, and biological evaluation of a new series of
peptidomimetics acting as potent anti-SARS-CoV-2 agents. Starting from our previously …

Structural basis for reversible and irreversible inhibition of human cathepsin L by their respective dipeptidyl glyoxal and diazomethylketone inhibitors

RT Shenoy, J Sivaraman - Journal of structural biology, 2011 - Elsevier
Cathepsin L plays a key role in many pathophysiological conditions including rheumatoid
arthritis, tumor invasion and metastasis, bone resorption and remodeling. Here we report the …