[HTML][HTML] Examination of multiple Trypanosoma cruzi targets in a new drug discovery approach for Chagas disease

I Beltran-Hortelano, V Alcolea, M Font… - Bioorganic & medicinal …, 2022 - Elsevier
Chagas disease (CD) is a centenarian neglected parasitosis caused by the protozoan
Trypanosoma cruzi (T. cruzi). Despite the continuous efforts of many organizations and …

[HTML][HTML] Marine cyanobacteria: A source of lead compounds and their clinically-relevant molecular targets

LT Tan, MY Phyo - Molecules, 2020 - mdpi.com
The prokaryotic filamentous marine cyanobacteria are photosynthetic microbes that are
found in diverse marine habitats, ranging from epiphytic to endolithic communities. Their …

Potent anti-SARS-CoV-2 activity by the natural product gallinamide A and analogues via inhibition of cathepsin L

AS Ashhurst, AH Tang, P Fajtová… - Journal of medicinal …, 2021 - ACS Publications
Cathepsin L is a key host cysteine protease utilized by coronaviruses for cell entry and is a
promising drug target for novel antivirals against SARS-CoV-2. The marine natural product …

Computer-aided design of 1, 4-naphthoquinone-based inhibitors targeting cruzain and rhodesain cysteine proteases

LR Silva, AS Guimaraes, J do Nascimento… - Bioorganic & Medicinal …, 2021 - Elsevier
Abstract Chagas disease and Human African Trypanosomiasis (HAT) are caused by
Trypanosoma cruzi and T. brucei parasites, respectively. Cruzain (CRZ) and Rhodesain …

[HTML][HTML] Native metabolomics identifies the rivulariapeptolide family of protease inhibitors

R Reher, AT Aron, P Fajtová, P Stincone… - Nature …, 2022 - nature.com
The identity and biological activity of most metabolites still remain unknown. A bottleneck in
the exploration of metabolite structures and pharmaceutical activities is the compound …

Structure-Based Identification of Naphthoquinones and Derivatives as Novel Inhibitors of Main Protease Mpro and Papain-like Protease PLpro of SARS-CoV-2

LH Santos, T Kronenberger, RG Almeida… - Journal of Chemical …, 2022 - ACS Publications
The worldwide COVID-19 pandemic caused by the coronavirus SARS-CoV-2 urgently
demands novel direct antiviral treatments. The main protease (Mpro) and papain-like …

[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 …

Structure-Based Optimization of Quinazolines as Cruzain and TbrCATL Inhibitors

E Barbosa da Silva, DA Rocha, IS Fortes… - Journal of Medicinal …, 2021 - ACS Publications
The cysteine proteases, cruzain and Tbr CATL (rhodesain), are therapeutic targets for
Chagas disease and Human African Trypanosomiasis, respectively. Among the known …

Impact of the recognition part of dipeptidyl nitroalkene compounds on the inhibition mechanism of cysteine proteases cruzain and cathepsin L

K Arafet, S Royo, T Schirmeister, F Barthels… - ACS …, 2023 - ACS Publications
Cysteine proteases (CPs) are an important class of enzymes, many of which are responsible
for several human diseases. For instance, cruzain of protozoan parasite Trypanosoma cruzi …

Intramolecular Interactions Enhance the Potency of Gallinamide A Analogues against Trypanosoma cruzi

E Barbosa Da Silva, V Sharma… - Journal of Medicinal …, 2022 - ACS Publications
Gallinamide A, a metabolite of the marine cyanobacterium Schizothrix sp., selectively
inhibits cathepsin L-like cysteine proteases. We evaluated the potency of gallinamide A and …