Emerging and Re-emerging Warheads for Targeted Covalent Inhibitors: An Update

L Hillebrand, XJ Liang, RAM Serafim… - Journal of Medicinal …, 2024 - ACS Publications
Covalent inhibitors and other types of covalent modalities have seen a revival in the past two
decades, with a variety of new targeted covalent drugs having been approved in recent …

Overview of antiviral drug therapy for COVID-19: where do we stand?

R Esposito, D Mirra, L Sportiello, G Spaziano… - Biomedicines, 2022 - mdpi.com
The vaccine weapon has resulted in being essential in fighting the COVID-19 outbreak, but it
is not fully preventing infection due to an alarming spreading of several identified variants of …

Dual Inhibitors of SARS-CoV-2 3CL Protease and Human Cathepsin L Containing Glutamine Isosteres Are Anti-CoV-2 Agents

V Kumar, J Zhu, BC Chenna, ZA Hoffpauir… - Journal of the …, 2025 - ACS Publications
SARS-CoV-2 3CL protease (Main protease) and human cathepsin L are proteases that play
unique roles in the infection of human cells by SARS-CoV-2, the causative agent of COVID …

Cysteine protease I29 propeptide from Calotropis procera R. Br. As a potent cathepsin L inhibitor and its suppressive activity in breast cancer metastasis

YJ Kwon, J Lee, EB Seo, J Lee, J Park, SK Kim, H Yu… - Scientific Reports, 2024 - nature.com
Breast cancer metastasis is associated with a poor prognosis and a high rate of mortality.
Cathepsin L (CTSL) is a lysosomal cysteine protease that promotes tumor metastasis by …

Synthesis and Biological Evaluation of New Chalcogen Semicarbazone (S, Se) and Their Azole Derivatives against Chagas Disease

M Rubio-Hernández, V Alcolea… - Journal of Medicinal …, 2024 - ACS Publications
Chagas disease is caused by the eukaryote parasite Trypanosoma cruzi. Current treatment
exhibits limited efficacy and selenium-based compounds emerged as promising candidates …

P 1 Glutamine isosteres in the design of inhibitors of 3C/3CL protease of human viruses of the Pisoniviricetes class

LA Stubbing, JG Hubert, J Bell-Tyrer… - RSC Chemical …, 2023 - pubs.rsc.org
Viral infections are one of the leading causes of acute morbidity in humans and much
endeavour has been made by the synthetic community for the development of drugs to treat …

Recent Advances on Targeting Proteases for Antiviral Development

PHO Borges, SB Ferreira, FP Silva Jr - Viruses, 2024 - mdpi.com
Viral proteases are an important target for drug development, since they can modulate vital
pathways in viral replication, maturation, assembly and cell entry. With the (re) appearance …

Covalent-reversible peptide-based protease inhibitors. Design, synthesis, and clinical success stories

A Feral, AR Martin, A Desfoux, M Amblard… - Amino Acids, 2023 - Springer
Dysregulated human peptidases are implicated in a large variety of diseases such as
cancer, hypertension, and neurodegeneration. Viral proteases for their part are crucial for …

[HTML][HTML] Activity of pyridyl-pyrazolone derivatives against Trypanosoma cruzi

DGJ Batista, LF de Almeida Fiuza, F Klupsch… - Experimental …, 2024 - Elsevier
New affordable drugs are needed for the treatment of infection with the protozoan parasite
Trypanosoma cruzi responsible for the Chagas disease (CD). Only two old drugs are …

Kinetic characterization of cerium and gallium ions as inhibitors of cysteine cathepsins L, K, and S

M Novinec, P Bembič, M Janković, M Kisilak… - International Journal of …, 2022 - mdpi.com
Heavy metal ions can disrupt biological functions via multiple molecular mechanisms,
including inhibition of enzymes. We investigate the interactions of human papain-like …