The current effectiveness of HAART in the management of HIV infection is compromised by the emergence of extensively cross-resistant strains of HIV-1, requiring a significant need for new therapeutic agents. Due to its crucial role in viral maturation and therefore HIV-1 replication and infectivity, the HIV-1 protease continues to be a major development target for antiretroviral therapy. Howeve...

Currently, there are a number of approved antiviral agents for use in the treatment of viral infections. However, many instances exist in which the use of a second antiviral agent would be beneficial because it would allow the option of either an alternative or a combination therapeutic approach. Accordingly, virus-encoded proteases have emerged as new targets for antiviral intervention. Molecu...

The infective third-stage larvae of Angiostrongylus cantonensis secrete a proteolytic enzyme that is thought to be essential for both larval penetration into the intestinal wall of the host and full development. Protease activity in these larvae during culture in vitro was determined by zymography, pH optimum, and substrate and inhibitor specificity. Excretory-secretory (ES) products of the thi...

Belfrage, A. K. 2015. Design and Synthesis of Hepatitis C Virus NS3 Protease Inhibitors. Targeting Different Genotypes and Drug-Resistant Variants. Digital Comprehensive Summaries of Uppsala Dissertations from the Faculty of Pharmacy 197. 108 pp. Uppsala: Acta Universitatis Upsaliensis. ISBN 978-91-554-9166-6. Since the first approved hepatitis C virus (HCV) NS3 protease inhibitors in 2011, num...

Objective: Investigations were carried out to isolate bacteria from saline-alkali soils and determined optimized alkaline protease activity and stability produced by a wild strain of bacillus sp. in submerged fermentation (SMF). Methods: Optimum temperature for enzyme activity in the crude extract was 40 ◦C at a pH between 8.0 and 9.0. The studies on pH stability showed that the enzyme...

BACKGROUND The kallikrein family is a group of 15 serine protease genes clustered on chromosome 19q13.4. Human kallikrein gene 13 (KLK13) is a member of this family and encodes for a trypsin-like, secreted serine protease (hK13). Given that other kallikreins are sequestered by serum protease inhibitors, we hypothesized that hK13 may also interact with similar inhibitors. Our objective was to id...

COVID-19 pandemic is the biggest public health problem of century so far.The main protease (Mpro) one enzymes studied as a pharmacological target. In this context, present work aimed to perform virtual screening possible inhibitors against enzyme Mpro, having limonoids object research supposed inhibitors. Molecular docking simulations indicated that have an affinity complex with M-pro.However, ...

Protease inhibitors are largely used for the treatment of HIV infection in combination with other antiretroviral drugs. Their improved pharmacokinetic profiles can be achieved through the concomitant administration of low doses of ritonavir (RTV), a protease inhibitor currently used as a booster, increasing the exposure of companion drugs. Since ritonavir-boosted regimens are associated with lo...

In the cultured HEK model, we observed that mustard stimulates protease activity, and the epidermaldermal attachment protein laminin-5 is a substrate. Addition of serine protease inhibitors (50 μM ICD 2812 or 1 mM phenyl methyl sulphonyl fluoride (PMSF)), the metalloprotease inhibitor 1, 10phenanthroline (1 mM), or the general caspase inhibitor Z-VAD-FMK (benzyl oxycarbonyl-Val-Ala-Asp (o-methy...