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Small Molecule Protease Inhibitors as Model Peptidomimetics [PDF]

open access: yesPharmaceuticals
Proteases constitute one of the largest sub-classes of enzymes, accounting for ca. 2% of the proteins encoded in the human genome. They play a key role in protein degradation and signaling, regulating a variety of physiological processes.
Patricia Gomez-Gutierrez, Juan J. Perez
doaj   +2 more sources

Optimized pipeline and designer cells for synthetic-biology-based high-throughput screening of viral protease inhibitors [PDF]

open access: yesCell Reports: Methods
Summary: A reliable, efficient, high-throughput pipeline to evaluate viral protease inhibitors would enhance antiviral drug discovery. Methods such as crystallography and phenotypic screening are often constrained by complex assay conditions, limited ...
Shlomi Edri   +10 more
doaj   +2 more sources

Comparative study of the unbinding process of some HTLV-1 protease inhibitors using unbiased molecular dynamics simulations.

open access: yesPLoS ONE, 2022
The HTLV-1 protease is one of the major antiviral targets to overwhelm this virus. Several research groups have developed protease inhibitors, but none has been successful.
Fereshteh Noroozi Tiyoula   +2 more
doaj   +1 more source

HIV Protease: Historical Perspective and Current Research

open access: yesViruses, 2021
The retroviral protease of human immunodeficiency virus (HIV) is an excellent target for antiviral inhibitors for treating HIV/AIDS. Despite the efficacy of therapy, current efforts to control the disease are undermined by the growing threat posed by ...
Irene T. Weber   +2 more
doaj   +1 more source

Combination of Antifungal Drugs and Protease Inhibitors Prevent Candida albicans Biofilm Formation and Disrupt Mature Biofilms

open access: yesFrontiers in Microbiology, 2020
Biofilms formed by the fungal pathogen Candida albicans are resistant to many of the antifungal agents commonly used in the clinic. Previous reports suggest that protease inhibitors, specifically inhibitors of aspartyl proteases, could be effective ...
Matthew B. Lohse   +5 more
doaj   +1 more source

NMR analysis of the dynamic exchange of the NS2B cofactor between open and closed conformations of the West Nile virus NS2B-NS3 protease. [PDF]

open access: yesPLoS Neglected Tropical Diseases, 2009
BACKGROUND: The two-component NS2B-NS3 proteases of West Nile and dengue viruses are essential for viral replication and established targets for drug development.
Xun-Cheng Su   +5 more
doaj   +1 more source

SjAPI, the first functionally characterized Ascaris-type protease inhibitor from animal venoms. [PDF]

open access: yesPLoS ONE, 2013
Serine protease inhibitors act as modulators of serine proteases, playing important roles in protecting animal toxin peptides from degradation. However, all known serine protease inhibitors discovered thus far from animal venom belong to the Kunitz-type ...
Zongyun Chen   +7 more
doaj   +1 more source

Structural similarities between SARS-CoV2 3CLpro and other viral proteases suggest potential lead molecules for developing broad spectrum antivirals

open access: yesFrontiers in Chemistry, 2022
Considering the significant impact of the recent COVID-19 outbreak, development of broad-spectrum antivirals is a high priority goal to prevent future global pandemics. Antiviral development processes generally emphasize targeting a specific protein from
Khushboo Bafna   +5 more
doaj   +1 more source

Interspecific differences between D. pulex and D. magna in tolerance to cyanobacteria with protease inhibitors. [PDF]

open access: yesPLoS ONE, 2013
It is known that cyanobacteria negatively affect herbivores due to their production of toxins such as protease inhibitors. In the present study we investigated potential interspecific differences between two major herbivores, Daphnia magna and Daphnia ...
Christian J Kuster, Eric Von Elert
doaj   +1 more source

Role of Protease-Inhibitors in Ocular Diseases

open access: yesMolecules, 2014
It has been demonstrated that the balance between proteases and protease-inhibitors system plays a key role in maintaining cellular and tissue homeostasis. Indeed, its alteration has been involved in many ocular and systemic diseases.
Nicola Pescosolido   +5 more
doaj   +1 more source

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