Plant Kunitz Inhibitors and Their Interaction with Proteases: Current and Potential Pharmacological Targets [PDF]
International Journal of Molecular Sciences, 2022 The action of proteases can be controlled by several mechanisms, including regulation through gene expression; post-translational modifications, such as glycosylation; zymogen activation; targeting specific compartments, such as lysosomes and mitochondria; and blocking proteolysis using endogenous inhibitors. Protease inhibitors are important molecules
Camila Ramalho Bonturi +7 more
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Pharmacological and therapeutic properties of ritonavir-boosted protease inhibitor therapy in HIV-infected patients [PDF]
Journal of Antimicrobial Chemotherapy, 2003 Boosted protease inhibitor regimens combine ritonavir with a second, 'boosted' protease inhibitor to enhance patient exposure to the latter agent, thereby preventing or overcoming resistance and allowing less frequent dosing, potentially improving adherence.
Robert K. Zeldin
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Network Pharmacology Analysis of Orally Bioavailable SARS-CoV-2 Protease Inhibitor Shows Synergistic Targets to Improve Clinical Efficacy [PDF]
Biology, Engineering, Medicine and Science Reports, 2021 Abstract Introduction: Orally bioavailable SARS-CoV2 antiviral drugs will significantly improve the clinical management of the disease. PF07321332 (PF32) one such orally bioavailable SARS-CoV2 protease inhibitor which can be helpful to prevent viral replication in the host.
Arun Kumar
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General and Modular Strategy for Designing Potent, Selective, and Pharmacologically Compliant Inhibitors of Rhomboid Proteases [PDF]
Cell Chemical Biology, 2017 Rhomboid-family intramembrane proteases regulate important biological processes and have been associated with malaria, cancer, and Parkinson's disease. However, due to the lack of potent, selective, and pharmacologically compliant inhibitors, the wide therapeutic potential of rhomboids is currently untapped. Here, we bridge this gap by discovering that
Anežka Tichá +14 more
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Novel Pan-Coronavirus 3CL Protease Inhibitor MK-7845: Bio-Logical and Pharmacological Profiling [PDF]
VirusesSevere acute respiratory syndrome coronavirus type 2 (SARS-CoV-2) continues to be a global threat due to its ability to evolve and generate new subvariants, leading to new waves of infection. Additionally, other coronaviruses like Middle East respiratory syndrome coronavirus (MERS-CoV, formerly known as hCoV-EMC) which first emerged in 2012, persists ...
Nadine Álvarez +30 more
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A Pharmacologic Inhibitor of the Protease Taspase1 Effectively Inhibits Breast and Brain Tumor Growth [PDF]
Cancer Research, 2011 Abstract The threonine endopeptidase Taspase1 has a critical role in cancer cell proliferation and apoptosis. In this study, we developed and evaluated small molecule inhibitors of Taspase1 as a new candidate class of therapeutic modalities.
David Y. Chen +16 more
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Virological and Pharmacological Parameters Predicting the Response to Lopinavir-Ritonavir in Heavily Protease Inhibitor-Experienced Patients [PDF]
Antimicrobial Agents and Chemotherapy, 2005 ABSTRACTThe genotypic inhibitory quotient (GIQ) has been proposed as a way to integrate drug exposure and genotypic resistance to protease inhibitors and can be useful to enhance the predictivity of virologic response for boosted protease inhibitors. The aim of this study was to evaluate the predictivity of the GIQ in 116 protease inhibitor-experienced
Anne‐Geneviève Marcelin +24 more
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Preclinical Pharmacology and Pharmacokinetics of GW433908, a Water-Soluble Prodrug of the Human Immunodeficiency Virus Protease Inhibitor Amprenavir [PDF]
Antimicrobial Agents and Chemotherapy, 2004 ABSTRACT GW433908 is the water-soluble, phosphate ester prodrug of the human immunodeficiency virus type 1 protease inhibitor amprenavir (APV). A high-yield synthesis of GW433908 is achieved by phosphorylation of the penultimate precursor of APV with phosphorous oxychloride (POCl 3 ) in pyridine.
Eric S. Furfine +9 more
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Pharmacological study and clinical effect of HIV protease inhibitor amprenavir (Prozei capsule).
Folia Pharmacologica Japonica, 2001 Amprenavir is a novel protease inhibitor with antiviral activity, and was approved in the U.S. (AGEN-ERASE) in 1999 for use in combination with other antiretrovirals for the treatment of HIV infection. The drug is developed by Kissei Pharmaceuticals Co., Ltd. in Japan, approved in the same year, and has been distributed by them (PROZEI).
M Ishizawa, H. Komatsu
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Pharmacological dissociation of memory: Anisomycin, a protein synthesis inhibitor, and leupeptin, a protease inhibitor, block different learning tasks [PDF]
Behavioral and Neural Biology, 1985 Inhibition of protein synthesis by anisomycin for a short duration impairs memory of a one-trial inhibitory avoidance task in rats. Memory of escape conditioning involving eight trials is disrupted only if the duration of protein synthesis is prolonged by repeated injections.
Ursula Stäubli +2 more
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