Results 21 to 30 of about 134,020 (288)

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, Isabelle Cohen-Codar, Martin S. King, Philippe Colson, Emmanuel Guillevic, Diane Descamps, C. Lamotte, Véronique Schneider, J. Ritter, Michel Segondy, H. Peigue‐Lafeuille, Laurence Morand‐Joubert, Anne Schmuck, Annick Ruffault, Pierre Palmer, Marie‐Laure Chaix, Vincent Mackiewicz, Véronique Brodard, Jacques Izopet, Jacqueline Cottalorda, Évelyne Kohli, Jean-Pierre Chauvin, Dale J. Kempf, Gilles Peytavin, Vincent Cálvez   +24 more
openalex   +4 more sources

Data from A Pharmacologic Inhibitor of the Protease Taspase1 Effectively Inhibits Breast and Brain Tumor Growth [PDF]

, 2023
<div>Abstract<p>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, Yi Shan Lee, Brian A. Van Tine, Adam C. Searleman, Todd D. Westergard, Han Liu, Ho-Chou Tu, Shugaku Takeda, Yiyu Dong, David Piwnica‐Worms, Kyoung Joon Oh, Stanley J. Korsmeyer, Ann Hermone, Richard Gussio, Robert H. Shoemaker, Emily H. Cheng, James J. Hsieh   +16 more
openalex   +2 more sources

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, Christopher Baker, Michael Hale, David J. Reynolds, Jo A. Salisbury, Andy D. Searle, Scott D. Studenberg, Dan Todd, Roger D. Tung, Andrew Spaltenstein   +9 more
openalex   +3 more sources

Pharmacological studies on a synthetic protease inhibitor, FUT-175. I. Effects on complements and kallikrein.

Japanese Journal of Pharmacology, 1983
Abstract FUT-175 has been reported by S.Fujii et al.1) to inhibit strongly Clr, Cls, trypsin and thrombin as well as kallikrein and plasmin. In the present study, effects of FUT-175 on the complement and kallikrein system were investigated in vitro and in vivo.
Masayuki Ozeki, Minoru Oda, Yoshitaka Ino, Akemi Motoyoshi, Mitsunobu Fujita, Takuo Aoyama, Setsuro Fujii   +6 more
openalex   +3 more sources

A Mini Review on New Pharmacological and Toxicological Considerations of Protease Inhibitors' Application in Cancer Prevention and Biological Research [PDF]

Asian Journal of Cell Biology, 2011
Hamid Reza Rahimi, E. Hasanli, Hossein Jamalifar   +2 more
openalex   +3 more sources

In silico screening of phenylethanoid glycosides, a class of pharmacologically active compounds as natural inhibitors of SARS-CoV-2 proteases

Computational and Structural Biotechnology Journal, 2023
Since the advent of Covid-19, several natural products have been investigated regarding their in silico interactions with SARS-CoV-2 proteases - 3CLpro and PLpro, two of the most important pharmacological targets for antiviral development. Phenylethanoid glycosides (PG) are a class of natural products present in important medicinal plants and a drug ...
Caio Cheohen, Maria Eduarda Alves Esteves, Thamirys Silva da Fonseca, Carla Monteiro Leal, Fernanda de Lemos Fernandes Assis, Mariana Freire Campos, Raianne Soares Rebelo, Diego Allonso, Gilda Guimarães Leitão, Manuela Leal da Silva, Suzana Guimarães Leitão   +10 more
openalex   +4 more sources

The intracellular pharmacology of antiretroviral protease inhibitors [PDF]

Journal of Antimicrobial Chemotherapy, 2004
Therapeutic drug monitoring (TDM) of antiretroviral protease inhibitors (PIs) has been suggested to have the potential to both reduce toxicity and optimize individual therapy. However, the major target of PIs is within cells infected with HIV. Therefore clinical outcome ultimately must be related to intracellular drug concentrations since antiviral ...
David Back, Saye Khoo, J. Ford
openaire   +2 more sources

20 IN VITRO ACTIVITY AND PHARMACOLOGIC PROPERTIES OF TWO NOVEL SERIES OF HCV PROTEASE INHIBITORS

Journal of Hepatology, 2008
David N. Standring, Christophe Parsy, François-René Alexandre, Michel Derock, Frédéric Leroy, Thierry Convard, Massimiliano La Colla, L. Lallos, A. G. Loi, Chiara Musiu, Tiziana Marceddu, Barbara Poddesu, L Vargiu, Michel Liuzzi, Dominique Surleraux   +14 more
openalex   +3 more sources

Pharmacologic Optimization of Protease Inhibitors and Nonnucleoside Reverse Transcriptase Inhibitors (POPIN)-A Randomized Controlled Trial of Therapeutic Drug Monitoring and Adherence Support

JAIDS Journal of Acquired Immune Deficiency Syndromes, 2006
We evaluated the feasibility and effectiveness of therapeutic drug monitoring (TDM) and adherence support (collectively, AT) vs standard of care (SOC) in patients receiving HIV protease inhibitors (PIs) and nonnucleoside reverse transcriptase inhibitors (NNRTIs) within a nurse-led clinic. Primary end points were failure to achieve viral load of
Saye Khoo, Judith Lloyd, Mark Dalton, Alec Bonington, Elizabeth A. Hart, Sara Gibbons, P J Flegg, John F. Sweeney, E.G.L. Wilkins, David Back   +9 more
openalex   +4 more sources

Synergistic inhibition of SARS-CoV-2 cell entry by otamixaban and covalent protease inhibitors: pre-clinical assessment of pharmacological and molecular properties

Chemical Science, 2021
SARS-CoV-2, the cause of the COVID-19 pandemic, exploits host proteins for viral entry into human lung cells and is blocked by otamixaban in combination with a covalent protease inhibitor.
Tim Hempel, Katarina Elez, Nadine Krüger, Lluı́s Raich, Jonathan H. Shrimp, Olga Danov, Danny Jonigk, Armin Braun, Min Shen, Matthew D. Hall, Stefan Pöhlmann, Markus Hoffmann, Frank Noé   +12 more
openalex   +9 more sources