Search results for "Protease Inhibitor"
showing 10 items of 125 documents
Consistency of Carbopol 971-P NF gels and influence of soluble and cross-linked PVP.
2002
A study is made of the polymerization process of polyacrylic acid, commercially known as Carbopol® 971 NF, assessing its consistency as a function of the degree of neutralization at pH values from 3 to 12, approximately. Percentage concentrations ranging from 0.1 to 1.4% (w/w) were studied. The gels obtained were non-Newtonian, and pseudoplastic. As concentration and pH rise, the consistency of the gels increase to a maximum, which appears between pH 6 and 8, allowing their use as vehicles in bioadhesive formulations for mucosal application. Over the increasing viscosity interval, functions were obtained to indicate the consistency of the gel as a function of pH and concentration. Since the…
Proteomic analysis of the acid-soluble nacre matrix of the bivalve Unio pictorum: detection of novel carbonic anhydrase and putative protease inhibit…
2010
10 pages; International audience; The matrix extracted from mollusc shell nacre is a mixture of proteins and glycoproteins that is thought to play a major role in controlling biomineral synthesis and in increasing its mechanical properties. We investigated the nacreous shell of the freshwater mussel Unio pictorum, to which we applied a proteomics approach adapted to mollusc shell proteins. On one hand, the acid-soluble nacre matrix was fractionated by SDS-PAGE and the five main protein bands (P95, P50, P29, P16, and P12) were digested with trypsin and analyzed by nanoLC-MS/MS followed by de novo sequencing. On the other hand, the acid-soluble nacre matrix was analyzed in a similar manner, w…
Induction of apoptosis in human osteosarcoma Saos-2 cells by the proteasome inhibitor MG132 and the protective effect of pRb
2003
Induction of apoptosis in human osteosarcoma Saos-2 cells by the proteasome inhibitor MG132 and the protective effect of pRb
Plasmodium falciparumMalaria: Reduction of Endothelial Cell Apoptosis In Vitro
2005
ABSTRACTOrgan failure inPlasmodium falciparummalaria is associated with neutrophil activation and endothelial damage. This study investigates whether neutrophil-induced endothelial damage involves apoptosis and whether it can be prevented by neutralization of neutrophil secretory products. Endothelial cells from human umbilical veins were coincubated with neutrophils from healthy donors and with sera from eight patients withP. falciparummalaria, three patients withP. vivaxmalaria, and three healthy controls. Endothelial apoptosis was demonstrated by terminal deoxynucleotidyltransferase-mediated dUTP-biotin nick end labeling (TUNEL) and annexin V staining. The rate of apoptosis of cells was …
Can Experimental Electron-Density Studies be Used as a Tool to Predict Biologically Relevant Properties of Low-Molecular Weight Enzyme Ligands?
2013
The case of protease inhibitor model compounds incorporating an aziridine or epoxide ring is used to exemplify how application of experimental electron-density techniques can be used to explain the biological properties of low-molecular weight enzyme ligands. This is furthermore seen in the light of a comparison of crystal and enzyme environments employing QM/MM computations to elucidate to which extent the properties in the crystal can be used to predict behavior in the biological surrounding.
Asymmetric One-Pot Synthesis of (3R,3aS,6aR)-Hexahydrofuro[2,3-b]furan-3-ol: A Key Component of Current HIV Protease Inhibitors
2017
A concise and efficient synthesis of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-ol, a key building block for several clinical and experimental HIV protease inhibitors including the highly important drug darunavir, was achieved via a one-pot procedure using furan and Cbz-protected glycol aldehyde as starting materials. A [2+2]-photocycloaddition between both reactants which can be prepared from wood-based starting materials according to the principles of xylochemistry, followed by hydrogenation and lipase-catalyzed kinetic resolution afforded the target compound in high yield and up to 99% ee.
Purification of ATP synthase from beef heart mitochondria (FoF1) and co-reconstitution with monomeric bacteriorhodopsin into liposomes capable of lig…
1993
ATP synthase was isolated from beef heart mitochondria by extraction with N,N-bis-(3-D-gluconamidopropyl)deoxycholamide or by traditional cholate extraction. The enzyme was purified subsequently by ion-exchange and gel-permeation chromatographies in the presence of glycerol and the protease inhibitor diisopropylfluorophosphate. The ATP synthase consisted of 12–14 subunits and contained three tightly bound nucleotides. The co-reconstitution of crude or purified ATP synthase with monomeric bacteriorhodopsin by the method of detergent incubation of liposomes yielded proteoliposomes capable of light-driven ATP synthesis, as detected with a luciferase system for at least 30 min. The reaction was…
Receptor for advanced glycation end products is subjected to protein ectodomain shedding by metalloproteinases.
2008
The receptor for advanced glycation end products (RAGE) is a 55-kDa type I membrane glycoprotein of the immunoglobulin superfamily. Ligand-induced up-regulation of RAGE is involved in various pathophysiological processes, including late diabetic complications and Alzheimer disease. Application of recombinant soluble RAGE has been shown to block RAGE-mediated pathophysiological conditions. After expression of full-length RAGE in HEK cells we identified a 48-kDa soluble RAGE form (sRAGE) in the culture medium. This variant of RAGE is smaller than a 51-kDa soluble version derived from alternative splicing. The release of sRAGE can be induced by the phorbol ester PMA and the calcium ionophore c…
Osmolality of various viscoelastic substances: comparative study.
2000
Abstract Purpose To determine the osmolality of various viscoelastic substances. Setting Department of Ophthalmology, Johannes Gutenberg-University, Mainz, and Institute for Medical Device Testing, Memmingen, Germany. Methods The analysis was carried out according to the European Pharmacopoeia by means of a calibrated osmometer using the freezing-point depression method. Each syringe was analyzed as a duplicate analysis. Results Mean osmolalities (mOsmol/kg) of the sodium hyaluronate viscoelastic substances were Allervisc® 299; Allervisc® Plus 307; Amvisc® Plus 335; AMO Vitrax® 284; Biolon® 279; Dispasan® 311; Dispasan® Plus 314; Healon® 295; Healon GV® 312; Healon®5 322; HYA-Ophtal® 376; M…
The dilemma for patients with chronic hepatitis C: treat now or warehouse?
2013
Dual therapy with peginterferon and ribavirin, the only treatent for chronic hepatitis C available In Italy and in many other ountries worldwide up to 2013, obtains satisfactory response ates in infections with hepatitis C virus (HCV) genotype 2, but far rom optimal for other genotypes [1,2]. Eradication requires 6–12 onths of therapy, with significant inconvenience for patients: dverse reactions force premature termination in about 20% of atients and reduced the quality of life for almost all who persist n treatment. In view of the important and prolonged side effects, nterferon-based treatment is perceived as a nightmare by many symptomatic,well-being, socially activepatients (the largema…