Compounds which inhibit or antagonize biosynthesis or actions of proteases (ENDOPEPTIDASES).
Inhibitors of HIV PROTEASE, an enzyme required for production of proteins needed for viral assembly.
Exogenous or endogenous compounds which inhibit SERINE ENDOPEPTIDASES.
Enzyme of the human immunodeficiency virus that is required for post-translational cleavage of gag and gag-pol precursor polyproteins into functional products needed for viral assembly. HIV protease is an aspartic protease encoded by the amino terminus of the pol gene.
Any member of the group of ENDOPEPTIDASES containing at the active site a serine residue involved in catalysis.
Hydrolases that specifically cleave the peptide bonds found in PROTEINS and PEPTIDES. Examples of sub-subclasses for this group include EXOPEPTIDASES and ENDOPEPTIDASES.
A proteinase inhibitor found in various BODILY SECRETIONS that coat mucosal surfaces such as SEMINAL PLASMA; CERVICAL MUCUS; and bronchial secretions. It plays a role in protecting epithelial tissues from LEUKOCYTE-derived serine proteases such as NEUTROPHIL ELASTASE.
A subclass of PEPTIDE HYDROLASES that catalyze the internal cleavage of PEPTIDES or PROTEINS.
An HIV protease inhibitor which acts as an analog of an HIV protease cleavage site. It is a highly specific inhibitor of HIV-1 and HIV-2 proteases, and also inhibits CYTOCHROME P-450 CYP3A.
A potent and specific HIV protease inhibitor that appears to have good oral bioavailability.
An HIV protease inhibitor that works by interfering with the reproductive cycle of HIV. It also inhibits CYTOCHROME P-450 CYP3A.
Peptides and proteins found in BODILY SECRETIONS and BODY FLUIDS that are PROTEASE INHIBITORS. They play a role in INFLAMMATION, tissue repair and innate immunity (IMMUNITY, INNATE) by inhibiting endogenous proteinases such as those produced by LEUKOCYTES and exogenous proteases such as those produced by invading microorganisms.
Serine proteinase inhibitors which inhibit trypsin. They may be endogenous or exogenous compounds.
A potent HIV protease inhibitor. It is used in combination with other antiviral drugs in the treatment of HIV in both adults and children.
A family of serine proteinase inhibitors which are similar in amino acid sequence and mechanism of inhibition, but differ in their specificity toward proteolytic enzymes. This family includes alpha 1-antitrypsin, angiotensinogen, ovalbumin, antiplasmin, alpha 1-antichymotrypsin, thyroxine-binding protein, complement 1 inactivators, antithrombin III, heparin cofactor II, plasminogen inactivators, gene Y protein, placental plasminogen activator inhibitor, and barley Z protein. Some members of the serpin family may be substrates rather than inhibitors of SERINE ENDOPEPTIDASES, and some serpins occur in plants where their function is not known.
A subclass of peptide hydrolases that depend on a CYSTEINE residue for their activity.
ENDOPEPTIDASES which have a cysteine involved in the catalytic process. This group of enzymes is inactivated by CYSTEINE PROTEINASE INHIBITORS such as CYSTATINS and SULFHYDRYL REAGENTS.
Exogenous and endogenous compounds which inhibit CYSTEINE ENDOPEPTIDASES.
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.
Extracellular protease inhibitors that are secreted from FIBROBLASTS. They form a covalent complex with SERINE PROTEASES and can mediate their cellular internalization and degradation.
Derivatives of carbamic acid, H2NC(=O)OH. Included under this heading are N-substituted and O-substituted carbamic acids. In general carbamate esters are referred to as urethanes, and polymers that include repeating units of carbamate are referred to as POLYURETHANES. Note however that polyurethanes are derived from the polymerization of ISOCYANATES and the singular term URETHANE refers to the ethyl ester of carbamic acid.
An HIV protease inhibitor used in a fixed-dose combination with RITONAVIR. It is also an inhibitor of CYTOCHROME P-450 CYP3A.
Plasma glycoprotein member of the serpin superfamily which inhibits TRYPSIN; NEUTROPHIL ELASTASE; and other PROTEOLYTIC ENZYMES.
The ability of viruses to resist or to become tolerant to chemotherapeutic agents or antiviral agents. This resistance is acquired through gene mutation.
A single-chain polypeptide derived from bovine tissues consisting of 58 amino-acid residues. It is an inhibitor of proteolytic enzymes including CHYMOTRYPSIN; KALLIKREIN; PLASMIN; and TRYPSIN. It is used in the treatment of HEMORRHAGE associated with raised plasma concentrations of plasmin. It is also used to reduce blood loss and transfusion requirements in patients at high risk of major blood loss during and following open heart surgery with EXTRACORPOREAL CIRCULATION. (Reynolds JEF(Ed): Martindale: The Extra Pharmacopoeia (electronic version). Micromedex, Inc, Englewood, CO, 1995)
A prokaryotic ATP-dependent protease that plays a role in the degradation of many abnormal proteins. It is a tetramer of 87-kDa subunits, each of which contains a proteolytic site and a ATP-binding site.
An inhibitor of SERINE ENDOPEPTIDASES. Acts as an alkylating agent and is known to interfere with the translation process.
A serine proteinase inhibitor used therapeutically in the treatment of pancreatitis, disseminated intravascular coagulation (DIC), and as a regional anticoagulant for hemodialysis. The drug inhibits the hydrolytic effects of thrombin, plasmin, and kallikrein, but not of chymotrypsin and aprotinin.
The type species of LENTIVIRUS and the etiologic agent of AIDS. It is characterized by its cytopathic effect and affinity for the T4-lymphocyte.
Proteases that contain proteolytic core domains and ATPase-containing regulatory domains. They are usually comprised of large multi-subunit assemblies. The domains can occur within a single peptide chain or on distinct subunits.
Peptides composed of between two and twelve amino acids.
A low-molecular-weight protein (minimum molecular weight 8000) which has the ability to inhibit trypsin as well as chymotrypsin at independent binding sites. It is characterized by a high cystine content and the absence of glycine.
Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).
N-acylated oligopeptides isolated from culture filtrates of Actinomycetes, which act specifically to inhibit acid proteases such as pepsin and renin.
Agents used to treat AIDS and/or stop the spread of the HIV infection. These do not include drugs used to treat symptoms or opportunistic infections associated with AIDS.
An oligopeptide produced by various bacteria which acts as a protease inhibitor.
A group of lysosomal proteinases or endopeptidases found in aqueous extracts of a variety of animal tissues. They function optimally within an acidic pH range. The cathepsins occur as a variety of enzyme subtypes including SERINE PROTEASES; ASPARTIC PROTEINASES; and CYSTEINE PROTEASES.
An inhibitor of Serine Endopeptidases. Acts as alkylating agent and is known to interfere with the translation process.
An enzyme inhibitor that inactivates IRC-50 arvin, subtilisin, and the fatty acid synthetase complex.
A high-molecular-weight protein (approximately 22,500) containing 198 amino acid residues. It is a strong inhibitor of trypsin and human plasmin.
A homologous group of endogenous CYSTEINE PROTEINASE INHIBITORS. The cystatins inhibit most CYSTEINE ENDOPEPTIDASES such as PAPAIN, and other peptidases which have a sulfhydryl group at the active site.
A characteristic feature of enzyme activity in relation to the kind of substrate on which the enzyme or catalytic molecule reacts.
A group of acylated oligopeptides produced by Actinomycetes that function as protease inhibitors. They have been known to inhibit to varying degrees trypsin, plasmin, KALLIKREINS, papain and the cathepsins.
A serine endopeptidase secreted by the pancreas as its zymogen, CHYMOTRYPSINOGEN and carried in the pancreatic juice to the duodenum where it is activated by TRYPSIN. It selectively cleaves aromatic amino acids on the carboxyl side.
A protease of broad specificity, obtained from dried pancreas. Molecular weight is approximately 25,000. The enzyme breaks down elastin, the specific protein of elastic fibers, and digests other proteins such as fibrin, hemoglobin, and albumin. EC 3.4.21.36.
Inhibitors of reverse transcriptase (RNA-DIRECTED DNA POLYMERASE), an enzyme that synthesizes DNA on an RNA template.
A serine endopeptidase that is formed from TRYPSINOGEN in the pancreas. It is converted into its active form by ENTEROPEPTIDASE in the small intestine. It catalyzes hydrolysis of the carboxyl group of either arginine or lysine. EC 3.4.21.4.
The rate dynamics in chemical or physical systems.
A protease nexin and serpin subtype that is specific for several SERINE PROTEASES including UROKINASE; THROMBIN; TRYPSIN; and PLASMINOGEN ACTIVATORS.
Proteins prepared by recombinant DNA technology.
The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.
An enzyme that catalyzes the hydrolysis of proteins, including elastin. It cleaves preferentially bonds at the carboxyl side of Ala and Val, with greater specificity for Ala. EC 3.4.21.37.
Any detectable and heritable change in the genetic material that causes a change in the GENOTYPE and which is transmitted to daughter cells and to succeeding generations.
The ability of viruses to resist or to become tolerant to several structurally and functionally distinct drugs simultaneously. This resistance phenotype may be attributed to multiple gene mutation.
A sub-subclass of endopeptidases that depend on an ASPARTIC ACID residue for their activity.
Peptide hydrolases that contain at the active site a SERINE residue involved in catalysis.
A group of compounds that contain the structure SO2NH2.
The sum of the weight of all the atoms in a molecule.
A family of SERINE ENDOPEPTIDASES isolated from Bacillus subtilis. EC 3.4.21.-
Drug regimens, for patients with HIV INFECTIONS, that aggressively suppress HIV replication. The regimens usually involve administration of three or more different drugs including a protease inhibitor.
Electrophoresis in which a polyacrylamide gel is used as the diffusion medium.
Established cell cultures that have the potential to propagate indefinitely.
Glycoproteins with a molecular weight of approximately 620,000 to 680,000. Precipitation by electrophoresis is in the alpha region. They include alpha 1-macroglobulins and alpha 2-macroglobulins. These proteins exhibit trypsin-, chymotrypsin-, thrombin-, and plasmin-binding activity and function as hormonal transporters.
A secretory proteinase inhibitory protein that was initially purified from human SKIN. It is found in a variety mucosal secretions and is present at high levels in SPUTUM. Elafin may play a role in the innate immunity (IMMUNITY, INNATE) response of the LUNG.
Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures.
Cysteine proteinase found in many tissues. Hydrolyzes a variety of endogenous proteins including NEUROPEPTIDES; CYTOSKELETAL PROTEINS; proteins from SMOOTH MUSCLE; CARDIAC MUSCLE; liver; platelets; and erythrocytes. Two subclasses having high and low calcium sensitivity are known. Removes Z-discs and M-lines from myofibrils. Activates phosphorylase kinase and cyclic nucleotide-independent protein kinase. This enzyme was formerly listed as EC 3.4.22.4.
A ubiquitously-expressed cysteine protease that plays an enzymatic role in POST-TRANSLATIONAL PROTEIN PROCESSING of proteins within SECRETORY GRANULES.
The process of cleaving a chemical compound by the addition of a molecule of water.
ENDOPEPTIDASES which use a metal such as ZINC in the catalytic mechanism.
The parts of a macromolecule that directly participate in its specific combination with another molecule.
A serine protease found in the azurophil granules of NEUTROPHILS. It has an enzyme specificity similar to that of chymotrypsin C.
A pancreatic trypsin inhibitor common to all mammals. It is secreted with the zymogens into the pancreatic juice. It is a protein composed of 56 amino acid residues and is different in amino acid composition and physiological activity from the Kunitz bovine pancreatic trypsin inhibitor (APROTININ).
Proteins encoded by a VIRAL GENOME that are produced in the organisms they infect, but not packaged into the VIRUS PARTICLES. Some of these proteins may play roles within the infected cell during VIRUS REPLICATION or act in regulation of virus replication or VIRUS ASSEMBLY.
A family of neutral serine proteases with CHYMOTRYPSIN-like activity. Chymases are primarily found in the SECRETORY GRANULES of MAST CELLS and are released during mast cell degranulation.
Any of various enzymatically catalyzed post-translational modifications of PEPTIDES or PROTEINS in the cell of origin. These modifications include carboxylation; HYDROXYLATION; ACETYLATION; PHOSPHORYLATION; METHYLATION; GLYCOSYLATION; ubiquitination; oxidation; proteolysis; and crosslinking and result in changes in molecular weight and electrophoretic motility.
The degree of similarity between sequences of amino acids. This information is useful for the analyzing genetic relatedness of proteins and species.
The quantity of measurable virus in a body fluid. Change in viral load, measured in plasma, is sometimes used as a SURROGATE MARKER in disease progression.
Urea compounds which are substituted with one or more methyl groups.
The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments.
The insertion of recombinant DNA molecules from prokaryotic and/or eukaryotic sources into a replicating vehicle, such as a plasmid or virus vector, and the introduction of the resultant hybrid molecules into recipient cells without altering the viability of those cells.
Keto-pyrans.
Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.
Agents used in the prophylaxis or therapy of VIRUS DISEASES. Some of the ways they may act include preventing viral replication by inhibiting viral DNA polymerase; binding to specific cell-surface receptors and inhibiting viral penetration or uncoating; inhibiting viral protein synthesis; or blocking late stages of virus assembly.
A proteolytic enzyme obtained from Carica papaya. It is also the name used for a purified mixture of papain and CHYMOPAPAIN that is used as a topical enzymatic debriding agent. EC 3.4.22.2.
Glycoprotein found in alpha(1)-globulin region in human serum. It inhibits chymotrypsin-like proteinases in vivo and has cytotoxic killer-cell activity in vitro. The protein also has a role as an acute-phase protein and is active in the control of immunologic and inflammatory processes, and as a tumor marker. It is a member of the serpin superfamily.
Physiologically inactive substances that can be converted to active enzymes.
Cleavage of proteins into smaller peptides or amino acids either by PROTEASES or non-enzymatically (e.g., Hydrolysis). It does not include Protein Processing, Post-Translational.
Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques.
Proteolytic enzymes from the serine endopeptidase family found in normal blood and urine. Specifically, Kallikreins are potent vasodilators and hypotensives and increase vascular permeability and affect smooth muscle. They act as infertility agents in men. Three forms are recognized, PLASMA KALLIKREIN (EC 3.4.21.34), TISSUE KALLIKREIN (EC 3.4.21.35), and PROSTATE-SPECIFIC ANTIGEN (EC 3.4.21.77).
The level of protein structure in which combinations of secondary protein structures (alpha helices, beta sheets, loop regions, and motifs) pack together to form folded shapes called domains. Disulfide bridges between cysteines in two different parts of the polypeptide chain along with other interactions between the chains play a role in the formation and stabilization of tertiary structure. Small proteins usually consist of only one domain but larger proteins may contain a number of domains connected by segments of polypeptide chain which lack regular secondary structure.
A family of neutral serine proteases with TRYPSIN-like activity. Tryptases are primarily found in the SECRETORY GRANULES of MAST CELLS and are released during mast cell degranulation.
Linear POLYPEPTIDES that are synthesized on RIBOSOMES and may be further modified, crosslinked, cleaved, or assembled into complex proteins with several subunits. The specific sequence of AMINO ACIDS determines the shape the polypeptide will take, during PROTEIN FOLDING, and the function of the protein.
The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.
Therapy with two or more separate preparations given for a combined effect.
Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.
The study of crystal structure using X-RAY DIFFRACTION techniques. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
The normality of a solution with respect to HYDROGEN ions; H+. It is related to acidity measurements in most cases by pH = log 1/2[1/(H+)], where (H+) is the hydrogen ion concentration in gram equivalents per liter of solution. (McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)
Members of the peptidase C19 family which regulate signal transduction by removing UBIQUITIN from specific protein substrates via a process known as deubiquitination or deubiquitylation.
The action of a drug that may affect the activity, metabolism, or toxicity of another drug.
A species of gram-negative, facultatively anaerobic, rod-shaped bacteria (GRAM-NEGATIVE FACULTATIVELY ANAEROBIC RODS) commonly found in the lower part of the intestine of warm-blooded animals. It is usually nonpathogenic, but some strains are known to produce DIARRHEA and pyogenic infections. Pathogenic strains (virotypes) are classified by their specific pathogenic mechanisms such as toxins (ENTEROTOXIGENIC ESCHERICHIA COLI), etc.
The arrangement of two or more amino acid or base sequences from an organism or organisms in such a way as to align areas of the sequences sharing common properties. The degree of relatedness or homology between the sequences is predicted computationally or statistically based on weights assigned to the elements aligned between the sequences. This in turn can serve as a potential indicator of the genetic relatedness between the organisms.
The number of CD4-POSITIVE T-LYMPHOCYTES per unit volume of BLOOD. Determination requires the use of a fluorescence-activated flow cytometer.
Conversion of an inactive form of an enzyme to one possessing metabolic activity. It includes 1, activation by ions (activators); 2, activation by cofactors (coenzymes); and 3, conversion of an enzyme precursor (proenzyme or zymogen) to an active enzyme.
A serine endopeptidase isolated from Bacillus subtilis. It hydrolyzes proteins with broad specificity for peptide bonds, and a preference for a large uncharged residue in P1. It also hydrolyzes peptide amides. (From Enzyme Nomenclature, 1992) EC 3.4.21.62.
A product of the lysis of plasminogen (profibrinolysin) by PLASMINOGEN activators. It is composed of two polypeptide chains, light (B) and heavy (A), with a molecular weight of 75,000. It is the major proteolytic enzyme involved in blood clot retraction or the lysis of fibrin and quickly inactivated by antiplasmins.
A cytastin subtype found at high levels in the SKIN and in BLOOD CELLS. Cystatin A incorporates into the cornified cell envelope of stratified squamous epithelial cells and may play a role in bacteriostatic properties of skin.
Members of the class of compounds composed of AMINO ACIDS joined together by peptide bonds between adjacent amino acids into linear, branched or cyclical structures. OLIGOPEPTIDES are composed of approximately 2-12 amino acids. Polypeptides are composed of approximately 13 or more amino acids. PROTEINS are linear polypeptides that are normally synthesized on RIBOSOMES.
Deficiency of the protease inhibitor ALPHA 1-ANTITRYPSIN that manifests primarily as PULMONARY EMPHYSEMA and LIVER CIRRHOSIS.
An ATP-dependent protease found in prokaryotes, CHLOROPLASTS, and MITOCHONDRIA. It is a soluble multisubunit complex that plays a role in the degradation of many abnormal proteins.
One of the mechanisms by which CELL DEATH occurs (compare with NECROSIS and AUTOPHAGOCYTOSIS). Apoptosis is the mechanism responsible for the physiological deletion of cells and appears to be intrinsically programmed. It is characterized by distinctive morphologic changes in the nucleus and cytoplasm, chromatin cleavage at regularly spaced sites, and the endonucleolytic cleavage of genomic DNA; (DNA FRAGMENTATION); at internucleosomal sites. This mode of cell death serves as a balance to mitosis in regulating the size of animal tissues and in mediating pathologic processes associated with tumor growth.
Proteins found in any species of bacterium.
Inhibitors of SERINE ENDOPEPTIDASES and sulfhydryl group-containing enzymes. They act as alkylating agents and are known to interfere in the translation process.
Proteases which use a metal, normally ZINC, in the catalytic mechanism. This group of enzymes is inactivated by metal CHELATORS.
Peptides composed of two amino acid units.
Cyclic compounds with a ring size of approximately 1-4 dozen atoms.
Identification of proteins or peptides that have been electrophoretically separated by blot transferring from the electrophoresis gel to strips of nitrocellulose paper, followed by labeling with antibody probes.
RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.
A long pro-domain caspase that has specificity for the precursor form of INTERLEUKIN-1BETA. It plays a role in INFLAMMATION by catalytically converting the inactive forms of CYTOKINES such as interleukin-1beta to their active, secreted form. Caspase 1 is referred as interleukin-1beta converting enzyme and is frequently abbreviated ICE.
Activated form of factor XI. In the intrinsic pathway, Factor XI is activated to XIa by factor XIIa in the presence of cofactor HMWK; (HIGH MOLECULAR WEIGHT KININOGEN). Factor XIa then activates factor IX to factor IXa in the presence of calcium.
Ribonucleic acid that makes up the genetic material of viruses.
Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed.
The naturally occurring or experimentally induced replacement of one or more AMINO ACIDS in a protein with another. If a functionally equivalent amino acid is substituted, the protein may retain wild-type activity. Substitution may also diminish, enhance, or eliminate protein function. Experimentally induced substitution is often used to study enzyme activities and binding site properties.
Elements of limited time intervals, contributing to particular results or situations.
The process of intracellular viral multiplication, consisting of the synthesis of PROTEINS; NUCLEIC ACIDS; and sometimes LIPIDS, and their assembly into a new infectious particle.
The region of an enzyme that interacts with its substrate to cause the enzymatic reaction.
Serum proteins that inhibit, antagonize, or inactivate COMPLEMENT C1 or its subunits.
The relationship between the dose of an administered drug and the response of the organism to the drug.
A family of intracellular CYSTEINE ENDOPEPTIDASES that play a role in regulating INFLAMMATION and APOPTOSIS. They specifically cleave peptides at a CYSTEINE amino acid that follows an ASPARTIC ACID residue. Caspases are activated by proteolytic cleavage of a precursor form to yield large and small subunits that form the enzyme. Since the cleavage site within precursors matches the specificity of caspases, sequential activation of precursors by activated caspases can occur.
A lysosomal cysteine proteinase with a specificity similar to that of PAPAIN. The enzyme is present in a variety of tissues and is important in many physiological and pathological processes. In pathology, cathepsin B has been found to be involved in DEMYELINATION; EMPHYSEMA; RHEUMATOID ARTHRITIS, and NEOPLASM INVASIVENESS.
A genus of FLAVIVIRIDAE causing parenterally-transmitted HEPATITIS C which is associated with transfusions and drug abuse. Hepatitis C virus is the type species.
Chromatography on non-ionic gels without regard to the mechanism of solute discrimination.
Amidines substituted with a benzene group. Benzamidine and its derivatives are known as peptidase inhibitors.
Proteins that are present in blood serum, including SERUM ALBUMIN; BLOOD COAGULATION FACTORS; and many other types of proteins.
Human immunodeficiency virus. A non-taxonomic and historical term referring to any of two species, specifically HIV-1 and/or HIV-2. Prior to 1986, this was called human T-lymphotropic virus type III/lymphadenopathy-associated virus (HTLV-III/LAV). From 1986-1990, it was an official species called HIV. Since 1991, HIV was no longer considered an official species name; the two species were designated HIV-1 and HIV-2.
Synthetic or naturally occurring substances related to coumarin, the delta-lactone of coumarinic acid.
A single-pass type I membrane protein. It is cleaved by AMYLOID PRECURSOR PROTEIN SECRETASES to produce peptides of varying amino acid lengths. A 39-42 amino acid peptide, AMYLOID BETA-PEPTIDES is a principal component of the extracellular amyloid in SENILE PLAQUES.
The molecular designing of drugs for specific purposes (such as DNA-binding, enzyme inhibition, anti-cancer efficacy, etc.) based on knowledge of molecular properties such as activity of functional groups, molecular geometry, and electronic structure, and also on information cataloged on analogous molecules. Drug design is generally computer-assisted molecular modeling and does not include pharmacokinetics, dosage analysis, or drug administration analysis.
Proteins found in the PERIPLASM of organisms with cell walls.
A member of the serpin family of proteins that is found in plasma and urine. It is dependent on heparin and is able to inhibit activated PROTEIN C; THROMBIN; KALLIKREIN; and other SERINE ENDOPEPTIDASES.
Proteins which are found in membranes including cellular and intracellular membranes. They consist of two types, peripheral and integral proteins. They include most membrane-associated enzymes, antigenic proteins, transport proteins, and drug, hormone, and lectin receptors.
A di-isopropyl-fluorophosphate which is an irreversible cholinesterase inhibitor used to investigate the NERVOUS SYSTEM.
A class of morphologically heterogeneous cytoplasmic particles in animal and plant tissues characterized by their content of hydrolytic enzymes and the structure-linked latency of these enzymes. The intracellular functions of lysosomes depend on their lytic potential. The single unit membrane of the lysosome acts as a barrier between the enzymes enclosed in the lysosome and the external substrate. The activity of the enzymes contained in lysosomes is limited or nil unless the vesicle in which they are enclosed is ruptured. Such rupture is supposed to be under metabolic (hormonal) control. (From Rieger et al., Glossary of Genetics: Classical and Molecular, 5th ed)
Transport proteins that carry specific substances in the blood or across cell membranes.
Genetically engineered MUTAGENESIS at a specific site in the DNA molecule that introduces a base substitution, or an insertion or deletion.
An enzyme formed from PROTHROMBIN that converts FIBRINOGEN to FIBRIN.
Six-membered heterocycles containing an oxygen and a nitrogen.
Domesticated bovine animals of the genus Bos, usually kept on a farm or ranch and used for the production of meat or dairy products or for heavy labor.
A family of serine endopeptidases found in the SECRETORY GRANULES of LEUKOCYTES such as CYTOTOXIC T-LYMPHOCYTES and NATURAL KILLER CELLS. When secreted into the intercellular space granzymes act to eliminate transformed and virus-infected host cells.
OXAZINES with a fused BENZENE ring.
A reverse transcriptase encoded by the POL GENE of HIV. It is a heterodimer of 66 kDa and 51 kDa subunits that are derived from a common precursor protein. The heterodimer also includes an RNAse H activity (RIBONUCLEASE H, HUMAN IMMUNODEFICIENCY VIRUS) that plays an essential role the viral replication process.
Proteins found in any species of virus.
An essential branched-chain amino acid important for hemoglobin formation.
Organic compounds that generally contain an amino (-NH2) and a carboxyl (-COOH) group. Twenty alpha-amino acids are the subunits which are polymerized to form proteins.
The concentration of a compound needed to reduce population growth of organisms, including eukaryotic cells, by 50% in vitro. Though often expressed to denote in vitro antibacterial activity, it is also used as a benchmark for cytotoxicity to eukaryotic cells in culture.
Short sequences (generally about 10 base pairs) of DNA that are complementary to sequences of messenger RNA and allow reverse transcriptases to start copying the adjacent sequences of mRNA. Primers are used extensively in genetic and molecular biology techniques.
Single-stranded complementary DNA synthesized from an RNA template by the action of RNA-dependent DNA polymerase. cDNA (i.e., complementary DNA, not circular DNA, not C-DNA) is used in a variety of molecular cloning experiments as well as serving as a specific hybridization probe.
The genetic constitution of the individual, comprising the ALLELES present at each GENETIC LOCUS.
Recombinant proteins produced by the GENETIC TRANSLATION of fused genes formed by the combination of NUCLEIC ACID REGULATORY SEQUENCES of one or more genes with the protein coding sequences of one or more genes.
The blood/lymphlike nutrient fluid of some invertebrates.
A plasma alpha 2 glycoprotein that accounts for the major antithrombin activity of normal plasma and also inhibits several other enzymes. It is a member of the serpin superfamily.
A non-essential amino acid that is synthesized from GLUTAMIC ACID. It is an essential component of COLLAGEN and is important for proper functioning of joints and tendons.
Proteins encoded by the GAG GENE of the HUMAN IMMUNODEFICIENCY VIRUS.
Activated form of factor X that participates in both the intrinsic and extrinsic pathways of blood coagulation. It catalyzes the conversion of prothrombin to thrombin in conjunction with other cofactors.
Proteins synthesized by organisms belonging to the phylum ARTHROPODA. Included in this heading are proteins from the subdivisions ARACHNIDA; CRUSTACEA; and HORSESHOE CRABS. Note that a separate heading for INSECT PROTEINS is listed under this heading.
Proteins found in plants (flowers, herbs, shrubs, trees, etc.). The concept does not include proteins found in vegetables for which VEGETABLE PROTEINS is available.
Agents used to treat RETROVIRIDAE INFECTIONS.
A proprotein convertase with specificity for the proproteins of PROALBUMIN; COMPLEMENT 3C; and VON WILLEBRAND FACTOR. It has specificity for cleavage near paired ARGININE residues that are separated by two amino acids.
The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.
Proteolytic enzymes that are involved in the conversion of protein precursors such as peptide prohormones into PEPTIDE HORMONES. Some are ENDOPEPTIDASES, some are EXOPEPTIDASES.
An intracellular proteinase found in a variety of tissue. It has specificity similar to but narrower than that of pepsin A. The enzyme is involved in catabolism of cartilage and connective tissue. EC 3.4.23.5. (Formerly EC 3.4.4.23).
A collection of heterogenous conditions resulting from defective LIPID METABOLISM and characterized by ADIPOSE TISSUE atrophy. Often there is redistribution of body fat resulting in peripheral fat wasting and central adiposity. They include generalized, localized, congenital, and acquired lipodystrophy.
A short pro-domain caspase that plays an effector role in APOPTOSIS. It is activated by INITIATOR CASPASES such as CASPASE 9. Isoforms of this protein exist due to multiple alternative splicing of its MESSENGER RNA.
Cells grown in vitro from neoplastic tissue. If they can be established as a TUMOR CELL LINE, they can be propagated in cell culture indefinitely.
A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by an azido group. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA during reverse transcription. It improves immunologic function, partially reverses the HIV-induced neurological dysfunction, and improves certain other clinical abnormalities associated with AIDS. Its principal toxic effect is dose-dependent suppression of bone marrow, resulting in anemia and leukopenia.
Separation technique in which the stationary phase consists of ion exchange resins. The resins contain loosely held small ions that easily exchange places with other small ions of like charge present in solutions washed over the resins.
Conjugated protein-carbohydrate compounds including mucins, mucoid, and amyloid glycoproteins.
The extent to which an enzyme retains its structural conformation or its activity when subjected to storage, isolation, and purification or various other physical or chemical manipulations, including proteolytic enzymes and heat.
Defective metabolism leading to fat maldistribution in patients infected with HIV. The etiology appears to be multifactorial and probably involves some combination of infection-induced alterations in metabolism, direct effects of antiretroviral therapy, and patient-related factors.
A proteolytic enzyme that converts PLASMINOGEN to FIBRINOLYSIN where the preferential cleavage is between ARGININE and VALINE. It was isolated originally from human URINE, but is found in most tissues of most VERTEBRATES.
The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.
Activated form of factor XII. In the initial event in the intrinsic pathway of blood coagulation, kallikrein (with cofactor HIGH MOLECULAR WEIGHT KININOGEN) cleaves factor XII to XIIa. Factor XIIa is then further cleaved by kallikrein, plasmin, and trypsin to yield smaller factor XII fragments (Hageman-Factor fragments). These fragments increase the activity of prekallikrein to kallikrein but decrease the procoagulant activity of factor XII.
Proteins encoded by the POL GENE of the HUMAN IMMUNODEFICIENCY VIRUS.
A mixture of related phosphoproteins occurring in milk and cheese. The group is characterized as one of the most nutritive milk proteins, containing all of the common amino acids and rich in the essential ones.
Immunologic method used for detecting or quantifying immunoreactive substances. The substance is identified by first immobilizing it by blotting onto a membrane and then tagging it with labeled antibodies.
A large multisubunit complex that plays an important role in the degradation of most of the cytosolic and nuclear proteins in eukaryotic cells. It contains a 700-kDa catalytic sub-complex and two 700-kDa regulatory sub-complexes. The complex digests ubiquitinated proteins and protein activated via ornithine decarboxylase antizyme.
A chromatographic technique that utilizes the ability of biological molecules to bind to certain ligands specifically and reversibly. It is used in protein biochemistry. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
Granular leukocytes having a nucleus with three to five lobes connected by slender threads of chromatin, and cytoplasm containing fine inconspicuous granules and stainable by neutral dyes.
A family of iminourea derivatives. The parent compound has been isolated from mushrooms, corn germ, rice hulls, mussels, earthworms, and turnip juice. Derivatives may have antiviral and antifungal properties.
The property of objects that determines the direction of heat flow when they are placed in direct thermal contact. The temperature is the energy of microscopic motions (vibrational and translational) of the particles of atoms.
An analytical method used in determining the identity of a chemical based on its mass using mass analyzers/mass spectrometers.
The uptake of naked or purified DNA by CELLS, usually meaning the process as it occurs in eukaryotic cells. It is analogous to bacterial transformation (TRANSFORMATION, BACTERIAL) and both are routinely employed in GENE TRANSFER TECHNIQUES.
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
The relationships of groups of organisms as reflected by their genetic makeup.
Serum proteins that have the most rapid migration during ELECTROPHORESIS. This subgroup of globulins is divided into faster and slower alpha(1)- and alpha(2)-globulins.
The outward appearance of the individual. It is the product of interactions between genes, and between the GENOTYPE and the environment.
A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.
The phenotypic manifestation of a gene or genes by the processes of GENETIC TRANSCRIPTION and GENETIC TRANSLATION.
The facilitation of a chemical reaction by material (catalyst) that is not consumed by the reaction.

Crystal structure of MHC class II-associated p41 Ii fragment bound to cathepsin L reveals the structural basis for differentiation between cathepsins L and S. (1/5338)

The lysosomal cysteine proteases cathepsins S and L play crucial roles in the degradation of the invariant chain during maturation of MHC class II molecules and antigen processing. The p41 form of the invariant chain includes a fragment which specifically inhibits cathepsin L but not S. The crystal structure of the p41 fragment, a homologue of the thyroglobulin type-1 domains, has been determined at 2.0 A resolution in complex with cathepsin L. The structure of the p41 fragment demonstrates a novel fold, consisting of two subdomains, each stabilized by disulfide bridges. The first subdomain is an alpha-helix-beta-strand arrangement, whereas the second subdomain has a predominantly beta-strand arrangement. The wedge shape and three-loop arrangement of the p41 fragment bound to the active site cleft of cathepsin L are reminiscent of the inhibitory edge of cystatins, thus demonstrating the first example of convergent evolution observed in cysteine protease inhibitors. However, the different fold of the p41 fragment results in additional contacts with the top of the R-domain of the enzymes, which defines the specificity-determining S2 and S1' substrate-binding sites. This enables inhibitors based on the thyroglobulin type-1 domain fold, in contrast to the rather non-selective cystatins, to exhibit specificity for their target enzymes.  (+info)

Bile duct epithelial cells exposed to alpha-naphthylisothiocyanate produce a factor that causes neutrophil-dependent hepatocellular injury in vitro. (2/5338)

The acute hepatotoxicity induced by alpha-naphthylisothiocyanate (ANIT) in rats is manifested as neutrophil-dependent necrosis of bile duct epithelial cells (BDECs) and hepatic parenchymal cells. This hepatotoxicity mirrors that of drug-induced cholangiolitic hepatitis in humans. Since BDECs are primary targets of ANIT-induced toxicity, we hypothesized that after exposure to ANIT, BDECs produce a factor(s) that causes neutrophil chemotaxis and neutrophil-dependent hepatocellular injury. To test this hypothesis BDECs were isolated from male Sprague Dawley rats and incubated with ANIT (6.25, 12.5, 25, or 50 microM) or vehicle for 24 h. The conditioned medium (CM) was collected and placed in the bottom chamber of a two-chambered chemotaxis system, while isolated neutrophils were placed in the top chamber. Chemotaxis was indicated by neutrophil migration through a membrane to the bottom chamber. CM from BDECs exposed to each concentration of ANIT was chemotactic, whereas CM from vehicle-treated BDECs was not. ANIT alone caused a modest degree of chemotaxis at 50 microM. The conditioned media were added to isolated hepatocytes or to hepatocyte-neutrophil cocultures and incubated for 24 h. Hepatocyte toxicity was indicated by alanine aminotransferase release into the culture medium. CM from vehicle-treated BDECs did not cause hepatocyte killing in either hepatocyte-neutrophil cocultures or hepatocyte cultures. In contrast, the addition of CM from ANIT-treated BDECs (CM-BDEC-A) to hepatocyte-neutrophil cocultures resulted in hepatocyte killing. The same CM was not cytotoxic to hepatocyte cultures devoid of neutrophils. The hepatocyte killing could not be explained by residual ANIT in the CM, which was below the limit of detection (< or = 0.5 microM). The addition of antiproteases afforded protection against neutrophil-dependent hepatocellular injury induced by CM-BDEC-A. These results indicate that ANIT causes BDECs to release a factor(s) that attracts neutrophils and stimulates them to injure hepatocytes in vitro.  (+info)

A new sugar chain of the proteinase inhibitor from latex of Carica papaya. (3/5338)

The structure of a sugar chain of the proteinase inhibitor from the latex of Carica papaya was studied. Sugar chains liberated on hydrazinolysis were N-acetylated, and their reducing-end residues were tagged with 2-aminopyridine. One major sugar chain was detected on size-fractionation and reversed-phase HPLC analyses. The structure of the PA-sugar chain was determined by two-dimensional sugar mapping combined with sequential exoglycosidase digestion and partial acid hydrolysis, and by 750 MHz 1H-NMR spectroscopy. The structure found was Manalpha1-6(Manalpha1-3)Manalpha1-6(Manalpha1-3) (Xylbeta1-2)Manbeta1- 4GlcNAcbeta1-4(Fucalpha1-3)GlcNAc. This sugar chain represents a new plant-type sugar chain with five mannose residues.  (+info)

CD44 cleavage induced by a membrane-associated metalloprotease plays a critical role in tumor cell migration. (4/5338)

CD44 is a cell surface receptor for hyaluronate, a component of the extracellular matrix (ECM). Although CD44 has been implicated in tumor invasion and metastasis, the molecular mechanisms remain to be elucidated. Here we find that CD44 expressed in cancer cells is cleaved at the membrane-proximal region of the ectodomain and the membrane-bound cleavage product can be detected using an antibody against the cytoplasmic domain of CD44. Furthermore, we report that CD44 cleavage is mediated by a membrane-associated metalloprotease expressed in cancer cells. A tissue inhibitor of metalloproteases-1 (TIMP-1), as well as metalloprotease inhibitors, inhibit CD44 cleavage in the cell-free assay. Contrary, serine protease inhibitors enhance CD44 cleavage, and the enhancement can be prevented by pretreatment with a metalloprotease inhibitor. Thus, CD44 cleavage is regulated by an intricate balance between some proteases and their inhibitors. Interestingly, treatment with the metalloprotease blocker 1,10-phenanthroline, which strongly prevent the CD44 cleavage, suppressed RERF-LC-OK lung cancer cell migration on a hyaluronate substrate, but not on several other substrates. These results suggest that CD44 cleavage plays a critical role in an efficient cell-detachment from a hyaluronate substrate during the cell migration and consequently promotes CD44-mediated cancer cell migration. Our present data indicate that CD44, not only ECM per se, is one of the targets of pericellular proteolysis involved in tumor invasion and metastasis.  (+info)

Role of proteases in implantation. (5/5338)

Implantation of the embryo into the endometrium is a critical step in the establishment of pregnancy and the failure of embryos to implant is a major limiting factor in the success of reproductive technologies. Furthermore, one or more of the molecules of importance at implantation could provide a suitable target for post-coital contraception. While there is considerable species variation in the extent to which the trophoblast invades the maternal endometrium and makes contact with the maternal blood supply, many of the molecular mechanisms are conserved among species. Three families of protease are involved in the matrix degradation required for implantation: the cysteine, serine and matrix metalloproteinases. Other proteases are required for the activation of regulatory molecules. Although trophoblast from all species appears to have a high invasive potential, this is limited by the presence of partner protease inhibitors, the presence of which provides restraint to this invasion. It is the balance between the proteases and their inhibitors at any focal point that determines the site and extent of trophoblast invasion. This review examines the literature regarding proteases and their inhibitors at early implantation sites across a range of species with very different forms of placentation and evaluates their common features and their dissimilarities.  (+info)

Dietary fish oils inhibit early events in the assembly of very low density lipoproteins and target apoB for degradation within the rough endoplasmic reticulum of hamster hepatocytes. (6/5338)

Dietary fish oils inhibited secretion and stimulated intracellular degradation of apolipoprotein (apo)B in hamster hepatocytes, while dietary sunflower oils stimulated secretion and had no effect on degradation of apoB. To investigate the intracellular site at which fish oils act, we have made use of our previous observations that inhibition of degradation by N-acetyl-leucyl-leucyl-norleucinal (ALLN) results in accumulation of apoB in the trans -Golgi membrane and does not stimulate secretion, while inhibition of degradation by o-phenanthroline results in accumulation of apoB in the rough endoplasmic reticulum membrane and stimulates secretion. Thus, ALLN protects apoB which has been diverted from secretion and o -phenanthroline protects apoB which is targetted for secretion. Addition of o -phenantholine to the incubation medium of hepatocytes from fish oil-fed hamsters inhibited degradation of apoB and stimulated its secretion in particles of the density of VLDL, while addition of ALLN had no effect. These observations suggest that dietary fish oils reversibly inhibit early steps in the assembly of very low density lipoprotein precursors and target apoB for degradation in the rough endoplasmic reticulum.  (+info)

Suppression of experimental abdominal aortic aneurysms by systemic treatment with a hydroxamate-based matrix metalloproteinase inhibitor (RS 132908). (7/5338)

BACKGROUND: Abdominal aortic aneurysms (AAAs) are associated with chronic inflammation, disruption of medial elastin, and increased local production of elastolytic matrix metalloproteinases (MMPs). The purpose of this study was to investigate how treatment with a hydroxamate-based MMP antagonist (RS 132908) might affect the development of experimental AAAs. METHODS: Male Wistar rats underwent intraluminal perfusion of the abdominal aorta with 50 units of porcine pancreatic elastase followed by treatment for 14 days with RS 132908 (100 mg/kg/day subcutaneously; n = 8) or with vehicle alone (n = 6). The external aortic diameter (AD) was measured in millimeters before elastase perfusion and at death, with AAA defined as an increase in AD (DeltaAD) of at least 100%. Aortic wall elastin and collagen concentrations were measured with assays for desmosine and hydroxyproline, and fixed aortic tissues were examined by light microscopy. RESULTS: AAAs developed in all vehicle-treated rats, with a mean AD (+/- SE) that increased from 1.60 +/- 0.03 mm before perfusion to 5.98 +/- 1.02 mm on day 14 (DeltaAD = 276.4 +/- 67.7%). AAAs developed in only five of eight animals (62.5%) after MMP inhibition, with a mean AD that increased from 1.56 +/- 0.05 mm to 3.59 +/- 0.34 mm (DeltaAD = 128.1 +/- 18.7%; P <.05, vs vehicle). The overall inhibition of aortic dilatation attributable to RS 132908 was 53.6 +/- 6.8%. Aortic wall desmosine fell by 85.4% in the vehicle-treated rats (1210.6 +/- 87.8 pmol/sample to 176.7 +/- 33.4 pmol/sample; P <.05) but only by 65.6% in the animals treated with RS 312908 (416.2 +/- 120.5 pmol/sample). In contrast, hydroxyproline was not significantly affected by either elastase perfusion or drug treatment. Microscopic examination revealed the preservation of pericellular elastin and a greater degree of fibrocollagenous wall thickening after MMP inhibition, with no detectable difference in the extent of inflammation. CONCLUSIONS: Systemic MMP inhibition suppresses aneurysmal dilatation in the elastase-induced rodent model of AAA. Consistent with its direct inhibitory effect on various MMPs, RS 132908 promotes the preservation of aortic elastin and appears to enhance a profibrotic response within the aortic wall. Hydroxamate-based MMP antagonists may therefore be useful in the development of pharmacologic approaches to the suppression of AAAs.  (+info)

HaCaT human keratinocytes express IGF-II, IGFBP-6, and an acid-activated protease with activity against IGFBP-6. (8/5338)

The insulin-like growth factor (IGF) system plays an important role in skin. HaCaT human keratinocytes proliferate in response to IGFs and synthesize IGF-binding protein-3 (IGFBP-3). Recently, IGFBP-6 was also identified by NH2-terminal sequencing, but it has not been identified by Western ligand blotting. In the present study, IGFBP-6 was detected in HaCaT-conditioned medium by use of immunoblotting and Western ligand blotting with 125I-labeled IGF-II. Proteolytic activity against IGFBPs, an important mechanism for regulation of their activity, was then studied. An acid-activated, cathepsin D-like protease that cleaved both IGFBP-6 and IGFBP-3 was detected. Although proteolysis did not substantially reduce the size of immunoreactive IGFBP-6, it greatly reduced the ability of IGFBP-6 to bind 125I-IGF-II as determined by Western ligand blotting and solution assay. HaCaT keratinocytes do not express IGF-I mRNA, but IGF-II mRNA and protein expression was detected. These observations suggest the possibility of an autocrine IGF-II loop that is regulated by the relative expression of IGF-II, IGFBP-3, and IGFBP-6, and IGFBP proteases in these keratinocytes, although demonstration of this loop requires further study.  (+info)

HIV (human immunodeficiency virus) infection is a condition in which the body is infected with HIV, a type of retrovirus that attacks the body's immune system. HIV infection can lead to AIDS (acquired immunodeficiency syndrome), a condition in which the immune system is severely damaged and the body is unable to fight off infections and diseases.

There are several ways that HIV can be transmitted, including:

1. Sexual contact with an infected person
2. Sharing of needles or other drug paraphernalia with an infected person
3. Mother-to-child transmission during pregnancy, childbirth, or breastfeeding
4. Blood transfusions ( although this is rare in developed countries due to screening processes)
5. Organ transplantation (again, rare)

The symptoms of HIV infection can be mild at first and may not appear until several years after infection. These symptoms can include:

1. Fever
2. Fatigue
3. Swollen glands in the neck, armpits, and groin
4. Rash
5. Muscle aches and joint pain
6. Night sweats
7. Diarrhea
8. Weight loss

If left untreated, HIV infection can progress to AIDS, which is a life-threatening condition that can cause a wide range of symptoms, including:

1. Opportunistic infections (such as pneumocystis pneumonia)
2. Cancer (such as Kaposi's sarcoma)
3. Wasting syndrome
4. Neurological problems (such as dementia and seizures)

HIV infection is diagnosed through a combination of blood tests and physical examination. Treatment typically involves antiretroviral therapy (ART), which is a combination of medications that work together to suppress the virus and slow the progression of the disease.

Prevention methods for HIV infection include:

1. Safe sex practices, such as using condoms and dental dams
2. Avoiding sharing needles or other drug-injecting equipment
3. Avoiding mother-to-child transmission during pregnancy, childbirth, or breastfeeding
4. Post-exposure prophylaxis (PEP), which is a short-term treatment that can prevent infection after potential exposure to the virus
5. Pre-exposure prophylaxis (PrEP), which is a daily medication that can prevent infection in people who are at high risk of being exposed to the virus.

It's important to note that HIV infection is manageable with proper treatment and care, and that people living with HIV can lead long and healthy lives. However, it's important to be aware of the risks and take steps to prevent transmission.

People with AATD have low levels of functional AAT in their blood, which can lead to premature lung disease and liver disease. The most common form of AATD is caused by the Pi*Z phenotype, which results from a missense mutation in the SERPINA1 gene. This mutation leads to misfolding and accumulation of AAT in the liver, where it is normally broken down and secreted into the bloodstream.

The most common symptoms of AATD are:

* Chronic obstructive pulmonary disease (COPD)
* Emphysema
* Lung fibrosis
* Liver cirrhosis
* Gallstones

The diagnosis of AATD is based on a combination of clinical symptoms, laboratory tests, and genetic analysis. Treatment for AATD typically involves managing the underlying symptoms and preventing complications. For example, individuals with COPD may receive bronchodilators and corticosteroids to help improve lung function and reduce inflammation. Liver disease may be treated with medications to slow the progression of cirrhosis or with liver transplantation in severe cases.

The goal of genetic counseling for AATD is to provide information about the risk of transmitting the disorder to offspring and to discuss options for prenatal testing and family planning. Prenatal testing can be performed on a fetus by analyzing a sample of cells from the placenta or amniotic fluid. Carrier testing can also be performed in individuals who have a family history of AATD.

The prognosis for AATD varies depending on the severity of the mutation and the specific symptoms present. With appropriate management, many individuals with AATD can lead active and productive lives. However, the disorder can be severe and life-threatening in some cases, especially if left untreated or if there is a delay in diagnosis.

Currently, there is no cure for AATD, and treatment is focused on managing symptoms and preventing complications. However, research into the genetics of AATD is ongoing, and new developments in gene therapy and other areas may provide hope for improved treatments and outcomes in the future.

Lipodystrophy can be caused by genetic mutations, hormonal imbalances, or certain medications. It can also be associated with other medical conditions such as metabolic disorders, endocrine problems, and neurological diseases.

The symptoms of lipodystrophy can vary depending on the type and severity of the condition. Common symptoms include:

1. Muscle wasting and weakness
2. Fat redistribution to certain areas of the body (such as the face, neck, and torso)
3. Metabolic problems such as insulin resistance and high blood sugar
4. Hormonal imbalances
5. Abnormal body shape and proportions
6. Poor wound healing
7. Easy bruising and bleeding
8. Increased risk of infections
9. Joint pain and stiffness
10. Mood changes such as depression, anxiety, and irritability

Treatment for lipodystrophy depends on the underlying cause of the condition. Medications, lifestyle modifications, and surgery may be used to manage symptoms and improve quality of life. In some cases, lipodystrophy can be a sign of an underlying medical condition that needs to be treated.

Lipodystrophy can have a significant impact on an individual's quality of life, affecting their physical appearance, self-esteem, and ability to perform daily activities. It is important to seek medical attention if symptoms persist or worsen over time. With proper diagnosis and treatment, individuals with lipodystrophy can improve their symptoms and overall health.

HALS typically involves the accumulation of fat in the face, neck, and torso, while the arms and legs become thin and wasted. This can lead to a characteristic "buffalo hump" appearance on the back of the neck and a "spare tire" around the waist. In addition to the cosmetic changes, HALS can also cause metabolic problems such as insulin resistance, high blood sugar, and high levels of lipids (fats) in the blood.

HIV-associated lipodystrophy syndrome is thought to be caused by a combination of factors, including genetics, hormonal imbalances, and side effects of certain HIV medications. Treatment for HALS typically involves a multidisciplinary approach, including lifestyle modifications such as diet and exercise, as well as medication therapy to manage metabolic abnormalities and reduce the risk of cardiovascular disease.

HIV-associated lipodystrophy syndrome is a significant health concern for individuals living with HIV, as it can increase the risk of other serious health problems such as heart disease and stroke. It is important for individuals infected with HIV to be aware of the risk of developing HALS and to work closely with their healthcare provider to manage this condition effectively.

The symptoms of AIDS can vary depending on the individual and the stage of the disease. Common symptoms include:

1. Fever
2. Fatigue
3. Swollen glands
4. Rash
5. Muscle aches and joint pain
6. Night sweats
7. Diarrhea
8. Weight loss
9. Memory loss and other neurological problems
10. Cancer and other opportunistic infections.

AIDS is diagnosed through blood tests that detect the presence of HIV antibodies or the virus itself. There is no cure for AIDS, but antiretroviral therapy (ART) can help manage the symptoms and slow the progression of the disease. Prevention methods include using condoms, pre-exposure prophylaxis (PrEP), and avoiding sharing needles or other injection equipment.

In summary, Acquired Immunodeficiency Syndrome (AIDS) is a severe and life-threatening condition caused by the Human Immunodeficiency Virus (HIV). It is characterized by a severely weakened immune system, which makes it difficult to fight off infections and diseases. While there is no cure for AIDS, antiretroviral therapy can help manage the symptoms and slow the progression of the disease. Prevention methods include using condoms, pre-exposure prophylaxis, and avoiding sharing needles or other injection equipment.

Symptoms of ichthyosis can include:

* Thickened, scaly skin on the arms, legs, back, and chest
* Redness and itching
* Cracking and splitting of the skin
* Increased risk of infection
* Respiratory problems

Treatment for ichthyosis typically involves the use of topical creams and ointments to help soften and hydrate the skin, as well as oral medications to reduce inflammation and itching. In severe cases, phototherapy or systemic corticosteroids may be necessary.

In addition to these medical treatments, there are also several home remedies and lifestyle modifications that can help manage the symptoms of ichthyosis. These include:

* Moisturizing regularly with a fragrance-free moisturizer
* Avoiding harsh soaps and cleansers
* Using lukewarm water when showering or bathing
* Applying cool compresses to the skin to reduce redness and inflammation
* Wearing loose, breathable clothing to avoid irritating the skin
* Protecting the skin from extreme temperatures and environmental stressors.

There are several types of hepatitis C, including genotype 1, which is the most common and accounts for approximately 70% of cases in the United States. Other genotypes include 2, 3, 4, 5, and 6. The symptoms of hepatitis C can range from mild to severe and may include fatigue, fever, loss of appetite, nausea, vomiting, joint pain, jaundice (yellowing of the skin and eyes), dark urine, pale stools, and itching all over the body. Some people with hepatitis C may not experience any symptoms at all.

Hepatitis C is diagnosed through a combination of blood tests that detect the presence of antibodies against HCV or the virus itself. Treatment typically involves a combination of medications, including interferon and ribavirin, which can cure the infection but may have side effects such as fatigue, nausea, and depression. In recent years, new drugs known as direct-acting antivirals (DAAs) have become available, which can cure the infection with fewer side effects and in a shorter period of time.

Prevention measures for hepatitis C include avoiding sharing needles or other drug paraphernalia, using condoms to prevent sexual transmission, and ensuring that any tattoos or piercings are performed with sterilized equipment. Vaccines are also available for people who are at high risk of contracting the virus, such as healthcare workers and individuals who engage in high-risk behaviors.

Overall, hepatitis C is a serious and common liver disease that can lead to significant health complications if left untreated. Fortunately, with advances in medical technology and treatment options, it is possible to manage and cure the virus with proper care and attention.

The symptoms of chronic hepatitis C may be mild or absent, but some people experience fatigue, joint pain, muscle aches, nausea, loss of appetite, and jaundice (yellowing of the skin and eyes).

Chronic hepatitis C is usually diagnosed through blood tests that detect the presence of antibodies against HCV or the virus itself. Imaging tests such as ultrasound and liver biopsy may also be performed to assess the extent of liver damage.

Treatment for chronic hepatitis C typically involves a combination of medications, including interferon and ribavirin, which can help clear the virus from the body. In severe cases, a liver transplant may be necessary. Prevention of the spread of HCV includes avoiding sharing of needles or other sharp objects, practicing safe sex, and getting tested for the virus before donating blood or organs.

See also: Hepatitis C; Liver; Virus

The main symptoms of Netherton Syndrome include:

1. Severe ichthyosis (dry, scaly skin)
2. Congenital papillomatoses (warts-like growths on the skin)
3. Ectodermal defects (abnormalities in the development of the skin, hair, and mucous membranes)
4. Respiratory problems (such as asthma or recurrent respiratory infections)
5. Increased risk of skin infections
6. Delayed physical growth and development
7. Abnormalities of the hair (such as thinning, brittleness, or absence of eyebrows and eyelashes)
8. Abnormalities of the nails (such as thickening, brittleness, or lack of nail plates)
9. Increased risk of allergies and atopic conditions (such as asthma or eczema)
10. Increased risk of eye problems (such as dry eyes, conjunctivitis, or cataracts)

Netherton Syndrome is usually diagnosed based on the presence of characteristic skin findings and the results of genetic testing. Treatment for the condition typically involves managing symptoms and preventing complications, such as using topical corticosteroids to reduce inflammation and prevent skin infections, and avoiding irritants that can exacerbate the condition. In some cases, surgery may be necessary to remove warts or other growths that are causing discomfort or difficulty.

1) They share similarities with humans: Many animal species share similar biological and physiological characteristics with humans, making them useful for studying human diseases. For example, mice and rats are often used to study diseases such as diabetes, heart disease, and cancer because they have similar metabolic and cardiovascular systems to humans.

2) They can be genetically manipulated: Animal disease models can be genetically engineered to develop specific diseases or to model human genetic disorders. This allows researchers to study the progression of the disease and test potential treatments in a controlled environment.

3) They can be used to test drugs and therapies: Before new drugs or therapies are tested in humans, they are often first tested in animal models of disease. This allows researchers to assess the safety and efficacy of the treatment before moving on to human clinical trials.

4) They can provide insights into disease mechanisms: Studying disease models in animals can provide valuable insights into the underlying mechanisms of a particular disease. This information can then be used to develop new treatments or improve existing ones.

5) Reduces the need for human testing: Using animal disease models reduces the need for human testing, which can be time-consuming, expensive, and ethically challenging. However, it is important to note that animal models are not perfect substitutes for human subjects, and results obtained from animal studies may not always translate to humans.

6) They can be used to study infectious diseases: Animal disease models can be used to study infectious diseases such as HIV, TB, and malaria. These models allow researchers to understand how the disease is transmitted, how it progresses, and how it responds to treatment.

7) They can be used to study complex diseases: Animal disease models can be used to study complex diseases such as cancer, diabetes, and heart disease. These models allow researchers to understand the underlying mechanisms of the disease and test potential treatments.

8) They are cost-effective: Animal disease models are often less expensive than human clinical trials, making them a cost-effective way to conduct research.

9) They can be used to study drug delivery: Animal disease models can be used to study drug delivery and pharmacokinetics, which is important for developing new drugs and drug delivery systems.

10) They can be used to study aging: Animal disease models can be used to study the aging process and age-related diseases such as Alzheimer's and Parkinson's. This allows researchers to understand how aging contributes to disease and develop potential treatments.

A type of pancreatitis that is caused by heavy and prolonged alcohol consumption. It is characterized by inflammation of the pancreas that can lead to scarring and impaired pancreatic function. Symptoms include abdominal pain, nausea, vomiting, fever, and diarrhea.

Etiology:

* Heavy and prolonged alcohol consumption (more than 4 drinks per day for men and more than 2 drinks per day for women)
* Binge drinking
* Poor nutrition
* Genetic predisposition

Pathophysiology:

* Alcohol causes pancreatic enzymes to activate prematurely, leading to autodigestion of the pancreas and inflammation
* Inflammation can lead to fibrosis and cirrhosis of the pancreas
* Chronic pancreatitis can lead to exocrine and endocrine insufficiency

Signs and Symptoms:

* Abdominal pain (midline, epigastric)
* Nausea and vomiting
* Fever
* Diarrhea
* Weight loss
* Jaundice

Diagnosis:

* Medical history and physical examination
* Laboratory tests (e.g., lipase, amylase, trypsinogen activation)
* Imaging studies (e.g., CT scan, MRI)

Treatment:

* Alcohol withdrawal and cessation
* Pain management (e.g., nonsteroidal anti-inflammatory drugs [NSAIDs], opioids)
* Nutritional support
* Pancreatic enzyme replacement therapy
* Antibiotics for infected pancreatitis

Prognosis:

* Chronic pancreatitis can lead to long-term impairment of pancreatic function and malnutrition
* Alcoholic pancreatitis is a leading cause of pancreatic cancer

Prevention:

* Avoid heavy and prolonged alcohol consumption
* Follow a healthy diet and lifestyle

Complications:

* Pancreatic cancer
* Chronic pancreatitis
* Pancreatic insufficiency
* Malnutrition
* Infections (e.g., pseudocysts, abscesses)

Epidemiology:

* Alcoholic pancreatitis is the most common form of acute pancreatitis
* The incidence of alcoholic pancreatitis has increased in recent years, possibly due to increased alcohol consumption and improved diagnostic tools
* Chronic pancreatitis affects approximately 5-10% of patients with alcoholic pancreatitis

Etiology:

* Alcohol (ethanol) consumption is the primary risk factor for both acute and chronic pancreatitis
* Other risk factors include gallstones, smoking, obesity, and certain medications (e.g., corticosteroids, NSAIDs)

Pathophysiology:

* Alcohol consumption can damage the pancreatic tissue and trigger an inflammatory response
* The pancreas is a vital organ that produces hormones (insulin, glucagon) and digestive enzymes. Damage to the pancreas can lead to impaired glucose metabolism and malnutrition.

Diagnosis:

* Clinical evaluation (history of alcohol consumption, symptoms, physical examination)
* Laboratory tests (blood tests, lipase levels)
* Imaging studies (CT scan, MRI)

Treatment:

* Supportive care (pain management, fluid replacement)
* Withdrawal of alcohol
* Anti-inflammatory medications (e.g., corticosteroids)
* Pancreatic enzyme replacement therapy
* Surgical intervention (e.g., pancreatectomy, cholecystectomy)

Prognosis:

* Acute pancreatitis has a high mortality rate if left untreated (approximately 20-30%)
* Chronic pancreatitis can lead to long-term morbidity and impaired quality of life

Complications:

* Infection (e.g., pneumonia, sepsis)
* Organ failure (e.g., respiratory, cardiovascular)
* Nutritional deficiencies (e.g., malnutrition, vitamin deficiencies)
* Psychological disorders (e.g., depression, anxiety)

There are several causes of pancreatitis, including:

1. Gallstones: These can block the pancreatic duct, causing inflammation.
2. Alcohol consumption: Heavy alcohol use can damage the pancreas and lead to inflammation.
3. High triglycerides: Elevated levels of triglycerides in the blood can cause pancreatitis.
4. Infections: Viral or bacterial infections can infect the pancreas and cause inflammation.
5. Genetic factors: Some people may be more susceptible to pancreatitis due to inherited genetic mutations.
6. Pancreatic trauma: Physical injury to the pancreas can cause inflammation.
7. Certain medications: Some medications, such as certain antibiotics and chemotherapy drugs, can cause pancreatitis as a side effect.

Symptoms of pancreatitis may include:

1. Abdominal pain
2. Nausea and vomiting
3. Fever
4. Diarrhea or bloating
5. Weight loss
6. Loss of appetite

Treatment for pancreatitis depends on the underlying cause and the severity of the condition. In some cases, hospitalization may be necessary to manage symptoms and address any complications. Treatment options may include:

1. Pain management: Medications such as nonsteroidal anti-inflammatory drugs (NSAIDs) or opioids may be used to manage abdominal pain.
2. Fluid replacement: Intravenous fluids may be given to replace lost fluids and electrolytes.
3. Antibiotics: If the pancreatitis is caused by an infection, antibiotics may be prescribed to treat the infection.
4. Nutritional support: Patients with pancreatitis may require nutritional support to ensure they are getting enough calories and nutrients.
5. Pancreatic enzyme replacement therapy: In some cases, pancreatic enzyme replacement therapy may be necessary to help the body digest food.
6. Surgery: In severe cases of pancreatitis, surgery may be necessary to remove damaged tissue or repair damaged blood vessels.

It is important to seek medical attention if you experience persistent abdominal pain or other symptoms of pancreatitis, as early treatment can help prevent complications and improve outcomes.

Acute angioedema is usually triggered by an allergic reaction or exposure to certain medications, such as nonsteroidal anti-inflammatory drugs (NSAIDs), blood pressure medications, or antibiotics. It can also be caused by infections, insect bites, and other environmental triggers.

Chronic angioedema, on the other hand, is a more persistent form of the condition that can last for weeks, months, or even years. It is often associated with conditions such as hereditary angioedema (HAE), which is caused by a genetic defect that affects the production of a protein called C1 esterase inhibitor.

The symptoms of angioedema can vary depending on the location and severity of the swelling, but they typically include:

* Swelling in the face, hands, feet, or other parts of the body
* Redness and warmth of the affected area
* Pain or discomfort
* Difficulty breathing or swallowing (in severe cases)

There is no cure for angioedema, but there are several treatments available to help manage the symptoms. These may include:

* Antihistamines or corticosteroids to reduce inflammation and relieve itching
* Ice packs or cool compresses to reduce swelling
* Compression stockings or bandages to prevent fluid buildup
* Pain relief medications, such as ibuprofen or acetaminophen, to manage discomfort

In severe cases of angioedema, hospitalization may be necessary to provide more intensive treatment and monitoring. In some cases, injectable medications such as epinephrine or corticosteroids may be administered to help reduce swelling and prevent complications.

Overall, angioedema is a serious condition that requires prompt medical attention to manage symptoms and prevent complications. If you suspect you or someone else may have angioedema, it is important to seek medical help right away.

There are several key features of inflammation:

1. Increased blood flow: Blood vessels in the affected area dilate, allowing more blood to flow into the tissue and bringing with it immune cells, nutrients, and other signaling molecules.
2. Leukocyte migration: White blood cells, such as neutrophils and monocytes, migrate towards the site of inflammation in response to chemical signals.
3. Release of mediators: Inflammatory mediators, such as cytokines and chemokines, are released by immune cells and other cells in the affected tissue. These molecules help to coordinate the immune response and attract more immune cells to the site of inflammation.
4. Activation of immune cells: Immune cells, such as macrophages and T cells, become activated and start to phagocytose (engulf) pathogens or damaged tissue.
5. Increased heat production: Inflammation can cause an increase in metabolic activity in the affected tissue, leading to increased heat production.
6. Redness and swelling: Increased blood flow and leakiness of blood vessels can cause redness and swelling in the affected area.
7. Pain: Inflammation can cause pain through the activation of nociceptors (pain-sensing neurons) and the release of pro-inflammatory mediators.

Inflammation can be acute or chronic. Acute inflammation is a short-term response to injury or infection, which helps to resolve the issue quickly. Chronic inflammation is a long-term response that can cause ongoing damage and diseases such as arthritis, asthma, and cancer.

There are several types of inflammation, including:

1. Acute inflammation: A short-term response to injury or infection.
2. Chronic inflammation: A long-term response that can cause ongoing damage and diseases.
3. Autoimmune inflammation: An inappropriate immune response against the body's own tissues.
4. Allergic inflammation: An immune response to a harmless substance, such as pollen or dust mites.
5. Parasitic inflammation: An immune response to parasites, such as worms or fungi.
6. Bacterial inflammation: An immune response to bacteria.
7. Viral inflammation: An immune response to viruses.
8. Fungal inflammation: An immune response to fungi.

There are several ways to reduce inflammation, including:

1. Medications such as nonsteroidal anti-inflammatory drugs (NSAIDs), corticosteroids, and disease-modifying anti-rheumatic drugs (DMARDs).
2. Lifestyle changes, such as a healthy diet, regular exercise, stress management, and getting enough sleep.
3. Alternative therapies, such as acupuncture, herbal supplements, and mind-body practices.
4. Addressing underlying conditions, such as hormonal imbalances, gut health issues, and chronic infections.
5. Using anti-inflammatory compounds found in certain foods, such as omega-3 fatty acids, turmeric, and ginger.

It's important to note that chronic inflammation can lead to a range of health problems, including:

1. Arthritis
2. Diabetes
3. Heart disease
4. Cancer
5. Alzheimer's disease
6. Parkinson's disease
7. Autoimmune disorders, such as lupus and rheumatoid arthritis.

Therefore, it's important to manage inflammation effectively to prevent these complications and improve overall health and well-being.

Here are some common causes of gingival hemorrhage:

1. Poor oral hygiene: When you don't brush and floss regularly, plaque and tartar can build up along the gum line, leading to inflammation and bleeding.
2. Gingivitis: This is an early stage of gum disease that can cause swollen, red gums that bleed easily.
3. Periodontitis: This is a more advanced stage of gum disease that can cause the gums to pull away from the teeth and create pockets where bacteria can grow, leading to bleeding.
4. Injury to the gums: If you accidentally bite your lip or tongue, or if you have a sharp object pierce your gum, it can cause bleeding.
5. Medications: Certain medications such as aspirin, warfarin, and prednisone can thin the blood and increase the risk of gingival hemorrhage.
6. Hormonal changes: Changes in hormone levels during pregnancy, menstruation, or menopause can increase the risk of gingival hemorrhage.
7. Vitamin deficiencies: Deficiencies in vitamins such as vitamin C and K can impair the body's ability to clot blood and increase the risk of bleeding gums.
8. Systemic diseases: Certain systemic diseases such as diabetes, rheumatoid arthritis, and liver disease can increase the risk of gingival hemorrhage.

If you experience gingival hemorrhage, your dentist may perform a thorough examination to determine the underlying cause. Treatment options will depend on the severity of the condition, but may include professional cleaning, antibiotics, or surgery. It is important to maintain good oral hygiene practices and visit your dentist regularly to prevent and manage gingival hemorrhage.

... can refer to: Protease inhibitor (pharmacology): a class of medication that inhibits viral protease Protease ... molecules that inhibit proteases This disambiguation page lists articles associated with the title Protease inhibitor. If an ...
This is a protease inhibitor. These are often synthesised as part of a larger precursor protein, either as a prepropeptide. The ... SSI is a protease inhibitor, it prevents enzymes from acting on a substrate. Some SSI's also inhibit trypsin, chymotrypsin and ... In molecular biology the protein SSI is a Subtilisin inhibitor-like which stands for Streptomyces subtilisin inhibitor. ... Protease binding induces the widening of a channel-like structure, in which hydrophobic side-chains are sandwiched between 2 ...
Classes of proteases are: Aspartic protease inhibitors Cysteine protease inhibitors Metalloprotease inhibitors Serine protease ... inhibitors Threonine protease inhibitors Trypsin inhibitors Kunitz STI protease inhibitor Classes of inhibitor mechanisms of ... Many naturally occurring protease inhibitors are proteins. In medicine, protease inhibitor is often used interchangeably with ... Suicide inhibitor Transition state inhibitor Protein protease inhibitor (see serpins) Chelating agents This is a family of ...
Protease inhibitors also are used to treat Hepatitis C. Researchers are investigating the use of protease inhibitors developed ... These protease inhibitors prevent viral replication by selectively binding to viral proteases (e.g. HIV-1 protease) and ... A cysteine protease inhibitor drug was found to cure Chagas disease in mice. Researchers are investigating whether protease ... Protease inhibitors that have been developed and are currently used in clinical practice include: Antiretroviral HIV-1 protease ...
In 2009, ten protease inhibitors have reached the market for treatment against HIV but one protease inhibitor, amprenavir, was ... All the FDA approved protease inhibitors are listed below. All the HIV protease inhibitors on the market contain a central core ... Tipranavir is a nonpeptidic HIV-1 protease inhibitor and reached the market in 2005. Unlike other HIV protease inhibitors on ... HIV protease inhibitors fit the active site of the HIV aspartic protease and were rationally designed utilizing knowledge of ...
Kunitz soybean trypsin inhibitor is a type of protein contained in legume seeds which functions as a protease inhibitor. Kunitz ... "Kunitz STI inhibitors". A web/HMMer based tool to study Kunitz protease inhibitors. Federal University of São Paulo. Retrieved ... Soybean Protease Inhibitors in Foods], DiPietro CM, Liener IE, 1989. J Food Sci. Gilani GS, Cockell KA, Sepehr E (2005). " ... "Inhibitor family I3 (Kunitz-P family)". MEROPS - the Protease Database. Retrieved 2008-12-19. Bassaneze V, Gozzo AJ, Nunes VA, ...
Kunitz STI protease inhibitor Rawlings ND, Tolle DP, Barrett AJ (March 2004). "Evolutionary families of peptidase inhibitors". ... In molecular biology, the Bowman-Birk protease inhibitor family of proteins consists of eukaryotic proteinase inhibitors, ... Proteins of the Bowman-Birk inhibitor family of serine proteinase inhibitors interact with the enzymes they inhibit via an ... Birk, Y (February 1985). "The Bowman-Birk inhibitor. Trypsin- and chymotrypsin-inhibitor from soybeans". International Journal ...
Protein Z-dependent protease inhibitor (ZPI) is a protein circulating in the blood which inhibits factors Xa and XIa of the ... It is a member of the class of the serine protease inhibitors (serpins). Its name implies that it requires protein Z, another ... Han X, Fiehler R, Broze GJ (August 1998). "Isolation of a protein Z-dependent plasma protease inhibitor". Proceedings of the ... Han X, Fiehler R, Broze GJ (November 2000). "Characterization of the protein Z-dependent protease inhibitor". Blood. 96 (9): ...
Improved protease inhibitors are now in development. Protease inhibitors have also been seen in nature. A protease inhibitor ... "protease inhibitors" to attack HIV at that phase of its life cycle. Protease inhibitors became available in the 1990s and have ... Anderson J, Schiffer C, Lee SK, Swanstrom R (2009). "Viral protease inhibitors". Antiviral Strategies. Handb Exp Pharmacol. ... "The Role of Protease Inhibitors in the Pathogenesis of HIV-Associated Lipodystrophy: Cellular Mechanisms and Clinical ...
It is of the protease inhibitor (PI) class and works by blocking HIV protease. Atazanavir was approved for medical use in the ... Atazanavir is distinguished from other protease inhibitors in that it has lesser effects on lipid profile and appears to be ... There may be some cross-resistant with other protease inhibitors. When boosted with ritonavir it is equivalent in potency to ... Lv, Z; Chu, Y; Wang, Y (2015). "HIV protease inhibitors: a review of molecular selectivity and toxicity". HIV/AIDS: Research ...
... such as protease inhibitors, which include drugs against AIDS and hypertension. These protease inhibitors bind to an enzyme's ... HIV protease inhibitors are used to treat patients having AIDS virus by preventing its DNA replication. HIV protease is used by ... There are different types of inhibitor, including both reversible and irreversible forms. Competitive inhibitors are inhibitors ... Schechter I (2005). "Mapping of the active site of proteases in the 1960s and rational design of inhibitors/drugs in the 1990s ...
HIV protease inhibitors; the antidepressant nefazodone; the cardiovascular drug gemfibrozil; the immunosuppressant ciclosporin ... This discovery encouraged scientists worldwide to find an effective inhibitor of this enzyme. By 1976, Akira Endo had isolated ... August 2015). "HMG-CoA Reductase Inhibitors Bind to PPARα to Upregulate Neurotrophin Expression in the Brain and Improve Memory ... Tobert JA (July 2003). "Lovastatin and beyond: the history of the HMG-CoA reductase inhibitors". Nature Reviews. Drug Discovery ...
"Protease and Phosphatase Inhibitors". Thermo Fisher Scientific. Retrieved 2018-05-30. Langenbach & Handschel (2013). "Effects ... It is often used in combination with other phosphatase/protease inhibitors for broad spectrum inhibition. β-Glycerophosphate is ... β-Glycerophosphate is an inhibitor of the enzyme serine-threonine phosphatase. ...
Protease inhibitors bind to the active site of the viral protease, which prevents the cleavage of the Gag and Gagpol proteins. ... Protease Inhibitors cause the immature formation of two essential precursor proteins known as Gag and Gagpol in HIV. These ... van Maarseveen, Noortje; Boucher, Charles (2006-01-01). Geretti, Anna Maria (ed.). Resistance to protease inhibitors. London: ... and protease inhibitors. Two NRTI mutations and four NNRTI mutations were commonly found, which can now be tested for using an ...
Inter-alpha-inhibitor at the US National Library of Medicine Medical Subject Headings (MeSH) v t e v t e (Protease inhibitors, ... They function as protease inhibitors. IαI form complexes with hyaluronan (HA), generating a serum-derived hyaluronan-associated ... Inter-alpha-trypsin inhibitors (IαI) are plasma proteins consisting of three of four heavy chains selected from the group ITIH1 ... Zhuo L, Hascall VC, Kimata K (September 2004). "Inter-alpha-trypsin inhibitor, a covalent protein-glycosaminoglycan-protein ...
"NS3/4A Protease Inhibitors - DrugBank". http://www.uniprot.org/uniprot/Q91RS4 v t e (Viral nonstructural proteins, Hepatitis C ... It acts as a serine protease. C-terminal two-thirds of the protein also acts as helicase and nucleoside triphosphatase. First ( ... 14 8687-8697 Schregel, V; Jacobi, S; Penin, F; Tautz, N (2009). "Hepatitis C virus NS2 is a protease stimulated by cofactor ... Stimulation of Hepatitis C Virus (HCV) Nonstructural Protein 3 (NS3) Helicase Activity by the NS3 Protease Domain and by HCV ...
A trypsin inhibitor (TI) is a protein and a type of serine protease inhibitor (serpin) that reduces the biological activity of ... "Trypsin Inhibitors". Sigma-Aldrich. Cohen, Maja; Davydov, Olga; Fluhr, Robert (2019-02-05). "Plant serpin protease inhibitors: ... protease inhibitors that interfere with digestion activity have an antinutritional effect. Therefore, trypsin inhibitors are ... "Foods containing protease". "Trypsin Inhibitors". Worthington Biochemical Corporation. Kadam, S.S., and Smithard, R.R. (1987 ...
Jönsson, A. G.; Torstensson, N. T. L. (1972). "Protease inhibitors from Streptomyces violascens". Archiv für Mikrobiologie. 83 ... Proteinase Inhibitors Proceedings of the 2nd International Research Conference. Berlin, Heidelberg: Springer Berlin Heidelberg ...
... (AG-7088, Rupinavir) is a peptidomimetic antiviral drug which acts as a 3C and 3CL protease inhibitor. It was ... Rocha-Pereira J, Nascimento MS, Ma Q, Hilgenfeld R, Neyts J, Jochmans D (August 2014). "The enterovirus protease inhibitor ... Santos MM, Moreira R (October 2007). "Michael acceptors as cysteine protease inhibitors". Mini Reviews in Medicinal Chemistry. ... October 1999). "In vitro antiviral activity of AG7088, a potent inhibitor of human rhinovirus 3C protease". Antimicrobial ...
In 1996, protease inhibitors were released. These consist of a combination of drugs which lower the HIV viral load in patients ...
Most CPs are serine protease inhibitors. Cyanopeptolin CP1020 exposure in zebrafish affected pathways related to DNA damage, ... Isolation of the Toxic Protease Inhibitor Cyanopeptolin 1020" (PDF). J. Nat. Prod. 73 (5): 980-984. doi:10.1021/np900818c. PMID ...
... inhibitors of FGF21 degradation by protease. The list of modified FGF21 proteins that have been developed include LY2405319, ... October 2020). "Optimization of Peptide Inhibitors of β-Klotho as Antagonists of Fibroblast Growth Factors 19 and 21". ACS ...
Ye S, Goldsmith EJ (2002). "Serpins and other covalent protease inhibitors". Curr. Opin. Struct. Biol. 11 (6): 740-5. doi: ... the Fas/APO-1 protease Mch5 is a CrmA-inhibitable protease that activates multiple Ced-3/ICE-like cysteine proteases". Proc. ... Caspases exist as inactive proenzymes composed of a prodomain, a large protease subunit, and a small protease subunit. ... Biochemically, caspase-8 was found to enter the complex of the inhibitor of NF-κB kinase (IKK) with the upstream Bcl10-MALT1 ( ...
Protease inhibitors changed the nature of AIDS from a terminal illness to a somewhat manageable one. It significantly increased ... They were the ones who started the process of research and development into protease inhibitors and its relation to the virus. ... Just like Study 035, patients couldn't be in the study if they had prior protease inhibitor treatment or lamivudine for more ... Indinavir (IDV; trade name Crixivan, made by Merck) is a protease inhibitor used as a component of highly active antiretroviral ...
Antiviral drugs include protease inhibitors used to treat HIV/AIDS and Hepatitis C, reverse-transcriptase inhibitors targeting ... Agbowuro AA, Huston WM, Gamble AB, Tyndall JD (July 2018). "Proteases and protease inhibitors in infectious diseases". ... and the protease inhibitors used to treat HIV/AIDS. Since anti-pathogen inhibitors generally target only one enzyme, such drugs ... protease inhibitor containing three peptide bonds, as shown in the "competitive inhibitor examples" figure. As this drug ...
Kim JY, Park SC, Hwang I, Cheong H, Nah JW, Hahm KS, Park Y (June 2009). "Protease inhibitors from plants with antimicrobial ... Lawrence, Paulraj; Koundal, Kripa (April 15, 2002). "Plant protease inhibitors in control of phytophagous insects". Plant ... The proteinase inhibitors work to disrupt the enzymatic ability of the digestive or microbial enzymes that are present in the ... Once the proteinase inhibitor has been ingested by the insect, it presents itself as a normal substrate for the digestive ...
It is one of the most potent of a large series of compounds developed as inhibitors of the viral enzyme 3CL protease, with an ... 3CLpro-1 is an antiviral drug related to rupintrivir which acts as a 3CL protease inhibitor and was originally developed for ... April 2015). "Protease inhibitors targeting coronavirus and filovirus entry". Antiviral Research. 116: 76-84. doi:10.1016/j. ... March 2020). "Crystal structure of SARS-CoV-2 main protease provides a basis for design of improved α-ketoamide inhibitors". ...
Maxson T, Deane CD, Molloy EM, Cox CL, Markley AL, Lee SW, Mitchell DA (May 2015). "HIV protease inhibitors block streptolysin ... It has also been observed that both Steptolysin O and SpeB protease limit the innate immune response. Streptolysin S (SLS; sagA ... of the cells were killed within the first two hours as a result of processes stimulated by Streptolysin O and SpeB proteases. ...
αM protease inhibitors inhibit by steric hindrance. The mechanism involves protease cleavage of the bait region, a segment of ... These protease inhibitors share several defining properties, which include (1) the ability to inhibit proteases from all ... In addition to tetrameric forms of α2-macroglobulin, dimeric, and more recently monomeric αM protease inhibitors have been ... Tetrameric, dimeric, and, more recently, monomeric αM protease inhibitors have been identified. α2-Macroglobulin is able to ...
Plant ICK proteins are often protease inhibitors. Knottins have high stability to pH, heat, and enzymes. Because of their ... An inhibitor cystine knot (aka ICK or Knottin) is a protein structural motif containing three disulfide bridges. Knottins are ... The motif is also found in some inhibitor proteins found in plants, but the plant and animal motifs are thought to be a product ... Zhu, S.; Darbon, H.; Dyason, K.; Verdonck, F.; Tytgat, J. (2003). "Evolutionary origin of inhibitor cystine knot peptides". The ...
Lundborg M, Ali E, Widmalm G (2013). "An in silico virtual screening study for the design of norovirus inhibitors: fragment- ... by the viral 3C-like protease (NS6), a major structural protein (VP1) of about 58~60 kDa and a minor capsid protein (VP2). The ...
Once the inhibitor is released and in order to properly function, two CAD monomers need to come together to form a functional ... Nie Z, Phenix BN, Lum JJ, Alam A, Lynch DH, Beckett B, Krammer PH, Sekaly RP, Badley AD (November 2002). "HIV-1 protease ... Therefore, ICAD has a double function; it acts as a CAD inhibitor and also as a chaperone for CAD synthesis assisting the ... McCarty JS, Toh SY, Li P (October 1999). "Study of DFF45 in its role of chaperone and inhibitor: two independent inhibitory ...
These digestive enzymes include proteases that digest proteins into amino acids, as well as glycoside hydrolases that digest ... The enzymes that catalyze these chemical reactions can then be purified and their kinetics and responses to inhibitors ...
... and a protease from Russell's viper venom". The Journal of Biological Chemistry. 253 (6): 1902-9. PMID 632245. Takeya H, ... platelet aggregation inhibitor)-like and C-type lectin-like domains". The Journal of Biological Chemistry. 267 (20): 14109-17. ...
... detection by the terminal deoxynucleotidyl transferase and nick translation assays and prevention by serine protease inhibitors ...
... ribavirin and recently approved protease inhibitors such as Telaprevir (Incivek) May 2011, Boceprevir (Victrelis) May 2011 or ... Interferon-containing regimens may also include protease inhibitors such as boceprevir and telaprevir. There are also ... Chang HW, Watson JC, Jacobs BL (June 1992). "The E3L gene of vaccinia virus encodes an inhibitor of the interferon-induced, ... Ho M, Enders JF (March 1959). "An Inhibitor of Viral Activity Appearing in Infected Cell Cultures". Proceedings of the National ...
... bifunctional inhibitor proteins from plant seeds and various serine proteases and their inhibitors have been determined by his ... These design rules are being exploited for making specific peptides to act as tight inhibitors of target enzymes and potent ... "Structures and binding studies of the complexes of phospholipase A2 with five inhibitors". Biochimica et Biophysica Acta (BBA ... and binding studies of peptidyl-tRNA hydrolase from Pseudomonas aeruginosa provide a platform for the structure-based inhibitor ...
"Factor influencing the production and properties of extracellur protease from Streptomyces bikiniensis". Chittagong University ... "Screening of melanin biosynthesis inhibitors from marine microalgae using Streptomyces bikiniensis bioassay". Biotechnology ...
The Fas/APO-1 protease Mch5 is a CrmA-inhibitable protease that activates multiple Ced-3/ICE-like cysteine proteases". Proc. ... NIH/UW entry on Autoimmune Lymphoproliferative Syndrome The MEROPS online database for peptidases and their inhibitors: C14.011 ... The Fas/APO-1 protease Mch5 is a CrmA-inhibitable protease that activates multiple Ced-3/ICE-like cysteine proteases". Proc. ... This gene encodes a protein that is a member of the cysteine-aspartic acid protease (caspase) family. Sequential activation of ...
Schwob, E; Böhm, T; Mendenhall, M. D.; Nasmyth, K (1994). "The B-type cyclin kinase inhibitor p40SIC1 controls the G1 to S ... "Cleavage of cohesin by the CD clan protease separin triggers anaphase in yeast". Cell. 103 (3): 375-386. doi:10.1016/s0092-8674 ...
... (loxistatin, E-64d, EST) is a drug which acts as a cysteine protease inhibitor and has anticoagulant effects. It is ... Hook G, Hook V, Kindy M (2011). "The cysteine protease inhibitor, E64d, reduces brain amyloid-β and improves memory deficits in ... "Brain pyroglutamate amyloid-β is produced by cathepsin B and is reduced by the cysteine protease inhibitor E64d, representing a ... Calpain inhibitor E-64-d provides neuroprotection in SCI lesion and penumbra". Annals of the New York Academy of Sciences. 939 ...
... is flanked by Ubiquitin Specific Protease 4 (USP4) and Coil-Coiled Domain Containing 36 (CCDC36). C3orf62 possesses the ... Inhibitor of growth protein 5 (ING5), Thioredoxin domain-containing protein 9 (TXNDC9), and MORF4-family associated proteins ( ...
Development of a new substrate, inhibitors, and an affinity ligand". The Journal of Biological Chemistry. 255 (8): 3482-6. PMID ... Dreyfus LA, Iglewski BH (March 1986). "Purification and characterization of an extracellular protease of Legionella pneumophila ...
Important antiretroviral drugs include the class of protease inhibitors. Herpes viruses, best known for causing cold sores and ... Some influenza A and B viruses have become resistant to neuraminidase inhibitors such as oseltamivir, and the search for new ...
Calcineurin inhibitors (such as pimecrolimus, tacrolimus or cyclosporin) are sometimes used. While topical steroids are widely ... the release of proinflammatory mediators and proteases by mast cells, and perturbations in the innate immune response that may ...
Boldin MP, Goncharov TM, Goltsev YV, Wallach D (1996). "Involvement of MACH, a novel MORT1/FADD-interacting protease, in Fas/ ... This protein binds adaptor protein TRAF2, reduces the recruitment of inhibitor-of-apoptosis proteins (IAPs) by TRAF2, and thus ...
... which encodes the serine protease inhibitor LEKTI (lymphoepithelial Kazal-type-related inhibitor). LEKTI is expressed in ... increased stratum corneum protease activities, and elevated kallikrein levels in the stratum corneum. Trichorrhexis invaginata ...
Kallikrein is a protease that functions to cleave kininogen, subsequently creating kininogen and bradykinin, a potent ... Patients have hereditary angioedema (HAE) because of a deficiency or dysfunctional C1 inhibitor, which is an enzyme that ... Poor regulation of the C1 inhibitor results in increased levels of kallikrein and subsequent proteolysis of kininogen. The ...
A protease inhibitor, it is also known as alpha1-proteinase inhibitor (A1PI) or alpha1-antiproteinase (A1AP) because it ... Like all serine protease inhibitors, A1AT has a characteristic secondary structure of beta sheets and alpha helices. Mutations ... In blood test results, the IEF results are notated as in PiMM, where Pi stands for protease inhibitor and "MM" is the banding ... A1AT is both an endogenous protease inhibitor and an exogenous one used as medication. The pharmaceutical form is purified from ...
"Multifaceted roles of human elafin and secretory leukocyte proteinase inhibitor (SLPI), two serine protease inhibitors of the ... domain-containing protease inhibitors such as trappin-2. This N-terminal domain enables it to become cross-linked to ...
Specifically, mannose binding triggers recruitment of MBL-associated serine proteases (MASPs). The serine proteases activate ... Type II kinase inhibitors, which are highly specific, have shown promising results in blocking the TNF arising from NOD- ... Additionally, research has been conducted on GSK583, a highly specific RIP2 inhibitor, which seems highly promising in ... September 2015). "Inflammatory Signaling by NOD-RIPK2 Is Inhibited by Clinically Relevant Type II Kinase Inhibitors". Chemistry ...
Serine protease inhibitor Kazal-type 6 (SPINK6) is a protein encoded by the SPINK6 gene in humans. It is a potent inhibitor of ... Kazal-type serine protease inhibitor domain Meyer-Hoffert U; Wu Z; Kantyka T; Fischer J; Latendorf T; Hansmann B; Bartels J; He ... October 2010). "Isolation of SPINK6 in human skin: selective inhibitor of kallikrein-related peptidases". J Biol Chem. 285 (42 ... epidermal proteases involved in maintaining skin homeostasis, including KLK5, KLK7 and KLK14. SPINK6 is a member of a gene ...
"Selective activator protein-1 inhibitor T-5224 prevents lymph node metastasis in an oral cancer model". Cancer Science. 107 (5 ... "Serratia marcescens serralysin induces inflammatory responses through protease-activated receptor 2". Infection and Immunity. ... and angiotensin II-induced type 1 plasminogen activator inhibitor (PAI-1) gene expression in cultured human vascular smooth ...
His research focuses on proteases and their inhibitors in humans, with particular emphasis on the caspases of the apoptotic ... specific Proteases: Profiling The Specificities And Activities Of Human Senps. J Biol Chem 282, 26217-26224 Timmer, J. C., ...
Additionally, in existence are a fixed-dose combination of cobicistat and protease inhibitor darunavir (darunavir/cobicistat; ... including HIV protease inhibitors and GS-7340, in vitro". Antimicrobial Agents and Chemotherapy. 56 (10): 5409-13. doi:10.1128/ ... marketed as Prezcobix by Janssen Therapeutics), and a fixed-dose combination of cobicistat and protease inhibitor atazanavir ( ... Cobicistat is a potent inhibitor of cytochrome P450 3A enzymes, including the important CYP3A4 subtype. It also inhibits ...
... using protease inhibitors. Within a week after the conference, over 75,000 patients who have been using antibiotics and ... an orally active type 5 cyclic GMP-specific phosphodiesterase inhibitor for the treatment of penile erectile dysfunction". ...
Cytokine induced apoptosis inhibitor 1) CKLF: Chemokine-like factor CLUAP1: CMTM2: encoding protein CKLF-like MARVEL ... Chymotrypsin-like protease DCTPP1: encoding enzyme dCTP pyrophosphatase 1 DEL16P12.1P11.2: Chromosome 16p12.2-p11.2 deletion ...
"Sequence organization and matrix attachment regions of the human serine protease inhibitor gene cluster at 14q32.1". Mammalian ...
HIV-protease inhibitors. Di Perri G, Del Bravo P, Concia E. Di Perri G, et al. N Engl J Med. 1998 Sep 10;339(11):773-4; author ... HIV protease inhibitors. Winslow DL, Otto MJ. Winslow DL, et al. AIDS. 1995;9 Suppl A:S183-92. AIDS. 1995. PMID: 8819585 Review ... HIV-protease inhibitors. Palleja S. Palleja S. N Engl J Med. 1998 Sep 10;339(11):774. doi: 10.1056/NEJM199809103391116. N Engl ... Cross-resistance within the protease inhibitor class. Race E. Race E. Antivir Ther. 2001;6 Suppl 2:29-36. Antivir Ther. 2001. ...
SEARCH RESULTS for: Protease Inhibitor [Drug Class] (62 results) *Share : JavaScript needed for Sharing tools. Bookmark & Share ...
Several protease inhibitors that are used in combination with other drugs to treat Human Immunodeficiency Virus (HIV) infection ... HIV Protease Inhibitors Show Potential as Cancer Treatments. Several protease inhibitors that are used in combination with ... When given in doses that were previously proven to be safe in HIV-infected patients, three of the six protease inhibitors ( ... Nelfinavir was the most effective of all the protease inhibitors tested, and was able to cause two different types of cancer ...
... levels associated with protease inhibitor therapy. Studies of the effects of protease inhibitors on lipoprotein receptors and ... The mechanism of action of the protease inhibitors is believed to be through their binding to the active site of HIV protease ... Combinations of various protease inhibitors with nucleoside and non-nucleoside reverse transcriptase inhibitors usually have ... Alternatively, there are systems in the body that depend on protease enzymes to function and perhaps the protease inhibitors ...
... from a native virus inhibitory sequence that blocks maturation of the virally encoded protease and inhibits the mature protease ... Transframe peptide inhibitor of viral protease (U.S. Patent Number 5,872,210). The present invention describes small, water ... and in the generation of a screening assay or kit that can be used to identify other similarly acting protease inhibitors. ... from a native virus inhibitory sequence that blocks maturation of the virally encoded protease and inhibits the mature protease ...
Consultation informelle sur les Incidences des Traitements antirétroviraux (‎1997: Genève, Switzerland)‎; Praag, Eric van; Fernyak, Susan; Martin Katz, Alison; World Health Organization. Office of HIV/AIDS and Sexually Transmitted Diseases; UNAIDS (‎Organisation mondiale de la Santé, 1997)‎ ...
... that inhibit the action of the protease of HIV so that the cleavage of viral proteins into mature functional infectious ... The meaning of PROTEASE INHIBITOR is a substance that inhibits the action of a protease; specifically : any of various drugs ( ... an HIV-1 protease inhibitor and CYP3A inhibitor. -. William A. Haseltine, Forbes, 9 June 2022 But a protease is an enzyme that ... 2022 Viracept became the best-selling drug in its class, called a protease inhibitor. -. Merrie Monteagudo, San Diego Union- ...
... protease inhibitors are a broad class of agents that are widely used in the therapy and prevention of HIV infection and the ... All of the currently available protease inhibitors have been associated with transient and usu … ... The antiretroviral protease inhibitors act by binding to the catalytic site of the HIV protease, thereby preventing the ... Protease Inhibitors (HIV) No authors listed In: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [ ...
... maintain and preserve cellular protein composition following cell lysis. When used with CelLytics ... We also now offer the only fully mass spectrometry-compatible protease inhibitor cocktail and phosphatase inhibitor cocktail on ... Our Protease Inhibitor Cocktails have been optimized to maintain and preserve protein functionality following cell lysis, and ... Our portfolio also includes protease inhibitor cocktails that are tailored to specific applications:. *We offer cocktails for ...
Therefore, it was hypothesized that protease inhibitors might protec … ... meconium caused significant cell detachment and that meconium-induced detachment of cells was prevented by a protease inhibitor ... Protection of Meconium-Induced Lung Epithelial Injury by Protease Inhibitors J Lung Pulm Respir Res. 2017;4(5):145. Epub 2017 ... Therefore, it was hypothesized that protease inhibitors might protect AEC monolayers against meconium-induced collapse of ...
... inhibitor can induce HIV resistance to the protease inhibitor and possibly to other drugs within the protease inhibitor class ( ... resulting in subtherapeutic levels of the protease inhibitors. In addition, protease inhibitors retard the metabolism of ... Protease inhibitor therapy may be resumed when treatment with rifampin is discontinued. Antiretroviral agents other than ... To minimize the interruption of protease inhibitor therapy, one option is to use a four-drug TB treatment regimen that includes ...
New protease inhibitors against Alzheimers disease. protein but did not affect the endoproteolysis of presenilins involved in ... designed and tested three new non-peptidic inhibitors of γ-secretase - the enzyme that cleaves the Aβ protein from its βAPP ... In human cells they show that these inhibitors markedly reduce the production of Aβ and increase the carboxy-terminal fragments ...
Prisoners Treated for Hepatitis C with Protease Inhibitor, New York, USA, 2012. Emerging Infectious Diseases. 2015;21(1):186- ... Prisoners Treated for Hepatitis C with Protease Inhibitor, New York, USA, 2012 On This Page ... Moorjani, H., Koenigsmann, C., Kim, M., & Spaulding, A. C. (2015). Prisoners Treated for Hepatitis C with Protease Inhibitor, ... Prisoners Treated for Hepatitis C with Protease Inhibitor, New York, USA, 2012. Volume 21, Number 1-January 2015 ...
... are ready-to-use concentrated stock solutions of protease inhibitors for addition to samples to prevent proteolytic ... Thermo Scientific™ Halt Protease Inhibitor Cocktails are ready-to-use concentrated stock solutions of protease inhibitors for ... Halt Protease Inhibitor Cocktails are 100X solutions containing optimized concentrations of six broad-spectrum protease ... Halt Protease Inhibitor Cocktail. 24 x 100 μL. Pack of 24 for $307.00 ...
1.70 A resolution structure of SARS-CoV-2 3CL protease in complex with inhibitor 7j ... 3C-like protease inhibitors block coronavirus replication in vitro and improve survival in MERS-CoV-infected mice.. Rathnayake ... We describe herein the structure-guided optimization of a series of inhibitors of the coronavirus 3C-like protease (3CLpro), an ... 1.70 A resolution structure of SARS-CoV-2 3CL protease in complex with inhibitor 7j. *PDB DOI: https://doi.org/10.2210/pdb6XMK/ ...
Two-drug protease inhibitor treatment as effective as three-drug treatment - and fewer stop due to side-effects ... Of the protease inhibitors used in the seven studies included in the meta-analysis, only darunavir/ritonavir is still ... Booster drugs are used to boost the effects of protease inhibitors and some other antiretrovirals. Adding a small dose of a ... "Our results question why we are still using protease inhibitor three-drug regimens when two-drug regimens are as effective, as ...
Learn how once-daily HIV medication PREZISTA® (darunavir) 800 mg in combination with other HIV medicines can impact CD4 cell count and viral load.
Characterization of protease inhibitor conjugated CAP256-VRC26.25 impurities. Wednesday, September 12, 2018. - Poster Session I ... The addition of a protease inhibitor, 4-(2-aminoethyl) benzenesulfonyl fluoride (AEBSF), to the cell culture media has shown to ...
Measurements are from triplicates, expressed seeing that means S.D. cancers cell lines MCF-7 and MDA-MB-453. Traditional western blots of lysates from Rabbit Polyclonal to C-RAF RAI3-transfected (RIII) and RAI3-GFP-transfected (RGFP) HEK293T cells, compared to HEK293Twt cells, and breasts cancer tumor Befiradol cell lines MCF-7 and MDA-MB-453 (MB453). Recognition with anti-RAI3 Mab 24 2.3, HRPO-labelled anti-mouse… Continue reading Measurements are from triplicates, expressed seeing that means S. ...
The MSDS of Protease for Inhibitor is available from Karlan upon request. ... Protease Inhibitor Cocktail (EDTA-Free, 100X in DMSO) - K1010-10x1m - 1 kit is backordered and will ship as soon as it is back ... The MSDS of Protease for Inhibitor is available from Karlan upon request. ... The MSDS of Protease for Inhibitor is available from Karlan upon request. ...
... uHTS identification of small molecule inhibitors of the catalytic domain of the SUMO protease, SENP1 in a FRET assay. ...
Activity profiling and structures of inhibitor-bound SARS-CoV-2-PLpro protease provides a framework for anti-COVID-19 drug ... Activity profiling and structures of inhibitor-bound SARS-CoV-2-PLpro protease provides a framework for anti-COVID-19 drug ... Activity profiling and structures of inhibitor-bound SARS-CoV-2-PLpro protease provides a framework for anti-COVID-19 drug ... Activity profiling and structures of inhibitor-bound SARS-CoV-2-PLpro protease provides a framework for anti-COVID-19 drug ...
A Phase 1 Study to Evaluate the Interaction of HCV NS5B Inhibitor MK-3682 With HCV NS3/4A Protease Inhibitor MK-5172 and HCV ...
Phase 1 single dose studies to optimize the pharmacokinetics of DG17, a novel HIV-protease inhibitor pro-drug, using sodium ... DG17 is an orally available prodrug of DG35 (a novel HIV protease inhibitor with variable pharmacokinetics). These studies ... Phase 1 single dose studies to optimize the pharmacokinetics of DG17, a novel HIV-protease inhibitor... ...
In silico Screening of Natural Compounds as Potential Inhibitors of SARS-CoV-2 Main Protease and Spike RBD: Targets for COVID- ... Finding potent inhibitors for COVID-19 main protease (M pro ): an in silico approach using SARS-CoV-3CL protease inhibitors for ... Majumder, R.; Mandal, M. 2020: Screening of plant-based natural compounds as a potential COVID-19 main protease inhibitor: an ... In silico Screening of Natural Compounds as Potential Inhibitors of SARS-CoV-2 Main Protease and Spike RBD: Targets for COVID- ...
Lysosomal cysteine proteases from mammalian cells and plants are regulated by endogenous tight-binding inhibitors from the ... Lysosomal cysteine proteases from mammalian cells and plants are regulated by endogenous tight-binding inhibitors from the ... This protein was subsequently characterized as a tight-binding and reversible inhibitor of papain-like cysteine proteases. ... This protein was subsequently characterized as a tight-binding and reversible inhibitor of papain-like cysteine proteases. ...
Abstrakt: Several recombinant derivatives of serine protease inhibitor called silk protease inhibitor 2 (SPI2), which is a silk ... Klíčová slova: Genetically modified organism, Silk protease inhibitor, Protease, Transgene, Insect, Resistance, Potato. ... Protease inhibitor from insect silk - activities of derivatives expressed in vitro and in transgenic potato. Kodrík D., ... Protease inhibitor from insect silk - activities of derivatives expressed in vitro and in transgenic potato ...
Since our previous studies have shown that SPIK is an inhibitor of serine protease-dependent apoptosis, it is hypothesized that ... Hepatitis B and hepatitis C virus replication upregulates serine protease inhibitor Kazal, resulting in cellular resistance to ... Hepatitis B and hepatitis C virus replication upregulates serine protease inhibitor Kazal, resulting in cellular resistance to ... have suggested that replication of either of these viruses upregulates a cellular protein called serine protease inhibitor ...
... a protease inhibitor drug can stop that from happening. If the term protease inhibitor rings a bell, thats because drugs that ... Pfizers antiviral pill is a protease inhibitor, originally called PF-07321332, or just 332 for short. A protease is an enzyme ... protease, protease inhibitor, Ridgeback, ritonavir, SARS, SARS-CoV-2, spike protein ... protease inhibitor. Early Data Suggest Pfizer Pill May Prevent Severe COVID-19 Posted on November 16th, 2021. by Dr. Francis ...
  • When given in doses that were previously proven to be safe in HIV-infected patients, three of the six protease inhibitors (nelfinavir, ritonavir and saquinavir) inhibited growth of non-small cell lung cancer and every cell type in the set of 60 kinds of cancer cells. (nih.gov)
  • Emily Rekstis, Allure , 26 Oct. 2022 Paxlovid combines nirmatrelvir, an inhibitor of the SARS-CoV-2 main protease (MPro, also known as 3CL or nsp5), and ritonavir, an HIV-1 protease inhibitor and CYP3A inhibitor. (merriam-webster.com)
  • In 1995 and 1996, the Food and Drug Administration (FDA) approved three products in the new protease inhibitor class of drugs -- saquinavir (InviraseTM), ritonavir (NorvirTM), and indinavir (CrixivanTM). (cdc.gov)
  • The COVID-19 Treatment Guidelines Panel (the Panel) recommends against the use of lopinavir/ritonavir and other HIV protease inhibitors for the treatment of COVID-19 in hospitalized patients ( AI ) . (nih.gov)
  • The Panel recommends against the use of lopinavir/ritonavir and other HIV protease inhibitors for the treatment of COVID-19 in nonhospitalized patients ( AIII ) . (nih.gov)
  • The pharmacodynamics of lopinavir/ritonavir raise concerns about whether it is possible to achieve drug concentrations that can inhibit the SARS-CoV-2 proteases. (nih.gov)
  • Lopinavir/ritonavir is a potent inhibitor of cytochrome P450 3A. (nih.gov)
  • Over the past five years a series of clinical trials led by Professor Pedro Cahn in Argentina and physicians in Europe have investigated whether treatment with a two-drug regimen of a ritonavir-boosted protease inhibitor and a nucleoside or nucleotide analogue, either lamivudine or tenofovir, is as effective as treatment with a three-drug regimen containing a boosted protease inhibitor. (aidsmap.com)
  • PAXLOVID™ is a formulation that combines the new protease inhibitor with a low dose of an existing drug called ritonavir, which slows the metabolism of some protease inhibitors and thereby keeps them active in the body for longer periods of time. (nih.gov)
  • The combination of protease inhibitors lopinavir and ritonavir contributed to an overall reduction of 40 percent in the rate of malaria among a group of HIV-positive infants and children up to 6 years old in Uganda who were also being treated with anti-malarial drugs. (nih.gov)
  • The NCI research team investigated HIV protease inhibitors because these drugs are known to inhibit the activation of Akt, a protein that has been implicated in the development of many types of cancer, including non-small cell lung cancer. (nih.gov)
  • All four drugs, which inhibit HIV protease and thus interfere with viral maturation and replication, are the most potent antiretroviral agents available to treat patients with HIV disease (1). (cdc.gov)
  • Inhibit proteolytic degradation during cell lysis and protein extraction with these ready-to-use concentrated stock solutions of protease inhibitors. (fishersci.com)
  • The cocktails effectively inhibit serine-proteases, cysteine-proteases, aspartic acid-proteases and aminopeptidases that are typically present in cellular lysate samples. (fishersci.com)
  • The present study is aimed at the investigation of antiviral action of several groups of phytoconstituents against SARS-CoV-2 using a molecular docking approach to inhibit Main Protease (Mpro) (PDB code: 6LU7) and spike (S) glycoprotein receptor binding domain (RBD) to ACE2 (PDB code: 6M0J) of SARS-CoV-2. (eurekamag.com)
  • Recent studies show that many other beans and peas also contain protease inhibitors that are shown to inhibit important steps in cancer development . (gim-academy.com)
  • The question has been Whether other legumes, besides soy beans, contain appreciable amounts of protease inhibitors that have an ability to inhibit cancer development and growth. (gim-academy.com)
  • Chickpea (Cicer arietinum) and Other Plant-Derived Protease Inhibitor Concentrates Inhibit Breast and Prostate Cancer Cell Proliferation In Vitro. (gim-academy.com)
  • The protease inhibitor combination used in the study did not appear to inhibit an initial bout of malaria--but reduce the chances of a recurrence of the disease following a successful treatment. (nih.gov)
  • Merrie Monteagudo, San Diego Union-Tribune , 15 Mar. 2022 Founded in February 2020 specifically to fight the pandemic, the company is pursuing a protease inhibitor antiviral compound called PBI-0451. (merriam-webster.com)
  • Viral Papain-Like cysteine protease (PLpro, NSP3) is essential for SARS-CoV-2 replication and represents a promising target for the development of antiviral drugs. (biorxiv.org)
  • Pfizer's antiviral pill is a protease inhibitor, originally called PF-07321332, or just 332 for short. (nih.gov)
  • In the study published earlier this month in Science [1], the Pfizer team led by Dafydd Owen, Pfizer Worldwide Research, Cambridge, MA, reported that the latest version of their M pro inhibitor showed potent antiviral activity in laboratory tests against not just SARS-CoV-2, but all of the coronaviruses they tested that are known to infect people. (nih.gov)
  • Highly active antiretroviral therapy failure and protease and reverse transcriptase human immunodeficiency virus type 1 gene mutations. (nih.gov)
  • In HBV or HCV coinfected patients, antiretroviral therapy with highly active antiretroviral therapy (HAART) including protease inhibitors may result in an exacerbation of the underlying chronic hepatitis B or C. (nih.gov)
  • Antiretroviral treatment with a boosted protease inhibitor and one other drug is just as effective as three-drug antiretroviral therapy containing a boosted protease inhibitor but results in fewer treatment discontinuations due to side-effects, a meta-analysis presented at the International Congress on Drug Therapy in HIV Infection (HIV Glasgow) shows. (aidsmap.com)
  • Page, MI 2004, ' β-sultams - Mechanism of reactions and use as inhibitors of serine proteases ', Accounts of Chemical Research , vol. 37, no. 5, pp. 297-303. (hud.ac.uk)
  • Lysosomal cysteine proteases from mammalian cells and plants are regulated by endogenous tight-binding inhibitors from the cystatin superfamily. (lu.se)
  • The presence of cystatin-like inhibitors in lower eukaryotes such as protozoan parasites has not yet been demonstrated, although these cells express large quantities of cysteine proteases and may also count on endogenous inhibitors to regulate cellular proteolysis. (lu.se)
  • This protein was subsequently characterized as a tight-binding and reversible inhibitor of papain-like cysteine proteases. (lu.se)
  • article{da17a34b-49f1-478c-b2fd-d9401dd13e53, abstract = {{Lysosomal cysteine proteases from mammalian cells and plants are regulated by endogenous tight-binding inhibitors from the cystatin superfamily. (lu.se)
  • 1 Two proteases are responsible for this cleavage: 3-chymotrypsin-like protease (3CLpro) and papain-like protease (PLpro). (nih.gov)
  • For these reasons, the protease inhibitors are heterogeneous molecules with little structural similarity, most of which are peptide-like and resemble the short peptide that is cleaved by the viral protease (usually the N terminal side of the middle proline residue is phenylalanine-proline-proline). (nih.gov)
  • The results are indicative of better potential of solanine, acetoside, and rutin, as Mpro and spike glycoprotein RBD dual inhibitors. (eurekamag.com)
  • Here, we determined the inhibitor-bound crystal structures of the main protease (Mpro) from the delta-CoV porcine HKU15 and gamma-CoV SW1 from the beluga whale. (umassmed.edu)
  • A comparison with the apo structure of SW1 Mpro, which is also presented here, enabled the identification of structural arrangements upon inhibitor binding at the active site. (umassmed.edu)
  • The cocrystal structures reveal binding modes and interactions of two covalent inhibitors, PF-00835231 (active form of lufotrelvir) bound to HKU15, and GC376 bound to SW1 Mpro. (umassmed.edu)
  • Petit et al designed and tested three new non-peptidic inhibitors of γ-secretase - the enzyme that cleaves the Aβ protein from its βAPP precursor protein. (the-scientist.com)
  • A protease is an enzyme that cleaves a protein at a specific series of amino acids. (nih.gov)
  • Increases in the prevalence of resistance to nonnucleoside reverse transcriptase inhibitors (NNRTIs) have been observed among previously untreated individuals in all areas of sub-Saharan Africa. (sussex.ac.uk)
  • This reduction was in comparison to malaria incidence among children receiving a drug treatment of one of a class of drugs called non-nucleoside reverse transcriptase inhibitors (NNRTIs). (nih.gov)
  • Here we report the isolation, biochemical characterization, developmental stage distribution and subcellular localization of chagasin, an endogenous cysteine protease inhibitor in T. cruzi. (lu.se)
  • As human infections have been caused by alpha- and beta-CoVs, structural characterization and inhibitor design mostly focused on these two genera. (umassmed.edu)
  • We also now offer the only fully mass spectrometry-compatible protease inhibitor cocktail and phosphatase inhibitor cocktail on the market, MSSAFE. (sigmaaldrich.com)
  • Earlier work form this laboratory showed that exposure of alveolar epithelial cells (AECs) to meconium caused significant cell detachment and that meconium-induced detachment of cells was prevented by a protease inhibitor cocktail. (nih.gov)
  • Protease Inhibitor Cocktail (EDTA-Free, 100X in DMSO) - K1010-10x1m - 1 kit is backordered and will ship as soon as it is back in stock. (dnamethsoc.com)
  • The antiretroviral protease inhibitors act by binding to the catalytic site of the HIV protease, thereby preventing the cleavage of viral polyprotein precursors into mature, functional proteins that are necessary for viral replication. (nih.gov)
  • Booster drugs are used to 'boost' the effects of protease inhibitors and some other antiretrovirals. (aidsmap.com)
  • In this study, nelfinavir and saquinavir were more potent than the other HIV protease inhibitors examined. (nih.gov)
  • To address these challenges, efforts are underway in the pursuit of more potent and less toxic HIV-1 protease inhibitors . (bvsalud.org)
  • Maintenance immunosuppressive therapies include small molecule drugs (calcineurin inhibitors and antiproliferatives), fusion proteins and glucorticorticoids. (medscape.com)
  • Our Protease Inhibitor Cocktails have been optimized to maintain and preserve protein functionality following cell lysis, and are available in powder, solution, or tablet forms. (sigmaaldrich.com)
  • Thermo Scientific™ Halt Protease Inhibitor Cocktails are ready-to-use concentrated stock solutions of protease inhibitors for addition to samples to prevent proteolytic degradation during cell lysis and protein extraction procedures. (fishersci.com)
  • The present invention describes small, water soluble peptides isolated from a native virus inhibitory sequence that blocks maturation of the virally encoded protease and inhibits the mature protease as well. (nih.gov)
  • Remarkably, the Bowman-Birk inhibitor does not interfere with function and replication of normal, healthy cells. (gim-academy.com)
  • Protease inhibitors interfere with the reproduction of HIV by blocking the protease enzyme of HIV. (nih.gov)
  • We describe herein the structure-guided optimization of a series of inhibitors of the coronavirus 3C-like protease (3CLpro), an enzyme essential for viral replication. (rcsb.org)
  • In fact, Pfizer originally synthesized and pre-clinically evaluated protease inhibitors years ago as a potential treatment for severe acute respiratory syndrome (SARS), which is caused by a coronavirus closely related to SARS-CoV-2. (nih.gov)
  • Halt Protease Inhibitor Cocktails are 100X solutions containing optimized concentrations of six broad-spectrum protease inhibitors stabilized in high-quality dimethylsulfoxide (DMSO). (fishersci.com)
  • Hepatitis B and hepatitis C virus replication upregulates serine protease inhibitor Kazal, resulting in cellular resistance to serine protease-dependent apoptosis. (nih.gov)
  • Our recent studies have suggested that replication of either of these viruses upregulates a cellular protein called serine protease inhibitor Kazal (SPIK). (nih.gov)
  • Since our previous studies have shown that SPIK is an inhibitor of serine protease-dependent apoptosis, it is hypothesized that the upregulation of SPIK caused by HBV and HCV replication leads to cell resistance to apoptosis. (nih.gov)
  • Pathogenic flaviviruses, including Zika, require the NS2B-NS3 protease for viral replication. (nih.gov)
  • On the scaffold of best hits from positional scanning we designed optimal fluorogenic substrates and irreversible inhibitors with a high degree of selectivity for SARS PLpro variants versus other proteases. (biorxiv.org)
  • We determined crystal structures of two of these inhibitors (VIR250 and VIR251) in complex with SARS-CoV-2-PLpro which reveals their inhibitory mechanisms and provides a structural basis for the observed substrate specificity profiles. (biorxiv.org)
  • Altogether this work has revealed the molecular rules governing PLpro substrate specificity and provides a framework for development of inhibitors with potential therapeutic value or drug repositioning. (biorxiv.org)
  • This version is updated with crystal structures of inhibitors with SARS-CoV-2-PLpro and biochemistry data. (biorxiv.org)
  • Solicited programs should address the possible basic mechanism(s) underlying the metabolic and hormonal alterations leading to dyslipidemias and lipodystrophy as well as insulin resistance observed in HIV- positive patients undergoing protease inhibitor treatment and the relationship between the development of these abnormal metabolic processes and the accelerated progression of atherosclerosis. (nih.gov)
  • However, these protease inhibitors interact with rifamycin derivatives, such as rifampin and rifabutin, which are used to treat and prevent the mycobacterial infections commonly observed in HIV-infected patients. (cdc.gov)
  • This report describes approaches for managing patients who are candidates for or who are undergoing protease inhibitor therapy when tuberculosis (TB) is diagnosed and presents interim recommendations for managing these patients until additional data are available and formal guidelines are issued. (cdc.gov)
  • Therefore, the pharmacokinetic interactions between protease inhibitors and rifampin are important for health-care workers involved in TB control and the care of patients co-infected with TB and HIV because clinicians may decrease or restrict the use of rifampin in the treatment of patients who are candidates for therapy with both protease inhibitors and rifampin. (cdc.gov)
  • Because of the common association of TB and HIV infection, an increasing number of patients probably will be considered candidates for rifampin and protease inhibitors. (cdc.gov)
  • In addition, all HIV-infected patients at risk for TB infection should be carefully evaluated and administered isoniazid for preventive treatment if indicated, regardless of their status for being prescribed protease inhibitor therapy. (cdc.gov)
  • For HIV-infected patients diagnosed with drug-susceptible TB and for whom protease inhibitor therapy is being considered but has not been initiated, the suggested management strategy is to complete TB treatment with a regimen containing rifampin before starting therapy with a protease inhibitor. (cdc.gov)
  • The clinical trials discussed below have not demonstrated a clinical benefit for protease inhibitors in patients with COVID-19. (nih.gov)
  • Protease inhibitors are known to combat cancer by preventing the synthesis of key proteins required for cancer cells to divide and invade neighbouring tissues and organs. (gim-academy.com)
  • Most of these agents were developed by rational drug design based upon chemical structures that would interact with the catalytic site of the HIV protease, based upon x-ray crystallographic studies defining the three-dimensional molecular structure of the protease. (nih.gov)
  • Laboratory studies also suggest that protease inhibitors can block the malaria parasite outright. (nih.gov)
  • Cross-resistance within the protease inhibitor class. (nih.gov)
  • PURPOSE The objective of this initiative is to support research on the effects of HIV protease inhibitors on lipid metabolism leading to hyperlipidemia and altered body fat distribution, the onset of insulin resistance, and the development of accelerated atherosclerosis. (nih.gov)
  • We aimed to examine whether first-line use of 2 NRTIs plus a boosted protease inhibitor (bPI) could protect against emergence of NRTI resistance mutations, compared to the use of 2 NRTIs plus 1 NNRTI. (sussex.ac.uk)
  • Our complete collection of Protease Inhibitor Cocktails offers a diverse portfolio that accommodates your different sample needs. (sigmaaldrich.com)
  • We offer cocktails for customers who require animal component-free (ACF) protease inhibitor cocktails in their work. (sigmaaldrich.com)
  • The stable, concentrated liquid cocktails are easy to use, and the several different package sizes make Halt Protease Inhibitor Cocktails exceptionally convenient for either small-scale or large-scale uses. (fishersci.com)
  • Protease inhibitor cocktails with EDTA include separate 0.5M EDTA solution. (fishersci.com)
  • Rifamycins accelerate the metabolism of protease inhibitors (through induction of hepatic P450 cytochrome oxidases), resulting in subtherapeutic levels of the protease inhibitors. (cdc.gov)
  • In addition, protease inhibitors retard the metabolism of rifamycins, resulting in increased serum levels of rifamycins and the likelihood of increased drug toxicity (2). (cdc.gov)
  • All of the currently available protease inhibitors have been associated with transient and usually asymptomatic elevations in serum aminotransferase levels, and several (atazanavir, indinavir) with mild-to-moderate elevations in indirect and total bilirubin concentration. (nih.gov)
  • Compared to nevirapine, the liquid formulation of the protease inhibitor combination is also unpleasant tasting. (nih.gov)
  • However, recent changes in the protease inhibitor formulation may overcome these barriers to expanding its use in resource poor settings, Dr. Mofenson said. (nih.gov)
  • DG17 is an orally available prodrug of DG35 (a novel HIV protease inhibitor with variable pharmacokinetics). (edu.au)
  • They found that their protease inhibitor, when taken orally, was safe and could reach concentrations in the bloodstream that should be sufficient to help combat the virus. (nih.gov)
  • Several recombinant derivatives of serine protease inhibitor called silk protease inhibitor 2 (SPI2), which is a silk component in Galleria mellonella (Lepidoptera, Insecta), were prepared in the expression vector Pichia pastoris. (cas.cz)
  • Using mouse models and in vitro studies, the researchers tested six different protease inhibitors against non-small cell lung cancer as well as a panel of 60 human cancer cell types, in cultures (called cell lines) derived from nine different kinds of malignant tissue. (nih.gov)
  • Therefore, it was hypothesized that protease inhibitors might protect AEC monolayers against meconium-induced collapse of epithelial barrier function both in vitro and in vivo . (nih.gov)
  • The human immunodeficiency virus (HIV) protease inhibitors are a broad class of agents that are widely used in the therapy and prevention of HIV infection and the acquired immunodeficiency syndrome (AIDS). (nih.gov)
  • It's possible that these protease inhibitors prevent antimalarial drugs from breaking down or have some other additive effect against the malarial parasite," said Lynne Mofenson, M.D., chief of the Pediatric, Adolescent, and Maternal AIDS Branch at the Eunice Kennedy Shriver National Institute of Child Health and Human Development, the NIH institute that funded the study. (nih.gov)
  • The study showed that the protease inhibitors found in chickpeas significantly inhibited the viability of certain Breast cancer cells, as well both androgen-dependent and androgen-independent prostate cancer cells at concentrations that were reasonable. (gim-academy.com)
  • Several protease inhibitors that are used in combination with other drugs to treat Human Immunodeficiency Virus (HIV) infection may also be effective against certain types of cancer, according to researchers from the National Cancer Institute (NCI), part of the National Institutes of Health. (nih.gov)
  • There are several successful examples of this approach, including the use of COX-2 inhibitors (anti-inflammatory drugs) for colon cancer prevention and lenalidomide (a morning sickness drug) for myelodysplastic syndromes. (nih.gov)
  • If the term protease inhibitor rings a bell, that's because drugs that work in this way already are in use to treat other viruses, including human immunodeficiency virus (HIV) and hepatitis C virus. (nih.gov)
  • This study screened FDA-approved and investigational drugs in the DrugBank database for their potential as HIV-1 protease inhibitors . (bvsalud.org)
  • The researchers found that blood levels of anti-malarial drugs were higher in children who had received the protease inhibitors, which may help explain their effectiveness at preventing malaria's return. (nih.gov)
  • The peptides may be used in the treatment of virally infected cells, in the preparation of vaccine formulations, in the generation of clinically relevant antibodies and anti-idiotypic antibodies and in the generation of a screening assay or kit that can be used to identify other similarly acting protease inhibitors. (nih.gov)
  • The data presented herein clearly demonstrate that protease inhibitors protect AEC barrier function against meconium-induced injury, and suggest the future possibility of using protease inhibitors in the treatment of meconium aspiration syndrome. (nih.gov)
  • The use of protease inhibitors in human immunodeficiency virus type 1 ( HIV-1 ) treatment is limited by adverse effects , including metabolic complications . (bvsalud.org)
  • They received either an NNRTI (nevirapine for children under age 3, efavirenz for children over age 3) or the protease inhibitor-based treatment. (nih.gov)
  • This invention includes a novel high-throughput assay to identify orthosteric inhibitors blocking the Zika virus NS2B-NS3 protease. (nih.gov)
  • The described assay is the first high-throughput method to aid in the identification of a flavivirus NS2B-NS3 protease inhibitor. (nih.gov)
  • Antiretroviral agents other than protease inhibitors may be used concurrently with this regimen. (cdc.gov)
  • It is less expensive than the protease inhibitor combination and, unlike the protease inhibitors, does not need refrigeration. (nih.gov)
  • Phase 1 single dose studies to optimize the pharmacokinetics of DG17, a novel HIV-protease inhibitor. (edu.au)
  • PROTEASE INHIBITOR RELATED ATHEROSCLEROSIS IN HIV INFECTION Release Date: October 5, 1999 RFA: HL-00-007 National Heart, Lung and Blood Institute National Institute of Diabetes and Digestive and Kidney Diseases Letter of Intent Receipt Date: December 15, 1999 Application Receipt Date: January 12, 2000 THIS RFA USES THE "MODULAR GRANT" AND "JUST-IN-TIME" CONCEPTS. (nih.gov)
  • Gabe Allen, Discover Magazine , 9 Feb. 2022 In 1999, a French study first confirmed that hair loss was a side effect of men using the protease inhibitor Crixivan (indinavir). (merriam-webster.com)
  • Merriam-Webster.com Dictionary , Merriam-Webster, https://www.merriam-webster.com/dictionary/protease%20inhibitor. (merriam-webster.com)
  • William A. Haseltine, Forbes , 9 June 2022 But a protease is an enzyme that is involved in copying a virus' genetic material, which meant that testing a protease inhibitor would involve using live viruses. (merriam-webster.com)
  • Secretory leukocyte protease inhibitor (SLPI) has been suggested as the main soluble factor responsible for the HIV inhibitory effect of saliva. (jpalliativecare.com)
  • The researchers concluded these findings suggest protease inhibitors from chickpeas, kidney beans, and mung beans may possess similar anticancer properties to that of the soybean Bowman-Birk protease inhibitor, and deserve further study as possible cancer preventive agents. (gim-academy.com)
  • In the case of 332, it targets a protease called M pro , also called the 3CL protease, coded for by SARS-CoV-2. (nih.gov)