Protease inhibitors. Medical search

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.

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)

Inhibitors[edit]. Main articles: Protease inhibitor (biology) and Protease inhibitor (pharmacology). The activity of proteases ... The natural protease inhibitors are not to be confused with the protease inhibitors used in antiretroviral therapy. Some ... Thus, protease inhibitors are developed as antiviral means. Other natural protease inhibitors are used as defense mechanisms. ... TopFIND - database of protease specificity, substrates, products and inhibitors. *MEROPS - Database of protease evolutionary ...

https://en.wikipedia.org/wiki/E1101

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". Handb Exp Pharmacol. Handbook of Experimental ... "The Role of Protease Inhibitors in the Pathogenesis of HIV-Associated Lipodystrophy: Cellular Mechanisms and Clinical ...

https://en.wikipedia.org/wiki/Antiviral_drug

It is of the protease inhibitor (PI) class and works by blocking HIV protease. Atazanavir was approved for medical use in the ... Lv, Z; Chu, Y; Wang, Y (2015). "HIV protease inhibitors: a review of molecular selectivity and toxicity. ". HIV/AIDS - Research ... PMC 4396582 . Graziani, Amy L (June 17, 2014). "HIV protease inhibitors". UpToDate. Bold, G; Fässler, A; Capraro, HG; Cozens, R ... "New Aza-Dipeptide Analogues as Potent and Orally Absorbed HIV-1 Protease Inhibitors: Candidates for Clinical Development". ...

https://en.wikipedia.org/wiki/Atazanavir

HIV protease inhibitors; the antidepressant nefazodone; the cardiovascular drug gemfibrozil; the immunosuppressant ciclosporin ... Tobert JA (2003). "Lovastatin and beyond: the history of the HMG-CoA reductase inhibitors". Nat Rev Drug Discov. 2 (7): 517-26 ... This discovery encouraged scientists worldwide to find an effective inhibitor of this enzyme.[citation needed] By 1976, Akira ... While developing and researching lovastatin, Merck scientists synthetically derived a more potent HMG-CoA reductase inhibitor ...

https://en.wikipedia.org/wiki/Simvastatin

For use only in patients with HIV receiving protease inhibitors *^ For treatment of latent TB infection (LTBI) only ...

https://en.wikipedia.org/wiki/List_of_World_Health_Organization_Essential_Medicines

Endogenous plasma protease inhibitors deactivate drotrecogin. Therefore, no dose adjustment is needed in elderly patients, or ... Factor Xa inhibitors. (with some II inhibition). Heparin group/. glycosaminoglycans/. (bind antithrombin). *Low molecular ... Drotrecogin alpha (activated) belongs to the class of serine proteases. Drotrecogin alfa has not been found to improve outcomes ... Recent administration (within 7 days) of ,650 mg/day of aspirin or other platelet inhibitors ...

https://en.wikipedia.org/wiki/Drotrecogin_alfa

HIV-1 protease inhibitor. S. acmella L.. Whole plant. Chloroform, methanol and water. In vitro HIV-1 protease solution assay ...

https://en.wikipedia.org/wiki/Acmella_oleracea

Protease inhibitorsEdit. Protease inhibitors found in HIV drugs are linked to insulin resistance.[35] ... Fantry, Lori E (2003-03-24). "Protease Inhibitor-Associated Diabetes Mellitus: A Potential Cause of Morbidity and Mortality". ... electron transport chain inhibitors, or mitochondrial superoxide dismutase mimetics.[49] ...

https://en.m.wikipedia.org/wiki/Insulin_resistance

Telaprevir is a protease inhibitor. In 2012 ivacaftor, was designated as an orphan drug, identifying cystic fibrosis as ...

https://en.wikipedia.org/wiki/Vertex_Pharmaceuticals

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 ...

https://en.wikipedia.org/wiki/Streptomyces_violascens

"Nucleotide Prodrug GS-5734 Is a Broad-Spectrum Filovirus Inhibitor That Provides Complete Therapeutic Protection Against the ... NS3/4A protease inhibitors (-previr). *Asunaprevir. *Boceprevir‡. *Ciluprevir§. *Danoprevir†. *Faldaprevir‡. *Glecaprevir. * ...

https://en.wikipedia.org/wiki/Remdesivir

NS3/4A protease inhibitors (-previr). *Asunaprevir. *Boceprevir‡. *Ciluprevir§. *Danoprevir†. *Faldaprevir‡. *Glecaprevir. * ...

https://en.wikipedia.org/wiki/Intron_A

... like several HIV protease inhibitors, its blood levels are greatly increased by low doses of ritonavir, a potent inhibitor of ... researchers found the points of attack of the HIV protease inhibitors - agents that block the breakdown of proteins. Protease ... Both medications are HIV protease inhibitors. Ritonavir functions by slowing down the breakdown of lopinavir. Lopinavir/ ... 1998) ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease. Antimicrob. Agents Chemother. 42: 3218- ...

https://en.wikipedia.org/wiki/Lopinavir/ritonavir

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 ( ...

https://en.wikipedia.org/wiki/Caspase_8

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. ... The CASP8 gene encodes a member of the cysteine-aspartic acid protease (caspase) family. Sequential activation of caspases ...

https://en.wikipedia.org/wiki/CASP8

aM 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 (i) the ability to inhibit proteases from all ... In addition to tetrameric forms of alpha-2-macroglobulin, dimeric, and more recently monomeric aM protease inhibitors have been ... The alpha-macroglobulin (aM) family of proteins includes protease inhibitors, typified by the human tetrameric alpha-2- ...

https://en.wikipedia.org/wiki/Alpha-2-Macroglobulin

"Protease inhibitors targeting coronavirus and filovirus entry". Antiviral Res. 116: 76-84. doi:10.1016/j.antiviral.2015.01.011 ... Another proposed therapy is inhibition of viral protease or kinase enzymes. Researchers are investigating a number of ways to ... Báez-Santos YM, St John SE, Mesecar AD (Mar 2015). "The SARS-coronavirus papain-like protease: structure, function and ... "Thiopurine analogs and mycophenolic acid synergistically inhibit the papain-like protease of Middle East respiratory syndrome ...

https://en.wikipedia.org/wiki/Middle_East_respiratory_syndrome

... (IDV; trade name Crixivan, made by Merck) is a protease inhibitor used as a component of highly active antiretroviral ... Protease inhibitors changed the nature of AIDS from a terminal illness to a somewhat manageable one. It significantly increased ... Cohen J (June 1996). "Protease inhibitors: a tale of two companies". Science. 272 (5270): 1882-3. Bibcode:1996Sci...272.1882C. ... Just like Study 035, patients couldn't be in the study if they had prior protease inhibitor treatment or lamivudine for more ...

https://en.wikipedia.org/wiki/Indinavir

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 ... A1PI is both an endogenous protease inhibitor and an exogenous one used as medication. The pharmaceutical form is purified from ...

https://en.wikipedia.org/wiki/Alpha-1_antitrypsin

Protein C inhibitor, a serine protease inhibitor. Other uses in science and technology[edit]. *Panel call indicator, telephone ... Potato carboxypeptidase inhibitor, a natural peptide usable for thrombolytic and cancer therapy ...

https://en.wikipedia.org/wiki/PCI

... current effective inhibitor targeting a 3C-like protease". Protein & Cell. 4 (4): 248-50. doi:10.1007/s13238-013-2841-3. PMC ... "Protease inhibitors targeting coronavirus and filovirus entry". Antiviral Research. 116: 76-84. doi:10.1016/j.antiviral.2015.01 ... Another proposed therapy is inhibition of viral protease[43] or kinase enzymes.[44] Researchers are investigating a number of ... "Thiopurine analogs and mycophenolic acid synergistically inhibit the papain-like protease of Middle East respiratory syndrome ...

https://en.wikipedia.org/wiki/MERS

nov., a marine bacterium that produces protease inhibitors". International Journal of Systematic and Evolutionary Microbiology ...

https://en.wikipedia.org/wiki/Algicola_sagamiensis

Protease inhibitors soybean, seeds, legumes, potatoes, eggs, cereals. Nutrient Essential nutrient List of macronutrients List ...

https://en.wikipedia.org/wiki/List_of_phytochemicals_in_food

Many types of plants produce protease inhibitors, which inactivate proteases. Protease inactivation can lead to many issues ... Some of these mechanisms include developing protease enzymes that are unaffected by the plant protease inhibitors, gaining the ... The Adaptation of Insects to Plant Protease Inhibitors. Journal of Insect Physiology. 43, 885-895. Musser, R. O., S. M. Hum- ... An important enzyme produced by herbivorous insects is protease. The protease enzyme is a protein in the gut that helps the ...

https://en.wikipedia.org/wiki/Herbivore_adaptations_to_plant_defense

... is a protease inhibitor: it inhibits HIV-1 and HIV-2 proteases. HIV protease is an aspartate protease which splits ... All protease inhibitors bind to the protease, the precise mode of binding determines how the molecule inhibits the protease. ... Pyrko P, Kardosh A, Wang W, Xiong W, Schönthal AH, Chen TC (2007). "HIV-1 protease inhibitors nelfinavir and atazanavir induce ... Nelfinavir's interaction profile is similar to that of other protease inhibitors. Most interactions occur at the level of the ...

https://en.wikipedia.org/wiki/Nelfinavir

Nixon AE, Wood CR (March 2006). "Engineered protein inhibitors of proteases". Curr Opin Drug Discov Dev. 9 (2): 261-8. PMID ...

https://en.wikipedia.org/wiki/Antibody_mimetic

Salier JP (1990). "Inter-alpha-trypsin inhibitor: emergence of a family within the Kunitz-type protease inhibitor superfamily ... Examples of Kunitz-type protease inhibitors are aprotinin (bovine pancreatic trypsin inhibitor, BPTI), Alzheimer's amyloid ... or basic protease inhibitor), but the family includes numerous other members, such as snake venom basic protease; mammalian ... tissue factor pathway inhibitor precursor; and Kunitz STI protease inhibitor contained in legume seeds. Kunitz domains are ...

https://en.wikipedia.org/wiki/Kunitz_domain

It is common that a protease inhibitor is added to lysis buffer, along with other enzyme inhibitors of choice, such as a ... 100 U/ml protease inhibitor, such as aprotinin. SDS (sodium dodecyl sulfate) lysis buffer[edit]. SDS is ionic denaturing ... For lysis buffers targeted at protein extraction, protease inhibitors are often included, and in difficult cases may be almost ... The important factors to be considered are: pH, ionic strength, usage of detergent, protease inhibitors to prevent proteolytic ...

https://en.wikipedia.org/wiki/Lysis_buffer

Important antiretroviral drugs include the class of protease inhibitors. Herpes viruses, best known for causing cold sores and ... influenza A and B viruses have become resistant to neuraminidase inhibitors such as oseltamivir and the search for new ...

https://en.wikipedia.org/wiki/Antimicrobial

Murdock, L. L.; Shade, R. E. (2002). "Lectins and Protease Inhibitors as Plant Defenses against Insects". Journal of ...

https://en.wikipedia.org/wiki/Genetically_engineered_potato

Dual serotonin and norepinephrine reuptake inhibitors. *Selective serotonin reuptake inhibitors. *Gliflozins. *HIV-protease ...

https://en.wikipedia.org/wiki/GABAA_receptor_positive_allosteric_modulator

Cysteine proteases. Trypsin inhibitors. *Kunitz inhibitor. *Bowman-Birk inhibitor. Other. *Soy lecithin (mix of Phospholipids) ...

https://en.wikipedia.org/wiki/Tương

The same step can be also blocked by several gamma-secretase inhibitors, shown in the same study.[19] These evidences ... "A presenilin-1-dependent gamma-secretase-like protease mediates release of Notch intracellular domain". Nature. 398 (6727): 518 ... "Photoactivated gamma-secretase inhibitors directed to the active site covalently label presenilin 1". Nature. 405 (6787): 689- ... Based on evidence that a gamma-secretase inhibitor binds to the fragments,[11] the cleaved presenilin complex is considered to ...

https://en.wikipedia.org/wiki/PSEN1

is modified to include binding of the inhibitor to the free enzyme:. EI. +. S. ⇌. k. 3. k. −. 3. E. +. S. +. I. ⇌. k. −. 1. k. ... is the inhibitor concentration.. V. max. {\displaystyle V_{\max }}. remains the same because the presence of the inhibitor can ... To compute the concentration of competitive inhibitor [. I. ]. {\displaystyle {\ce {[I]}}}. that yields a fraction f. V. 0. {\ ... At this point, we can define the dissociation constant for the inhibitor as K. i. =. k. −. 3. /. k. 3. {\displaystyle K_{i}=k ...

https://en.wikipedia.org/wiki/Competitive_inhibition

CTRL: Chymotrypsin-like protease. *DCTPP1: encoding enzyme dCTP pyrophosphatase 1. *DEL16p13.3, RSTSS: Chromosome 16p13.3 ... CIAPIN1: Anamorsin (originally, Cytokine induced apoptosis inhibitor 1). *CKLF: Chemokine-like factor ...

https://en.wikipedia.org/wiki/Chromosome_16

Protease Inhibitors (PI). (Discovery and development). 1st generation. *Amprenavir (APV)◊. *Fosamprenavir (FPV) ... Dolutegravir is an HIV integrase strand transfer inhibitor which blocks the functioning of HIV integrase which is needed for ... who are treatment-naïve or treatment-experienced but have not previously taken other integrase strand transfer inhibitors.[8] ... including those who have been treated with other integrase strand transfer inhibitors. Tivicay is also approved for children ...

https://en.wikipedia.org/wiki/Dolutegravir

Multiple human trials utilizing HMG-CoA reductase inhibitors, known as statins, have repeatedly confirmed that changing ... 2 protease), two enzymes that are activated by SCAP when cholesterol levels are low. The cleaved SREBP then migrates to the ...

https://si.wikipedia.org/wiki/කොලෙස්ටරෝල්

Wang Y, Macke JP, Abella BS, Andreasson K, Worley P, Gilbert DJ, Copeland NG, Jenkins NA, Nathans J (Jun 1996). "A large family of putative transmembrane receptors homologous to the product of the Drosophila tissue polarity gene frizzled". J Biol Chem. 271 (8): 4468-76. doi:10.1074/jbc.271.8.4468. PMID 8626800 ...

https://en.wikipedia.org/wiki/FZD5

t-PA and urokinase are themselves inhibited by plasminogen activator inhibitor-1 and plasminogen activator inhibitor-2 (PAI-1 ... leading to the production of circulating fragments that are cleared by other proteases or by the kidney and liver. ... Factor Xa inhibitors. (with some II inhibition). Heparin group/. glycosaminoglycans/. (bind antithrombin). *Low molecular ... Coagulation inhibitors. *Antithrombin (inhibits II, IX, X, XI, XII). *Protein C (inhibits V, VIII)/Protein S (cofactor for ...

https://en.wikipedia.org/wiki/Fibrinolysis

... protease - protease inhibitors - protease-sparing regimen - proteins - protocol - protozoa - provirus - pruritus - pseudo- ... entry inhibitors - Env - envelope - enzyme - enzyme-linked immunosorbent assay (ELISA) - eosinophil - eosinophilic folliculitis ... integrase inhibitors - interaction - interferon - interleukin-1 (IL-1) - interleukin-2 (IL-2) - interleukin-4 (IL-4) - ... nucleoside reverse transcriptase inhibitors (NRTI) - nucleotide - nucleotide analogs - nucleus - null cell ...

https://en.m.wikipedia.org/wiki/Index_of_AIDS-related_topics

protein kinase inhibitor activity. • histone binding. • Tat protein binding. • NF-kappaB binding. • ligação a proteínas ... 2008). «Nucleolar protein B23/nucleophosmin regulates the vertebrate SUMO pathway through SENP3 and SENP5 proteases.». J Cell ... 2008). «The nucleolar SUMO-specific protease SENP3 reverses SUMO modification of nucleophosmin and is required for rRNA ...

https://pt.m.wikipedia.org/wiki/NPM1

... and breakdown of the connective tissue of the lungs by proteases that are insufficiently inhibited by protease inhibitors. The ... are phosphodiesterase-4 inhibitors (PDE4) and act as anti-inflammatories. They show promise in decreasing the rate of ... "Phosphodiesterase-4 inhibitors for chronic obstructive pulmonary disease". The Cochrane Database of Systematic Reviews. 5 ...

https://en.wikipedia.org/wiki/COPD

Protease Inhibitors (PI). (Discovery and development). 1st generation. *Amprenavir (APV)◊. *Fosamprenavir (FPV) ...

https://en.wikipedia.org/wiki/Ceragenins

Industrial drugs that are designed as protease and reverse-transcriptase inhibitors are made such that they target specific ... Protease is expressed differently in different viruses. It functions in proteolytic cleavages during virion maturation to make ... However these drugs can quickly become ineffective due to the fact that the gene sequences that code for the protease and the ... Proteins: consisting of gag proteins, protease (PR), pol proteins, and env proteins. *Group-specific antigen (gag) proteins are ...

https://en.wikipedia.org/wiki/SsRNA-RT_virus

These infectious agents produce proteases and collagenases which break down the corneal stroma. Complete loss of the stroma can ... Treatment includes antibiotics and collagenase inhibitors such as acetylcysteine. Surgery in the form of corneal ...

https://en.m.wikipedia.org/wiki/Corneal_ulcer

The molecule ritonavir, marketed as Norvir, was developed as a protease inhibitor and used to target HIV infection. However, it ... "How an inhibitor of the HIV-I protease modulates proteasome activity". The Journal of Biological Chemistry. 274 (50): 35734-40 ... See also: threonine protease § mechanism. The proteasome functions as an endoprotease.[64][65][66][67] The mechanism of ... The inner two rings are made of seven β subunits that contain three to seven protease active sites. These sites are located on ...

https://en.m.wikipedia.org/wiki/Proteasome

... has the ability to inhibit the replication of viruses that are resistant to other protease inhibitors and it ... Tipranavir (TPV), or tipranavir disodium, is a nonpeptidic protease inhibitor (PI) manufactured by Boehringer Ingelheim under ... "Selection and Characterization of HIV-1 Showing Reduced Susceptibility to the Non-Peptidic Protease Inhibitor Tipranavir". ...

https://en.wikipedia.org/wiki/Tipranavir

Cysteine proteinase inhibitors screening of fungal species growing in Slovenia]. Acta Pharmaceutica (in Slovenian). 50 (1): 39- ... Cortinarius violaceus extract demonstrates an inhibitory activity against cysteine protease.[28] ...

https://en.m.wikipedia.org/wiki/Cortinarius_violaceus

Wlodawer A, Vondrasek J (1998). "Inhibitors of HIV-1 protease: a major success of structure-assisted drug design". 》Annual ... "Protease - GMO Database". 》GMO Compass》. European Union. 10 July 2010. 24 February 2015에 원본 문서에서 보존된 문서. 28 February 2015에 확인함. ... "The discovery and development of HMG-CoA reductase inhibitors" (PDF). 》J. Lipid Res.》 33 (11): 1569-82. PMID 1464741 ... "Allosteric small-molecule kinase inhibitors" (PDF). 》Pharmacology & Therapeutics》 (영어) 156: 59-68. doi:10.1016/j.pharmthera. ...

https://ko.wikipedia.org/wiki/효소

Robert A. Copeland (2013). Evaluation of Enzyme Inhibitors in Drug Discovery: A Guide for Medicinal Chemists and ... "Some characteristics of hydrolysis of synthetic substrates and proteins by the alkaline proteases from Aspergillus sojae". ... http://books.google.com/books/about/Evaluation_of_Enzyme_Inhibitors_in_Drug.html?id=l2rMy8QNUk0C. ...

https://sh.wikipedia.org/wiki/Orizin

Roberts SB (December 2002). "γ-secretase inhibitors and Alzheimer's disease". Adv. Drug Deliv. Rev. 54 (12): 1579-88. PMID ... necesítase un composto que poida bloquear o sitio activo das aspartil proteases e que poida atravesar a barreira ... an inhibitor of beta-amyloid(1-42) aggregation". Bioorg. Med. Chem. 10 (11): 3565-9. PMID 12213471. doi:10.1016/S0968-0896(02) ... "New class of inhibitors of amyloid-beta fibril formation. Implications for the mechanism of pathogenesis in Alzheimer's disease ...

https://gl.wikipedia.org/wiki/Amiloide_beta

protease binding. • tumor necrosis factor receptor binding. • cytokine activity. • identical protein binding. ... These disorders are sometimes treated by using a TNF inhibitor. This inhibition can be achieved with a monoclonal antibody such ... Nevertheless, TRADD binds FADD, which then recruits the cysteine protease caspase-8. A high concentration of caspase-8 induces ... On the other hand some patients treated with TNF inhibitors develop an aggravation of their disease or new onset of ...

https://en.wikipedia.org/wiki/TNF-alpha

The cathelicidin family shares primary sequence homology with the cystatin[9] family of cysteine proteinase inhibitors, ... Zaiou M, Nizet V, Gallo RL (May 2003). "Antimicrobial and protease inhibitory functions of the human cathelicidin (hCAP18/LL-37 ... "Increased serine protease activity and cathelicidin promotes skin inflammation in rosacea". Nature Medicine. 13 (8): 975-80. ... Cathelicidin is cleaved into the antimicrobial peptide LL-37 by both kallikrein 5 and kallikrein 7 serine proteases. Excessive ...

https://en.wikipedia.org/wiki/Cathelicidin

G-protein coupled receptor 120 is a protein that in humans is encoded by the GPR120 gene.[5][6] GPR120 is a member of the rhodopsin family of G protein-coupled receptors (GPRs).[5][6] GPR120 has also been shown to mediate the anti-inflammatory and insulin-sensitizing effects of omega 3 fatty acids.[7] Lack of GPR120 is responsible for reduced fat metabolism, thereby leading to obesity.[8] Additionally, GPR120 has been implicated to be involved in the ability to taste fats.[9] It is expressed in taste bud cells (specifically cell type II, which contain other G-protein coupled taste receptors), and its absence leads to reduced preference to two types of fatty acid (linoleic acid and oleic acid), as well as decreased neuronal response to oral fatty acids.[10] ...

https://en.wikipedia.org/wiki/GPR120

... such as the production of protease inhibitors to slow the growth of insects. The hormone was first identified in tomatoes, but ...

https://en.wikipedia.org/wiki/🍅

Neuraminidase inhibitors. Overall the benefits of neuraminidase inhibitors in those who are otherwise healthy do not appear to ... However, in highly virulent strains, such as H5N1, the hemagglutinin can be cleaved by a wide variety of proteases, allowing ... M2 inhibitors. The antiviral drugs amantadine and rimantadine inhibit a viral ion channel (M2 protein), thus inhibiting ... The two classes of antiviral drugs used against influenza are neuraminidase inhibitors (oseltamivir, zanamivir, laninamivir and ...

https://en.m.wikipedia.org/wiki/Influenza

... inducing the NK cell to release proteins such as perforin and proteases known as granzymes, which causes the lysis of the ... C1-inhibitor (Angioedema/Hereditary angioedema). *Complement 2 deficiency/Complement 4 deficiency. *MBL deficiency ...

https://en.wikipedia.org/wiki/Antibody-dependent_cellular_cytotoxicity

As well, the amino-thalidomide and amino-EM-12 were potent inhibitors of TNF-α. These two analogs later got the name ... an important cysteine protease expressed in osteoclasts. In vitro, apremilast reduces PDE4 activity leading to an increase in ... This effect is not related to TNF-α inhibition since potent TNF-α inhibitors such as rolipram and pentoxifylline did not ... Inhibition of TNF-α is not the mechanism of thalidomide's inhibition of angiogenesis since numerous other TNF-α inhibitors do ...

https://en.wikipedia.org/wiki/Development_of_analogs_of_thalidomide

... mol1 at ifm.mh-hannover.de mol1 at ifm.mh-hannover.de Tue May 9 08:41:27 EST 1995 *Previous message ... protease inhibitors , 100 mM PMSF , 1 mM EDTA , 1,5 microg/ml Pepstatin , 1 mM Benzamidin , 2 microg/ml Leupeptin , , ... phosphatase inhibitors , 1,25 microM Ocadaic Acid , 5 mM Natriumfluoride , , others , 10 microl/ml NP-40 Sorry, I made a ...

http://www.bio.net/bionet/mm/proteins/1995-May/002585.html

... or other protease inhibitors. Kaletra® is thus far the only protease inhibitor for which resistance has not been observed in ... New protease inhibitor held HIV at undetectable levels for four years. 30.09.2002 ... A study from The Feinberg School of Medicine has shown that the protease inhibitor lopinavir/ritonavir (Kaletra®) suppressed ...

http://www.innovations-report.com/html/reports/medicine-health/report-13260.html

Poster #1885: Combination of the NS3/4A Protease Inhibitor ITMN-191 (R7227) with the Active Moiety of the NS5B Inhibitors R1626 ... Home › News › Clinical Trials › InterMune to Present Four Abstracts on HCV Protease Inhibitor ITMN-191 at the AASLD Meeting ... InterMune to Present Four Abstracts on HCV Protease Inhibitor ITMN-191 at the AASLD Meeting. Print this page ... ITMN-191 is a hepatitis C virus (HCV) NS3 protease inhibitor, currently in a Phase 1b clinical trial in combination with ...

https://www.drugs.com/clinical_trials/intermune-present-four-abstracts-hcv-protease-inhibitor-itmn-191-aasld-meeting-5634.html

Our protease inhibitor systems offer superior protease inhibition and easily out-perform competitors. ... A huge selection of proteases including Trypsin and Proteinase K are available. ... Protease & Protease Inhibitor Systems. Our Protease & Protease Inhibitor Systems include proteases, protease assays and ... A range of protease inhibitor cocktails and individual inhibitors can be found in our protease inhibitor section. ...

https://www.gbiosciences.com/Protease-Protease-Inhibitor-Systems?page=3

Notes: Sales, means the sales volume of Protease Inhibitor Revenue,... ... Check for Discount on United States Protease Inhibitor Market Report 2016 report by QYResearch Group. ... 1 Protease Inhibitor Overview 1.1 Product Overview and Scope of Protease Inhibitor 1.2 Classification of Protease Inhibitor 1.2 ... of Protease Inhibitor (2011-2021) 1.4.1 USA Protease Inhibitor Sales and Growth Rate (2011-2021) 1.4.2 USA Protease Inhibitor ...

http://www.reportsnreports.com/reports/689631-united-states-protease-inhibitor-market-report-2016.html

Proteases are also capable of cleaving non-extracellular matrix molecules. Inhibitors of proteases to some extent can reduce ... protease inhibitor;tumor metastasis;targeted cancer therapy; Proteases are important molecules that are involved in many key ... In this review, we focus on the role of a few proteases and their inhibitors in tumors as a basis for cancer prognostication ... Protease signaling pathways are strictly controlled, and disorders in protease activity can result in pathological changes such ...

http://koreascience.or.kr/article/JAKO201605555186235.page

Pfizer is investigating selective site-1 protease inhibitors for the potential treatment of lipid and metabolic disorders. Site ... Mechanism of Action Cholesterol synthesis inhibitors; Transcription factor inhibitors * Orphan Drug Status Orphan designation ... Research programme: site-1 protease inhibitors - Pfizer Alternative Names: PF 429242; Research programme: sterol regulatory ... element binding protein site-1 protease inhibitors Latest Information Update: 16 Jul 2016 ...

http://adisinsight.springer.com/drugs/800027792?error=cookies_not_supported&code=dbdd75d7-e4ea-44bf-912b-d167afcba417

For natural protease inhibitors, see protease inhibitor (biology).. Protease inhibitors (PIs) are a class of antiviral drugs ... Protease inhibitors prevent viral replication by selectively binding to viral proteases (e.g. HIV-1 protease) and blocking ... Protease inhibitors can cause a syndrome of lipodystrophy, hyperlipidemia, diabetes mellitus type 2, and kidney stones.[13] ... Protease inhibitors that have been developed and are currently used in clinical practice include: *Antiretroviral HIV-1 ...

https://en.wikipedia.org/wiki/HIV_protease_inhibitor

... protease) necessary in the late stages of its reproduction. Clinical trials of the protease inhibitor indinavir have shown ... protease inhibitor prō´tē-ās˝ [key], any of a class of drugs that interfere with replication of the AIDS virus ( HIV ), by ... Clinical trials of the protease inhibitor indinavir have shown it to be especially beneficial in combination with the anti-HIV ... blocking an enzyme (protease) necessary in the late stages of its reproduction. ...

https://www.infoplease.com/encyclopedia/medicine/drug/pharmacology/protease-inhibitor

Protease inhibitors Protease inhibitors (pronounced PRO-tee-ace in-HIH-bi-ters) are a new type of drugs that slow down the ... Protease Inhibitors. Definition. A protease inhibitor is a type of drug that cripples the enzyme protease. An enzyme is a ... Protease inhibitors. Protease inhibitors (pronounced PRO-tee-ace in-HIH-bi-ters) are a new type of drugs that slow down the ... How protease inhibitors work. Protease inhibitors are antiviral drugs that interrupt how HIV uses a healthy cell to make copies ...

https://www.encyclopedia.com/medicine/drugs/pharmacology/protease-inhibitor

Protease accumulated by inhibitors (PABI) is a protein participating in eukaryotic translation, by making interaction between ... "Isolation and characterization of a novel large protease accumulated in mammalian cells in the presence of inhibitors". J. Biol ...

https://en.wikipedia.org/wiki/Protease_accumulated_by_inhibitors

Protease inhibitor can refer to: Protease inhibitor (pharmacology): a class of medication that inhibits viral protease Protease ...

https://en.wikipedia.org/wiki/Protease_inhibitor

The present invention also provides methods of inhibiting proteases, more specifically aspartyl proteases. In certain ... the compounds of the invention are inhibitors of proteases, and more specifically inhibitors of aspartyl proteases. In certain ... As noted above, there has been increasing interest ion recent years in the development of aspartyl protease inhibitors, ... As discussed above, certain of the compounds as described herein exhibit activity generally as inhibitors of aspartyl proteases ...

http://www.google.nl/patents/US7115652

PIs work by preventing protease from cutting long chains of proteins into shorter ones ... ... Commonly known as Viracept this is the most commonly prescribed protease inhibitor today. Viracept is usually taken as three ... PIs work by preventing protease from cutting long chains of proteins into shorter ones necessary for HIV to make new copies of ...

http://www.thebody.com/content/art2005.html

Protein which inhibits the activity of a thiol protease, a class of proteases that contains an active site cysteine residue ( ...

http://www.uniprot.org/keywords/KW-0789

... ) and How do antimalarials and protease inhibitors (PIs) interact? ... Drug-Drug Interactions Between HMG-CoA Reductase Inhibitors (Statins) and Antiviral Protease Inhibitors. Clin Pharmacokinet. ... Drugs & Diseases , Infectious Diseases , Common Drug Interactions with Protease Inhibitors Q&A ... Complex drug interactions of the HIV protease inhibitors 3: effect of simultaneous or staggered dosing of digoxin and ritonavir ...

https://www.medscape.com/answers/2041624-172352/how-do-antimalarials-and-protease-inhibitors-pis-interact

PIs block the protease enzyme and prevent the cell from producing new viruses. It is recommended that they be used in ... The proteins must be cut up by the HIV protease-a protein-cutting enzyme-to make functional new HIV particles. ...

https://www.poz.com/drugs/classes/Protease-Inhibitors

... James Howard Since some questions have been posted here regarding protease inhibitors ... I suggest this is why some individuals, who take protease inhibitors are developing diabetes. I suggest protease inhibitors ... briefly describes my explanation of how protease inhibitors work in relation to the recent findings that protease inhibitors ... Protease Inhibitors and Benzodiazepines. James Howard jmhoward at sprynet.com Mon Jul 7 07:18:42 EST 1997 *Previous message: ...

http://www.bio.net/bionet/mm/neur-sci/1997-July/029064.html

Species: Protease inhibitor I35 (TIMP) (IPR001820). Key Species. Key species. Number of proteins. FASTA. Protein IDs. ...

http://www.ebi.ac.uk/interpro/entry/IPR001820/taxonomy

Patterns of protease inhibitor cross-resistance in viral isolates with reduced susceptibility to ABT-378. 8th CROI. Poster 452 ... The change yielded a molecule that was more than a potent inhibitor of the HIV protease enzyme. It also strongly inhibited the ... that contain two protease inhibitors (PIs), usually ritonavir (Norvir) plus another PI. Ritonavirs function is not primarily ... None of them had ever taken saquinavir or any non-nucleoside reverse transcriptase inhibitor (NNRTI). At week 48, 56% had viral ...

http://www.thebody.com/content/art2639.html

The ability to replace an inhibitor bound to the HIV-1 protease in single crystals with other potent inhibitors offers the ... The ability to replace an inhibitor bound to the HIV-1 protease in single crystals with other potent inhibitors offers the ... Rapid X-ray diffraction analysis of HIV-1 protease-inhibitor complexes: inhibitor exchange in single crystals of the bound ... HIV-1 PROTEASE. A, B. 99. Human immunodeficiency virus 1. Mutation(s): 0 Gene Names: HIV-1 PROTEASE FROM THE NY5 ISOLATE. EC: ...

https://www.rcsb.org/structure/2BPZ

... and safety of cysteine protease inhibitors in cell culture or in vivo. We now report that specific cysteine protease inhibitors ... By labeled inhibitor studies, the predominant target of the cysteine protease inhibitors is Leishmania cpB (Fig. 2). However, ... Cysteine protease inhibitors as chemotherapy: Lessons from a parasite target. Paul M. Selzer, Sabine Pingel, Ivy Hsieh, ... Cysteine protease inhibitors as chemotherapy: Lessons from a parasite target. Paul M. Selzer, Sabine Pingel, Ivy Hsieh, ...

https://www.pnas.org/content/96/20/11015?ijkey=608dc206e4fe7879fd0cde335cde194ec944189a&keytype2=tf_ipsecsha

3. Protease inhibition The compounds provided herein have activity as inhibitors of proteases, such cysteine proteases, ... Scheibel, et al., "Protease inhibitors and antimalarial effects," Malaria and the Red Cell, pp. 131-142 (1984). Selkoe, " ... 1984) Protease inhibitors and antimalarial effects. In: Malaria and the Red Cell, Progress in CLinical and Biolgoical Research ... Cysteine protease inhibitors effective for in vivo use. 1994-12-20. Zimmerman et al.. 514/17. ...

https://www.freepatentsonline.com/5714471.html

Sequences matching input query are shown below. Original reference, patient identifier, isolate name, partial treatment histories and accession number are indicated. Complete treatment histories, when available, can be accessed by clicking the isolate name. Sequences may additionally be downloaded in the fasta format, or viewed as individual or composite alignments using the options above. If the user wishes to view individual alignments of isolates for which there are multiple clones, the user can choose to view either an alignment of consensus sequences derived from the clones or an alignment of each clone as well as a consensus sequence ...

http://hivdb.stanford.edu/cgi-bin/GetIsolateDataResiSubtype.cgi?class=PI&subtype=D&pos=58&cons=Q&aa=E&rx=PI_Naive&includeMixtures=No

... depend on activation of their envelope glycoproteins by host cell proteases. The respective enzymes are thus excellent targets ... Protease inhibitors targeting coronavirus and filovirus entry Antiviral Res. 2015 Apr;116:76-84. doi: 10.1016/j.antiviral. ... We report here that the cysteine protease inhibitor K11777, ((2S)-N-[(1E,3S)-1-(benzenesulfonyl)-5-phenylpent-1-en-3-yl]-2-{[(E ... Our results indicate that camostat, or similar serine protease inhibitors, might be an effective option for treatment of SARS ...

https://pubmed.ncbi.nlm.nih.gov/25666761/?dopt=Abstract

Both LCMI I and II are inhibitors of chymotrypsin and elastase (in vitro). They both inhibit the prophenol oxidase activation ... Protease inhibitor LCMI-IIAdd BLAST. 36. Amino acid modifications. Feature key. Position(s). DescriptionActions. Graphical view ... Protease inhibitor LCMI-IAdd BLAST. 35. PeptideiPRO_0000026709. 57 - 92. ... Belongs to the protease inhibitor I19 family. [View classification]PROSITE-ProRule annotation. Manual assertion according to ...

https://www.uniprot.org/uniprot/P80060

Although indinavir was one of the first protease inhibitors to be studied in children, its use in pediatrics has never been ... A phase I/II study of the protease inhibitor indinavir in children with HIV infection. Pediatrics. 1998;102(1 Pt 1):101-109. ... Pharmacokinetics of the protease inhibitor indinavir in human immunodeficiency virus type 1-infected children. Antimicrob ... Protease Inhibitors (PIs). Indinavir. Last Updated: May 22, 2018; Last Reviewed: May 22, 2018 ...

https://aidsinfo.nih.gov/guidelines/html/2/pediatric-arv/131/indinavir

Tableted formulation containing water-soluble protease inhibitors with broad specificity for the inhibition of serine, cysteine ... Protease Inhibitor Cocktails References Our portfolio of protease inhibitor cocktails are frequently cited in peer-reviewed ... Molecular Biology, Native Protein Sample Preparation, Protease Inhibitor Cocktails, Protease Inhibitors, Proteomics, Research ... What is the concentration of the inhibitors in Product S8820, SIGMAFAST™ Protease Inhibitor Tablets? ...

https://www.sigmaaldrich.com/catalog/product/SIGMA/S8820?lang=en®ion=US

It belongs to a class of drugs known as protease inhibitors, which block a key enzyme that helps viruses replicate.. AbbVie, ... The therapy, which is also a protease inhibitor combining two antiviral agents, should arrive by Tuesday, he said.. "Industry ... Kaletras two antiretroviral components, lopinavir and ritonavir, are protease inhibitors designed to block HIV viral ... is normally used to treat HIV patients and belongs to a class of drugs known as protease inhibitors, which block a key enzyme ...

http://www.natap.org/2020/newsUpdates/020420_02.htm

Inhibition of retroviral protease activity by an aspartyl proteinase inhibitor.. Katoh I1, Yasunaga T, Ikawa Y, Yoshinaka Y. ... Retrovirus protease is an enzyme that cleaves gag and gag-pol precursor polyproteins into the functional proteins of mature ... The primary structure has so far been determined for the protease of avian myeloblastosis virus, and of murine, feline and ... In this report we show that retrovirus proteases belong to the aspartyl proteinase group and demonstrate an inhibition by the ...

https://www.ncbi.nlm.nih.gov/pubmed/2821409?dopt=Abstract

Protease Inhibitors. Fosamprenavir. HIV Protease Inhibitors. Enzyme Inhibitors. Molecular Mechanisms of Pharmacological Action ... Fosamprenavir Versus Other Protease Inhibitors. The safety and scientific validity of this study is the responsibility of the ... Be on your first protease inhibitor (PI) containing regimen, and the regimen must consist of a PI +/- ritonavir and 2 ... and Efficiency of HIV-1 Infected Subjects Switching Their Current Protease-inhibitor Therapies for a Fosamprenavir Therapy Over ...

https://clinicaltrials.gov/show/NCT00094523?order=286

Protease Inhibitors. Fosamprenavir. HIV Protease Inhibitors. Enzyme Inhibitors. Molecular Mechanisms of Pharmacological Action ... Comparative Tolerability of Protease Inhibitors. The safety and scientific validity of this study is the responsibility of the ... Comparative Tolerability of Protease Inhibitors and the Associated Impact on Persistence, Healthcare Utilization, and ... Initiated treatment with a Protease inhibitor (PI)-based Combination antiretroviral therapy (cART) regimen ...

https://clinicaltrials.gov/show/NCT01450618?order=282

How do protease inhibitors work?. Protease inhibitors resemble the protein chain that the protease cuts. The protease inhibitor ... Protease inhibitors are a new class of drugs that works by blocking the HIV protease. Once the protease is blocked, HIV makes ... The combination of protease inhibitors and reverse transcriptase inhibitors is possible because there is no bad interaction ... This shows the interaction between HIV protease inhibitor and the residues that hydrogen bond to the inhibitor. Aspartate A25 ...

http://community.middlebury.edu/~sontum/chemistry/students/kim/inhibitor.html

Metallo-protease inhibitor with selectivity for aminopeptidases, Metallo-protease inhibitor, aminopeptidases M and B, Papain, ... Pepsin, Plasmin, Pro-caspase 3, Pronase E, Protease (Non-selective serine and cysteine protease inhibitor), Protease of ... Factor Xa Protease Inhibitor, Ficin, Granzyme B, Kallikrein tissue, Kallikrein, Plasma, Leucine Aminopeptidase, Leucine ... Bacteroides gingivalis, Proteasome inhibitor, Proteinase K, Renin, Thermolysin, Thrombin, Trypsin ...

https://www.sigmaaldrich.com/life-science/biochemicals/biochemical-products.html?TablePage=14573189

Protease-inhibitors have been extensively studied, rather than proteases, because they may represent a therapeutic approach for ... on a possible role of proteases and protease-inhibitors in molecular remodeling that may lead to some ocular diseases. Recently ... α1-proteinase inhibitor (α1-PI), metalloproteinase inhibitor (TIMP), maspin, SERPINA3K, SERPINB13, secretory leukocyte protease ... The protease-inhibitors mainly involved in the onset of the above-mentioned ocular pathologies are: α2-macroglobulin, ...

http://www.mdpi.com/1420-3049/19/12/20557

Novel macromolecular inhibitors of human immunodeficiency virus-1 protease.. Miklóssy G1, Tözsér J, Kádas J, Ishima R, Louis JM ... Molecular models of defective heterodimeric proteases (PR) containing a wild-type monomer A and PRRE (A) or PRRER (B) as ... 1H-15N Heteronuclear Single Quantum Coherence spectra of mutant proteases acquired either alone (A, C) or in the presence of ... Western blot analyses of viral particles containing wild-type or mutant proteases (1: wt PR, 2: PR5-95, 3: PRKWW, 4: PRRE, 5: ...

https://www.ncbi.nlm.nih.gov/pubmed/18480092

The major protease, cruzain, is a target for the development of new chemotherapy. We report the first successful treatment of ... an animal model of Chagas disease with inhibitors designed to inactivate cruzain. Treatment with fluoromethyl ke … ... Cysteine protease inhibitors cure an experimental Trypanosoma cruzi infection J Exp Med. 1998 Aug 17;188(4):725-34. doi: ... This study provides proof of concept that cysteine protease inhibitors can be given at therapeutic doses to animals to ...

https://pubmed.ncbi.nlm.nih.gov/9705954/

S)-1-Carboxy-2-Phenyl]-carbamoyl-Arg-Val-arginal Specificity: Inhibits Ca2+-dependent endopeptidases, including papain, trypsin-like serine proteases, some cysteine proteases and to a lesser extent plasmin. (gbiosciences.com)
N-[(S)-1-carboxy-isopentyl)-carbamoyl-alpha-(2-iminohexahydro-4(S)-pyrimidyl]-L-glycyl-L-phenylalaninal Specificity: Inhibits serine proteases having a chymotrypsin-like specificity, including α, β γ, and δ chymotrypsin, and most cysteine proteases including ca. (gbiosciences.com)
Features Specificity: Inhibits serine, plasmin, porcine kallikrein and cysteine proteases, including papain and cathepsin B. Does not inhibit chymotrypsin and thrombin. (gbiosciences.com)
N-alpha-L-rhamnopyranosyloxy(hydroxyphosphinyl)-L-Leucyl-L-Tryptophan Specificity: Inhibits some metalloproteases, including thermolysin, collagenase and bacterial metallo proteases from Bacillus subtilis, Streptomyces griseus and Pseudomonas aeruginosa (metallo elastase). (gbiosciences.com)

Isovaleryl-Val-Val-AHMHA-Ala-AHMHA where AHMHA= (3S, 4S)-4-amino-3-hydroxy-6-methyl-heptanoic acid Specificity: A potent inhibitor of various aspartic proteases, including cathepsin D, renin, pepsin, bacterial aspartic proteases and HIV proteases. (gbiosciences.com)

Activity: Approx 6,000 KIU/mg Specificity: A broad range, competitive and reversible inhibitor of chymotrypsin, plasmin, trypsin, kallikrein and other serine proteases Solubility: Soluble in water (Stoc. (gbiosciences.com)

They found that nearly two-thirds of the people who had taken protease inhibitors-such as indinavir, saquinavir and ritonavir-had abnormal fat distribution on their bodies and many also had high levels of triglycerides and cholesterol in their blood (see Figure) . (newscientist.com)

95% of protease enzyme activity making it 80% more effective than tablet cocktail formats. (gbiosciences.com)

Also known as bovine pancreatic trypsin inhibitor. (gbiosciences.com)

Our conclusion, after more than seven years of research, is that simplification of a suppressive triple antiretroviral therapy to boosted protease inhibitor monotherapy has demonstrated safety and efficacy in a high proportion of patients. (universidadeuropea.es)

A range of protease inhibitor cocktails and individual inhibitors can be found in our protease inhibitor section. (gbiosciences.com)

EDTA disodium salt is a reversible metalloprotease inhibitor that is used for chelating metal ions. (gbiosciences.com)

N-[(2S,3R)-3-Amino-2-hydroxy-4-phenylbutyryl]-L-leucine hydrochloride Specificity: Competitive inhibitor of surface aminopeptidases, including aminopeptidase B (Ki=2nM), leucine aminopeptidase (Ki=20nM). (gbiosciences.com)

Protease Inhibitors used in protein purification procedures Whenever proteins are analyzed in biological samples or purified from a natural source, protease activity is a potential threat. (biosynth.com)
During sample preparation, cells are frequently lysed and in this way they set free high amounts of protease activities that may digest the proteins of interest. (biosynth.com)

Serum alpha-thiol protease inhibitor concentrations in health. (mysciencework.com)
Serum alpha-thiol protease inhibitor concentrations in health and disease. (mysciencework.com)
Serum alpha-thiol protease inhibitor (alpha-TPI) concentration was assayed by radial immunodiffusion in normal subjects, pregnant women, and in a wide variety of diseases. (mysciencework.com)

Both resorufin and FITC Casein protease substrates are also available. (gbiosciences.com)

Although this is not a strategy to implement indiscriminately in all patients, it could be a good option for those patients with toxicity related to nucleoside reverse transcriptase inhibitors, or for trying to avoid such toxicities in virologically controlled patients without previous failure to protease inhibitors, restarting nucleosides if the viral load does not remain undetectable. (universidadeuropea.es)

Our Protease & Protease Inhibitor Systems include proteases, protease assays and screening systems, and protease inhibitors. (gbiosciences.com)
A selection of assays and screening systems for the detection of proteases are also available. (gbiosciences.com)
We have protease activity assays such as our Protease Screening Kit and Protease Assay Kit. (gbiosciences.com)

Called protease inhibitors, they have dramatically reduced death rates from AIDS, emptied hospital wards and allowed people with the virus to go back to work. (newscientist.com)

For that reason our main goal was the discovery of protease inhibitors as therapeutic agents. (tesisenred.net)

Doctors are shocked by the reported side effects because they had hoped that protease inhibitors were free of the serious complications that have dogged other anti-HIV drugs. (newscientist.com)

Inhibition of Leishmania cysteine protease activity was accompanied by defects in the parasite's lysosome/endosome compartment resembling those seen in lysosomal storage diseases. (pnas.org)
Tableted formulation containing water-soluble protease inhibitors with broad specificity for the inhibition of serine, cysteine, and metalloproteases. (sigmaaldrich.com)
One mL is recommended for the inhibition of proteases equivalent to 1 mg of USP pancreatin. (sigmaaldrich.com)
One tablet is recommended for the inhibition of proteases present in a maximum of 20 g of cell extract. (sigmaaldrich.com)
Inhibition of retroviral protease activity by an aspartyl proteinase inhibitor. (nih.gov)
In this report we show that retrovirus proteases belong to the aspartyl proteinase group and demonstrate an inhibition by the aspartyl proteinase-specific inhibitor, pepstatin A, on the activity of bovine leukaemia, Moloney murine leukaemia and human T-cell leukaemia virus proteases. (nih.gov)
Verseon's potent, highly selective, oral direct thrombin inhibitors act through reversible covalent inhibition, a unique mode of action. (biospace.com)
It is suggested that the two beta-turns play an essential role in the process of trypsin inhibition by protein protease inhibitors. (biomedsearch.com)
The percentage of protease inhibition is indicated. (thermofisher.com)
This thesis describes the synthesis of molecules designed for inhibition of two aspartic proteases, viral HIV-1 PR and human BACE-1. (diva-portal.org)
also roche has a guide to protease inhibition which also tells you what is in the tablets (and later on tells you what it is). (protocol-online.org)
The aim of the present paper was to determine the best kinetic model and kinetic parameters for production of protease and calculating Ki (inhibition constant) of different inhibitors to find the most effective one. (doaj.org)
As novel promising scaffold for HIV protease inhibition pyrrolidine-derived inhibitors have recently been reported. (uni-marburg.de)
The most potent compounds of the series achieve one-digit micromolar inhibition towards wild type as well as two mutant proteases (Ile50Val and Ile84Val). (uni-marburg.de)
Altogether, our findings suggest that a cascade of inhibition of host proteases initiated by EPI1 occurs in the tomato apoplast during infection by P. infestans. (osu.edu)
Inhibition of protease activity in protein preparations of bacterial lysates. (gbiosciences.com)
95% protease inhibition. (gbiosciences.com)

HIV-1 protease ) and blocking proteolytic cleavage of protein precursors that are necessary for the production of infectious viral particles . (wikipedia.org)
that the virus produces an enzyme or protein called protease that it must have to reproduce itself. (encyclopedia.com)
Protease accumulated by inhibitors (PABI) is a protein participating in eukaryotic translation, by making interaction between the 5' end and the 3' end of mRNA. (wikipedia.org)
Protein which inhibits the activity of a thiol protease, a class of proteases that contains an active site cysteine residue (Cys), e.g. papain, cathepsins, etc. (uniprot.org)
The proteins must be cut up by the HIV protease-a protein-cutting enzyme-to make functional new HIV particles. (poz.com)
The human EPPIN gene codes for EPPIN protein, which is a protease inhibitor. (endocrineweb.com)
Protease inhibitors are often structural mimics of protein active (binding) sites on which the proteases would normally bind. (citizendium.org)
The "complex" band is presumably an aggregate of protease with itself or with a carrier protein. (nih.gov)
Protease inhibitors resemble the protein chain that the protease cuts. (middlebury.edu)
The protease inhibitor binds to the site that normally binds the protein chain. (middlebury.edu)
Once the inhibitor binds the protease cannot bind the protein to be cleaved and is not functional. (middlebury.edu)
MicroRNA-650 targets inhibitor of growth 4 to promote colorectal cancer progression via mitogen activated protein kinase signaling. (abcam.com)
Serine proteases and their natural protein inhibitors are among the most intensively studied protein complexes. (springer.com)
Protease and phosphatase inhibitors are essential components of most cell lysis and protein extraction procedures. (thermofisher.com)
Disruption of cellular and tissue architecture during protein extraction distorts the in vivo state by making all proteins potentially accessible for degradation or modification by endogenous proteases and phosphatases. (thermofisher.com)
Protease and phosphatase inhibitors can be added to the lysis reagents in order to prevent degradation of extracted proteins, and to obtain the best possible protein yield and activity following cell lysis. (thermofisher.com)
Rather, most researchers prepare or use a mixture or "cocktail" of several different inhibitor compounds to ensure that protein extracts do not degrade before analysis for targets of interest. (thermofisher.com)
Particular research experiments may necessitate the use of single inhibitors or customized mixtures, but most protein work is best served by using a suitable protease inhibitor cocktail (see additional discussion below table). (thermofisher.com)
Pancreatic extract (50 μL, 1 μg/μL protein) or trypsin (25 μL, 0.1 units/μL) was incubated with a quenched-fluorescent, protease-cleavable substrate for cysteine (A) or serine proteases (B) in the presence or absence of commercially available protease inhibitors with EDTA-containing (blue) or EDTA-free (purple) formulations. (thermofisher.com)
A predicted secondary structure of protein protease inhibitors. (biomedsearch.com)
1974) and the known amino acid sequences, the alpha-helical, beta-sheet, beta-turn and random-coil regions were predicted for protein protease inhibitors. (biomedsearch.com)
Inhibit proteolytic degradation during cell lysis and protein extraction with these ready-to-use concentrated stock solutions of protease inhibitors. (fishersci.ca)
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.ca)
I am trying to test HCV protease inhibitor on NS3 protein expressed in adenovirus vector. (protocol-online.org)
Cooper MD, Roberts MH, Barauskas OL, Jarvis GA. Secretory leukocyte protease inhibitor binds to Neisseria gonorrhoeae outer membrane opacity protein and is bactericidal. (springer.com)
Ghidoni R, Flocco R, Paterlini A, Glionna M, Caruana L, Tonoli E, Binetti G, Benussi L. Secretory leukocyte protease inhibitor protein regulates the penetrance of frontotemporal lobar degeneration in progranulin mutation carriers. (springer.com)
Jiménez-Vega F, Vargas-Albores F. A secretory leukocyte proteinase inhibitor (SLPI)-like protein from Litopenaeus vannamei haemocytes. (springer.com)
Non-structural protein 3 (NS3) of HCV is a bifunctional serine protease/helicase, and the protease has become a prime target in the search for anti-HCV drugs. (dissertations.se)
The goal of this puzzle is to change the chemical structure of the ligand in the center of the protein to find better inhibitors of HIV protease. (fold.it)
Free shipping on inhibitor and protein orders over $500. (adooq.com)
HCV-IN-3 is a hepatitis C virus (HCV) NS3/4a protein inhibitor, with an IC50 of 20 μM, a Kd of 29 μM. (adooq.com)
Ombitasvir is a potent inhibitor of the hepatitis C virus protein NS5A, with EC50s of 0.82 to 19.3 pM against HCV genotypes 1 to 5, and 366 pM against genotype 6a. (adooq.com)
Paritaprevir (ABT-450) is a potent non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. (adooq.com)
Voxilaprevir (GS-9857) is a fluorinated macrocyclic hepatitis C virus (HCV) nonstructural protein (NS) 3/4A protease inhibitor with potent in vitro antiviral activity against genotypes 1-6 HCV and broad coverage of NS3/4A protease polymorphisms. (adooq.com)
Protease inhibitors act by mimicking the natural substrates of the HIV protease enzyme, interfering with assembly of new virus by inhibiting post-translational protein cleavage. (thefreelibrary.com)
Coimmunoprecipitation experiments revealed that EPIC2 interacts with a novel papain-like extracellular cysteine protease, termed Phytophthora Interacting Protein 1 (PIP1). (osu.edu)
We constructed a novel series of recombinant anticoagulant fusion proteins by linking annexin V (ANV), a PS-binding protein, to the Kunitz-type protease inhibitor (KPI) domain of tick anticoagulant protein, an aprotinin mutant ( 6L15 ), amyloid β-protein precursor, or tissue factor pathway inhibitor. (bloodjournal.org)
The resulting ANV-KPI fusion proteins were 6- to 86-fold more active than recombinant tissue factor pathway inhibitor and tick anticoagulant protein in an in vitro tissue factor-initiated clotting assay. (bloodjournal.org)

The protease-inhibitors mainly involved in the onset of the above-mentioned ocular pathologies are: α2-macroglobulin, α1-proteinase inhibitor (α1-PI), metalloproteinase inhibitor (TIMP), maspin, SERPINA3K, SERPINB13, secretory leukocyte protease inhibitor (SLPI), and calpeptin. (mdpi.com)
Effect of Semen on Vaginal Fluid Cytokines and Secretory Leukocyte Protease Inhibitor," Infectious Diseases in Obstetrics and Gynecology , vol. 2008, Article ID 820845, 4 pages, 2008. (hindawi.com)
Secretory leukocyte protease inhibitor mediates non-redundant functions necessary for normal wound healing. (springer.com)
Devoogdt N, Hassanzadeh Ghassabeh G, Zhang J, Brys L, De Baetselier P, Revets H. Secretory leukocyte protease inhibitor promotes the tumorigenic and metastatic potential of cancer cells. (springer.com)
Overexpression of protease inhibitor-dead secretory leukocyte protease inhibitor causes more aggressive ovarian cancer in vitro and in vivo. (springer.com)
Location of the protease-inhibitory region of secretory leukocyte protease inhibitor. (springer.com)
Secretory leukocyte protease inhibitor: a secreted pattern recognition receptor for mycobacteria. (springer.com)
Iłżecka J, Stelmasiak Z. Increased serum levels of endogenous protectant secretory leukocyte protease inhibitor in acute ischemic stroke patients. (springer.com)
Jin FY, Nathan C, Radzioch D, Ding A. Secretory leukocyte protease inhibitor: a macrophage product induced by and antagonistic to bacterial lipopolysaccharide. (springer.com)
Human buccal epithelium acquires microbial hyporesponsiveness at birth, a role for secretory leukocyte protease inhibitor. (biomedsearch.com)

The three main protease inhibitors -- atazanavir, darunavir and lopinavir -- are generally taken with a small dose of another protease inhibitor, ritonavir. (thebodypro.com)
Ritonavir was used by four subjects at a pharmacokinetic (not virologic) dose of 100 mg twice daily in combination with another protease inhibitor. (diabetesjournals.org)
I have another protease inhibitor cocktail which includes: AEBSF, bestatin, E-64, and pepstatin A (E.coli protease inhibitor cocktail) but it does not include the aprotinin or the leupeptin inhibitors. (scientistsolutions.com)

All subjects also take a background regimen of two nucleoside/nucleotide reverse transcriptase inhibitors. (clinicaltrials.gov)
Be on your first protease inhibitor (PI) containing regimen, and the regimen must consist of a PI +/- ritonavir and 2 Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (N[t]RTIs). (clinicaltrials.gov)
The combination of protease inhibitors and reverse transcriptase inhibitors is possible because there is no bad interaction between the two drugs. (middlebury.edu)
Highly active antiretroviral therapy (HAART), which combined protease and reverse transcriptase inhibitors, quickly became the standard therapy for treating patients infected with HIV and Acquired Immune Deficiency Syndrome (AIDS). (dissertations.se)
All were receiving a stable PI-containing antiretroviral regimen that containing 2 to 3 nucleoside analogue reverse transcriptase inhibitors (NRTIs) in addition to 1 to 2 PIs for a median duration of 21 months (range: 5-50) before study entry. (aappublications.org)
RTI, reverse transcriptase inhibitors. (diabetesjournals.org)

We now report that specific cysteine protease inhibitors kill Leishmania parasites in vitro , at concentrations that do not overtly affect mammalian host cells. (pnas.org)
Both LCMI I and II are inhibitors of chymotrypsin and elastase (in vitro). (uniprot.org)
The correct processing of precursor polyproteins is necessary for the infectivity of virus particles: in vitro mutagenesis which introduces deletions into the murine leukaemia virus genome produces a protease-defective virus of immature core form and lacking infectivity. (nih.gov)
Additionally, results from in-vitro experiments of the antiviral effect of ITMN-191 in combination with two separate HCV polymerase inhibitors in the Roche portfolio suggest the potential benefit of treatment regimens that simultaneously target the HCV protease and polymerase. (drugs.com)
Inhibitors of HIV protease have been shown to have antiapoptotic effects in vitro, yet whether these effects are seen in vivo remains controversial. (jci.org)
CAMBRIDGE, Mass., April 16 /PRNewswire-FirstCall/ -- Idenix Pharmaceuticals, Inc. ( NASDAQ:IDIX ) , a biopharmaceutical company engaged in the discovery and development of drugs for the treatment of human viral diseases, today reported promising in vitro data for IDX320, an HCV protease inhibitor, demonstrating potent and selective antiviral activity in multiple genotypes, or strains, of the virus. (drugs.com)
With the in vitro potency and favorable pharmacokinetic profile seen to date combined with the potential for once-daily dosing and multi-genotypic coverage, we believe IDX320 could offer improvements over other protease inhibitors currently in development," said David Standring, Ph.D., Idenix's executive vice president, biology. (drugs.com)
The signature mutation observed in vitro was D168V, consistent with other macrocyclic inhibitors. (drugs.com)
Lallos, et al, "In Vitro Antiviral Activity of IDX320, a Novel and Potent Macrocyclic HCV Protease Inhibitor", Poster #768. (drugs.com)
Double and triple combination in vitro studies of Idenix's HCV direct-acting antiviral drug candidates from different HCV drug classes, including IDX184 (a nucleotide inhibitor), IDX320 (a protease inhibitor), IDX375 (a non-nucleoside inhibitor) and a prototype Idenix NS5A inhibitor, were reported. (drugs.com)
Data demonstrated that double combinations (IDX320 with IDX184, IDX375 or NS5A inhibitor) resulted in additive to mildly synergistic effects after 3 days of treatment in vitro. (drugs.com)

It was believed that a renin inhibitor could be a highly effective drug for controlling hypertension. (middlebury.edu)
All the protease inhibitors were modeled after the compounds first developed for renin. (middlebury.edu)
The compounds of this invention are also renin inhibitors and thus are useful in treating hypertension. (patentgenius.com)
An initial library comprising eleven inhibitors based on easily accessible achiral linear oligoamines was developed and screened against six selected aspartic proteases (HIV-1 protease, plasmepsin II, plasmepsin IV, renin, BACE-1, and pepsin). (uni-marburg.de)
Isovaleryl-Val-Val-AHMHA-Ala-AHMHA where AHMHA= (3S, 4S)-4-amino-3-hydroxy-6-methyl-heptanoic acid Specificity: A potent inhibitor of various aspartic proteases, including cathepsin D, renin, pepsin, bacterial aspartic proteases and HIV proteases. (gbiosciences.com)

Grütter MG, Fendrich G, Huber R, Bode W. The 2.5 A X-ray crystal structure of the acid-stable proteinase inhibitor from human mucous secretions analysed in its complex with bovine alpha-chymotrypsin. (springer.com)
Patients with hereditary α 1 ‐proteinase inhibitor (α 1 ‐PI) deficiency are at risk of developing lung emphysema. (ersjournals.com)
This inhibitor according to the alignment with homologous from NCBI and Pfam databases is a member of proteinase inhibitors II. (scirp.org)
It is worthwhile to mention a major compositional difference between the proteinase inhibitor II families which have 8 Cys residues. (scirp.org)
PIJP is the first purified proteinase inhibitor, member of this family with only 6 Cys residues. (scirp.org)
Mägert, H.J., Drögemüller, K. and Raghunath, M. (2005) Serine Proteinase Inhibitors in the Skin: Role in Homeostasis and Disease. (scirp.org)
Mosolov, V. and Valueva, T. (2005) Proteinase Inhibitors and Their Function in plants: A Review. (scirp.org)
Christeller, J. and Laing, W. (2005) Plant Serine Proteinase Inhibitors. (scirp.org)

Protease Inhibitor Cocktail Set III, EDTA-Free - Calbiochem" as a good general protease inhibitor cocktail. (scientistsolutions.com)

Clinical trials of the protease inhibitor indinavir have shown it to be especially beneficial in combination with the anti-HIV drugs AZT and 3TC, which act by blocking a different enzyme, reverse transcriptase. (infoplease.com)
Although indinavir was one of the first protease inhibitors to be studied in children, its use in pediatrics has never been common and is currently very rare. (nih.gov)
These protease inhibitors seem to be less toxic and seem to have less severe side affects than other anti-AIDS drugs (nucleoside analogs like AZT) Saquinavir , ritonavir , and indinavir are the three main HIV protease inhibitors available today. (middlebury.edu)
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)
Indinavir was one of the first four first-generation protease inhibitors. (thefreelibrary.com)

These inhibitors were also tested against an HIV protease inhibitor resistant strain carrying the M46I, V82F, and I84V mutations. (diva-portal.org)
Poveda E, de Mendoza C, Martin-Carbonero L, Corral A, Briz V, Gonzalez-Lahoz J, Soriano V. Prevalence of darunavir resistance mutations in HIV-1-infected patients failing other protease inhibitors. (proteopedia.org)
Subsequently the influence of the active site mutations Ile50Val and Ile84Val on these inhibitors is investigated by structural and kinetic analysis. (uni-marburg.de)
Even without boosting, protease inhibitors have a higher genetic barrier to resistance than the other main classes with mutations appearing sequentially with a stepwise increase in resistance over time. (thefreelibrary.com)
Additionally, IDX320 retained activity against mutations that produce resistance to other protease inhibitors in clinical development. (drugs.com)

Protease inhibitors were the second class of antiretroviral drugs developed. (wikipedia.org)
The past couple of years have seen a marked increase in the use of combinations of highly active antiretroviral therapy (HAART) that contain two protease inhibitors (PIs), usually ritonavir (Norvir) plus another PI. (thebody.com)
For information regarding the protease inhibitor (PI) class of drugs and potential metabolic complications during pregnancy and pregnancy outcome, see Combination Antiretroviral Drug Regimens and Pregnancy Outcome . (nih.gov)
As long as the threat of human immunodeficiency virus (HIV) protease drug resistance still exists, there will be a need for more potent antiretroviral agents. (rcsb.org)
A large, multinational study published in JAIDS reports an increased risk of some cancers for people taking protease inhibitor-based combination antiretroviral therapy (PI-based cART) compared to non-nucleoside reverse transcriptase inhibitor-based cART (NNRTI-based cART). (thebodypro.com)
Etravirine is a second generation non-nucleoside analogue reverse transcriptase inhibitor (NNRTI) approved by the U.S. Food and Drug Administration (FDA) in January 2008 and by the European Medicines Agency in September 2008 for clinical use in adults with incomplete virologic suppression and resistance to previous NNRTI and other antiretroviral classes. (bioportfolio.com)
We designed a proof-of-concept study to test the efficacy and safety of switching from a Protease Inhibitor (PI) to etravirine in subjects with viral suppression as an antiretroviral strategy of simplification therapy, based on the high antiviral potency, low toxicity, together with its easy posology (in water dissolution). (bioportfolio.com)

The first part of the text deals with preparation of inhibitors of the hepatitis C virus (HCV) NS3 serine protease. (dissertations.se)
Velpatasvir, also known as GS-5816, is a potent and selective Hepatitis C virus NS5A inhibitor. (adooq.com)
Vaniprevir is a non-covalent competitive inhibitor of the hepatitis C virus (HCV) NS3/4A protease. (adooq.com)
HCV-796 is a selectively inhibitor of hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase. (adooq.com)
Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon. (adooq.com)
ITMN-191 is a hepatitis C virus (HCV) NS3 protease inhibitor, currently in a Phase 1b clinical trial in combination with Pegasys(R) (peginterferon alfa-2a) and Copegus(R) (ribavirin). (drugs.com)

To compare 48-week changes in body fat distribution and bone mineral density (BMD) between patients switching from a ritonavir-boosted protease inhibitor (PI/r) to raltegravir (RAL) and patients continuing with PI/r. (natap.org)
The current role of ritonavir-boosted protease inhibitors in the management of HIV infection. (thefreelibrary.com)

Activity: Approx 6,000 KIU/mg Specificity: A broad range, competitive and reversible inhibitor of chymotrypsin, plasmin, trypsin, kallikrein and other serine proteases Solubility: Soluble in water (Stoc. (gbiosciences.com)
N-[(2S,3R)-3-Amino-2-hydroxy-4-phenylbutyryl]-L-leucine hydrochloride Specificity: Competitive inhibitor of surface aminopeptidases, including aminopeptidase B (Ki=2nM), leucine aminopeptidase (Ki=20nM). (gbiosciences.com)

Proteases inhibitors are nearly always needed, while phosphatase inhibitors are required only when phosphorylation states (activation states) are being investigated. (thermofisher.com)

Proteases and phosphatases are important enzymes in a variety of biochemical pathways in living cells. (thermofisher.com)
All living organisms contain proteolytic enzymes (proteases and peptidases). (thermofisher.com)
Thus, while numerous compounds have been identified and used to inactivate or block these enzymes, no single chemical is effective for all types of proteases and phosphatases (see table). (thermofisher.com)
We agree it is unlikely that inhibitors of an aspartyl protease, such as the HIV protease inhibitors, would interfere with proteolytic events usually performed by serine proteases, such as the prohormone-converting enzymes. (annals.org)
The viral-encoded enzymes reverse transcriptase and protease have been main targets for drug design. (dissertations.se)
Ritonavir has this effect in a large part because it impairs the activity of enzymes in the intestine and liver that can break down protease inhibitors. (thebodypro.com)

They found that, in general, exposure to protease inhibitors (singly) reduced the cells' production of progesterone. (thebodypro.com)

The cocrystal structure of one derivative in complex with the Ile84Val HIV protease revealed that two inhibitor molecules are bound in the large active site cavity comprising an area encompassed by the catalytic dyad and the flaps in the open conformation. (uni-marburg.de)
The remaining sequences of AEPI-I and II were deduced from analyses of peptide fragments obtained by digestion of S-carboxamidomethylated molecules with either V8 protease or lysyl endopeptidase. (go.jp)
Furthermore, water molecules were shown to be important binding links between the protease and the inhibitors. (diva-portal.org)

Cell lysis disturbs the carefully controlled cellular environment, allowing proteases and phosphatases to become unregulated. (thermofisher.com)

SLPI (secretory leucocyte protease inhibitor) is a potent inhibitor of serine proteases with important functions in immunity and healing processes. (ahajournals.org)

In preclinical studies, the Company's oral direct thrombin inhibitors have demonstrated efficacy comparable to current anticoagulants along with reduced bleeding risk and are expected to enter clinical trials in 2017. (biospace.com)
Ten years ago, the first protease inhibitor targeting the human immunodeficiency virus (HIV) was approved for clinical use. (dissertations.se)
Adramatic decline in clinical progression and HIV-related deaths followed the introduction of the protease inhibitor (PI) class of antiretrovirals in 1995. (thefreelibrary.com)
There are many inhibitors of HCV NS3/4A protease in the clinical trial and improvement indicating significant reduction in the viral infection rate. (omicsonline.org)

Most known proteases belong to one of four evolutionarily distinct enzyme families based on the functional groups involved in cleavage of the peptide bond. (thermofisher.com)
Peptide mimics, having a constrained peptide backbone conformation, are HIV protease inhibitors. (patentgenius.com)
3. An inhibitor of claim 2 wherein the cysteine protease binding moiety comprises (i) amino acids, (ii) amino acids and amino acid mimetics, or (iii) amino acid mimetics, wherein the moiety corresponds to a peptide of 5 amino acid residues. (patentgenius.com)

Complex drug interactions of the HIV protease inhibitors 3: effect of simultaneous or staggered dosing of digoxin and ritonavir, nelfinavir, rifampin, or bupropion. (medscape.com)
In this study, we have evaluated the impact of the HIV protease inhibitor (PI) nelfinavir, boosted with ritonavir, in models of nonviral disease associated with excessive apoptosis. (jci.org)

I suggest protease inhibitors exert their actions, in vivo, by reducing the production of DHEA. (bio.net)
Little is known, however, about the efficacy, selectivity, and safety of cysteine protease inhibitors in cell culture or in vivo . (pnas.org)
The inhibitors were sufficiently absorbed and stable in vivo to ameliorate the pathology associated with a mouse model of Leishmania infection. (pnas.org)

The purpose of the small dose of ritonavir is to raise the concentration of the main protease inhibitor in the blood and keep it elevated for about 24 hours. (thebodypro.com)
TY - JOUR T1 - Potential of NO donor furoxan as SARS-CoV-2 main protease (Mpro) inhibitors: in silico analysis. (unboundmedicine.com)

Recently, however, an R155K protease mutation was reported as the dominant quasispecies in a treatment-naïve individual, raising concerns about possible full drug resistance. (microsoft.com)

This prevents the substrate from reacting with the protease and thus, the polypeptides are not cleaved. (middlebury.edu)
We appreciate Stricker and Goldberg's comments on the distinctive substrate specificities of aspartic and serine proteases. (annals.org)
Herein, we evaluated the phenyl furoxan, a well-known exogenous NO donor to identify the possible potent inhibitors through in silico studies such as molecular docking as per target analysis for candidates bound to substrate binding pocket of SARS-COV-2 Mpro. (unboundmedicine.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)

Saquinavir which has the trade name Invirase was the first protease inhibitor to be approved by the FDA (December 1995) for the treatment of HIV infection. (middlebury.edu)
This study provides proof of concept that cysteine protease inhibitors can be given at therapeutic doses to animals to selectively arrest a parasitic infection. (nih.gov)
The Protease Inhibitor Monotherapy Versus Ongoing Triple Therapy (PIVOT) trial: a randomised controlled trial of a protease inhibitor monotherapy strategy for long-term management of human immunodeficiency virus infection. (openaire.eu)
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)
SAN FRANCISCO, Calif.--Researchers at the San Francisco Veterans Affairs Medical Center and UC San Francisco have demonstrated that a type of drug known as a cysteine protease inhibitor may be highly effective against American trypanosomiasis or Chagas1 disease, which is caused by an infection with the parasite Trypansoma cruzi (T. cruzi). (eurekalert.org)
The study provides proof that this new class of protease inhibitors can be safely used in animals to treat a parasitic infection, the researchers said. (eurekalert.org)
A pyrrolidinone derivative and HIV INTEGRASE INHIBITOR that is used in combination with other ANTI-HIV AGENTS for the treatment of HIV INFECTION. (bioportfolio.com)
The use of protease inhibitors has revolutionized the treatment of HIV infection through the ability of these drugs to decrease viral load [1]. (annals.org)

The study isolated two Kunitz-type protease inhibitors with very similar sequences but quite divergent inhibitory potencies when assayed against bovine trypsin, chymostrypsin, and a selection of human sequence-related peptidases. (diva-portal.org)
Sequences of these inhibitors were then used to search for Kunitz homologs in an A. tenebrosa transcriptome library, resulting in the discovery of a further 14 related sequences. (diva-portal.org)
Consensus analysis of these variants identified a rich molecular diversity of Kunitz domains and expanded the palette of potential residue substitutions for rational inhibitor design using this domain. (diva-portal.org)
The positions of half-Cys residues and the entire-chain homology identified these inhibitors as members of the Kunitz-type family. (go.jp)

This analysis identifies the strongest interactions between the protease and the inhibitors, suggests ways to improve potency by building into the S2 subsite, and reveals how conformational changes and unique features of the viral protease increase the binding affinity of HIV protease inhibitors. (rcsb.org)

UK-371804 is a potent and selective urokinase-type plasmogen activator (uPA) inhibitor with excellent enzyme potency (Ki=10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin). (selleckchem.com)
Inhibitors bearing smaller N-alkyl substituents revealed a selectivity profile not being explicable with the initial SAR. (uni-marburg.de)

Due to great commercial application of protease, it is necessary to study kinetic characterization of this enzyme in order to improve design of enzymatic reactors. (doaj.org)
Purification and Biochemical Characterization of a Protease Inhibitor II Family from Jalapeño Pepper (Capsicum annuum L. (scirp.org)
Carrillo-Montes, J. , Arreguín-Espinosa, R. , Muñoz-Sánchez, J. and Soriano-García, M. (2014) Purification and Biochemical Characterization of a Protease Inhibitor II Family from Jalapeño Pepper ( Capsicum annuum L.). Advances in Bioscience and Biotechnology , 5 , 661-668. (scirp.org)

Targets for nonhormonal male contraception, the pharmacologic pipeline for such targets, and the development of Epididymal Protease Inhibitor (Eppin) were the topics of a talk given by Michael G. O'Rand, PhD, Cofounder, President, and Chief Scientific Officer of Eppin Pharma, Inc, Chapel Hill, NC. (endocrineweb.com)
Inhibitor targets and Western blot analysis of promastigote lysates. (nih.gov)
Homology modeling and molecular dynamics simulations of these inhibitors in complex with their targets were carried out and, collectively, these methodologies enabled the definition of a versatile scaffold for inhibitor design. (diva-portal.org)

PSI-6206 is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase. (adooq.com)

In this way, many regimens containing protease inhibitors can be taken just once daily. (thebodypro.com)
The researchers found that protease inhibitor-based regimens significantly reduced progesterone concentrations in mice. (thebodypro.com)
There is limited knowledge about lipodystrophic adverse events in nucleoside reverse transcriptase inhibitor (NRTI)-sparing regimens. (clinicaltrials.gov)

The therapy, which is also a protease inhibitor combining two antiviral agents, should arrive by Tuesday, he said. (natap.org)

In order to gain entry into cells, diverse viruses, including Ebola virus, SARS-coronavirus and the emerging MERS-coronavirus, depend on activation of their envelope glycoproteins by host cell proteases. (nih.gov)
In addition, SARS- and MERS-coronavirus can use serine proteases localized at the cell surface, for their activation. (nih.gov)
Addgene: A simplified cell-based assay to identify coronavirus 3CL protease inhibitors. (addgene.org)

In studies with Leishmania mexicana , elimination of selected cysteine protease genes by homologous recombination showed that null mutants of the cpL gene array designated "cpb" had reduced virulence in highly susceptible BALB/c mice, and they produced no lesions at all in C57BL/6 or CBA/Ca mice ( 3 , 4 ). (pnas.org)
Data mining of genomic and cDNA sequences revealed that P. infestans evolved 18 extracellular protease inhibitor genes belonging to two major structural classes: (i) Kazal-like serine protease inhibitors (EPI1-14) and (ii) cystatin-like cysteine protease inhibitors (EPIC1-4). (osu.edu)

The present invention also provides methods of inhibiting proteases, more specifically aspartyl proteases. (google.nl)
Amino acid sequencing of the retrovirus proteases, either after their purification or from prediction from the nucleotide sequence, shows that they possess the Asp-Thr-Gly sequence characteristic of the aspartyl proteinases. (nih.gov)
In particular, evidence suggests that the yeast aspartyl protease, Yap3, is capable of accurate endoproteolysis of both prosomatostatin (1) and proopiomelanocortin (2), functions usually performed by the prohormone convertases. (annals.org)

Cortexyme was cofounded by University of California, San Francisco, psychiatrist Stephen Dominy, who discovered bacteria and accumulations of a bacterial protease in the brains of people with Alzheimer's. (acs.org)

The change yielded a molecule that was more than a potent inhibitor of the HIV protease enzyme. (thebody.com)
The start-up developed a small-molecule inhibitor of this protease and will begin testing it in a Phase II trial next year. (acs.org)
1. Computer image of the cysteine protease inhibitor molecule (blue object) blocking the T. cruzi protease (pink ribbon). (eurekalert.org)
The study shows that the protease molecule could accommodate its structure to different sizes of the P2/P2' groups. (diva-portal.org)

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)
Due to a severely disturbed protease/antiprotease balance, these patients are at risk of developing lung emphysema at a young age, especially if they also smoke 1 - 3 . (ersjournals.com)
All patients were naïve to nonnucleoside reverse transcriptase inhibitor therapy. (aappublications.org)
We noted a strong temporal relation between the onset of hyperglycemia and the initiation or change in protease inhibitor therapy in five HIV-infected patients. (annals.org)

Anatomy11

Organisms11

Diseases5

Chemicals and Drugs157

Analytical, Diagnostic and Therapeutic Techniques and Equipment27

Phenomena and Processes45

Disciplines and Occupations1

Information Science4

Health Care2

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)

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

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

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

Role of proteases in implantation. (5/5338)

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)

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

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

Protease Inhibitors

HIV Protease Inhibitors

Serine Proteinase Inhibitors

HIV Protease

Serine Endopeptidases

Peptide Hydrolases

Secretory Leukocyte Peptidase Inhibitor

Endopeptidases

Saquinavir

Indinavir

Ritonavir

Proteinase Inhibitory Proteins, Secretory

Trypsin Inhibitors

Nelfinavir

Serpins

Cysteine Proteases

Cysteine Endopeptidases

Cysteine Proteinase Inhibitors

Molecular Sequence Data

Amino Acid Sequence

Protease Nexins

Carbamates

Lopinavir

alpha 1-Antitrypsin

Pyrimidinones

Drug Resistance, Viral

Aprotinin

Protease La

Tosyllysine Chloromethyl Ketone

Gabexate

HIV-1

ATP-Dependent Proteases

Oligopeptides

Trypsin Inhibitor, Bowman-Birk Soybean

HIV Infections

Pepstatins

Anti-HIV Agents

Antipain

Cathepsins

Tosylphenylalanyl Chloromethyl Ketone

Phenylmethylsulfonyl Fluoride

Trypsin Inhibitor, Kunitz Soybean

Cystatins

Substrate Specificity

Leupeptins

Chymotrypsin

Pancreatic Elastase

Reverse Transcriptase Inhibitors

Trypsin

Kinetics

Serpin E2

Recombinant Proteins

Base Sequence

Leukocyte Elastase

Mutation

Drug Resistance, Multiple, Viral

Aspartic Acid Endopeptidases

Serine Proteases

Sulfonamides

Molecular Weight

Subtilisins

Antiretroviral Therapy, Highly Active

Electrophoresis, Polyacrylamide Gel

Cell Line

alpha-Macroglobulins

Elafin

Models, Molecular

Calpain

Cathepsin L

Hydrolysis

Metalloendopeptidases

Binding Sites

Cathepsin G

Trypsin Inhibitor, Kazal Pancreatic

Viral Nonstructural Proteins

Chymases

Protein Processing, Post-Translational

Sequence Homology, Amino Acid

Viral Load

Methylurea Compounds

$Gentaur Molecular :Pantomics \ QG ViewRNA HC Screening Protease \ QVP0521$ Gentaur Molecular :Pantomics \ QG ViewRNA HC Screening Protease \ QVP0521