Protease Inhibitors
Leupeptins
Pepstatins
Carbamates
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.
Endopeptidases
Serine Endopeptidases
Serine Proteases
Trypsin
Cysteine Proteases
DNA-Activated Protein Kinase
Arginase
Aminocaproates
Scopolamine Hydrobromide
An alkaloid from SOLANACEAE, especially DATURA and SCOPOLIA. Scopolamine and its quaternary derivatives act as antimuscarinics like ATROPINE, but may have more central nervous system effects. Among the many uses are as an anesthetic premedication, in URINARY INCONTINENCE, in MOTION SICKNESS, as an antispasmodic, and as a mydriatic and cycloplegic.
Kidney Papillary Necrosis
A complication of kidney diseases characterized by cell death involving KIDNEY PAPILLA in the KIDNEY MEDULLA. Damages to this area may hinder the kidney to concentrate urine resulting in POLYURIA. Sloughed off necrotic tissue may block KIDNEY PELVIS or URETER. Necrosis of multiple renal papillae can lead to KIDNEY FAILURE.
Amino Acids
Glutamine
Der p 1 facilitates transepithelial allergen delivery by disruption of tight junctions. (1/34)
House dust mite (HDM) allergens are important factors in the increasing prevalence of asthma. The lung epithelium forms a barrier that allergens must cross before they can cause sensitization. However, the mechanisms involved are unknown. Here we show that the cysteine proteinase allergen Der p 1 from fecal pellets of the HDM Dermatophagoides pteronyssinus causes disruption of intercellular tight junctions (TJs), which are the principal components of the epithelial paracellular permeability barrier. In confluent airway epithelial cells, Der p 1 led to cleavage of the TJ adhesion protein occludin. Cleavage was attenuated by antipain, but not by inhibitors of serine, aspartic, or matrix metalloproteinases. Putative Der p 1 cleavage sites were found in peptides from an extracellular domain of occludin and in the TJ adhesion protein claudin-1. TJ breakdown nonspecifically increased epithelial permeability, allowing Der p 1 to cross the epithelial barrier. Thus, transepithelial movement of Der p 1 to dendritic antigen-presenting cells via the paracellular pathway may be promoted by the allergen's own proteolytic activity. These results suggest that opening of TJs by environmental proteinases may be the initial step in the development of asthma to a variety of allergens. (+info)Assembly and activation of HK-PK complex on endothelial cells results in bradykinin liberation and NO formation. (2/34)
Prekallikrein (PK) activation on human umbilical endothelial cells (HUVEC) presumably leads to bradykinin liberation. On HUVEC, PK activation requires the presence of cell-bound high-molecular-weight kininogen (HK) and Zn(2+). We examined the Zn(2+) requirement for HK binding to and the consequences of PK activation on endothelial cells. Optimal HK binding (14 pmol/10(6) HUVEC) is seen with no added Zn(2+) in HEPES-Tyrode buffer containing gelatin versus 16--32 microM added Zn(2+) in the same buffer containing bovine serum albumin. The affinity and number of HK binding sites on HUVEC are a dissociation constant of 9.6 +/- 1.8 nM and a maximal binding of 1.08 +/- 0.26 x 10(7) sites/cell (means +/- SD). PK is activated to kallikrein by an antipain-sensitive mechanism in the presence of HK and Zn(2+) on HUVEC, human microvascular endothelial cells, umbilical artery smooth muscle cells, and bovine pulmonary artery endothelial cells. Simultaneous with kallikrein formation, bradykinin (5.0 or 10.3 pmol/10(6) HUVEC in the absence or presence of lisinopril, respectively) is liberated from cell-bound HK. Liberated bradykinin stimulates the endothelial cell bradykinin B2 receptor to form nitric oxide. Assembly and activation of PK on endothelial cells modulates their physiological activities. (+info)Identification of prolylcarboxypeptidase as the cell matrix-associated prekallikrein activator. (3/34)
Investigations determined that the cell matrix-associated prekallikrein (PK) activator is prolylcarboxypeptidase. PK activation on human umbilical vein endothelial cell (HUVEC) matrix is inhibited by antipain (IC(50)=50 microM) but not anti-factor XIIa antibody, 3 mM benzamidine, 5 mM iodoacetic acid or iodoacetamide, or 3 mM N-ethylmaleimide. Corn trypsin inhibitor (IC(50)=100 nM) or Fmoc-aminoacylpyrrolidine-2-nitrile (IC(50)=100 microM) blocks matrix-associated PK activation. Angiotensin II (IC(50)=100 microM) or bradykinin (IC(50)=3 mM), but not angiotensin 1-7 or bradykinin 1-5, inhibits matrix-associated PK activation. ECV304 cell matrix PK activator also is blocked by 100 microM angiotensin II, 1 microM corn trypsin inhibitor, and 50 microM antipain, but not angiotensin 1-7. 1 mM angiotensin II or 300 microM Fmoc-aminoacylpyrrolidine-2-nitrile indirectly blocks plasminogen activation by inhibiting kallikrein formation for single chain urokinase activation. On immunoblot, prolylcarboxypeptidase antigen is associated with HUVEC matrix. These studies indicate that prolylcarboxypeptidase is the matrix PK activator. (+info)Involvement of secreted Aspergillus fumigatus proteases in disruption of the actin fiber cytoskeleton and loss of focal adhesion sites in infected A549 lung pneumocytes. (4/34)
Aspergillus fumigatus is an opportunistic pathogenic fungus that predominantly infects the respiratory system. Penetration of the lung alveolar epithelium is a key step in the infectious process. The cytoskeleton of alveolar epithelial cells forms the cellular basis for the formation of a physical barrier between the cells and their surroundings. This study focused on the distinct effects of A. fumigatus on the actin cytoskeleton of A549 lung pneumocytes. Of the 3 major classes of cytoskeletal fibers--actin microfilaments, microtubules, and intermediate filaments--only the actin cytoskeleton was found to undergo major structural changes in response to infection, including loss of actin stress fibers, formation of actin aggregates, disruption of focal adhesion sites, and cell blebbing. These changes could be specifically blocked in wild-type strains of A. fumigatus by the addition of antipain, a serine and cysteine protease inhibitor, and were not induced by an alkaline serine protease-deficient strain of A. fumigatus. Antipain also reduced, by approximately 50%, fungal-induced A549 cell detachment from the plates and reduction in viability. Our findings suggest that A. fumigatus breaches the alveolar epithelial cell barrier by secreting proteases that act together to disorganize the actin cytoskeleton and destroy cell attachment to the substrate by disrupting focal adhesions. (+info)Enzymatic characterization of a cubilin-related serine proteinase from the hard tick Haemaphysalis longicornis. (5/34)
In the present study, we performed enzymatic characterization of Haemaphysalis longicornis serine proteinase (HlSP) with a view to shed light on the mechanisms of blood digestion in the hard ticks. Escherichia coli-expressed recombinant HlSP (rHlSP) was shown to potently hydrolyze the synthetic substrates Bz-(DL)-Arg-pNA, Z-Ala-Ala-Leu-pNA and Suc-Ala-Ala-Ala-pNA and yielded an activity of 31.5, 88.2 and 18.3 mumol/min/mg protein, respectively at an optimum temperature of 25 degrees C. However, the enzyme showed little activity to hydrolyze the substrates Suc-Arg-Pro-Phe-His-Leu-Leu-Val-Tyr-MCA and Pyr-Phe-Leu-pNA. The optimum pH for the enzyme was shown to be 4.0 to 5.0. Several inhibitors such as antipain, leupeptin and phenylmethylsulfonyl fluoride (PMSF), specific for serine proteinase were shown to inhibit enzyme activity by 20-82%, while E-64 (specific for cysteine proteinases) and pepstatinA (specific for aspartic proteinases) had shown only little inhibitory effects on it. This is the first report on enzymatic characterization of a functional serine proteinase from the hard ticks. (+info)Light-induced D1 protein degradation is catalyzed by a serine-type protease. (6/34)
Light-induced degradation of the D1 protein in isolated spinach photosystem II core preparations was studied after addition of various protease inhibitors. The degradation was selectively inhibited by several serine protease inhibitors in particular diisopropylfluorophosphate. The results demonstrate that the D1 protein is degraded by a serine-type of proteolytic activity that is an integral part of photosystem II. (+info)Antipain-induced suppression of oncogene expression in H-ras-transformed NIH3T3 cells. (7/34)
Antipain (AP; 50 micrograms/ml) inhibits transformation of NIH3T3 cells after transfection with an activated H-ras oncogene. To determine whether AP effects on transformation are associated with alterations in oncogene expression, NIH3T3 cells were cotransfected with an activated H-ras oncogene and the selectable marker gene aph, and gene expression was quantified. Fifty percent of geneticin-resistant colonies which were exposed to AP failed to express the transformed phenotype as determined by their inability to grow in soft agar. Northern blot analysis of the transformed and nontransformed colonies revealed that suppression of H-ras transformation by AP was associated with a decrease in expression of the exogenously transfected H-ras gene by approximately 4-fold. Expression of the endogenous oncogene c-myc was decreased by approximately 2.5-fold, to levels seen in untransfected cells. AP-treated colonies that retained the transformed phenotype had levels of oncogene expression that were similar to untreated ras-transformed colonies. Southern blot analysis revealed no effects of AP on incorporation or copy number of the H-ras gene. (+info)Repression of serotonin secretion by an endogenous Ca2(+)-activated protease in electropermeabilized bovine platelets. (8/34)
Micromolar levels of free calcium ions added to the extracellular medium elicit secretion of serotonin from electropermeabilized bovine platelets in the presence of millimolar levels of Mg-ATP. Such Ca2(+)-dependent secretion of serotonin was almost completely impaired when the permeabilized platelets were preincubated for 1 min at 35 degrees C in 100 microM Ca2+ without Mg-ATP. The half-maximal effect was observed with about 45 microM Ca2+ in the preincubation medium. Inhibitors of serine-thiol protease, such as leupeptin and antipain, suppressed the impairment of the secretion of serotonin by the preincubation with Ca2+. Electron microscopic observation revealed that disorganization of the cytoskeletal structures, in particular of the membrane undercoat and the network of microfilaments, accompanied the impairment of secretion of serotonin. Microfilaments were also found to be dissociated from dense granules that contained serotonin. These morphological changes were also suppressed when antipain was included in the Ca2(+)-preincubation medium. Coincident with these morphological changes, the following biochemical changes were observed in 100 microM Ca2+ but not in the presence of Ca2+ and antipain. The amount of Triton-insoluble cytoskeleton and the acto-myosin content of the dense-granule fraction were markedly decreased. The decrease in Triton-insoluble cytoskeletons was quantitatively correlated with the degree of impairment of secretion of serotonin. Immunoblot analysis of EGTA extracts of the cells showed that the 240-kDa spectrin in platelets was degraded to a 235-kDa fragment, and a 260-kDa actin-binding protein (ABP) in platelets was partially degraded to 190- and 110-kDa components.(ABSTRACT TRUNCATED AT 250 WORDS) (+info)
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Prolylcarboxypeptidase regulates food intake by inactivating α-MSH in rodents
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Ester - Wikipedia
A secreted cystatin from the tick Haemaphysalis longicornis and its distinct expression patterns in relation to innate immunity
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Streptomyces michiganensis
... produces actinomycin X, antipain and mitomycin. Xue, Jinghua; Wu, Min (27 March 2015). "Cyclic ...
Sofia Areal
2009 "An Anti-pain practice", Pró-Évora Group, Évora, Portugal. 2006 "360 degrees in the SUN", Museu de Arte Contêmporanea do ... In 2016 a documentary by Jorge Silva Melo, entitled Sofia Areal: An Anti-Pain Practice was premiered at the São Luíz National ...
William Thomas Rawleigh
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Oligopeptide
Antipain - An oligopeptide produced by various bacteria which acts as a protease inhibitor. Ceruletide - A specific decapeptide ...
Horse welfare
The "anti-pain crop" invented in England is actually as painful as others. The discreet use of electric shocks on racing horses ...
Clinical neurochemistry
... antipain) medications. Sensitization, in the clinical sense of the word, is a phenomenon in which nociceptors in an area beyond ...
Flurbiprofen
Antipain, Baenazin, Benactiv, Biprofin, Biprotec, Bro-Z, Brufen, Brufoz, Cebutid, Clinadol, Coryfin, Dispain, Edolfene, Eyeflur ...
Jerry Baker (author)
2003 ISBN 0922433437 Jerry Baker's Anti-Pain Plan, 2004 ISBN 0922433496 Jerry Baker's Backyard Problem Solver, 2004 ISBN ...
Madrigal v. Quilligan
While under the influence of anti-pain medication and labor pain, she signed a consent form thinking it was for the c-section ...
List of MeSH codes (D12.644)
... antipain MeSH D12.644.456.193 - bradykinin MeSH D12.644.456.193.400 - kallidin MeSH D12.644.456.241 - caerulein MeSH D12.644. ...
Antipain
It was shown to have properties as a protease inhibitors but it had a low IC50 than a antipain. Antipain analogue Y was able to ... A recent research article indicated that antipain Y is a new type of anti-pain analog, which can inhibit the release of ... The antiretroviral drug Nelfinavir is one example of an antipain. It was classified as an antipain after a study published by ... "Antipain Y, a new antipain analog that inhibits neurotransmitter release from rat dorsal root ganglion neurons". The Journal of ...
Anti-pain
... may refer to: A colloquial term for analgesia Antipain, a peptide used in biochemical research This disambiguation ... page lists articles associated with the title Anti-pain. If an internal link led you here, you may wish to change the link to ...
Antipain - Wikipedia
It was shown to have properties as a protease inhibitors but it had a low IC50 than a antipain. Antipain analogue Y was able to ... A recent research article indicated that antipain Y is a new type of anti-pain analog, which can inhibit the release of ... The antiretroviral drug Nelfinavir is one example of an antipain. It was classified as an antipain after a study published by ... "Antipain Y, a new antipain analog that inhibits neurotransmitter release from rat dorsal root ganglion neurons". The Journal of ...
Anti-pain - Wikipedia
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Antipain dihydrochloride | VWR
Learn more about Antipain dihydrochloride. We enable science by offering product choice, services, process excellence and our ... Description: Antipain is a reversible protease inhibitor that inhibits cathepsin A, B, and D as well as papain, trypsin and ... Description: Antipain inhibits trypsin, papain, and catherpsins A and B (a reversible inhibitor of cysteine and serine ...
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Antipain dihydrochloride | Ser/Thr Protease Inhibitor | MedChemExpress
Antipain dihydrochloride inhibits N-methyl-N-nitro-N-nitrosoguanidine (MNNG)-induced transformation and increases chromosomal ... Antipain dihydrochloride restricts uterine DNA synthesis and function in mice. - Mechanism of Action & Protocol. ... Antipain dihydrochloride is a protease inhibitor isolated from Actinomycetes. ... Antipain dihydrochloride Cat. No.: HY-127034 Data Sheet Handling Instructions Antipain dihydrochloride is a protease inhibitor ...
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Plasminogen activator inhibitor 1 and Antipain preserve acrosome integrity of bovine spermatozoa during cryopreservation | Arq...
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Suppression of the radiation-induced expression of a tumor-associated antigen in human cell hybrids by the protease inhibitor...
The effect of the protease inhibitor antipain (1.25 μg/ml) on the radiation-induced expression of a tumor-associated antigen in ... A possible explanation for this observation is that antipain may inhibit an error-prone DNA repair process. However, it is ... A possible explanation for this observation is that antipain may inhibit an error-prone DNA repair process. However, it is ... N2 - The effect of the protease inhibitor antipain (1.25 μg/ml) on the radiation-induced expression of a tumor-associated ...
Dihydrochloride5
- Antipain dihydrochloride is a protease inhibitor isolated from Actinomycetes . (medchemexpress.com)
- Antipain dihydrochloride inhibits N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced transformation and increases chromosomal aberrations. (medchemexpress.com)
- Antipain dihydrochloride restricts uterine DNA synthesis and function in mice. (medchemexpress.com)
- The intact, cycling female mice received subcutaneous injections of Antipain dihydrochloride (3 mg) for 16 days, their uteri shows significant diminution in weight and total DNA when compared to untreated controls [4] . (medchemexpress.com)
- AEBSF ALLN Antipain, dihydrochloride Aprotini. (gbiosciences.com)
Papain3
- Antipain is an oligopeptide that is isolated from actinomycetes and used in biochemical research as a protease inhibitor of trypsin and papain. (wikipedia.org)
- Citation needed}} Antipain is a protease inhibitor, usually 1-2 μg/mL, and is well-against to cathepsin A, cathepsin B, papain and trypsin protease enzymes. (wikipedia.org)
- Antipain inhibits trypsin, papain, and catherpsins A and B (a reversible inhibitor of cysteine and serine proteases). (alfa.com)
Inhibits2
- Antipain analogue Y was able to suppress Trypsin, which inhibits the secretion of an excitatory neuropeptide that leads to inflammation and other disorders. (wikipedia.org)
- Antipain inhibits N-methyl-N'-nitro-N-nitrosoguanidine-induced transformation and increases chromosomal aberrations. (medchemexpress.com)
Leupeptin2
- Antipain and leupeptin restrict uterine DNA synthesis and function in mice. (medchemexpress.com)
- Because this proteolytic activity was strongly inhibited by leupeptin and antipain, it was concluded that this protease was a member of the family of cysteine proteases of C. perfringens . (asm.org)
Serine3
- It has been crystallised in complexes with carboxypeptidase, which is obtained from wheat, and Leishmania major oligopeptidase B. In both cases, the backbone carbonyl of the terminal arginine of antipain forms a covalent bond to the active site serine in the protease. (wikipedia.org)
- The effects of different concentrations of two serine protease inhibitors were analyzed, Plasminogen activator inhibitor 1 - PAI-1 (70Æ g, 140Æ g and 210 Æ g) and Antipain (10µg, 50µg and 100µg) as supplementation to bovine semen cryopreservation extender. (bvsalud.org)
- In conclusion, the serine protease inhibitors , Antipain and PAI-1 (70 and 140Æ g) are able to preserve the acrosome integrity of cryopreserved bovine sperm . (bvsalud.org)
Inflammation1
- Seraza Antipain and Inflammation uses natural ingredients to help soothe pain and inflammation and boost the regeneration properties of the body. (medisilk.com)
Proteases1
- used antipain for evaluating the role of proteases in the process of malignant transformation of BALB/c 3T3 cells. (bachem.com)
Inhibitors2
- Protease inhibitors or antipain are enzymes that are used to regulate their performance. (wikipedia.org)
- It was shown to have properties as a protease inhibitors but it had a low IC50 than a antipain. (wikipedia.org)
Research2
- A recent research article indicated that antipain Y is a new type of anti-pain analog, which can inhibit the release of neurotransmitter in rat dorsal root ganglion neurons. (wikipedia.org)
- Anti-pain may refer to: A colloquial term for analgesia Antipain, a peptide used in biochemical research This disambiguation page lists articles associated with the title Anti-pain. (wikipedia.org)
Study4
- It was classified as an antipain after a study published by Ovid that investigated the in vitro effect of Nelfinavir using proteolytic foot printing and found that it selectively inhibited HER2- positive, a growth factor in breast cancer. (wikipedia.org)
- During the study, an antipain analogue Y was developed and studied. (wikipedia.org)
- Testing the Implementation of a Pain Self-Management Support Intervention for Oncology Patients in Clinical Practice: A Randomized Controlled Pilot Study (ANtiPain). (fhsg.ch)
- Testing the feasibility and effects of a self-management support intervention for patients with cancer and their family caregivers to reduce pain and related symptoms (ANtiPain): Study protocol of a pilot study. (fhsg.ch)
Days1
- However, it is clear that this is not the only mechanism whereby the inhibitor can exert its effect since suppression was obtained even when antipain was added 10 days post-irradiation, a time when any DNA repair processes would be expected to be over. (utmb.edu)
Human2
- The effect of the protease inhibitor antipain (1.25 μg/ml) on the radiation-induced expression of a tumor-associated antigen in human cell hybrids has been investigated. (utmb.edu)
- Sun, C, Colman, M & Redpath, JL 1988, ' Suppression of the radiation-induced expression of a tumor-associated antigen in human cell hybrids by the protease inhibitor antipain ', Carcinogenesis , vol. 9, no. 12, pp. 2333-2335. (utmb.edu)
Effect1
- Antipain and PAI-1 had no effect on the integrity parameters of the plasma membrane , mitochondrial membrane potential and sperm defects. (bvsalud.org)
Process1
- A possible explanation for this observation is that antipain may inhibit an error-prone DNA repair process. (utmb.edu)