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Topic: Serine protease inhibitor


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In the News (Sun 20 Dec 09)

  
  Serine protease inhibitor - Wikipedia, the free encyclopedia
Serine protease inhibitors or serpins (short for serine protease inhibitor) are a group of proteins that inhibit peptidases (old name: proteases).
Serine proteases are defined by the presence of a serine residue in their active domain.
Cysteine proteases differ from serine proteases in that they are defined by the presence of a cystein residue, rather than a serine residue, in their active domain.
en.wikipedia.org /wiki/Serine_protease_inhibitor   (450 words)

  
 PHRI :: Richard Pine, Ph.D.
Induction of IRF-1 and a serine protease inhibitor.
A serine protease on the cytoplasmic surface of an organelle or vesicle in the "lysosomal/mitochondrial" fraction from undifferentiated cells was responsible for the modification of IRF-1.
Thus, the simplest explanation of the modification is cleavage of IRF-1 by the serine protease.
www.phri.org /research/res_abs_pine01.asp   (238 words)

  
 BILN 2061 HCV Protease Inhibitor Development Held Due to Toxicity
Although the NS3 serine protease is within a highly conserved region, first clinical results indicate that the antiviral potency of this compound is less in patients infected with genotype 2 and 3 HCV, indicating that other factors might interact with the binding of BILN 2061 to the NS3 serine protease.
The NS3/NS4a serine protease mediates proteolysis at the NS3/NS4a, NS4a/NS4b, NS4b/NS5a, and NS5a/NS5b junctions.
Because this serine protease is essential for viral replication, identifying inhibitors of this enzyme is a logical method of developing agents for the treatment of HCV infection.
www.natap.org /2004/HCV/113004_01.htm   (3793 words)

  
 Alpha 1-antitrypsin - Wikipedia, the free encyclopedia
A1AT is a 52 kDa serine protease inhibitor, and in medicine it is considered the most prominent one, given the fact that the words α1-antitrypsin and protease inhibitor (Pi) are often used interchangeably.
In the acute phase reaction, a further elevation is required to "limit" the damage caused by activated neutrophil granulocytes and their enzyme elastase, which breaks down the connective tissue fiber elastin.
In blood test results, the electrofocusing results are notated as in PiMM, where Pi stands for protease inhibitor and "MM" is the banding pattern of that patient.
en.wikipedia.org /wiki/Alpha_1-antitrypsin   (670 words)

  
 Coagulation - Wikipedia, the free encyclopedia
The pathways are a series of reactions, in which a zymogen of a serine protease and its glycoprotein co-factor are activated to become active components that then catalyze the next reaction in the cascade.
The coagulation factors are serine proteases (enzymes) except FVIII and FV which are glycoproteins.
Antithrombin is a serine protease inhibitor (serpin) that degrades the serine proteases; thrombin and FXa, as well as FXIIa, and FXIa.
en.wikipedia.org /wiki/Blood_clotting   (2222 words)

  
 EID Vol. 4 No.1: Proteases of Malaria Parasites: New Targets for Chemotherapy
Proteases appear to be required for the rupture and subsequent reinvasion of erythrocytes by merozoite-stage parasites and for the degradation of hemoglobin by intraerythrocytic trophozoites (Figure).
This protease, called falcipain, degraded denatured and native hemoglobin in vitro; its acid pH optimum, substrate specificity, and inhibitor sensitivity indicated that it was a papain family cysteine protease (64,70,71).
Inhibitors of aspartic and cysteine proteases have synergistic effects in inhibiting the growth of cultured malaria parasites (67), and these proteases also act synergistically to degrade hemoglobin in vitro (41).
www.cdc.gov /ncidod/eid/vol4no1/rosenth.htm   (4136 words)

  
 Serine protease inhibitor -- Facts, Info, and Encyclopedia article   (Site not responding. Last check: 2007-10-08)
(Click link for more info and facts about Serine protease) Serine proteases are defined by the presence of a (A sweetish crystalline amino acid involved in the synthesis by the body of cysteine) serine residue in their active domain.
They are part of the larger group of (An antiviral drug used against HIV; interrupts HIV replication by binding and blocking HIV protease; often used in combination with other drugs) protease inhibitors.
In 2001, a consensus (Silverman et al) was published in which the circa 500 serpins were classified in sixteen (A group of biological taxa or species that share features inherited from a common ancestor) clades (based on structural similarity), with the remaining ten as orphans.
www.absoluteastronomy.com /encyclopedia/s/se/serine_protease_inhibitor.htm   (542 words)

  
 109_Serine Proteases
Ecotin is a serine protease inhibitor that is found in the periplasm of Escherichia coli.
SBTI is acts as a reversable competitive inhibitor of trypsin an proteases such as chymotrypsin, plasmin and plasma kallikren.
Serine protease neutrophil elastase is stored in high abundance contained in azurphlic granules of the neutrophil and act to digest the phagocytized foreign partilcles.
www.oxfordbiomed.com /vb109serpro.html   (188 words)

  
 Apoptosis II: Beyond Cytochrome c; the Other Mitochondrial Proteins   (Site not responding. Last check: 2007-10-08)
Caspases are a family of cysteine proteases expressed as latent zymogens, requiring cleavage for activation.
At least three pieces of evidence suggest that the serine protease activity of HtrA2/Omi may be of equal or greater importance than IAP binding in mediating its apoptotic function.
Upon subsequent examination of the serine protease activity of HtrA2/Omi, it was discovered that this quality is required for its pro-apoptotic effects.
www.rndsystems.com /asp/g_sitebuilder.asp?bodyID=554   (2847 words)

  
 Pfam 18.0 : Kazal_1   (Site not responding. Last check: 2007-10-08)
Peptide proteinase inhibitors can be found as single domain proteins or as single or multiple domains within proteins; these are referred to as either simple or compound inhibitors, respectively.
Kazal inhibitors, which inhibit a number of serine proteases (such as trypsin and elastase), belong to family of proteins that includes pancreatic secretory trypsin inhibitor; avian ovomucoid; acrosin inhibitor; and elastase inhibitor.
The presence of this Pfam domain is usually indicative of serine protease inhibitors, however, Kazal-like domains are also seen in the extracellular part of agrins which are not known to be proteinase inhibitors.
pfam.wustl.edu /cgi-bin/getdesc?acc=PF00050   (307 words)

  
 HCV Protease Inhibitors-BILN 2061: a major step toward new therapeutic strategies in hepatitis C
Here we identify a class of specific and potent NS3 protease inhibitors and report the evaluation of BILN 2061, a small molecule inhibitor biologically available through oral ingestion and the first of its class in human trials.
The serine protease activity of NS3 is an attractive target for new drugs that could block viral replication efficiently.
The article by Lamarre et al., describes very preliminary results and there are important potential limitations for the use of protease inhibitors in the treatment of chronic hepatitis C. Strong specificity of these inhibitors might be associated with limitation of efficiency in different genotypes.
www.natap.org /2004/HCV/080904_05.htm   (1602 words)

  
 Cardioprotective effects of the serine protease inhibitor aprotinin after regional ischemia and reperfusion on the ...
Cardioprotective effects of the serine protease inhibitor aprotinin after regional ischemia and reperfusion on the beating heart -- Pruefer et al.
Cardioprotective effects of the serine protease inhibitor aprotinin after regional ischemia and reperfusion on the beating heart
infiltration with subsequent release of proteases and oxygen-derived
jtcs.ctsnetjournals.org /cgi/content/abstract/124/5/942   (434 words)

  
 HCV Protease Inhibitors: Glimpses of Hope on a Distant Horizon   (Site not responding. Last check: 2007-10-08)
An effective protease inhibitor might also make treatment more attractive and tolerable by eliminating the need for ribavirin, shortening the length of treatment, and/or possibly enabling lower doses of pegylated interferon and thus fewer side effects.
This work suggests that HCV protease inhibitors could work synergistically with pegylated interferon, boosting its effectiveness and possibly allowing for lower doses of interferon during treatment.
The field of HCV protease inhibitor development was poised to take off in the late 1990s, with a number of major companies working on compounds.  But research was set back for several years when Chiron filed lawsuits against four companies working on protease inhibitors in 1998, claiming patent infringement. 
www.hivandhepatitis.com /hep_c/news/2004/063004_a.html   (1158 words)

  
 Serpine2 identified as novel candidate gene for COPD   (Site not responding. Last check: 2007-10-08)
Researchers have identified a serine protease inhibitor as a novel candidate susceptibility gene for chronic obstructive pulmonary disease (COPD).
The discovery has major implications, especially in smokers, where the role of the cell protease inhibitor in the lung was previously unrecognised.
The study, entitled: "Expression of Serine Proteinase Inhibitor E2, a novel candidate COPD susceptibility gene, in the lung was recently presented at the 35th Congress of the International Union of Physiological Sciences in San Diego, March 31 - April 5, 2005.
www.drugresearcher.com /news/news-ng.asp?n=59167-serpine-identified-as   (824 words)

  
 Serine protease inhibitor - Wikipedia, the free encyclopedia   (Site not responding. Last check: 2007-10-08)
Although initially considered a class of protease inhibitors (agents that block the action of protein-degrading enzymes), it was discovered later that it has members that do not inhibit any enzymes, but serve as storage proteins (ovalbumin, in egg white), carriage proteins (thyroxine-binding globulin,) and hormone precursors (angiotensinogen).
PDB molecule of the month: Serine protease inhibitor (http://nist.rcsb.org/pdb/molecules/pdb53_1.html)
This page was last modified 10:09, 17 May 2005.
www.marylandheights.us /project/wikipedia/index.php/Serine_protease_inhibitor   (416 words)

  
 Na+ transport in normal and CF human bronchial epithelial cells is inhibited by BAY 39-9437 -- Bridges et al. 281 (1): ...
BAY 39-9437 is a recombinant human serine protease inhibitor.
The substrate of the channel-activating protease or the exogenous trypsin is unknown and may be ENaC or some regulatory protein closely associated with ENaC.
inhibition of ENaC by the Kunitz-type protease inhibitors.
ajplung.physiology.org /cgi/content/full/281/1/L16   (4617 words)

  
 Alpha-1-Antitrypsin Deficiency   (Site not responding. Last check: 2007-10-08)
It is a glycoprotein with broad inhibitory capacity against a variety of serine proteases and its main physiological target is neutrophil elastase.
The protease docks on to the RCL, and cleavage of a methionine-serine bond at positions 358-359 in the loop results in a major conformational change.
The protease is then translocated to the opposite pole of the molecule and the active site of the protease is distorted.
www.dekker.com /sdek/4696497-33621364/abstract~content=a713544902~db=enc   (352 words)

  
 M&I • Xuanyong Lu, PhD   (Site not responding. Last check: 2007-10-08)
The probable mechanism is that the SPI by inactivating vital proteases in the virus-cell fusion process prevents infecting and gives immunity to the HepG2 cells.
The relevant anti-apoptosis mechanism of cancer cells is thought to inactivate the crucial protease involving in the cell apoptosis by over-expression of a kind of regulation protein named apoptosis inhibitor (IAP) and serine protease inhibitor (SPI).
If it were true, down regulation of over-expressed apoptosis inhibitor, consequently reinstating the apoptosis of cancer cell, probably could be used to control the cancer development.
www.drexel.edu /med/microbiology_immunology/faculty/lu.html   (1082 words)

  
 Molecular Evolution of the Wound-Induced Serine Protease Inhibitor wip1 in Zea and Related Genera -- Tiffin and Gaut 18 ...
of a wound-induced serine protease inhibitor, wip1, in the genus
diversity of the wip1 gene, a wound-induced serine protease
to inhibit chymotrypsin proteases (Rohrmeier and Lehle 1993
mbe.oxfordjournals.org /cgi/content/full/18/11/2092   (4842 words)

  
 A Kazal-like Extracellular Serine Protease Inhibitor from Phytophthora infestans Targets the Tomato ...
protease assay kit as described under "Materials and Methods." Activity is expressed as a percentage of total protease activity in the absence of protease inhibitors.
Protease activity was measured as absorbance at 405 nm based on hydrolysis of a chromogenic substrate.
The amino acid sequence of P69B subtilisin-like protease precursor is shown with the signal peptide sequence in italics and the propeptide domain sequence in gray.
www.jbc.org /cgi/content/full/279/25/26370   (5042 words)

  
 Directory of open access journals
The role of Serine Proteases and Serine Protease Inhibitors in the migration of Gonadotropin-Releasing Hormone neurons
We have studied the effects of proteases and their inhibitors on the extracellular matrix and the consequences to the migration of gonadotropin releasing hormone (GnRH) neurons in the embryonic chick.
Affigel blue beads were used to deliver a serine protease inhibitor, protease nexin-1 (PN-1), and a target protease, trypsin, to the olfactory epithelium coincident with initiation of GnRH neuronal migration.
www.doaj.org /abstract?id=80846&toc=y   (236 words)

  
 Activity-based protein profiling: The serine hydrolases -- Liu et al. 96 (26): 14694 -- Proceedings of the National ...
to biotin as serine hydrolase inhibitors (19, 20).
To explore further FP-biotin's reactivity with serine hydrolases, we incubated soluble fractions of rat testis with this inhibitor.
serine hydrolase as an integral membrane protein (17, 31).
www.pnas.org /cgi/content/full/96/26/14694   (5237 words)

  
 UCSF Craik Lab   (Site not responding. Last check: 2007-10-08)
Serine Proteases from Nematode and Protozoan Parasites: Isolation of Sequence Homologues Using Generic Molecular Probes.
An Alternate Geometry for the Catalytic Triad of Serine Proteases.
In Vitro Characterization of Nonpeptide Irreversible Inhibitors of HIV Proteases.
www.craiklab.ucsf.edu /pub.html   (4152 words)

  
 At3g45220 -   (Site not responding. Last check: 2007-10-08)
At3g45220 is a homologue of At2g25240 (serpin, putative / serine protease inhibitor, putative) from Arabidopsis thaliana.
At3g45220 is a homologue of Spn4 (Serine protease inhibitor 4) from Drosophila melanogaster.
At3g45220 is a homologue of Spn6 (Serine protease inhibitor 6) from Drosophila melanogaster.
www.pdg.cnb.uam.es /UniPub/iHOP/gg/9007.html   (97 words)

  
 BILN 2061: HCV protease inhibitor
Schering Plough is in phase I now with SCH-7, an HCV protease inhibitor and is planning the next phase of studies for 2004.
BILN 2061 is a potent and specific inhibitor of the HCV serine protease in-vitro and in patients infected with HCV genotype 1 (GT 1).
BILN 2061 is a potent and specific inhibitor of the HCV serine protease in-vitro and in patients infected with genotype 1 (GT 1) as recently reported.
www.natap.org /2003/AASLD/day4_1.htm   (811 words)

  
 Directory of open access journals
The protease activity of NS3 was reflected by the activity of SEAP in the culture media of transient or stable expression cells.
Pefabloc SC, a potent irreversible serine protease inhibitor, was used to treat the stably expressing cell lines to assess the system for screening NS3 inhibitors.
To compare the activity of serine proteases from 1b and 1a, two chimeric clones were constructed and introduced into both transient and stable expression systems.
www.doaj.org /abstract?id=90900&toc=y   (268 words)

  
 antithrombin / heparin system - General Practice Notebook   (Site not responding. Last check: 2007-10-08)
Antithrombin is a serine protease inhibitor which inhibits the following coagulation factors:
In vivo, glycosaminoglycans on the endothelial cells serve as the endogenous catalysts for antithrombin activation.
Heparin cofactor II is a distinct serine protease inhibitor which inhibits thrombin in the presence of heparin.
www.gpnotebook.co.uk /cache/-771358677.htm   (143 words)

  
 Expression of Serine Protease Inhibitor 3 in Ocular Tissues in Endotoxin-Induced Uveitis in Rat -- Takamiya et al. 42 ...
Expression of Serine Protease Inhibitor 3 in Ocular Tissues in Endotoxin-Induced Uveitis in Rat -- Takamiya et al.
Expression of Serine Protease Inhibitor 3 in Ocular Tissues in Endotoxin-Induced Uveitis in Rat
Simar-Blanchet, AE, Paul, C, Mercier, L, Le Cam, A. (1996) Regulation of expression of the rat serine protease inhibitor 2.3 gene by glucocorticoids and interleukin-6.
www.iovs.org /cgi/content/full/42/11/2427   (4553 words)

  
 Mailgate: sci.life-extension: Serine protease inhibitor 2A increases memory T-cells
The finding could help scientists create more effective vaccines and may lead to potent immune system-based therapies against diseases that have previously eluded vaccines, such as cancer or AIDS.
Scientists know a great deal about the rapid proliferation and differentiation of these T cells but very little about the factors that regulate contraction.
In the September, 2004, issue of Nature Immunology published on-line August 15 -- the researchers show that activation of the gene for the Serine protease inhibitor 2A (Spi2A) can prevent the death of T cells during the contraction phase, resulting in about five times as many memory T cells.
mailgate.supereva.it /sci/sci.life-extension/msg11942.html   (499 words)

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