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Topic: Protease inhibitor (biology)

	Protease inhibitor (pharmacology) - Wikipedia, the free encyclopedia
		Protease inhibitors (PIs) are a class of medication used to treat or prevent infection by viruses, including HIV and Hepatitis C.
		PIs prevent viral replication by inhibiting the activity of protease, an enzyme used by the viruses to cleave nascent proteins for final assembly of new virons.
		Protease inhibitors were the second class of antiretroviral drugs developed.
	en.wikipedia.org /wiki/Protease_inhibitor_(pharmacology) (348 words)

	Protease inhibitor (biology) - Wikipedia, the free encyclopedia
		In biology and biochemistry, protease inhibitors are molecules that inhibit the function of peptidases (old name: protease, hence the term protease inhibitor).
		In medicine, protease inhibitor is often used interchangeably with alpha 1-antitrypsin (A1AT, which is abbreviated P
		A1AT is indeed the protease inhibitor most often involved in disease, namely in alpha 1-antitrypsin deficiency.
	en.wikipedia.org /wiki/Protease_inhibitor_(biology) (110 words)

	NIH Guide: PROTEASE INHIBITOR RELATED ATHEROSCLEROSIS IN HIV INFECTION
		It is not known whether the lipid changes observed with protease inhibitor therapy are due to altered synthesis or catabolism of the lipids directly, or reflect changes in lipoprotein receptor function or lipoprotein metabolizing enzymes.
		However, statins may not be as effective in patients on protease inhibitors and greater caution needs to be exerted with their use since protease inhibitors may interfere with the metabolic pathway for statins in the liver.
		It is expected that the various side effects of protease inhibitors will encourage investigators with expertise in a variety of disciplines to focus on lipid metabolism and possible alterations due to protease inhibitors, and to integrate these studies with approaches involving vascular cell biology, tissue-specific pathology, clinical investigations, and molecular biology (gene expression and regulation).
	grants.nih.gov /grants/guide/rfa-files/RFA-HL-00-007.html (6761 words)

	PI3 - protease inhibitor 3, skin-derived (SKALP)
		It is not inhibited by a PLA2 inhibitor (4 bromophenacyl bromide [B phi B]) and the PI3 kinase inhibitor, wortmannin.
		NECA-mediated IL-6 release was inhibited by the PLC inhibitor 1-[6-((17beta-3-methoxyestra-1,3,5(10)-tiene-17-yl)amino)hexyl]-1H-pyrrole-2,5-dione, the PI3 kinase inhibitor wortmannin and the PKC inhibitors bisindolylmaleimide 1 and bisindolymaleimide X1 HCl (Ro-32-0432).
		Protease inhibitors, elafin and stefin-B as well as beta-actin and two epithelial-specific small proline-rich (spr) proteins, which we have named SPRC and SPRK and which are distinct from salivary proline-rich proteins, were differentially expressed.
	www.ihop-net.org /UniPub/iHOP/gg/91009.html (6782 words)

	Anthrax toxin inhibitor identified
		Described in the January 2004 issue of Nature Structural & Molecular Biology, these findings could eventually lead to the development of a protease inhibitor drug, which in combination with antibiotics could be used to treat anthrax cases later in the disease, at a point when antibiotics alone are no longer effective.
		The protease activity of this toxin is known to attack a family of protein kinases called map kinase kinases (MEKKs), which mediate many cellular responses, including cytokine release and cell survival.
		Protease inhibitor drugs have gained popularity in recent years, notably in the treatment of HIV infections.
	www.eurekalert.org /pub_releases/2003-12/hms-ati122403.php (646 words)

	Structural Biology
		Since, HIV protease recognizes various cleavage sites in the gag and gag-pol polyproteins, it is one of the examples of which one molecularsurface can recognize a variety of other seemingly non-homologous surfaces.
		Also, mutational studies on HIV-1 protease (Loeb et al., 1989) indicate that the activity of the enzyme is compromised by mutations that occur in the regions of the three-dimensional structure that are rigid.
		Each residue of the substrate is in contact with at least five protease residues and between one and three water molecules; the residues with the most contacts are the P2 and P2' residues that are surrounded by eight and seven residues, respectively.
	www.arches.uga.edu /~ketona/bcmb8010/Structbio.html (2253 words)

	Full Text - Nucleotide sequence of a genomic clone encoding a cowpea (Vigna unguiculata L.) trypsin inhibitor
		The gene size and coding regions of these inhibitors are small, devoid of introns (Boulter, 1993), and comprised of readily identifiable core region covering the invariant cysteine residues and active serine centers that are bound to highly variable amino and carboxy terminal regions.
		The reaction sites of these inhibitors are mutating faster than amino acids in rest of the proteins, implying their role in defense against insect pests, which may exert a strong selection pressure on these proteins to conserve the reaction sites related to plant defense (Laskowski et al.
		The protease inhibitor genes are typically devoid of any intervening sequences (Boulter, 1993) and none of the genes sequenced so far have any introns, similarly the isolated sequenced cowpea trypsin inhibitor gene is also devoid of introns.
	www.ejbiotechnology.info /content/vol4/issue1/full/4 (1963 words)

	Bugs in the News - Protease Inhibitor and HIV
		A protease inhibitor would be any substance which partially or completely blocks the ability of a proteolytic enzyme to carry out its activity.
		The inhibitor must necessarily have a shape which can bind to the protease at the place within the structure of the protease within which bond formation/breakage occurs, e.g., the catalytic site (active site), or, at some place on the protease's structure which prevents the active site from functioning properly.
		Further, as each new potential inhibitor appeared, all kinds of tests had to be done to assure that the inhibitor inhibited only HIV protease, and not one of the many different proteases necessary for our cells to normally live.
	people.ku.edu /~jbrown/protease.html (1790 words)

	Proteases.net: protease inhibitors (Site not responding. Last check: 2007-10-13)
		Protease inhibitors are molecules, both natural and synthetic that inhibit the activity of proteases in complex solutions such as cell lysates, blood or even within cells.
		For research purposes, complex protein solutions are treated with a cocktail of several protease inhibitors in an effort to preserve the native state of proteins.
		Protease inhibitors prevent the processing of viral proteins and therefore the formation of mature virus particles.
	www.proteases.net /pi.html (437 words)

	Title of Invention: Transgenic plants expressing M. sexta protease inhibitor
		This invention relates to a protease inhibitor of the insect Manduca sexta, its purification, cloning of a DNA sequence encoding the inhibitor, modifications to change inhibitor specificity, transgenic plants carrying and expressing said DNA sequence and insect resistance conferred thereby on said transgenic plants.
		The only proteinase inhibitors isolated from invertebrates which are similar in size and characteristics to the serpins are a trypsin inhibitor (M.sub.r =42,000) and a chymotrypsin inhibitor (M.sub.r =43,000) which have been isolated from the hemolymph of the silkworm Bombyx mori.
		Proteinase inhibitor activity was assayed by mixing 10.mu.l samples from column fractions with 1.mu.g porcine pancreatic elastase and residual activity assayed by placing the reaction mixture in a well cut into an agarose gel containing casein (protease substrate gel tablets, Bio-Rad).
	www.nal.usda.gov /bic/Biotech_Patents/1995patents/05436392.html (9627 words)

	Introduction
		Protease inhibitors are the latest addition to the arsenal of drugs designed to combat the HIV virus.
		Protease inhibitors were not available at that time, so it would have been very unlikely that these subjects received protease inhibitor treatment prior to the sequence analysis study.
		Protease inhibitor therapy has been shown to decrease viral load substantially, but in the long run, it has not been shown to maintain its antiviral potency.
	www.stanford.edu /~siegelr/philhsu.htm (3300 words)

	FDA Approves Once-Daily Combination of Abbott's Protease Inhibitor Kaletra (Site not responding. Last check: 2007-10-13)
		Pharmaceutical company Abbott Laboratories on Monday announced that the FDA has approved a once-daily formulation of its antiretroviral protease inhibitor Kaletra, which is used in combination with other drugs for initial treatment of HIV,...
		Protease inhibitors work by blocking the action of an enzyme that cuts HIV proteins into the shorter sections that the virus needs to replicate (Kaiser Daily HIV/AIDS Report, 2/28).
		According to Abbott, Kaletra is the most-prescribed protease inhibitor in the United States, Dow Jones/SmartMoney.com reports.
	www.medicalnewstoday.com /medicalnews.php?newsid=23867 (348 words)

	AEGiS-PRn: Schering-Plough Reports Novel Investigational Protease Inhibitor Shows In Vitro Antiviral Activity in ...
		The hepatitis C protease is a viral enzyme complex that is essential to the replication of the hepatitis C virus.
		By interfering with viral replication, HCV protease inhibitors may represent a new antiviral approach to treating hepatitis C patients.
		Its researchers, leaders in the structural biology of HCV, are using their expertise to design potent antiviral agents that can inhibit the enzyme activities required for HCV maturation and replication.
	www.aegis.com /news/pr/2003/PR031048.html (1677 words)

	A new broad-spectrum protease inhibitor from the entomopathogenic bacterium Photorhabdus luminescens -- Wee et al. 146 ...
		A new broad-spectrum protease inhibitor from the entomopathogenic bacterium Photorhabdus luminescens -- Wee et al.
		Primary-phase protease was incubated with various amounts of secondary-phase protease inhibitor and the remaining protease activity was assayed as described in Methods.
		nematophila protease was 87% inhibited by the heterologous
	mic.sgmjournals.org /cgi/content/full/146/12/3141 (2962 words)

	Paradigm Therapeutics Ltd and Medivir enter alliance to discover protease inhibitor drugs
		The collaboration will combine Medivir's experience and methods in protease inhibitor drug discovery, which includes proprietary screening methods and extensive protease inhibitor compound libraries, with Paradigm's bioinformatics, functional biology and drug target validation technologies.
		We are therefore delighted to have forged an alliance with Medivir to exploit the potential for generating small-molecule drugs to Paradigm's novel protease targets".
		Medivir's research focuses on the development of new pharmaceutical compounds as inhibitors of target enzymes with protease or polymerase activity.
	www.bioportfolio.com /news/paradigm_4.htm (588 words)

	HIV Infection: Protease and Protease Inhibitors
		Inhibitors of this viral protease can be used to fight HIV infection.
		By blocking the ability of the protease to cleave the viral polypeptide into functional enzymes, protease inhibitors interfere with continued infection.
		Mutations enable HIV to avoid treatments that involve only one drug, so there is growing use of multiple-drug therapies in which both a protease inhibitor AND a reverse transcript inhibitor are combined.
	www.cellsalive.com /hiv4.htm (124 words)

	Protease-inhibitor cocktail protects, increases anti-microbial action of promising new peptide
		A protease inhibitor cocktail containing compounds that inactivate the enzymes that normally would degrade the small pieces of protein enabled the potential treatments for oral infections to more than double their anti-microbial action, results showed.
		To test their theory, they exposed the microbes to the peptide in the presence of saliva and a commercially available protease inhibitor cocktail.
		Without the inhibitors, the peptide killed 18 percent, 21 percent and 40 percent of three strains and approximately 74 percent of two strains.
	www.eurekalert.org /pub_releases/2004-03/uab-pcp030804.php (447 words)

	Pierce Biotechnology’s HALT Protease Inhibitor Cocktail - Biocompare Product Review
		Inhibition of intracellular proteases is necessary to maintain and preserve cellular protein integrity during cell lysis, protein extraction and subsequent analyses.
		However, ready to use commercial protease inhibitor cocktails are a convenient and economical alternative.
		The HALT Protease Inhibitor Cocktail from Pierce Biotechnology is an easy to use, convenient protease inhibitor cocktail that inhibits a wide variety of cellular proteases.
	www.biocompare.com /prorev.asp?profrevid=188 (397 words)

	F C DENISON et al.: Uterine secretory leukocyte protease inhibitor (Journal of Endocrinology) (Site not responding. Last check: 2007-10-13)
		Secretory leukocyte protease inhibitor is a potent inhibitor of neutrophil function, a mediator of mucosal immunity and an inhibitor of NFkappaB regulated inflammatory responses.
		High levels of secretory leukocyte protease inhibitor were released by decidua (135.2±12.4 pg/mg; mean±s.e.m.) and chorio-decidua (325.1±26.4 pg/mg) with less by amnion (55.6±6.0 pg/mg) and placenta (9.2±1.9 pg/mg).
		Intense immunoreactivity for secretory leukocyte protease inhibitor was detected predominately in decidua parietalis cells adherent to the chorion laeve and myometrium, and also in decidua basalis.
	journals.endocrinology.org /joe/161/joe1610299.htm (325 words)

	ScienceDaily: HIV Patients May Be At Risk Of Heart Problems When Taking Protease Inhibitor Drugs (Site not responding. Last check: 2007-10-13)
		Badley's research group earlier discovered that protease inhibitors affect "pore function" of "channels" in a specific cell type they were studying.
		They investigated the hypothesis that the widely-used protease inhibitors may, in fact, be linked to the development of heart rhythm problems through the mechanism of blocking a channel.
		New Protease Inhibitor Could Thwart AIDS Resistance To Current Drugs (February 4, 1999) -- Researchers have developed a new protease inhibitor effective against mutating strains of the human AIDS virus that are resistant to current drugs, according to a just-released report in the...
	www.sciencedaily.com /releases/2005/02/050218161626.htm (1148 words)

	Spink3 - serine protease inhibitor, Kazal type 3
		The COX-2 inhibitor, rofecoxib (15 mg/kg body weight intraperitoneally) was administered to normal and ROP mice from P12 to P17.
		Transcription of the mouse secretory protease inhibitor p12 gene is activated by the developmentally regulated positive transcription factor Sp1.
		Major virion low-molecular-weight polypeptides were isolated from the Moloney strain of murine leukemia virus (type C) by agarose chromatography in 6M guanidine hydrochloride and were shown to have molecular weights of 15,000 (p15), 12,000 (p12), and 10,000 (p10) by their elution volumes and by their relative mobilities in sodium dodecyl sulfate-polyacrylamide gels.
	www.ihop-net.org /UniPub/iHOP/gg/124827.html (5629 words)

	Protease Inhibitor Cocktails - Biocompare Buyer's Guide (Site not responding. Last check: 2007-10-13)
		Protease Inhibitor Cocktail for use in purification of Histidine-tagged proteins
		Protease Inhibitor Cocktail for use with fungal and yeast extracts
		Protease Inhibitor Cocktail for use with mammalian cell and tissue extracts
	www.biocompare.com /matrix/3222/Protease-Inhibitor-Cocktails.html (197 words)

	Double Protease Inhibitor Regimens Containing Vertex's HIV Protease Inhibitor, Amprenavir, Show Promise
		Investigational Protease Inhibitor Amprenavir Appears Potent, Well Tolerated CHICAGO, Feb. 2 /PRNewswire/ -- Combining the investigational anti-HIV protease inhibitor amprenavir (formerly 141W94, VX-478) with any one of three currently available protease inhibitors may result in highly potent antiviral regimens that appear to be generally well tolerated by patients.
		The concept behind studying two protease inhibitors together is to try to further maximize the strength of anti-HIV treatment regimens.
		"Treatment with two protease inhibitors is becoming more common, and this study highlights amprenavir's versatility in double-protease combinations." Amprenavir was discovered by scientists at Vertex Pharmaceuticals which licensed the compound to Glaxo Wellcome.
	www.prnewswire.com /cgi-bin/stories.pl?ACCT=104&STORY=/www/story/2-2-98/406752&EDATE= (985 words)

	New Developments in the Biology and Treatment of HIV
		Combination therapy, generally involving two reverse transcriptase inhibitors and a protease inhibitor, has decreased the chance of drug-resistance development compared to earlier protease inhibitor monotherapy.
		It appears that latent infections of HIV in certain cells occur even during combination therapy, but there is no evidence that the viruses mutate to confer drug-resistance during latent infection.
		However, new infections with drug-resistant HIV have been documented, and it is estimated that up to 40 percent of infected people in the United States may have protease inhibitor-resistant viruses.
	www.aegis.com /news/ads/1998/AD981895.html (593 words)

	Investigational HIV Drug Brecanavir, Positive Data For Protease Inhibitor (Site not responding. Last check: 2007-10-13)
		Brecanavir is an HIV protease inhibitor in Phase 2b clinical development at GSK.
		HIV protease is an enzyme involved in HIV replication.
		Protease inhibitors block the protease enzyme, yielding copies of HIV that cannot infect new cells.
	www.medicalnewstoday.com /medicalnews.php?newsid=35427&nfid=rssfeeds (612 words)

	Secretory leukocyte protease inhibitor promotes the tumorigenic and metastatic potential of cancer cells -- Devoogdt et ...
		secretory leukocyte protease inhibitor (SLPI), as one of the genes
		inhibitors are therefore expected to be antimalignant (2).
		Secretory leukocyte protease inhibitor (SLPI) is a member of the kazal-type SPI family.
	www.pnas.org /cgi/content/full/100/10/5778 (3820 words)

	New protease inhibitor held HIV at undetectable levels for four years
		A study from The Feinberg School of Medicine has shown that the protease inhibitor lopinavir/ritonavir (Kaletra®) suppressed HIV to undetectable levels and was well tolerated through four years of treatment in patients who had not previously received antiretroviral therapy.
		To date in the Kaletra® study, none of the patients has developed resistance to Kaletra® or other protease inhibitors.
		Kaletra® is thus far the only protease inhibitor for which resistance has not been observed in patients receiving it as an initial therapy.
	www.innovations-report.com /html/reports/medicine_health/report-13260.html (355 words)

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