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Topic: Protease inhibitor

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	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) (356 words)

	Encyclopedia: Protease inhibitor (pharmacology)
		Protease inhibitors are a class of medication used to treat or prevent viral infections.
		Saquinavir (FortovaseÂ®, Roche) is a protease inhibitor, used as a component of HIV therapy.
		In biology and biochemistry, protease inhibitors are molecules that inhibit the function of peptidases (old name: protease, hence the term protease inhibitor).
	www.nationmaster.com /encyclopedia/Protease-inhibitor-(pharmacology) (558 words)

	NIH Guide: PROTEASE INHIBITOR RELATED ATHEROSCLEROSIS IN HIV INFECTION
		These observations have led to the hypothesis that use of the protease inhibitors may be associated with the development of a new syndrome consisting of peripheral lipodystrophy, hyperlipidemia and insulin resistance.
		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)

	Simple FactSheet: Protease Inhibitors
		Protease is a chemical, known as an enzyme, that HIV needs in order to make new viruses.
		Protease Inhibitors are pills that need to be taken at least twice a day.
		Protease inhibitors can make hepatitis worse, so it's important to know if you have hepatitis B and/or C before starting a protease inhibitor.
	www.aegis.com /factshts/network/simple/protease.html (1169 words)

	SF AIDS Fdn: BETA Live! 8/97 -- Protease Inhibitor Drug Interactions
		What we’re most concerned about with the protease inhibitors specifically is that they rely very heavily on the cytochrome P450 system for their own metabolism and, in addition, they can effects the activity of the cytochrome P450 system.
		It is a nucleoside reverse transcriptase inhibitor or nucleoside analog.
		The five protease inhibitors that we’ve been talking about (including the 141 drug) are "pepto- mimetic," that is, they have a chemical structure that similar to a protein compound.
	www.sfaf.org /treatment/betalive/bl897pi.html (7693 words)

	USC HIV/AIDS researcher announces new protease inhibitor
		A new protease inhibitor has been shown to be safe, tolerable and effective at holding off HIV in HIV-positive patients with only one dose a day, according to data presented today by a University of Southern California researcher at the Eighth Conference on Retroviruses and Opportunistic Infections.
		Today’s commonly used protease inhibitors are associated with increases in cholesterol and triglycerides, which are known to increase the risk of cardiovascular problems.
		Lipodystrophy is a common problem linked to protease inhibitors in which a patient’s belly swells or a pad of fat may grow behind the neck, while the arms, legs and face become gaunt.
	www.eurekalert.org /pub_releases/2001-02/UoSC-UHra-0402101.php (643 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)

	Protease inhibitor (pharmacology) - Encyclopedia.WorldSearch (Site not responding. Last check: 2007-11-05)
		Protease inhibitors are a class of medication used in viral infections.
		Medical Aspects of Proteases and Proteases Inhibitors (Biomedical and Health Research, Vol.
		Proteases, Protease Inhibitors & Proteasederived Peptides : Importance in Human...
	encyclopedia.worldsearch.com /protease_inhibitor_(pharmacology).htm (198 words)

	SF AIDS Fdn: BETA 9/97 -- Protease Inhibitor Drug Interactions
		Protease inhibitors may also cause increased levels of rifampin and rifabutin, potentially resulting in toxic side effects.
		Stopping a protease inhibitor may result in the development of drug resistance and may preclude later use of that drug.
		Protease inhibitors in patients with HIV disease: clinically important pharmacokinetic considerations.
	www.sfaf.org /treatment/beta/b34/b34piint.html (3441 words)

	The Body: Debate Widens Over Protease Inhibitor Side Effects
		According to their research, the region of the HIV protease enzyme to which protease inhibitors bind is structurally similar to regions on two human proteins that regulate the breakdown of lipids: low density lipoprotein-
		Kotler theorizes that the association between protease inhibitors and the metabolic abnormalities is indirect, and might be inversely related to HIV replication.
		Sixteen percent of the protease inhibitor group had elevations of greater than 65 mg/dl and 5.7% had increases of greater than 100 mg/dl.
	www.thebody.com /gmhc/issues/julaug98/lipo.html (2593 words)

	AllRefer.com - protease inhibitor (Pharmacology) - Encyclopedia
		protease inhibitor[prO´tE-As´´] Pronunciation Key, any of a class of drugs that interfere with replication of the AIDS virus (HIV), by blocking an enzyme (protease) necessary in the late stages of its reproduction.
		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.
		Saquinavir, the first member of the class to be marketed, was approved for use in 1995 by the Food and Drug Administration.
	reference.allrefer.com /encyclopedia/P/proteas.html (187 words)

	HIV & AIDS - JAMA study shows increased mortality from protease inhibitor use
		Protease inhibitors were introduced on the market in December 1995 with much fanfare, but only two randomized studies were ever done that claimed reduced infections or death from use of protease inhibitors.
		The increased mortality in people using protease inhibitors was found in the second study to be reviewed, but the first study also found many inconsistencies with conventional beliefs about HIV and AIDS.
		These toxicities could explain why people who started on these drugs showed increased mortality when compared with people who were not started on protease inhibitors, but this possibility is not even entertained by the authors of the study.
	www.virusmyth.net /aids/news/mijama.htm (1280 words)

	Time-Resolved Fluorescence Anisotropy of HIV-1 Protease Inhibitor Complexes Correlates with Inhibitory Activity (Site not responding. Last check: 2007-11-05)
		The tryptophan time-resolved fluorescence intensity and anisotropy of the HIV-1 protease dimer is shown to be a quick and efficient method for the conformational characterization of protease inhibitor complexes.
		As a result of the wavelength dependence of the respective amplitudes, the 2.06 ns and the 4.46 ns decay constants were suggested to be the intrinsic fluorescence lifetimes of the more solvent-exposed W6 and the less exposed W42 residues, respectively.
		The effects of 11 different inhibitors including statine-derived, hydroxyethylamine-derived, and 2 symmetrical inhibitors on the protease fluorescence dynamics were investigated.
	pubs.acs.org /cgi-bin/abstract.cgi/bichaw/1998/37/i09/abs/bi971654w.html (291 words)

	FDA Approves a Once Daily Protease Inhibitor for HIV Infection
		The Food and Drug Administration (FDA) today announced the approval of Reyataz (atazanavir sulfate), a protease inhibitor to be used in combination with other anti-retroviral agents for the treatment of patients with HIV infection.
		Approval of this drug will now allow patients access to a protease inhibitor that only needs to be taken once daily with food and has a low "pill burden" (two pills each day).
		A significant safety concern commonly observed with the use of protease inhibitors is hyperlipidemia (high cholesterol).
	www.fda.gov /bbs/topics/ANSWERS/2003/ANS01233.html (390 words)

	Distribution of the Human Intracellular Serpin Protease Inhibitor 8 in Human Tissues -- Strik et al. 50 (11): 1443 -- ...
		Buzza MS, Hirst CE, Bird CH, Hosking P, McKendrick J, Bird PI (2001) The granzyme B inhibitor, PI-9, is present in endothelial and mesothelial cells, suggesting that it protects bystander cells during immune responses.
		Riewald M, Schleef RR (1995) Molecular cloning of bomapin (protease inhibitor 10), a novel human serpin that is expressed specifically in the bone marrow.
		Scott FL, Hirst CE, Sun J, Bird CH, Bottomley SP, Bird PI (1999) The intracellular serpin proteinase inhibitor 6 is expressed in monocytes and granulocytes and is a potent inhibitor of the azurophilic granule protease, cathepsin G. Blood 93:2089-2097
	www.jhc.org /cgi/content/full/50/11/1443 (4685 words)

	Protease inhibitor definition - HIV: health and medical information about HIV and AIDS
		Protease inhibitor: One of a class of anti-HIV drugs designed to inhibit the enzyme protease and thereby interfere with virus replication.
		Protease inhibitors prevent the cleavage of HIV precursor proteins into active proteins, a process that normally occurs when HIV replicates.
		Side effects associated with protease inhibitors include a lipodystrophy syndrome in which the face, arms and legs become thin due to loss of subcutaneous fat, the skin becomes dry, weight loss occurs, and abnormal deposits of fat occur.
	www.medterms.com /script/main/art.asp?articlekey=5080 (322 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)

	Halt Protease Inhibitor Cocktail
		Add the appropriate volume of inhibitor cocktail to the sample (10 µl per 1 ml of cell extract) and continue with your purification.
		The Halt Protease Inhibitor Cocktails can be used with animal cells and tissues, bacteria, plants and yeast.
		Bovine serum albumin (BSA) was incubated overnight at 37°C in the presence of the protease papain.
	www.piercenet.com /Products/Browse.cfm?fldID=02040806&Format=Print (154 words)

	The secretory leukocyte protease inhibitor gene is a target of epidermal growth factor receptor action in endometrial ...
		of the Kazal superfamily of serine protease inhibitors, inhibits
		Badinga L, Michel FJ and Simmen RCM 1999 Uterine-associated serine protease inhibitors stimulate deoxyribonucleic acid synthesis in porcine endometrial glandular epithelial cells of pregnancy.
		Shigemasa K, Tanimoto H, Underwood LJ, Parmley TH, Arihiro K, Ohama K and O’Brien TJ 2001 Expression of the protease inhibitor antileukoprotease and the serine protease stratum corneum chymotryptic enzyme (SCCE) is coordinated in ovarian tumors.
	joe.endocrinology-journals.org /cgi/content/full/184/1/141 (5878 words)

	Inhibitor, protease definition - HIV: health and medical information about HIV and AIDS
		Inhibitor, protease: An agent that can keep a protease from working and splitting a protein into peptides.
		The abdomen swells producing a sometimes painful pot belly that is dubbed "a protease paunch." A woman may look pregnant when she is not.
		Another problem with the protease inhibitors is the development of strains of HIV that are resistant to these drugs, as was reported at the 12th World AIDS Conference in 1998 by a team led by Frederick M. Hecht at the University of California, San Francisco and workers from Switzerland.
	www.medterms.com /script/main/art.asp?articlekey=7106 (342 words)

	AEGiS-GMHC: Delavirdine/Protease Inhibitor Interactions
		A major issue that remains unresolved with both delavirdine and nevirapine is how these drugs affect the body's metabolism of protease inhibitors.
		Nevirapine seems to increase destruction of protease inhibitors whereas delavirdine (and ritonavir) inhibits this loss.
		The result of these hepatic changes on protease inhibitor blood levels or efficacy has been little explored up to now.
	www.aegis.com /pubs/gmhc/1996/GM100904.html (732 words)

	FDA Approves Once-Daily Combination of Abbott's Protease Inhibitor Kaletra
		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)

	PRESS RELEASE Schering-Plough Reports Novel Investigational Protease Inhibitor Shows In Vitro Antiviral Activity in ... (Site not responding. Last check: 2007-11-05)
		The hepatitis C protease is a viral enzyme complex that is essential to the replication of the hepatitis C virus.
		Negro, along with fellow scientists from University Hospital and working with a team of SPRI researchers, used multiple procedures to assess the antiviral activity of a novel protease inhibitor in the Schering-Plough portfolio known as SCH6 in a standard cell line (Huh-7 hepatoma cells) that was infected with HCV.
		Researchers noted that while HCV protease inhibitors show promise in early stage development, much additional work will be required before this class of compounds becomes available to patients.
	www.marketwire.com /mw/release_html_b1?release_id=59099 (1472 words)

	Science & Medicine \| Long-Term Protease Inhibitor Treatment Increases Men's Risk for Heart Attack, Study Says - ...
		Long-term antiretroviral drug treatment including protease inhibitors increases HIV-positive men's risk for heart attack, according to a study published in the Nov. 21 issue of the journal
		The heart attack rate nearly doubled to 15.9 for men treated with a protease inhibitor for 18 to 29 months and doubled again to 33.8 for those treated with a protease inhibitor for 30 months or longer.
		Although the life expectancy gained by taking antiretroviral treatments that include protease inhibitors "far outweighs" the increased heart attack risk, physicians should consider patients' cardiovascular disease risk factors when deciding whether to prescribe protease inhibitors, the researchers concluded.
	www.kaisernetwork.org /daily_reports/rep_index.cfm?DR_ID=21427 (278 words)

	HIV protease inhibitor
		The inhibitor shown, called a macrocycle, possesses two amides and an aromatic group within 15-17 membered rings designed to replace N- or C-terminal tripeptides from peptidic inhibitors of HIV protease.
		HIV protease, like the other proteins of this virus, is subject to rapid mutation that allows the virus to become resistant to the drug.
		The protease is green and the Saquinavir is in cpk color (gray, red, blue) as it was in the enlarged image of the drug that you just saw.
	pathmicro.med.sc.edu /chime2/hiv-prot-frmleft.htm (759 words)

	News - Data Supports Development of Investigational HIV Protease Inhibitor Brecanavir (Site not responding. Last check: 2007-11-05)
		Brecanavir is an HIV protease inhibitor in Phase IIb clinical development.
		Protease is one such enzyme involved in HIV replication.
		HIV protease inhibitors block the HIV protease enzyme, yielding copies of HIV that cannot infect new cells.
	www.docguide.com /news/content.nsf/news/8525697700573E18852570EC006970F2 (660 words)

	CROI: HIV in Patients with Multiple Protease Inhibitor Mutations Remain Susceptible to Tipranavir
		Conference on Retroviruses and Opportunistic Infections, researchers said that 93% of the patients recruited into their study had 10 or more mutations that compromised treatment with available antiretroviral drugs, and 41 of the isolates from the cohort of 216 patients had genotypes that were indicative of resistance to all currently marketed protease inhibitors.
		All of the patients in the multicenter, international, randomized, blinded study had been heavily pretreated with nucleoside reverse transcriptase inhibitors, non-nucleoside reverse transcriptase inhibitors, and protease inhibitors.
		Cooper noted that few isolates with only 1 or 2 of the universal protease inhibitor-associated mutations result in reduced effectiveness of tipranavir to control replication of the virus.
	www.docguide.com /dg.nsf/PrintPrint/1A9B9D608573169E85256CCB00526520 (512 words)

	Granzyme M Is a Regulatory Protease That Inactivates Proteinase Inhibitor 9, an Endogenous Inhibitor of Granzyme B -- ...
		Granzyme M Is a Regulatory Protease That Inactivates Proteinase Inhibitor 9, an Endogenous Inhibitor of Granzyme B -- Mahrus et al.
		Granzyme M is a trypsin-fold serine protease that is specifically
		and proteinase inhibitor 9 was characterized by using a candidate-based
	www.jbc.org /cgi/content/abstract/279/52/54275 (483 words)

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