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Topic: Protease

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  Protease - Wikipedia, the free encyclopedia
Proteases (proteinases, peptidases, or proteolytic enzymes) are enzymes that break peptide bonds between amino acids of proteins.
Examples of protease inhibitors are the class of serpins (serine protease or peptidase inhibitors), incorporating alpha 1-antitrypsin.
The natural protease inhibitors are not to be confused with the protease inhibitors used in antiretroviral therapy.
en.wikipedia.org /wiki/Protease   (485 words)

 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_inhibitors   (383 words)

 Greenwood Health Systems ... Protease   (Site not responding. Last check: 2007-10-23)
Protease is responsible for digesting proteins in your food, which is probably one of the most difficult substances to metabolize.
Because of this, protease is considered to be one of the most important enzymes that we have.
Protease refers to a group of enzymes whose catalytic function is to hydrolyze (breakdown) peptide bonds of proteins.
greenwoodhealth.net /np/protease.htm   (416 words)

 The Body: Protease Inhibitors
So decisions about using protease inhibitors should be made with the help of your physician (and, if you are in a clinical trial studying a protease inhibitor, with the help of the team of health care workers involved in the clinical trial).
Protease is one of HIV's enzymes, and it is required to continue the process of HIV infection.
Protease inhibitors are drugs that resemble pieces of the protein chain that protease normally cuts.
www.thebody.com /iapac/sep97proinbk.html   (3121 words)

 Searching for protease substrates   (Site not responding. Last check: 2007-10-23)
Proteases clearly do a lot more than digest your meals; they act on substrates that are fundamental to a raft of physiological processes, from ovulation to programmed cell death or apoptosis.
Some proteases are intracellular agents, keeping cells tidy by degrading proteins that are past their 'use-by' date, whereas others work outside the cell, nipping and tucking the extracellular matrix that makes up the environment in which cells live and tissues function.
Both methods require that the protease binds the substrate but does not cleave it; that is, the proteases act as 'substrate traps'.
www.nature.com /horizon/proteases/background/searching.htm   (1525 words)

 Full Text - Potential application of protease isolated from Pseudomonas aeruginosa PD100
This protease could be useful for degradation of protein in the presence of solvent, dehairing of cow skin and degradation of natural proteins.
Although proteases are widespread in nature, microbes serve as a preferred source of these enzymes because of their rapid growth, the limited space required for their cultivation and the ease with which they can be genetically manipulated to generate new enzymes with altered properties that are desirable for their various applications.
Incubation of the protease with SDS for 60 min at 55ºC showed that the rate of tyrosine released at a particular time for SDS remained constant but in case of Tween 80 inactivation of the protease was time dependent (Figure 1).
www.ejbiotechnology.info /content/vol8/issue2/full/5   (2900 words)

 Protease Enzyme Supplement - Virastop - Enzyme Protease   (Site not responding. Last check: 2007-10-23)
Protease is able to dissolve almost all proteins as long as they are not components of living cells.
This formulation is used to optimize the amount of protease absorbed into the bloodstream to break down the protein invaders which are not part of the natural body.
This is based on the absorbability of the protease into the circulatory system, their hydrolytic activity and ability to remove proteinaceous debris in blood and extracellular fluid, and their susceptibility due to their unfolding and other conformational modifications from their native state.
www.enzymedica.com /protease_enzyme.php   (512 words)

 HIV Protease 3D Structures Index
A tutorial on HIV protease inhibitor design from the Chemistry department at the University of Wisconsin at Madison.
Protease complexed with tripeptide inhibitor from HIV-1 trans-frame region.
Protease Complexed bound to JE-2147 (also named AG1776 or KNI-764; a peptidomimetic protease inhibitor containing a unique unnatural amino acid, allophenylnorstatine [Apns; (2S, 3S)-3-amino-2-hydroxy-4-phenylbutyric acid], with a hydroxymethylcarbonyl (HMC) isostere as the active moiety) at 1.09 A resolution.
hiv-web.lanl.gov /content/hiv-db/STRUCTURE/PROTEASE.HTML   (865 words)

 AEGiS-GMHC: Protease Inhibitors: Overview and Analysis
Protease inhibitors are the one class of new, promising anti- HIV therapies likely to be available in the near future.
Protease inhibitors will be unavailable for the foreseeable future to those who wish to avoid the toxicities of AZT and similar medications.
As Treatment Issues went to press, a new study of protease inhibitor-resistant HIV appeared in the March issue of the Journal of Virology.* It described the protease produced by HIV mutant strains that are resistant to Abbott Laboratories' original protease inhibitor, A-77003, and similar compounds.
www.aegis.com /pubs/gmhc/1994/gm080201.html   (5077 words)

 (BETA) Protease-Sparing Combination Regimens
These changes have been given names such as "buffalo hump" and "protease paunch," and are characterized by accumulations of fatty tissue at the back of the neck, in the breasts, or on the abdomen or lower torso.
Many people have taken protease inhibitors without developing serious side effects and their health status has improved while taking them, but for a markedly finite amount of time before their immunological markers indicate that benefits are waning.
One problem, currently associated with protease inhibitor therapy, is abnormal fat metabolism, described in the previous section; one motive behind the new, protease-sparing strategies is the possibility of evading this side effect.
www.aegis.com /pubs/beta/1998/BE981005.html   (4013 words)

 Antiretrovirals: Protease Inhibitors
Ritonavir is a potent, orally bioavailable protease inhibitor that has been licensed based on promising surrogate marker data, as well as observed clinical benefits, including a short-term survival advantage in late-stage patients.
Further study is needed to define the clinical effects of regimens containing protease inhibitors in different stages of HIV disease, the optimal time for initiation of therapy, and strategies for managing patients who fail on regimens including protease inhibitors.
Great thought should be given to the selection of a protease inhibitor for an individual patient, as differences in efficacy, tolerability, ease of administration, drug interactions, and cross resistance patterns may substantially affect treatment outcome.
www.hivpositive.com /f-Topics/f-RetroviralConf/proteaseinhibitors.html   (2917 words)

 HIV Protease Inhibitor
Protease inhibitors are a new class of drugs that works by blocking the HIV protease.
This prevents the substrate from reacting with the protease and thus, the polypeptides are not cleaved.
Protease inhibitors are processed by the liver while reverse transcriptase inhibiters are processed in nonliver cells.
cat.middlebury.edu /~chem/chemistry/students/kim/inhibitor.html   (869 words)

 tpan.com - What's PK Got to Do With It? - The Protease Inhibitor Drugs
Of all classes of HIV medications, the protease inhibitors are the most complex in terms of pharmacokinetics, drug interactions and dosing changes based on those interactions.
The pharmacokinetics of the available protease inhibitors are summarized in Table 1, with and without Norvir boosting.
Protease inhibitors should not be taken without the other antiretrovirals that are prescribed, and vice versa.
www.tpan.com /publications/positively_aware/winter_05_pk/protease.html   (1321 words)

 HIV Protease inhibitors
Rifamycins acceleratethe metabolism of protease inhibitors (through induction of hepatic P450cytochromeoxidases), resulting in subtherapeutic levels of the proteaseinhibitors.In addition, protease inhibitors retard the metabolism of rifamycins,resultingin increased serum levels of rifamycins and the likelihood ofincreased drugtoxicity.
All of the HIV protease inhibitors that have been approved and most that are in development, are non-hydrolysable transition state peptidomimetics in which the cleavage site peptide linkage is replaced is replaced by transition state isosteres, such as statine, norstatine, hydroxyethylene, a reducedamide,hydroxyethyl, or dihydroxyethylene.
Nelfinavir is a relatively small protease inhibitor with goodoral bioavailability (52% in rats at 50 mg/kg; 9-42% in monkeys at 25mg/kg).Although, the half life after 25 mg/kg i.v.
www.arches.uga.edu /~ketona/bcmb8010/inhibitors.html   (2446 words)

 PureZyme-Digestive Enzymes-Protease-Tissue Repair, Enhance Immune System
Protease is also known to act as a scavenger of oxidized and damaged proteins, is active in helping to eliminate blood toxins, modulate the immune system, addresses hormonal imbalances, speeds wound and tissue repair, helps to chelate heavy metals and removes their toxins.
This duality in effect is due to the size of the protease and/or its substrates: large substrates may not be able to reach the active site of the trapped protease whereas smaller substrates may easily reach within the complex and be acted upon by the protease.
There is a change in the conformation of a2M when protease is bound to it, which is evident, as an increase in mobility in polyacrylamide gel electrophoresis, referred to as a shift from the "slow" to the "fast" form.
www.enzymeessentials.com /HTML/purezyme.html   (1953 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)

 New protease inhibitor shows promise in fighting AIDS   (Site not responding. Last check: 2007-10-23)
A new protease inhibitor has been shown to be safe, tolerable and effective at warding off HIV in HIV-positive patients with only one dose a day, according to data presented recently by a USC researcher at the Eighth Conference on Retroviruses and Opportunistic Infections in Chicago.
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.usc.edu /hsc/info/pr/1vol7/704/AIDS.html   (638 words)

 Bugs in the News - Protease Inhibitor and HIV
This article describes the use of protease inhibitor formulations in concert with at least two reverse transcriptase inhibitor preparations to effectively treat HIV infection.
A protease inhibitor would be any substance which partially or completely blocks the ability of a proteolytic enzyme to carry out its activity.
Therefore, protease inhibitors inhibit the ability of a particular protease to break the peptide bonds within a given protein.
people.ku.edu /~jbrown/protease.html   (1790 words)

Proteases refers to a group of enzymes whose catalytic function is to hydrolyze (breakdown) proteins.
Protease is able to hydrolyze almost all proteins as long as they are not components of living cells.
Protease also has an ability to digest unwanted debris in the blood including certain bacteria and viruses.
www.enzymeessentials.com /HTML/protease.html   (842 words)

 Two New Protease Inhibitors Approved By FDA, AIDS AGENDA - March, 1996
Protease inhibitors are compounds that block the protease enzyme of HIV, thereby preventing the production of infectious viral particles.
Central to the FDA approval of the new protease inhibitors were data presented at the 3rd Conference on Retroviruses and Opportunistic Infections in Washington, D.C., in late January.
The first licensed protease inhibitor, saquinavir (Invirase, Hoffmann-La Roche), was approved for use in conjunction with nucleoside analogues by the Food and Drug Administration in December 1995.
www.niaid.nih.gov /publications/agenda/0396/page4.htm   (1031 words)

 Protease Platform - Novartis.com
Proteases play a key role in a number of pathological processes.
Disregulation of proteases has been shown to play a role in diseases such as rheumatoid arthritis, cardiovascular diseases, bacterial and viral infections, cancer or Alzheimer’s disease.
In the past protease inhibitors have mainly been derived from the peptide substrate of the enzyme and have therefore retained a significant peptidic character which has precluded good oral bioavailability.
www.nibr.novartis.com /ExpertisePlatforms/ProteasePlatform/index.shtml   (751 words)

 protease enzyme
Protease refers to a group of enzymes whose function it is to break down proteins and are also referred to as proteolytic enzymes or proteinases.
Protease from aspergillis (Aspergillus Niger / Aspergillus oryzae) may also be able to assist in breaking down dietary proteins and polypeptides which have leaked into the bloodstream as food antigens.
A deficiency of this compound can cause anxiety and insomnia, since it will affect the blood alkaline level, and since it is involved in carrying protein-bound calcium in the bloodstream a deficiency may also influence the susceptibility for arthritis, osteoporosis and calcium related diseases.
www.anyvitamins.com /xramekopie/protease.htm   (462 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   (134 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   (240 words)

 Protease inhibitors
Protease inhibitors are considered one of the most potent medications for HIV developed so far.
Each of the types of protease inhibitor may have to be taken in a different way.
In most cases, protease inhibitors are part of a combination therapy, used in conjunction with other classes of HIV drugs.
www.healthatoz.com /healthatoz/Atoz/ency/protease_inhibitors.jsp   (602 words)

 HIV protease inhibitor
HIV protease, like the other proteins of this virus, is subject to rapid mutation that allows the virus to become resistant to the drug.
In order to accommodate a valine side chain (which is much larger than glycine, the smallest amino acid) at position 48, the inhibitor moves away from the protease, resulting in the formation of larger gaps between the inhibitor and the enzyme.
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)

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