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Topic: Protease



  
 NIH Guide: PROTEASE INHIBITOR RELATED ATHEROSCLEROSIS IN HIV INFECTION
Combinations of various protease inhibitors with nucleoside and non-nucleoside reverse transcriptase inhibitors usually have synergistic effects and are used effectively in clinical practice.
Proposed Research The known information on the dyslipidemias and lipodystrophy associated with protease inhibitor therapy for HIV-positive patients is derived from clinical observations.
Four protease inhibitors are currently in use: saquinavir mesylate, ritonavir, indinavir sulfate and nelfinavir.
http://grants.nih.gov/grants/guide/rfa-files/RFA-HL-00-007.html   (6761 words)

  
 HIV protease inhibitors promote atherosclerotic lesion formation independent of dyslipidemia by increasing ...
Premature atherosclerosis in HIV-infected individuals—focus on protease inhibitor therapy.
HIV protease inhibitors induce the accumulation of cholesteryl ester in THP-1 macrophages and human PBMCs.
Use of human immunodeficiency virus-1 protease inhibitors is associated with atherogenic lipoprotein changes and endothelial dysfunction.
http://www.jci.org/cgi/content/full/111/3/389   (5485 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.
Resistance to protease inhibitors may be slower to develop and at a lower level than for reverse transcriptase inhibitors.
Protease inhibitors will be unavailable for the foreseeable future to those who wish to avoid the toxicities of AZT and similar medications.
http://www.aegis.com/pubs/gmhc/1994/gm080201.html   (5077 words)

  
 Searching for protease substrates
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.
Borrowing and building on techniques from the plethora of genome-sequencing initiatives, and consequent efforts to map all the proteins,'degradomics' is the application of techniques used to unravel the genome and identify all the proteases and their substrates.
However, despite major advances in our understanding of proteases, their substrates and biological functions are not fully understood.
http://www.nature.com/horizon/proteases/background/searching.htm   (1525 words)

  
 Simple FactSheet: Protease Inhibitors
Protease inhibitors can affect the absorption of other drugs by the body.
For anyone with HIV, a thorough medical check-up is a good idea before starting protease inhibitor treatment.
Your health care provider should go over any potential drug interactions with you when starting a protease inhibitor.
http://www.aegis.com/factshts/network/simple/protease.html   (1169 words)

  
 Full Text - Potential application of protease isolated from Pseudomonas aeruginosa PD100
Capability of the protease to digest different natural substrates with base of fibrin, albumin and collagen suggesting usefulness of this enzyme for different applications such as extraction of collagen from skin for collagen replacement therapy, waste treatment and other related applications.
With respect to the results from this experiment, it was found that the protease of P.
The skin was checked for removal of hair at different incubation times.
http://www.ejbiotechnology.info/content/vol8/issue2/full/5   (2900 words)

  
 The Body: Protease Inhibitors
This information will change as protease inhibitors are used by more people with HIV infection and as more is learned about how they work.
Should protease inhibitors be combined with other drugs?
Doctors are advised to combine nonnucleosides and protease inhibitors with caution until there is more specific information on how they affect each other.
http://www.thebody.com/iapac/sep97proinbk.html   (3121 words)

  
 The HCMV Protease Project
There are large conformational changes in the protease upon inhibitor binding (induced-fit behavior).
Investigating the role of histidine157 in the catalytic activity of human cytomegalovirus protease.
A rational approach towards successful crystallization and crystal treatment of human cytomegalovirus protease and its inhibitor complex.
http://como.bio.columbia.edu/tong/Research/hcmv.html   (310 words)

  
 HIV Protease Inhibitor
Protease inhibitors are a new class of drugs that works by blocking the HIV protease.
These protease inhibitors seem to be less toxic and seem to have less severe side affects than other anti-AIDS drugs (nucleoside analogs like AZT) Saquinavir, ritonavir, and
One problem with the drug was that it had limited oral bioavailability (did not absorb into the body well).
http://cat.middlebury.edu/~chem/chemistry/students/kim/inhibitor.html   (869 words)

  
 HIV Protease inhibitors
Protease inhibitors used in combination with reverse transcriptase (RT) inhibitors represent the most effective anti-HIV therapies developed to date.
Four protease inhibitors, saquivanir (Invirase®, Hoffman-LaRoche), ritonavir (Norvir®, Abbott), indinavir (Crixivan®, Merck) and nelfinavir (Viracept®,Agouron) have already been approved and several others are in the late stagesof clinical development.
Low bioavailability(~ 4%) due to poor absorption and extensive first pass metabolism limitstheuse of saquinavir in potent triple combination therapies (Ohta, Y.et al 1997).
http://www.arches.uga.edu/~ketona/bcmb8010/inhibitors.html   (2446 words)

  
 Protease inhibitors
In most cases, protease inhibitors are part of a combination therapy, used in conjunction with other classes of HIV drugs.
Protease inhibitors are considered one of the most potent medications for HIV developed so far.
These drugs do not necessarily reduce the risk of transmitting HIV to others through sexual contact, so patients should avoid sexual activities or use condoms.
http://www.healthatoz.com/healthatoz/Atoz/ency/protease_inhibitors.jsp   (602 words)

  
 Production of Alkaline Protease With Immobilized Cells of Bacillus subtilis PE-11 in Various Matrices by Entrapment ...
Protease activity was assessed by the modified procedure based on the method of Tsuchida et al
The success achieved with the entrapment technique prompted us to study the production of alkaline protease with immobilized cells using this technique.
Calcium alginate was found to be an effective and suitable matrix for higher alkaline protease productivity compared to the other matrices studied.
http://www.aapspharmscitech.org/view.asp?art=pt060348   (3634 words)

  
 Protease Platform - Novartis.com
Several protease inhibitors are already available as drugs.
To this end, all activities focussing on the molecular aspects of protease-directed drug discovery are integrated in the Expertise Program.
The availability of the necessary skills in the Expertise Program allows us to remain highly innovative and competitive in protease-directed drug discovery.
http://www.nibr.novartis.com/ExpertisePlatforms/ProteasePlatform/index.shtml   (751 words)

  
 An Extracellular Protease of Streptococcus gordonii Hydrolyzes Type IV Collagen and Collagen Analogues -- Juarez and ...
Purification and characterization of a human IgA1 specific protease.
limited conditions and that protease was not produced during the
experiments focused on the protease(s) contained in the 55 to
http://iai.asm.org/cgi/content/full/67/1/271   (5018 words)

  
 Structural aspects of activation pathways of aspartic protease zymogens and viral 3C protease precursors -- Khan et al. ...
Structures on the conversion pathway of the aspartic protease zymogen progastricsin.
of the gastric aspartic proteases interacting with the catalytic
Active Site Contribution to Specificity of the Aspartic Proteases Plasmepsins I and II
http://www.pnas.org/cgi/content/full/96/20/10968   (5186 words)

  
 HCV Protease Inhibitors: Glimpses of Hope on a Distant Horizon
But despite considerable research on HCV PIs over the past decade, it will require at least several more years before an HCV protease inhibitor will win FDA approval and reach the market.  Only two HCV protease inhibitors are currently in human studies, and both are at the very earliest stage of clinical research.
The issue of whether patients and clinicians should base current treatment decisions on the future prospect of improved therapies is a critical one in the current clinical management of hepatitis C. 
While it certainly is reasonable to offer patients the anticipation of future treatment opportunities, hope is not a particularly effective method of viral eradication.”
http://www.hivandhepatitis.com/hep_c/news/2004/063004_a.html   (1158 words)

  
 Protease - Wikipedia, the free encyclopedia
The natural protease inhibitors are not to be confused with the protease inhibitors used in antiretroviral therapy.
This may be an important method of regulation of peptidase activity.
Thus, protease inhibitors are developed as antiviral means.
http://en.wikipedia.org/wiki/Protease   (476 words)

  
 HIV Protease 3D Structures Index
Viability of a drug-resistant human immunodeficiency virus type 1 protease variant: structural insights for better antiviral therapy.
The application of structure-based drug design to members of the aspartic proteinase family.
The HIV Drug Resistance Database at LANL and the HIV Drug Resistance Database at Stanford are both sources of information on sites in the protease and reverse transcriptase proteins which mutate to create drug resistance in the virus.
http://hiv-web.lanl.gov/content/hiv-db/STRUCTURE/PROTEASE.HTML   (851 words)

  
 Nature's Sunshine Products Protease Plus Capsules
Studies show that protease helps keep the intestines protected from parasites and other organisms that may weaken the intestinal system.
These have been linked to a variety of unsavory health concerns.
At the same time, malabsorption of nutrients and chronic health conditions increase.
http://www.greatestherbsonearth.com/nsp/proteaseplus.htm   (993 words)

  
 Protease inhibitor (pharmacology) - Wikipedia, the free encyclopedia
Protease inhibitors were the second class of antiretroviral drugs developed.
Protease inhibitors (PIs) are a class of medication used to treat or prevent infection by viruses, including HIV and Hepatitis C.
Protease inhibitors have been developed or are presently undergoing testing for treating various viruses:
http://en.wikipedia.org/wiki/Protease_inhibitor_(pharmacology)   (348 words)

  
 Introduction
Another pathway consists in the compartmentation of proteases e.g in lysosomes.
This family includes the plant proteases such as papain, actinidin or bromelain, several mammalian lysosomal cathepsins, the cytosolic calpains (calcium-activated) as well as several parasitic proteases (e.g Trypanosoma, Schistosoma).
The pepsin family includes digestive enzymes such as pepsin and chymosin as well as lysosomal cathepsins D and processing enzymes such as renin, and certain fungal proteases (penicillopepsin, rhizopuspepsin, endothiapepsin).
http://delphi.phys.univ-tours.fr/Prolysis/introprotease.html   (1184 words)

  
 Protease Inhibitor Letter DIABETES AND HYPERGLYCEMIA
At the present time there exists no conclusive evidence establishing a definite causal relationship between protease inhibitor therapy and the incidence of diabetes and hyperglycemia.
Hyperglycemia persisted in some patients after protease inhibitor therapy was withdrawn including patients not known to be diabetic at baseline; however a causal relationship between protease inhibitor therapy and these events has not been established.
Many of these reports occurred in patients with confounding medical conditions, some of which required therapy with agents that have been associated with the development of diabetes mellitus or hyperglycemia.
http://www.fda.gov/oashi/aids/prolet.html   (434 words)

  
 Cysteine protease inhibitors as chemotherapy: Lessons from a parasite target -- Selzer et al. 96 (20): 11015 -- ...
consistent with a pathway of protease trafficking from flagellar
and protease in the flagellar pocket of treated parasites were
Papain family cysteine proteases are key factors in the pathogenesis of cancer invasion, arthritis, osteoporosis, and microbial
http://www.pnas.org/cgi/content/abstract/96/20/11015   (804 words)

  
 PROTEASE INHIBITORS IN DEVELOPMENT
Several firms are trying to develop a new type of protease inhibitor that will not be cross-resistant with existing drugs.
These drugs have not been approved by the Food and Drug Administration (FDA) for use against HIV.
Protease inhibitors being tested in humans include Brecanavir (GW640385), Darunavir (TMC114), and PPL-100.
http://www.aids.org/factSheets/440-Protease-Inhibitors-in-Development.html   (298 words)

  
 Halt Protease Inhibitor Cocktail
Inhibit a variety of proteases using Halt Protease Inhibitor Cocktails.
SDS-PAGE analysis of the inhibition of protease activity using Halt Protease Inhibitor Cocktails.
Lane 2 shows BSA digestion in the presence of Halt Protease Inhibitor Cocktail.
http://www.piercenet.com/Products/Browse.cfm?fldID=02040806   (169 words)

  
 NEJM -- HIV-Protease Inhibitors
OLIVÉ, A., SALAVERT, A., MANRÍQUEZ, M., CLOTET, B., MORAGAS, A. Parotid lipomatosis in HIV positive patients: a new clinical disorder associated with protease inhibitors.
Substitution of Nevirapine, Efavirenz, or Abacavir for Protease Inhibitors in Patients with Human Immunodeficiency Virus Infection.
Lee, E. C., Walmsley, S., Fantus, I. New-onset diabetes mellitus associated with protease inhibitor therapy in an HIV-positive patient: case report and review.
http://content.nejm.org/cgi/content/extract/338/18/1281?ck=nck   (2321 words)

  
 Inhibitor, protease definition - HIV: health and medical information about HIV and AIDS
Inhibitor, protease definition - HIV: health and medical information about HIV and AIDS
The protease inhibitors represented a major advance in treating HIV infection and AIDS.
A lipodystrophy syndrome appears associated with the protease inhibitors.
http://www.medterms.com/script/main/art.asp?articlekey=7106   (342 words)

  
 Oviductin, the Xenopus laevis Oviductal Protease That Processes Egg Envelope Glycoprotein gp43, Increases Sperm Binding ...
protease domain) is 66 kDa, we conclude that the oviductin-
to the serine proteases found to be most similar to the first
protease domains, were analyzed for similarity to other proteins
http://www.biolreprod.org/cgi/content/full/60/4/989   (5086 words)

  
 BioAfrica - HIV-1 Protease (PR) sequence, structure and function information
5 - Crystal structure of a retroviral protease proves relationship to aspartic protease family.
6 - Three-dimensional structure of aspartyl protease from human immunodeficiency virus HIV-1.
a database of the structures of human immunodeficiency virus protease.
http://www.bioafrica.net/proteomics/POL-PRprot.html   (347 words)

  
 Greenwood Health Systems ... Protease
Commercially, proteases are produced in highly controlled aseptic conditions for food supplementation and systemic enzyme therapy.
Protease refers to a group of enzymes whose catalytic function is to hydrolyze (breakdown) peptide bonds of proteins.
Protease helps in the healing and recovery from cancer by dissolving the fibrin coating on cancer cells, and thereby giving your immune system a chance to do its job.
http://greenwoodhealth.net/np/protease.htm   (416 words)

  
 Diabetes and Hyperglycemia in Patients Receiving Protease Inhibitors
Diabetes and Hyperglycemia in Patients Receiving Protease Inhibitors
The benefits of protease inhibitors for patients with HIV infection are still believed to outweight their risks.
Patients should always discuss with their physician the risks and benefits before discontinuing or initiating protease inhibitor therapy.
http://www.fda.gov/cder/news/proteaseqa.htm   (582 words)

  
 International Protease Network
International researchers are studying proteases, their receptors and inhibitors to better understand the biology of life and the treatment of diseases.
They are important in conception and birth, life, ageing, and death of all organisms.
Proteases are enzymes that account for about 2% of the human genome, and 1-5% of genomes of infectious organisms.
http://www.protease.net   (122 words)

  
 JCE 1996 (73) 63 [Jan] HIV-1 Protease: An Enzyme at Work
HIV-1 Protease: An Enzyme at Work is a set of materials designed to help instructors explain enzymatic processes through the example of HIV-1 protease.
One can then extend the protease example to a generalized picture of enzymatic processes.
A potential treatment for HIV focuses on the enzyme known as HIV-1 protease, which is essential for the maturation of new virus particles.
http://jchemed.chem.wisc.edu/Journal/Issues/1996/Jan/abs63.html   (470 words)

  
 Staphylococcus aureus V-8 protease
This is related to the fact that the native structure of the protease is stabilized mainly by electrostatic interactions, and not by hydrogen bonding and ß-structures.
With immobilized proteases, no quenching is necessary and there are no problems with protease contamination of the sample or autodigestion of the protease.
The protease is further specific for only glutamic digestion in buffers which do not contain phosphate at either pH optimum.
http://www.piercenet.com/Products/Browse.cfm?fldID=02040708&Format=Print   (391 words)

  
 HIV Infection: Protease and Protease Inhibitors
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.
Viral protease cuts the long chain into its individual enzyme components which then facilitate the production of new viruses.
By blocking the ability of the protease to cleave the viral polypeptide into functional enzymes, protease inhibitors interfere with continued infection.
http://www.cellsalive.com/hiv4.htm   (124 words)

  
 Incorporation of Protease K into Larval Insect Membrane Vesicles Does Not Result in Disruption of Integrity or Function ...
protease on toxin integrity and function were then
Protease activity was detected only in solubilized BBMV which
Immunoblot of extracts of BBMV which had been preincubated with Cry1Ac1 toxin.
http://aem.asm.org/cgi/content/full/66/10/4568   (1718 words)

  
 HIV Protease
The Structure of HIV Protease and the Design of Inhibitors
Inhibitors of HIV Protease: An Introduction to Carbonyl Chemistry
Hybridization Does Not Predict the Structure of a Piece of HIV Protease
http://www.chem.wisc.edu/~newtrad/CurrRef/AIDStopic/AIDStext/AIDStoc.html   (130 words)

  
 FISH guide - protease pretreatment
Trypsin treatment proved too extensive, and the only acceptable slide was the one without exposure to the protease.
A few hybridization tests were done in which slides were first aged and denatured and only afterwards subjected to enzymatic pretreatment.
For example, in our laboratory, fibroblasts or tumor cells required less pepsin pretreatment than lymphocytes.
http://info.med.yale.edu/genetics/ward/tavi/fi03.html   (659 words)

  
 TEV NIa protease homepage
Polypeptides that are not natural substrates of TEV protease are proteolyzed if they carry the appropriate cleavage site.
Because of its specificity it is often used to remove tags such as 6His tags after protein purification.
There are many potential uses for TDP in vivo for example controlled inactivation of essential proteins and topological studies of integral membrane proteins, among others.
http://www.cf.ac.uk/biosi/staff/ehrmann/tools/TEVprot.html   (179 words)

  
 Cholesterol - Wikipedia, the free encyclopedia
The cleaved SREBP then migrates to the nucleus and acts as a transcription factor to bind to the SRE (Sterol regulatory element) of a number of genes to stimulate their transcription.
When cholesterol levels fall, Insig-1 dissociates from the SREBP-SCAP complex, allowing the complex to migrate to the Golgi apparatus, where SREBP is cleaved by S1P and S2P (site 1/2 protease), two enzymes that are activated by SCAP when cholesterol levels are low.
In the presence of cholesterol, SREBP is bound to two other proteins: SCAP (SREBP-cleavage activating protein) and Insig-1.
http://en.wikipedia.org/wiki/Cholesterol   (1926 words)

  
 The Body: Protease Inhibitors
Pharmacist James D. Scott explains how protease inhibitors work, and how they might interact with other HIV meds
New HIV Protease Inhibitors: New Options in the PI Class for Treatment-Naive Persons (Spring 2004)
HIV 101: Antiretroviral Agents Dosing and Administration Recommendations: PIs (January 2002)
http://www.thebody.com/treat/protinh.html   (263 words)

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