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Inhibitor in Biological News

HIV-1 protease inhibitor induced oxidative stress in pancreatic B-cells: thymoquinone protection

Researchers at the Tulane University School of Medicine, New Orleans, Louisiana have discovered that the HIV-1 protease inhibitors (PIs), such as nelfinavir included in highly active antiretroviral therapy (HAART) regimen for the treatment of HIV-1 patients, induce deleterious effects on insulin s...

Plasminogen activator inhibitor type-1 -- a potential link between heart failure and diabetes

Researchers at the University of Vermont Cardiovascular Research Institute, Colchester, Vermont have found that increased expression in the heart of plasminogen activator inhibitor type-1 (PAI-1) is profibrotic. The results, which appear in the March 2009 issue of Experimental Biology and Medici...

Researchers describe protease inhibitor that may aid in diabetic retinopathy treatment

NEW YORK, Jan. 21, 2009 Researchers from Joslin Diabetes Center, Boston, and ActiveSite Pharmaceuticals, Inc., San Francisco, announced today that they have demonstrated that a specific inhibitor of the protease plasma kallikrein, ASP-440, developed by ActiveSite Pharmaceuticals, may provide a ne...

Scientists identify novel inhibitor of human microRNA

Scientists at The Wistar Institute and their colleagues have identified, for the first time, a molecule that can regulate microRNAs short strands of RNA that play a vital role in gene expression and are closely associated with cancer. The discovery points the way to the development of a new gener...

New oral angiogenesis inhibitor offers potential nontoxic therapy for a wide range of cancers

The first oral, broad-spectrum angiogenesis inhibitor, specially formulated through nanotechnology, shows promising anticancer results in mice, report researchers from Children's Hospital Boston. Findings were published online on June 29 by the journal Nature Biotechnology . Because it is nont...

New inhibitor has potential as cancer drug

Laboratory experiments have previously shown that cancer cells overproduce an enzyme, heparanase, which splits the bodys own polysaccharide heparan sulfate into shorter fragments. The amount of enzyme is related to the degree of malignancy. Today a study is being published in the journal Nature ...

New protein inhibitor impedes growth of cancerous cells

Researchers have developed a small-molecule inhibitor of a protein that plays key roles in the control of cell division, and they show that the inhibitor can halt the growth of tumors in mice and cancer-derived cells growing in culture. The findings are reported in companion papers reported by two ...

Discovery of an HIV inhibitor in human blood points to new drug class

A new study has pinpointed a natural ingredient of human blood that effectively blocks HIV-1, the virus predominantly responsible for human AIDS, from infecting immune cells and multiplying. The virus blocker might play a role in the progression of HIV to full-blown AIDS and—because it works in a d...

Unique dual target specificity of kinase inhibitor key for success against cancer

Scientists have identified a new molecule that inhibits proliferation of a broad range of lethal malignant glioma cells in vitro and in vivo. The findings, published in the May issue of Cancer Cell, shed light on which PI3 kinase family members are most likely to play a role in cancer progression. ...

Anthrax inhibitor counteracts toxin, may lead to new therapeutics

Researchers from Rensselaer Polytechnic Institute and the University of Toronto have designed a nanoscale assembly of molecules that successfully counteracts and inhibits anthrax toxin in animal and laboratory experiments. The novel approach used to neutralize anthrax toxin could be applied in desi...

Small molecule inhibitor of cholera discovered

Study appears in ScienceJust as hurricanes in the Gulf states and Guatemala have raised the risks of cholera outbreaks, researchers at Harvard Medical School have identified a new type of antibiotic against the cholera bacteria. While traditional antibiotics kill bacteria outright by interfering wi...

UNC scientists discover new role for protein as fundamental inhibitor of cell movement

Scientists from the University of North Carolina at Chapel Hill School of Medicine and the UNC Lineberger Comprehensive Cancer Center have identified a protein that may inhibit cellular movement, or migration. The protein, CIB1, or calcium and integrin-binding protein 1, was originally discovered...

HIV Patients May Be at Risk of Heart Problems When Taking Protease Inhibitor Drugs

A widely-used class of drugs that keep the HIV-virus infection from progressing to AIDS may cause serious and potentially lethal heart rhythm disturbances in some patients. The finding of a Mayo Clinic-led investigation appears in the current edition of The Lancet. In collaboration with colleag...

Bladder cells feel stretch

...e observed in urothelial cells. These phenomena were almost completely attributed to TRPV4 activation, since such responses were eliminated by a TRPV4 inhibitor and reduced in TRPV4-deficient urothelial cells. Dr. Sokabe said, "This is the first report to show that TRPV4 is a primal stretch-detector in uroth...

UCSF researchers identify new drug target for Kaposi's sarcoma

...s are structurally similar," Craik explained. "The inhibitor we found knocks out not only KS, but also the cyto...entified here could be a target for a broad-acting inhibitor against the entire viral family." To their know...researchers said, this is the first small-molecule inhibitor of a herpes virus protease to not only act outside...

Experimental treatment halts hypoxic-ischemic brain injury in newborns

...am examined the therapeutic effect of injecting PAI-1 into newborn rats suffering from the brain blood flow reduction and systemic hypoxia. The enzyme inhibitor was injected into the intracerebroventricular region of the brain, which includes a system of canals that distribute cerebrospinal fluid throughout th...

Building memories with actin

...ts phosphorylation and inactivation of cofilin, an inhibitor of actin filament assembly, the team found. Cofili...c-PAK pathways. The researchers showed that a ROCK inhibitor stalled actin polymerization and resulted in a sho... in LTP, however. The team discovered that the Rac inhibitor prolonged cells' vulnerability to a molecule that ...

Alzheimer's disease drug treats traumatic brain injury, report GUMC researchers

...ion 2009 International Conference on Alzheimer's Disease, the scientists will show that deactivating these pathways in part by using a gamma secretase inhibitor - a class of Alzheimer's disease drugs currently being tested - reduced loss of neurons in animal models of traumatic brain injury and protected the a...

Pitt team finds molecule that regulates heart size by using zebrafish screening model

... PITTSBURGH, July 5 Using zebrafish, researchers at the University of Pittsburgh have identified and described an enzyme inhibitor that allows them to increase the number of cardiac progenitor cells and therefore influence the size of the developing heart. The findings are describ...

Axel Ullrich named winner of 2009 Dr. Paul Janssen Award for Biomedical Research

...rowth factor receptor or VEGFR) suppresses the generation of blood vessels in tumors and slows down cancer cell growth. Years later, a small molecule inhibitor of the VEGFR2 kinase function was developed, from which a derivative was approved in 2006 for the treatment of kidney carcinoma and gastro-intestinal ...

Powe Award supports research on how enzymes enable the pathogenicity of 2 human disease organisms

...ns, we can perhaps identify inhibitors that can be developed as antibiotics or antifungal agents," he said. "Since humans do not have siderophores, an inhibitor should not be toxic to us." Using modern biology techniques, Sobrado's group is the first in the world to obtain recombinant functional siderophore...

Huntington's disease deciphered

...egan looking for a mechanism that could explain all the pieces of the puzzle. They found that at extremely low concentrations, huntingtin was a potent inhibitor of axonal transport, the system within the neuron that shuttles proteins from the cell body where they are synthesized to the synaptic terminals where...

Universitat Autonoma de Barcelona researchers first to clone mice in Spain

...pproximately 1% for mice using standard procedures. Valproic acid is an inhibitor of the enzyme histone deacetylase, located at the cell nucleus where the DN...t used two years ago and research until now has focused on trichostatin, an inhibitor which has significantly improved the efficiency of mouse cloning, raising i...

American Society for Microbiology honors Deborah T. Hung

...ng chemical genetics and small molecular screening to dissect essential steps in pathogenesis. She published her findingsa new small molecule inhibitor of Vibrio cholerae virulence and intestinal colonization, virstatin, which directly inhibited dimerization of the virulence transcriptional activator ...

The challenges of avian influenza virus: Mechanism, epidemiology and control

...etween the sequence conservation and the atomic structure. This provides the basis for identifying structurally and functionally important regions for inhibitor design. Crystal structures of some parts of the polymerase complex, PA alone or PA with part of PB1, have been solved. Zihe RAO, Yingfang LIU and coll...

Clinical trials for shingles drug take an important step forward

...mistry Chris McGuigan, who led the team which discovered the anti-viral drug said: "We believe this drug has the potential to be the most powerful inhibitor ever discovered to treat shingles. "Each year only 25 new medicines are approved for clinical use [worldwide or by the FDA]. Although FV-100 is ...

KINAXOs Cellular Target Profiling reveals mTOR as a new target of Celebrex

... identify the protein kinase mTOR as a new cellular target of celecoxib (Celebrex®, Pfizer). Celecoxib is a non-steroidal, anti-inflammatory Cox-2 inhibitor approved for the treatment of osteoarthritis, rheumatoid arthritis and acute pain. In addition, celecoxib’s anti-proliferative effect has earned...

A longer lasting tumor blocker

...similar to other recent reports, the tumors bounced back when the drug treatment was curtailed. Tumor growth in mice on a similar regiment of an M-CSF inhibitor remained suppressed in the absence of drug. Another distinction between the two inhibitors was the type of vessel growth that was blocked. Blocking...

Joining forces to improve lung cancer treatment

...r (Poland) Confirmation that EGFR mutations (deletion in exon 19, missense L858R) are the most important predictors of sensitivity to tyrosine-kinase inhibitor targeted therapies (Italy) Barbara Zolty from the World Health Organization (WHO) will also highlight the importance of preventing lung cancer as ...

Newly discovered epidermal growth factor receptor active in human pancreatic cancers

...s to be activated in a subset of lung cancers. And, most promising, an EGFR inhibitor named erlotinib already has been through the long and complex Food and Drug...es, they found that the only case in 12 cases that had responded to the EGF inhibitor was the only case with an activated EGF receptor. Dr. Pandey would like to ...

Burnham researchers present at 100th AACR Meeting

...present two papers: Cyclosporin A Sensitizes Cancer Cells to Death Receptor-Mediated Apoptosis and Chemical Biology Strategy Reveals Pathway-Selective inhibitor of NFκB Activation Induced by Protein Kinase C and Antigen Receptors. Changming Fang, Ph.D., who will also present two papers: Ileal Bile Acid B...

Laughter remains good medicine

...roup C (control) and Group L (laughter). Both groups were started on standard medications for diabetes (glipizide, TZD, metformin), hypertension (ACE inhibitor or ARB)) and hyperlipidemia (statins). The researchers followed both groups for 12 months, testing their blood for the stress hormones epinephrine and...

Laughter remains good medicine

...roup C (control) and Group L (laughter). Both groups were started on standard medications for diabetes (glipizide, TZD, metformin), hypertension (ACE inhibitor or ARB)) and hyperlipidemia (statins). The researchers followed both groups for 12 months, testing their blood for the stress hormones epinephrine and...

Team identifies a molecular switch linking infectious disease and depression

...ice exposed to BCG exhibited typical sickness behavior (low appetite, reduced activity), from which they soon recovered. But pretreatment with the IDO inhibitor eliminated the subsequent development of depressive-like behavior. Mice that had the IDO gene deleted were also completely resistant to the depressive...

New high-throughput screening technique makes probing puzzling proteins possible

... polarization, causing fluorescence polarization values to climb. If an inhibitor binds efficiently with a given protein, it can outcompete a probe, slowing ...pounds in search of those that might inhibit RBBP9. They identified some 20 inhibitor compounds that bound effectively with the enzyme, and further ABPP studies ...

UC Davis bench-to-bedside research: Promising treatment in clinical trials

...sion. Each patient will receive 28 days of treatment. The AR9281 enzyme inhibitor will be studied for safety, tolerability, reduction of blood pressure and v...e officer of Arte Therapeutics. "This is the first clinical study of a s-EH inhibitor in patients, and the first study designed to establish proof of concept tha...

Protein is key to embryonic stem cell differentiation

...s in hESCs reduce Shp2 expression and subsequent cell differentiation. Feng and colleagues screened chemical libraries and identified a small-molecule inhibitor of Shp2 that, in small doses, partially inhibits differentiation in both mESCs and hESCs. Taken together, these results suggest a conserved role for S...

Alzheimer's disease therapeutic prevents long-term damage from TBI in pre-clinical studies

... to amyloid peptide as a cause of this continuing damage." The study using DAPT then proved that in mice able to produce amyloid, a gamma secretase inhibitor reduced amyloid peptide production, and significantly improved learning, Burns says. "This is an exciting finding that we hope can be readily tested ...

New potential therapeutic target discovered for genetic disorder -- Barth syndrome

...of Sciences , shows the benefits of targeted intervention with an iPLA2-VIA inhibitor that prevents a major symptom of the disease- cardiolipin deficiency. "...nt of BTHS patients lymphoblasts within a tissue culture with the iPLA2-VIA inhibitor BEL partially restored the tissue cultures cardiolipin homeostasis. "Ta...

Lowering your cholesterol may decrease your risk of cancer

...A Current research suggests that lowering cholesterol may block the growth of prostate tumors. The related report by Solomon et al, "Ezetimibe Is an inhibitor of Tumor Angiogenesis," appears in the March 2009 issue of The American Journal of Pathology . High cholesterol not only leads to atherosclerosis ...
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