#New drug-like compounds may improve odds of men battling prostate cancer, researchers find Researchers at Southern Methodist University,
Dallas, have discovered three new drug-like compounds that could ultimately offer better odds of survival to prostate cancer patients.
The drug-like compounds can be modified and developed into medicines that target a protein in the human body that is responsible for chemotherapy resistance in cancers,
So far there's no approved drug on the market that reverses cancer chemotherapy resistance caused by P-glycoprotein
One potential drug, Tariquidar, is currently in clinical trials, but in the past, other potential drugs have failed at that stage."
"The problem when a person has cancer is that the treatment itself is composed of cellular toxins--the chemotherapeutics that prevent the cells from dividing.
who is director of SMU's Center for Drug Discovery, Design, and Delivery.""Sometimes, however, the cancer returns,"she said."
"As a result, P-gp causes resistance of the diseased cells to a majority of drugs currently available for the treatment of cancer,
as well as drugs used for treatment of infectious diseases like HIV/AIDS. Using computer-generated model speeds up the drug discovery process The new drug-like compounds discovered by Vogel
and her co-authors offer hope that using a computer-generated P-gp model, explained here http://bit. ly/1lvmr7a,
chemical and biological functions of the protein in the human body, will speed up the drug discovery process
so that's a pretty good predictor that they may be good candidates for drug development. But we need to do much more work."
so it can eventually be delivered to patients as a therapeutic drug. In the case reported here,
The timeline from drug discovery to development to clinical trials and approval can take a decade or more.
Researchers virtually screened 15 million drug-like compounds via SMU supercomputer The SMU researchers discovered the three hit compounds after virtually screening more than 15 million small drug-like compounds made publically available
including interactions with drug-like compounds while taking on different shapes. The ultra-high throughput computational searches by Maneframe led the researchers to 300 compounds that looked like they may inhibit P-gp.
Also, each was tested on a companion cell line already multi-drug resistant, as if the patient already had undergone chemotherapy using Paclitaxel.
"said Joseph Falkinham, a professor of microbiology in the College of Science and an affiliate of the Virginia Tech Center for Drug Discovery."
who is also an affiliate of the Virginia Tech Center for Drug Discovery. In both the U s. and Europe, the spread of MRSA is a major threat to people in hospitals and other health care facilities.
it is possible that EVLP could be used to deliver drugs before the lung is implanted so that the patient's immune system does not recognise the transplanted organ as harmful."
and provides a fresh perspective on the etiology of Alzheimer's disease that could inform novel drug strategies,
so this opens up a brand new pathway to pursue in developing drugs to block the disease,"Dr. Richards,
The research team discovered a new gene involved in muscle wasting that could be a good target for drug development.
a leading journal in the field of developmental biology, open up new avenues for design of drugs for ataxia, a motor coordination disorder.
a journal in the field of developmental biology, open up new avenues for design of drugs for ataxia, a motor coordination disorder.
This enzyme activates a harmless drug precursor called CB 1954, which the researchers added to the petri dish where the cells were growing.
#Silicone vaginal rings deliver antiviral drugs, protect women against HIV Researchers at University Jean Monnet of Saint-Etienne,
which allowed the drugs to be released from their reservoirs. Vaginal rings with multiple reservoirs present a promising way for preventing sexually transmitted infections (STIS) and notably HIV infection in young women with high risk of exposure.
Some of the rings presented in this study were shown to release concentrations of drugs between 1. 5 and 3. 5 mg/day for acyclovir and 3 to 5 mg/day for tenofovir for as long as 50 days,
"Massachusetts institute of technology Professor Robert Langer, a leader in targeted drug delivery research who was connected not to the Stanford experiments,
"Targeted drug delivery is one of the ultimate goals of medicine because it seeks to focus remedies on diseased cells,
The discovery provides a new platform for drug delivery systems and an entirely different view of cellular functions.
Chilkoti's lab has designed self-assembling proteins for drug delivery systems for several years. Simply by adding heat
and when drugs are released inside the body through non-temperature-related mechanisms such as changes in acidity levels.
however, drugs could be encapsulated in protein cages that accumulate inside of a tumor and dissolve once heated.
Not only would this provide a more accurate way of delivering drugs, but the cages themselves could be used therapeutically."
#Two-drug combination shows promise against one type of pancreatic cancer One form of pancreatic cancer has a new enemy:
a two-drug combination discovered by UF Health researchers that inhibits tumors and kills cancer cells in mouse models.
They also found that pairing a synthetic compound with an existing drug provides a more effective anticancer punch than a single drug.
we looking for drug combinations that would increase efficacy, "he said. Among the substances they tested was a synthetic, small-molecule compound known as PF-04554787.
It did, with the two-drug combination killing off pancreatic cancer cells more effectively than everolimus alone.
In testing on two mouse cell lines, the drug combination reduced the viability of cancer cells by about 50 percent
That an existing drug can be made more effective is especially encouraging because the synthetic compound that was paired with everolimus is already undergoing human clinical trials,
"This is important because we're focused on everolimus, a drug that is already approved, nontoxic and given to patients.
Next, researchers would like to study how the two-drug approach works in humans, although no clinical trials have yet been designed or scheduled h
and suggest new drugs to track down and disable its deadly seeds. For the most part, modern cancer drugs ignore differences between primary
Insights could lead to targeted therapies The research team performed a proof of principle experiment to demonstrate how valuable information about metastatic gene expression could be for drug development.
a CDK inhibiting drug known to kill off cells with high MYC levels. Whereas 44 percent of control mice (11 of 25) developed secondary tumors within four weeks, researchers could only find metastatic cells in one drug-treated mouse (4 percent.
Werb emphasized that this test was just a proof of principal and that dinaciclib itself may
or may not prove be the ideal drug to target metastases. The key point, she said,
was that the drug managed to nearly eliminate metastases without shrinking the primary tumor.""If this drug had only been tested on primary tumors,
we would have said it doesn't work, "she said.""This tells us you actually have to look at metastases
Customizable viruses The Food and Drug Administration has approved a handful of bacteriophages for treating food products,
a drug that inhibits the action of tyrosine kinases--enzymes that function as an"on
"Although treatment with VEGFR-targeted drugs has been very effective in the first line of therapy for patients with advanced kidney cancer,
in many cases tumour cells find ways to escape control by these drugs. Cabozantinib is a new drug that targets possible escape mechanisms of tumour cells,
including the tyrosine kinases MET, VEGFR and AXL. The results of the METEOR trial indicate that cabozantinib is able to shrink tumours
and slow down tumour growth much better than current standard treatment in patients who previously received VEGFR-targeted drugs.
The incidence of serious side effects was similar for both drugs and discontinuation of treatment due to side effects occurred in 9. 1%of cabozantinib and 10%of everolimus patients.
In the USA, the Food and Drug Administration (FDA) has designated it as a breakthrough therapy,
which may allow expedited development of the drug. Professor Peter Naredi, the ECCO scientific co-chair of the Congress,
the most serious being BCG infections that need to be treated with antituberculous drugs. A study on the characteristics of a wide group of mycobacteria begun seven years ago by the Mycobacteria Research Group
which can be used to design new personalized drug regimens for SS patients based on their unique genetic makeup.
In preliminary drug-mutation matching studies they found that JAK1-mutated SS cells were sensitive to JAK inhibitors,
drugs that are approved currently for treatment of other hematologic cancers such as polycythemia vera and myelofibrosis."
"We knew nano diamonds were of interest for delivering drugs during chemotherapy because they are largely nontoxic and non-reactive,
The finding could be used to develop new drugs to treat cancers such as leukaemia, caused by malfunctioning of the Trib1 protein.
which will provide critical clues for developing drugs that target Trib1 to treat cancers.""Lead investigator Dr Mace said Trib1 acted as a scaffold to bring many proteins together,
Scientists at the University of Nebraska Medical center designed a new delivery system for these drugs that,
when coupled with a drug developed at the University of Rochester School of medicine and Dentistry, rid immune cells of HIV and kept the virus in check for long periods.
Nebraska researcher Howard E. Gendelman designed the investigational drug delivery system-a so-called"nanoformulated"protease inhibitor.
The nanoformulation process takes a drug and makes it into a crystal, like an ice cube does to water.
Next, the crystal drug is placed into a fat and protein coat, similar to what is done in making a coated ice-cream bar.
The coating protects the drug from being degraded by the liver and removed by the kidney.
a new drug discovered in the laboratory of UR scientist Harris A.("Handy")Gelbard M d.,Ph d,
URMC-099 boosted the concentration of the nanoformulated drug in immune cells and slowed the rate at
"The chemical marriage between URMC-099 and antiretroviral drug nanoformulations could increase drug longevity, improve patient compliance,
whether the drugs could be administered safely together. Much to Gelbard and Gendelman's surprise, URMC-099 increased the effectiveness of the nanoformulated drug."
"Our ultimate hope is that we're able to create a therapy that could be given much less frequently than the daily therapy that is required today,
"If a drug could be given once every six months or longer that would greatly increase compliance,
electrical devices (pacemakers or defibrillators) or drugs (eg beta blockers. However, these methods are relatively crude: they can stop
and Ear/Harvard Medical school and Boston University have shown successfully neuroprotection in a Parkinson's mouse model using new techniques to deliver drugs across the naturally impenetrable blood-brain barrier.
lend hope to patients around the world with neurological conditions that are difficult to treat due to a barrier mechanism that prevents approximately 98 percent of drugs from reaching the brain and central nervous system."
"We are developing a platform that may eventually be used to deliver a variety of drugs to the brain,
and histological data capture that their delivery method was equivalent to direct injection of GDNF--the current gold standard for delivering this drug in Parkinson's disease despite its traumatic nature and high complication rates--in diffusing drugs to the brain.
Dr. Bleier saw an opportunity to apply these techniques to the widespread clinical dilemma of delivering drugs across the barrier to the brain and central nervous system.
surgeons may create a"screen door"to allow for drug delivery to the brain and central nervous system. The technique has the potential to benefit a large population of patients with neurodegenerative disorders,
Currently, no durable, long-term right ventricular assist device (RVAD) has received Food and Drug Administration approval,
San diego researchers developed a new computational strategy to search for molecules that could be developed into glioblastoma drugs.
"Most drugs target stable pockets within proteins, so when we started out, people thought it would be impossible to inhibit the transient interface between two transcription factors,
and created a new strategy for drug design--one that we expect many other researchers will immediately begin implementing in the development of drugs that target similar proteins, for the treatment of a variety of diseases."
The most effective of these candidate drug molecules, called SKOG102, shrank human glioblastoma tumors grown in mouse models by an average of 50 percent."
the cells were barely able to take up any of the anticancer drugs.""For a long time, there has indeed been a hypothesis that VRAC plays a decisive role in apoptosis
and cellular resistance to Pt-based anticancer drugs,"has appeared just in the EMBO Journal r
which, Martin notes, has already been approved FDA for drug-delivery applications. They then apply ultralow magnetic fields to individual sections of the composite material--the ceramic fibers immersed in liquid plastic--to align the fibers according to the exacting specifications dictated by the product they are printing."
providing the basic building blocks for other researchers to perform experiments on tissue regeneration and/or for drug screening studies."
#Simple Test Makes Blood-clot-busting Drug Safer Scientists in China have developed a fluorescent probe to detect both heparin and its major contaminant.
but can lead to severe adverse reactions. 150 deaths between 2004 and 2008 in the US were thought to be a result of drug manufacturers deliberately cutting heparin with OSCS to save money.
a key malaria-drug ingredient that was derived previously from trees (see Reuters story of August 12, 2014, http://reut. rs/1j2ovkj).
The finding is also significant as currently there is no drug available to prevent the recurrence of tumours in the intestine after the cancerous tumours have been removed by surgery.
since Imatinib is a potentially novel drug for the treatment of tumour formation and cancer progression in patients predisposed to develop colorectal cancer,
#Unusual Chance to Study Patient's Residual Tumor Leads to New Finding Capitalizing on a rare opportunity to thoroughly analyze a tumor from a lung cancer patient who had developed resistance to targeted drug treatment,
In experiments that combined the drug the patient had taken with a second compound that blocks off this newly discovered resistance pathway,
the researchers were able to durably wipe out cancer cells in mice implanted with cells from the drug-resistant tumor. ven in cancers that are responding to targeted therapy by conventional criteria,
As many as 30 percent of patients exhibit so-called primary resistance to EGFR inhibitors, in which the drugs have no detectable effect.
which drug-resistant cells that survive treatment form residual, often lethal, tumors. Understanding the biological basis of acquired resistance has proved difficult,
leaving scientists with few drug-resistant tumors to use in research. But as described in the online edition of Cell Reports on Thursday, April 2, 2015,
or any other mutations known to confer drug resistance. These results suggested that the cells were still potentially susceptible to erlotinib,
The drug effectively inhibited EGFR activity, but the researchers also observed a rapid, 10-fold increase in the activity of a pathway known as NF-KAPPA-B,
An experimental drug known as PBS-1086 directly targets the NF-KAPPA-B pathway, and when the researchers coupled this drug with erlotinib,
the implanted tumors shrank significantly, suggesting that combining a compound like PBS-1086 with erlotinib at the outset of therapy may help to prevent acquired drug resistance in EGFR-mutant NSCLC.
Combined drug regimens designed to overcome drug resistance at the outset of therapy are now the norm in treating certain forms of melanoma,
said Bivona, and he believes PBS-1086 as a shotto play a similar role in NSCLC. he NF-KAPPA-B pathway is engaged by cells in response to EGFR inhibitors as a way to survive treatment,
if we block that pathway with a novel drug while simultaneously administering the EGFR inhibitor,
In lung cancer patients treated with these drugs, and that a substantial number of patients, this could be a very powerful companion therapy to minimize
and how it relates to disease or response to drug therapies. Gersbach added, ot only can you start to answer those questions,
and the Whitehead Institute have discovered a vulnerability of brain cancer cells that could be exploited to develop more-effective drugs against brain tumors.
who are now seeking potential drug compounds that could do just that t
#In first human study, new antibody therapy shows promise in suppressing HIV infection In the first results to emerge from HIV patient trials of a new generation of so-called broadly neutralizing antibodies,
which serve as viral reservoirs inaccessible to current antiretroviral drugs. Most likely 3bnc117, like other anti-retrovirals,
however by the Food and Drug Administration for the treatment of recurrent glioblastomas r
#Brain imaging Explains Reason For good and Poor Language Outcomes in ASD Toddlers Using functional magnetic resonance imaging (fmri), University of California,
Moreover, tumors contain a small portion of cancer stem cells that are believed to be responsible for tumor initiation, metastasis and drug resistance.
but there are no drugs available that specifically attack cancer stem cells. A Surprising Discovery Now a research team led by investigators at Harvard Medical school and the Cancer Center at Beth Israel Deaconess Medical center
A Different Approach Until now, agents that inhibit Pin1 have been developed mainly through rational drug design. Although these inhibitors have proven active against Pin1 in the test tube
200 chemical compounds, including both approved drugs and other known bioactive compounds. To increase screening success,
such as nutrient intake, efflux of waste or drug, and cell signaling, for instance, between nerve cells in the brain and spinal cord. o our knowledge, this is the first transport protein designed from scratch that is,
They also added two other drugs that temporarily inhibited key biochemical pathways associated with the pluripotent state of the stem cells.
or for transporting lethal drugs into the cancer cells. Since the protein is not found in all of the cells of our body,
including biodegradable plastics, pharmaceutical drugs and even liquid fuels. Scientists with the U s. Department of energy (DOE) Lawrence Berkeley National Laboratory (Berkeley Lab) and the University of California (UC) Berkeley have created a hybrid system of semiconducting nanowires and bacteria that mimics
a fuel comparable to gasoline, 25-percent for amorphadiene, a precursor to the antimaleria drug artemisinin,
is the creation of drugs to turn white fat into brown fat through brown fat recruitment. f you think about obesity,
#An electronic micropump to deliver treatments deep within the brain Many potentially efficient drugs have been created to treat neurological disorders,
Drugs constitute the most widely used approach for treating brain disorders. However, many promising drugs failed during clinical testing for several reasons:
they are diluted in potentially toxic solutions, they may themselves be toxic when they reach organs to which they were directed not initially, the blood-brain barrier,
drugs that succeed in penetrating the brain will act in a nonspecific manner, i e. on healthy regions of the brain, altering their functions.
which many drugs could not be commercialised because of their harmful effects, when they might have been effective for treating patients resistant to conventional treatments 1. During an epileptic seizure,
whether these are ions or drugs. When an electrical current is applied to it the flow of electrons generated projects the molecules of interest toward the target area.
in order to activate the pump to inject the drug at just the right moment. It may therefore be possible to control brain activity where
this state-of-the-art technology, combined with existing drugs, offers new opportunities for many brain diseases that remain difficult to treat at this time a
A New Direction for Drug Research The startling discovery of TMPRSS2 role in triggering cancer pain may lead to the creation of targeted cancer pain therapies that effectively shut down the expression of this gene
Inhibition of its activity in patients might provide a new form of treatment for cancer pain. ny cancer that is painful before initiating drug treatment we can label the cancer cells for TMPRSS2
#Researchers'"hugely exciting"asthma discovery Cardiff scientists have identified for the first time the potential root cause of asthma and an existing drug that offers a new treatment.
Crucially, the paper highlights the effectiveness of a class of drugs known as calcilytics in manipulating Casr to reverse all symptoms associated with the condition.
Professor Riccardi and her collaborators are now seeking funding to determine the efficacy of calcilytic drugs in treating asthmas that are especially difficult to treat,
and to test these drugs in patients with asthma. Calcilytics were developed first for the treatment of osteoporosis around 15 years ago with the aim of strengthening deteriorating bone by targeting Casr to induce the release of an anabolic hormone.
But this latest breakthrough has provided researchers with the unique opportunity to re-purpose these drugs,
the group aim to be trialling the drugs on humans within two years. f we can prove that calcilytics are administered safe
Antiretroviral drugs can slow the spread of the virus, but it remains hidden dormant in cells and returns when the treatments cease.
The antiparasitic drug ivermectin, or IVM, can be used to treat these diseases, but mass public health campaigns to administer the medication have been stalled because of potentially fatal side effects for patients co-infected with Loa loa,
The achievement was made possible by a new generation of drug-containing coating applied to the inner surface of the vessel.
The lifetime of such grafts is determined often by the amount of drug stored within the graft
The system, developed by the researchers, is based on the entrapment of the drug inside a porous protective shell,
You just need to take the right kind of drug. For example, after the implantation of an artificial ureter, urease crystals often start to grow inside
It is possible to apply a similar drug-containing coating that dissolves urease. The same approach may be used for kidney or liver surgery
or replacement genes or drugs inside a man-made biodegradable nanoparticle rapperthat patients inhale could penetrate the mucus barrier
patients would experience fewer side effects common to drugs that must be taken regularly over long stretches of time.
Most of the existing drugs for CF help clear infections but do not solve the disease underlying problems.
A couple of recently approved drugs designed to target the underlying cause of CF require daily treatment for the entire lifetime
and explore potential drug targets to help cancer patients p
#How chronic inflammation can lead to cancer Chronic inflammation caused by disease or exposure to dangerous chemicals has long been linked to cancer,
Yount lab has begun using experimental drugs to test this flu prevention strategy in mice. Any possibility for human use is still many years away,
and plans to continue his research in the quickly expanding field. hereas traditional pharmaceutical drugs have a transient effect,
members of a family of painkilling drugs sourced from the opium poppy. It can take more than a year to produce a batch of medicine, starting from the farms in Australia,
where the active drug molecules are extracted and refined into medicines. hen we started work a decade ago,
The materials that pharmaceutical companies use to test drugseffects on cells don allow for three-dimensional vascularization, a network of capillaries that carry drugs and other materials throughout the body.
but also aid in drug screening. he microenvironment actually has a significant effect on how the cells respond to a drug,
Grolman said. hese companies might have the next big drug, but they might not know it. he long-term vision would be:
whether they be targeted drug delivery, electrical stimulation or even light-plus-optogenetics through fiber optics, will all be closed loop.
and Emory University to clamp firing at normal levels during the addition of a drug that inhibits neurotransmission.
They could be used for therapeutic drug screening and to help teach researchers how to grow whole human organs.
and building a model of their tissue to use as a personalized drug screening platform.
#New method for modifying natural polymers could help bring lifesaving medications to market In drug-delivery research,
the drug must also be able to safely reach its target. Xiangtao Meng, a fourth-year graduate student in the College of Natural resources and Environment, has developed a new technique to make that easier.
a natural polymer often used for drug delivery. According to Kevin Edgar, a professor of sustainable biomaterials and Meng doctoral adviser, the new method an get drugs to market,
and to patients, that would otherwise fail. Taking medications orally is typically much more practical for patients than methods like intravenous injections
but the bioavailability of a drug the amount that actually reaches the bloodstream often suffers.
a drug taken orally must dissolve in the digestive tract. But many pharmaceutically active compounds tend to crystallize,
That means that patients have to ingest more of a drug to get the therapeutic dose increasing the cost, risk of side effects,
Suspending the drug in a polymer matrix can help. Polymers are long chains of repeating units.
Dispersing a drug in a polymer matrix protects it and suppresses the formation of insoluble crystals.
and releases the drug, allowing it to be absorbed into the bloodstream. Because medications have broadly diverse chemical structures, properties,
finding the right polymer matrix to work well with most drugs involves making and testing many different options.
Cellulose is an attractive material for drug delivery because it nontoxic breaks down into components that are already present in the body,
limiting the number of options for drug delivery. Meng decided to investigate whether he could modify cellulose using a technique called olefin cross-metathesis,
and could be used to make a huge array of potential drug-delivery matrices, but it had never been applied to cellulose.
which he sends to collaborators in a drug-delivery group at Purdue University. The team is currently targeting HIV drugs,
which have notoriously poor solubility. Meng, an ICTAS doctoral scholar from Shandong Province, China, is now working on incorporating another type of chemical reaction that will allow even more versatility like rowing apples and peaches on the same tree,
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