Researchers discovered that simple modifications to the drug furamidine have a major impact on its ability to affect specific human proteins involved in the on-off switches of certain genes.
“This was rather unexpected, given how relatively simple the molecules are that we modified and how difficult it has been to affect these proteins,” said Gregory Poon, pharmaceutical scientist at Washington State University.
The proteins – known as transcription factors – regulate the expression of genes in a highly coordinated and intricate manner, making them attractive targets for therapeutic drugs. But it has proven difficult to design drugs to affect them, Poon said.
“For this reason, they have been called undruggable,” he said. “Recently, however, scientists have been making headway in targeting these transcription factors with drugs, and now our results suggest this class of drugs can be a useful addition to the arsenal.”
Furamidine belongs to a family of drugs known as heterocyclic dications. The drug has a long history of use in serious parasitic diseases such as malaria, African sleeping sickness and PCP, a common infection in HIV/AIDS.
“There is tremendous knowledge and experience with using furamidine and related drugs in humans, so these drugs have an important advantage over other classes of drugs that are relatively behind in clinical experience,” Poon said.
Poon collaborated with researchers at Georgia State University. The team found that derivatives of furamidine can target a specific transcription factor known as PU.1.
Their findings were published in Nucleic Acids Research journal (http://nar.oxfordjournals.org/content/early/2013/10/23/nar.gkt955.full).
PU.1 is a major factor in development and function of the human immune system, and it plays important roles in diseases such as some leukemias, multiple sclerosis and diabetes. PU.1 is also a member of a large family of related transcription factors, known as ETS, that is involved in a broader range of cancers and other diseases.
“I am fortunate to be working with some of the best people in this area,” Poon said, referring to his collaborators, Dave Boykin and David Wilson of Georgia State University. “The challenge now is to fine-tune this class of drugs to make them as specific as possible to other ETS-family transcription factors as well.”
Their research is supported by the WSU College of Pharmacy and by the National Institutes of Health at Georgia State University.Contacts:
Gregory Poon | EurekAlert!
Bacteria as pacemaker for the intestine
22.11.2017 | Christian-Albrechts-Universität zu Kiel
Researchers identify how bacterium survives in oxygen-poor environments
22.11.2017 | Columbia University
The WHO reports an estimated 429,000 malaria deaths each year. The disease mostly affects tropical and subtropical regions and in particular the African continent. The Fraunhofer Institute for Silicate Research ISC teamed up with the Fraunhofer Institute for Molecular Biology and Applied Ecology IME and the Institute of Tropical Medicine at the University of Tübingen for a new test method to detect malaria parasites in blood. The idea of the research project “NanoFRET” is to develop a highly sensitive and reliable rapid diagnostic test so that patient treatment can begin as early as possible.
Malaria is caused by parasites transmitted by mosquito bite. The most dangerous form of malaria is malaria tropica. Left untreated, it is fatal in most cases....
The formation of stars in distant galaxies is still largely unexplored. For the first time, astron-omers at the University of Geneva have now been able to closely observe a star system six billion light-years away. In doing so, they are confirming earlier simulations made by the University of Zurich. One special effect is made possible by the multiple reflections of images that run through the cosmos like a snake.
Today, astronomers have a pretty accurate idea of how stars were formed in the recent cosmic past. But do these laws also apply to older galaxies? For around a...
Just because someone is smart and well-motivated doesn't mean he or she can learn the visual skills needed to excel at tasks like matching fingerprints, interpreting medical X-rays, keeping track of aircraft on radar displays or forensic face matching.
That is the implication of a new study which shows for the first time that there is a broad range of differences in people's visual ability and that these...
Computer Tomography (CT) is a standard procedure in hospitals, but so far, the technology has not been suitable for imaging extremely small objects. In PNAS, a team from the Technical University of Munich (TUM) describes a Nano-CT device that creates three-dimensional x-ray images at resolutions up to 100 nanometers. The first test application: Together with colleagues from the University of Kassel and Helmholtz-Zentrum Geesthacht the researchers analyzed the locomotory system of a velvet worm.
During a CT analysis, the object under investigation is x-rayed and a detector measures the respective amount of radiation absorbed from various angles....
The quantum world is fragile; error correction codes are needed to protect the information stored in a quantum object from the deteriorating effects of noise. Quantum physicists in Innsbruck have developed a protocol to pass quantum information between differently encoded building blocks of a future quantum computer, such as processors and memories. Scientists may use this protocol in the future to build a data bus for quantum computers. The researchers have published their work in the journal Nature Communications.
Future quantum computers will be able to solve problems where conventional computers fail today. We are still far away from any large-scale implementation,...
15.11.2017 | Event News
15.11.2017 | Event News
30.10.2017 | Event News
22.11.2017 | Business and Finance
22.11.2017 | Physics and Astronomy
22.11.2017 | Physics and Astronomy