The central nervous systems of humans and cattle alike are attacked by prions (abnormal insoluble amyloidogenic proteins) when they suffer from Creutzfeldt–Jakob disease (CJD) or bovine spongiform encephalopathy (BSE).
This causes a steady deterioration of neurological function and ultimately leads to death. There is no currently approved treatment for prion diseases, and no drug candidates are expected to enter clinical trials soon. In ChemMedChem, Maria Laura Bolognesi (University of Bologna, Italy) and colleagues argue in support of a multitarget drug discovery strategy as an alternative way to develop effective anti-prion agents.
Under the dominant drug discovery paradigm "one disease, one target, one molecule," which ignores the polyetiological nature of prion diseases and similar maladies, developing anti-prion therapies is a particular challenge; indeed, this paradigm could be a factor in the ongoing failure of current neurotherapeutic drugs. Bolognesi and colleagues now describe the discovery of rationally designed molecules endowed with various activities relevant for combating prion neurodegeneration.
A new series of chimeric molecules were generated by linking the antioxidant fragment of lipoic acid to heteroaromatic prion-recognition motifs. These compounds effectively counter both prion fibril formation and oxidative stress in a cell culture model of prion replication. The reported in vitro results make these compounds effective candidates for further in vivo investigations into their multiple biological properties against prion diseases.
Author: Maria Laura Bolognesi, Università di Bologna (Italy), http://www.unibo.it/docenti/marialaura.bolognesiTitle: Hybrid Lipoic Acid Derivatives to Attack Prion Disease on Multiple Fronts
Immune Defense Without Collateral Damage
23.01.2017 | Universität Basel
The interactome of infected neural cells reveals new therapeutic targets for Zika
23.01.2017 | D'Or Institute for Research and Education
For the first time ever, a cloud of ultra-cold atoms has been successfully created in space on board of a sounding rocket. The MAIUS mission demonstrates that quantum optical sensors can be operated even in harsh environments like space – a prerequi-site for finding answers to the most challenging questions of fundamental physics and an important innovation driver for everyday applications.
According to Albert Einstein's Equivalence Principle, all bodies are accelerated at the same rate by the Earth's gravity, regardless of their properties. This...
An important step towards a completely new experimental access to quantum physics has been made at University of Konstanz. The team of scientists headed by...
Yersiniae cause severe intestinal infections. Studies using Yersinia pseudotuberculosis as a model organism aim to elucidate the infection mechanisms of these...
Researchers from the University of Hamburg in Germany, in collaboration with colleagues from the University of Aarhus in Denmark, have synthesized a new superconducting material by growing a few layers of an antiferromagnetic transition-metal chalcogenide on a bismuth-based topological insulator, both being non-superconducting materials.
While superconductivity and magnetism are generally believed to be mutually exclusive, surprisingly, in this new material, superconducting correlations...
Laser-driving of semimetals allows creating novel quasiparticle states within condensed matter systems and switching between different states on ultrafast time scales
Studying properties of fundamental particles in condensed matter systems is a promising approach to quantum field theory. Quasiparticles offer the opportunity...
19.01.2017 | Event News
10.01.2017 | Event News
09.01.2017 | Event News
23.01.2017 | Health and Medicine
23.01.2017 | Physics and Astronomy
23.01.2017 | Process Engineering