Many drug candidates fail because of low solubility or poor pharmacokinetic behavior. Ron Raines and colleagues at the University of Wisconsin–Madison (USA) have devised a new prodrug strategy to overcome these limitations.
Their approach takes advantage of the capacity of an enzyme prevalent in human serum–pancreatic-type ribonuclease—to catalyze the cleavage of a drug conjugated to a ribonucleoside 3'-phosphate; the results of their work are reported in ChemMedChem.
They demonstrated efficacy by using metronidazole, a sparingly soluble antibiotic that is often administered orally. In the absence of ribonuclease, metronidazole conjugates are stable and inactive. Physiological levels of enzyme render the conjugate toxic to Bacteroides fragilis, a common penicillin-resistant bacillus that is responsible for anaerobic infections.
Alterations to the ribonucleoside enable modulation of key attributes, such as the rate of drug delivery. This study paves the way for further research into the activation and timed release of drugs of varying aqueous solubility.About the Author
ChemMedChem 2012, 7, No. 8, Permalink to the article: http://dx.doi.org/10.1002/cmdc.201200243
Protein linked to cancer acts as a viscous glue in cell division
08.07.2020 | Rensselaer Polytechnic Institute
Enzymes as double agents: new mechanism discovered in protein modification
08.07.2020 | Westfälische Wilhelms-Universität Münster
Kiel physics team observed extremely fast electronic changes in real time in a special material class
In physics, they are currently the subject of intensive research; in electronics, they could enable completely new functions. So-called topological materials...
Solar cells based on perovskite compounds could soon make electricity generation from sunlight even more efficient and cheaper. The laboratory efficiency of these perovskite solar cells already exceeds that of the well-known silicon solar cells. An international team led by Stefan Weber from the Max Planck Institute for Polymer Research (MPI-P) in Mainz has found microscopic structures in perovskite crystals that can guide the charge transport in the solar cell. Clever alignment of these "electron highways" could make perovskite solar cells even more powerful.
Solar cells convert sunlight into electricity. During this process, the electrons of the material inside the cell absorb the energy of the light....
Empa researchers have succeeded in applying aerogels to microelectronics: Aerogels based on cellulose nanofibers can effectively shield electromagnetic radiation over a wide frequency range – and they are unrivalled in terms of weight.
Electric motors and electronic devices generate electromagnetic fields that sometimes have to be shielded in order not to affect neighboring electronic...
A promising operating mode for the plasma of a future power plant has been developed at the ASDEX Upgrade fusion device at Max Planck Institute for Plasma...
Live event – July 1, 2020 - 11:00 to 11:45 (CET)
"Automation in Aerospace Industry @ Fraunhofer IFAM"
The Fraunhofer Institute for Manufacturing Technology and Advanced Materials IFAM l Stade is presenting its forward-looking R&D portfolio for the first time at...
07.07.2020 | Event News
02.07.2020 | Event News
19.05.2020 | Event News
08.07.2020 | Physics and Astronomy
08.07.2020 | Agricultural and Forestry Science
08.07.2020 | Materials Sciences