Timely delivery: Ribonucleoside 3'-phosphates as pro-moieties for an orally administered drug

Aug 06, 2012
Timely delivery: Ribonucleoside 3'-phosphates as pro-moieties for an orally administered drug

(Phys.org) -- 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 .

Explore further: New technique reveals immune cell motion through variety of tissues

More information: Ronald T. Raines, Ribonucleoside 3'-Phosphates as Pro-Moieties for an Orally Administered Drug, ChemMedChem 2012, 7, No. 8, dx.doi.org/10.1002/cmdc.201200243

add to favorites email to friend print save as pdf

Related Stories

Researchers make neurological disease breakthrough

Oct 07, 2011

(Medical Xpress) -- Results of a study by a group of University of Notre Dame researchers represent a promising step on the road to developing new drugs for a variety of neurological diseases.

Research team gives drug dropouts a second chance

May 07, 2012

(Phys.org) -- A cross-disciplinary team of researchers at the University of Maryland has designed a molecular container that can hold drug molecules and increase their solubility, in one case up to nearly ...

Recommended for you

'Global positioning' for molecules

Dec 19, 2014

In everyday life, the global positioning system (GPS) can be employed to reliably determine the momentary location of one en route to the desired destination. Scientists from the Institute of Physical and ...

Cells build 'cupboards' to store metals

Dec 17, 2014

Lawrence Livermore researchers in conjunction with collaborators at University of California (link is external), Los Angeles have found that some cells build intracellular compartments that allow the cell ...

User comments : 0

Please sign in to add a comment. Registration is free, and takes less than a minute. Read more

Click here to reset your password.
Sign in to get notified via email when new comments are made.