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: Four billion-year-old chemistry in cells today

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

A new approach to creating organic zeolites

Jul 24, 2014

Yushan Yan, Distinguished Professor of Engineering at the University of Delaware, is known worldwide for using nanomaterials to solve problems in energy engineering, environmental sustainability and electronics.

User comments : 0