Highlights in Chemical Biology

Chemical biology news from across RSC Publishing.



Predicting drug response


27 August 2010

Scientists in China have developed a probe that could be used to test how well a patient will respond to certain drug treatments. 

The new probe measures the activity of N-acetyltransferase 2 (NAT2), an enzyme that metabolises drugs and other toxins containing aryl amines and hydrazines. The activity of NAT2 differs between individuals, which affects how well a drug will work, and dysfunction of the enzyme has been linked to breast cancer, Parkinson's and other diseases. A simple measure of NAT2 activity could help ensure patients are given drugs that they can metabolise effectively with minimal side effects. 

Xuhong Qian and colleagues at the East China University of Science and Technology in Shanghai found that the fluorescent molecule amonafide is metabolised specifically by NAT2. The enzyme acetylates the probe molecule, shifting its flourescence wavelength. Hence, this fluorescence change correlates to NAT2 activity. Current methods for predicting patient response to certain drugs require complex genetic analysis, but this probe could provide a simple and sensitive test. 

Amonafide and NAT2 reaction scheme

Acetylation by NAT2 changes the fluorescence wavelength of amonafide

AP de Silva, an expert in fluorescent sensors at Queen's University Belfast, UK, admires the team's use of fluorescence in two colours to monitor an intracellular enzyme. He adds 'this work is likely to attract favourable attention.' 

'The probe has significant potential applications in personal medicine,' Qian says. 'We also hope that it can be used to study the mechanism of different kinds of diseases related to NAT2.' The team now intends to design probes for other important enzymes. 

Harriet Brewerton 

 

Enjoy this story? Spread the word using the 'tools' menu on the left or add a comment to the Chemistry World blog. 

Link to journal article

Selective and sensitive detection and quantification of arylamine N-acetyltransferase 2 by a ratiometric fluorescence probe
Lei Cui, Ye Zhong, Weiping Zhu, Yufang Xu and Xuhong Qian, Chem. Commun., 2010, 46, 7121
DOI: 10.1039/c0cc01000f

Also of interest

Medicine made to measure

Healthcare tailored to suit the genetic makeup of the patient is finally coming to fruition, as Anna Lewcock reports

Smart drug delivery via thermo-triggered squirting

Chinese researchers have developed a method for delivering nanoparticles to a specific site of action using temperature-triggered squirting