Studying Noncovalent Small Molecule Interactions with Protein and RNA Targets by Mass Spectrometry

Abstract

Developing methods for elucidating the mechanism of action of drugs and inhibitors on a structural level is an active area of biomedical and pharmaceutical research. To develop new therapies at an increasing pace, more new drugs need to be synthesized or discovered, more novel macromolecular targets need to be identified, and compounds need to be characterized, screened and evaluated at a faster rate. Advances and application of combinatorial chemistry address the need for more compounds [1, 2], whereas research endeavors such as genomics [3] and proteomics [4, 5] have shown great potential for uncovering novel targets. Methods for high-throughput screening using a variety of large-scale automated processes and robotics have been developed to further address some of these important needs [6]. However, biophysical techniques are still needed to fully elucidate the fundamental aspects of inhibitor action on its target.