Small Molecule - Research Tools

Research Tools

Enzymes and receptors are often activated or inhibited by endogenous protein, but can be also inhibited by endogenous or exogenous small molecule inhibitors or activators with can bind to the active site or on the allosteric site.

An example is the teratogen and carcinogen phorbol 12-myristate 13-acetate which is a plant terpene which activates protein kinase C promoting cancer, making it a very useful investigative tool. There is also interest in creating small molecule artificial transcription factors to regulate gene expression, examples include wrenchnol (a wrench shaped molecule).

Binding of ligand can be characterised using a variety of analytical techniques such as surface plasmon resonance, microscale thermophoresis or dual polarisation interferometry to quantify the reaction affinities and kinetic properties and also any induced conformational change.