Through the Looking Glass
There is a shocking lack of attention given to racemization in drug discovery, despite it having huge implications on the efficacy – and safety – of drugs. We hope the tool we have developed will be the first step towards change.
Niek Buurma |
Many drugs are chiral molecules: they have the potential to “flip” and exist as different enantiomers – non-superimposable mirror images of the original molecule with an identical chemical structure. In some cases, this flipping behavior can occur when an enantiomerically pure drug enters the body, in a process known as racemization. Typically, only one of the two enantiomers is useful, meaning that the pharmaceutical action of a significant fraction of all drugs depends on administering the correct enantiomer. The reason why typically only one enantiomer is useful is that biological targets of drugs are usually just one mirror image. Therefore, when we administer a mixture of enantiomers, one will act as intended but the other enantiomer could be a bad fit with the target, leading to this unwanted enantiomer binding to unintended targets, potentially causing serious side effects.
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