“Asymmetric catalysis” won the Nobel chemistry prize in 2001 for Dr Knowles, Dr Noyori and Dr Sharpless. The pursuit of chiral drugs has been feverish for ever. Among resolution, separation, chiral synthesis, biocatalysis, etc. there is the effort of using enzyme to synthesize its own inhibitor. The Economist reported such an effort in the article "telling right from left", September 19, 2002, stated as following:
Dr Sharpless goes even further. People are not very good at making medicines, he says. Life is short, while conventional drug-discovery is a long and uncertain process. So why not put nature, which is much more patient and sophisticated at doing the job, to work directly? Just as a mould can be used to make a copy of a three-dimensional object, Dr Sharpless proposes to use biological targets as templates to guide the formation of their own perfect drugs. He calls the method “click chemistry”, because of the ease with which the molecular building-blocks fit together. He and his colleagues have already used it in the laboratory to identify a molecule that blocks an enzyme related to Alzheimer's disease. Sometimes the best ideas are also the most obvious.