Tuesday, January 1, 2013

In situ click chemistry 10 years mark

Happy New Year 2013

C&EN did a brief piece "revisiting 2002" and took a look at in situ click chemistry. Some key points:

Original publication by Scripps Group in Angew Chem Int 2002, 1053 
Acetylcholinesterase directs the synthesis of its own potent inhibitor when induced-and-fit
Difficulties: large quantity of protein, little quantity of inhibitor, slow reaction, etc
Ten years have seem a few successes but limited adoption

Copper catalyzed version (CuAAC) enjoyed widespread popularity
Original publication by the Group in Angew Chem Int 2002, 2596
Forget Not the Key ----  
Fast "molecular discovery" for functions