Wednesday, November 30, 2011

A biomimetic polyketide-inspired approach to small-molecule ligand discovery



In this paper C. Aquino and co-workers designed polyketide derived oligomers called ‘chirlal oligomers of pentenoic amides’ (COPA) by using the split pool technique. They were able to make a diverse set of COPA library and screened these compounds against the DNA binding domain of p53 which is an important transcription factor that regulates cell cycle and apoptosis. It was interesting that they  increased conformational constraints for the small molecules for a higher affinity towards target proteins.  

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