Circling back to basics
Macrocycles have been a hot topic for chemists and pharmacologists alike for the promise they hold of reaching druggable targets that small molecules cannot. Although they are still much more challenging than small molecules to develop, a trio of studies might offer a way forward by proposing new design guidelines,1 identifying protein-protein interfaces to target2 and providing a new method to synthesize cyclic peptides (see Box 1, "Cyclotide synthesis").3
The papers were published in Nature Chemical Biology alongside an editorial call to action for research to support macrocycle discovery and development.4The proposals echoed those discussed by academic and industry leaders at SciBX's 2012 Summit on Innovation in Macrocycle Drug Discovery.5...