Macrocycles by the trillions

Japanese researchers have developed a method for creating large libraries of N-methylated peptide macrocycles,¹ a class of molecules that are sized between small molecules and biologics and have the potential to combine the pharmacological versatility of the former and the therapeutic specificity of the latter. PeptiDream Inc. has exclusively licensed the technology and entered collaborations with six pharmas.

Small molecules are typically less than 500 Da in size, whereas biologics start at approximately 5,000 Da and cover a range of one to two orders of magnitude. Macrocycles, a structure frequently found in natural products, range in size from 500-2,000 Da...