A chemoenzymatic solution for cell-permeable therapeutic macrocycles


P Killoran1; W Van der Linden1; M Jaspers2; J Naismith3; B Primrose1
1 GyreOx, UK;  2 Marine Biodiscovery Centre, University of Aberdeen, UK;  3 Rosalind Franklin Institute, UK


A chemoenzymatic solution for cell-permeable therapeutic macrocycles

Current drugs address only ca. 30% of the estimated 3000 disease-relevant targets. Many of these untapped therapeutic applications are intracellular protein-protein interactions (PPIs). The two common classes of drugs, small molecules and biologics, are not a universal solution to all drug discovery challenges.

GyreOx is exploiting this opportunity using its proprietary discovery platform (‘MACRO’) to create unique Gyrocycle(TM) highly modified macrocyclic peptides. These compounds combine the target-engagement power of biologics with the cell-entry ability of small molecules.

GyreOx’s platform technology is a combined chemistry / synthetic biology process, protected by 4 patent applications, allowing rapid access to novel and drug-like macrocycles for hit-to-lead drug discovery.

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