Microcycles are head-to-tail cyclic hexapeptides that hold much promise in drug discovery. We have developed several methods for the preparation of genetically encoded Microcycle libraries in cells and in microfluidic droplets. These libraries have been interfaced with a number of high-throughput assays for the direct identification of functional inhibitors of various protein-protein and protein-DNA interactions, including several first in class compounds. The presentation will include examples in which Microcycle hits from these screens have been further optimised as a first step towards the design of novel low molecular weight clinical candidates.

Prof. Ali Tavassoli / University of Southhampton, UK