University of Cambridge > > Experimental and Computational Aspects of Structural Biology and Applications to Drug Discovery > Cyclofluidic: Quick hit-to-lead optimization using an integrated microfluidic approach

Cyclofluidic: Quick hit-to-lead optimization using an integrated microfluidic approach

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Small molecule lead discovery involves an iterative process of molecular design, chemical synthesis, biological assay and data analysis to feed into the next learning cycle. The Cyclofluidic technology platform CyclOps™ integrates all the processes key to medicinal chemistry on the bench-top, allowing drug lead molecules to be assayed minutes (rather than weeks) after they are designed. CyclOps™ connects flow chemistry, purification, screening and drug design with complex algorithms developed in collaboration with Accelerys. Each potential lead molecule is synthesised, purified and screened in fast serial mode, incorporating activity data from every iteration into the algorithm for the selection of the next compound to make. Cyclofluidic’s technology platform CyclOps™ is based on ground breaking research developed in the laboratories of Professor Steve Ley at Cambridge University and at GlaxoSmithKline. The power of the platform was recently demonstrated with the rapid generation of structure activity relationship (SAR) data around Abl Kinase inhibitors, which led to the identification of 4 novel potent inhibitor molecules that had not been described before in any patents or literature.

Selected References: 1) Desai B, Dixon K, Farrant E, Feng Q, Gibson KR, van Hoorn WP, Mills J, Morgan T, Parry DM, Ramjee MK, Selway CN, Tarver GJ, Whitlock G, Wright AG. (2013). Rapid discovery of a novel series of Abl kinase inhibitors by application of an integrated microfluidic synthesis and screening platform. J Med Chem., 56(7), 3033-47. 2) Werngard Czechtizky, Jüergen Dedio, Bimbisar Desai, Karen Dixon, Elizabeth Farrant, Qixing Feng, Trevor Morgan, David M. Parry, Manoj K. Ramjee, Christopher N. Selway, Thorsten Schmidt, Gary J. Tarver, and Adrian G. Wright. (2013). Integrated Synthesis and Testing of Substituted Xanthine Based DPP4 Inhibitors: Application to Drug Discovery. ACS Med. Chem. Lett., 4(8), 768–772.

This talk is part of the Experimental and Computational Aspects of Structural Biology and Applications to Drug Discovery series.

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