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Research overview

Professor Ian Collins, Medicinal Chemistry 2

The discovery and development of new small molecules as anticancer therapeutics.

The core of our research is the design and synthesis of new molecules to inhibit the activity of proteins responsible for the development and progression of cancer. The team is involved in several anticancer drug discovery projects at different points in the drug discovery pathway. We have particular interests in the discovery and development of small-molecule inhibitors of proteins that use nucleotides as substrates, such as oncogenic signalling kinases, ATP-dependent molecular chaperones and kinesin motor proteins. Our current targets of interest include CHK1, IRE1, HSP70, HSET and tankyrase.

We design and synthesise new compound libraries for biochemical or cell-based screening, often inspired by biologically active natural products or using information from structural biology studies. We develop new synthetic chemistry to prepare the compounds and have a strong track record in the assembly of functionalised heterocyclic molecules. As many of our current drug discovery targets have the nucleotide ATP as a common natural substrate, we are involved in the design of new scaffolds for inhibitors based on the binding modes of nucleotide cofactors.

We explore the structure-activity of hits arising from fragment-based or high-throughput screening to select lead series for further development. We collaborate with structural biologists and molecular modellers to use structure-based methods to improve the properties of the compounds. An important goal is the generation of selective inhibitors with cellular activity, suitable for use as chemical tools to probe the biology of new target proteins.

We contribute synthetic and medicinal chemistry expertise to the multi-disciplinary drug discovery projects in the CR-UK Cancer Therapeutics Unit. Through collaborations with in vitro and in vivo biology teams, we optimise lead molecules to produce potent compounds with antitumour activity, leading ultimately to the selection of preclinical development candidates.

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