ICR and Enamine Launch Fragment-Based Drug Discovery Collaboration to Accelerate Cancer Drug Development
核心洞察
The Institute of Cancer Research and Enamine Ltd (搜索). have announced a new 12-month research collaboration to develop fluorinated fragment compounds for fragment-based drug discovery.
Enamine will supply carefully selected fluorinated fragments from its extensive compound collection, which ICR researchers will profile using advanced analytical tools including NMR spectroscopy and mass spectrometry.
The collaboration builds on previous joint research to design carboxylic acid bioisostere fragment libraries and aims to create well-characterized compounds for global drug discovery efforts.
The Institute of Cancer Research (ICR) and Enamine Ltd (搜索). have announced a new research collaboration aimed at advancing fragment-based drug discovery (FBDD) tools for cancer therapeutics. The 12-month partnership will focus on developing and characterizing fluorinated fragment compounds to accelerate early-stage drug discovery efforts worldwide.
Collaborative Framework and Compound Selection
Under the joint initiative, Enamine will supply a curated set of fluorinated fragment compounds to the ICR, selected from its extensive in-stock collection and the Enamine 'REAL Space' of made-to-order compounds. This collaboration builds on previous joint research between the two organizations to design a carboxylic acid bioisostere fragment library.
Researchers at the ICR's Centre for Cancer Drug Discovery will profile these compounds using sophisticated in-house analytical tools, including proton and fluorine nuclear magnetic resonance (NMR) spectroscopy, liquid chromatography-high resolution mass spectrometry (LC-HRMS), and solubility testing. The annotated compounds will subsequently be screened against a panel of protein targets to assess their potential value in fragment-based screening campaigns.
Fragment-Based Drug Discovery Approach
The ICR has established itself as a pioneer in fragment-based drug discovery, a methodology that involves creating very small molecules capable of fitting into pockets on the surface of proteins of interest, particularly those that drive cancer progression. Medicinal chemists then build upon these fragments to create larger molecules that block the action of their target protein, which through further iteration can become cancer drugs.
This approach represents a strategic method for identifying novel therapeutic compounds by starting with small molecular fragments and systematically expanding them into drug-like molecules with enhanced potency and selectivity.
Commercial and Research Applications
Once testing is complete, Enamine will use the results to refine and commercialize new fragment libraries, making them available through its global distribution network. The ICR will retain priority rights to explore the findings and will collaborate with Enamine to publish joint results in peer-reviewed journals.
The project is expected to run for 12 months with the option to extend. Both teams will contribute to a final research report, and future communications will highlight key takeaways for the scientific and drug discovery communities.
Track Record and Future Impact
The ICR's Centre for Cancer Drug Discovery has demonstrated significant success as a world-leading academic center for drug discovery in oncology, having discovered 21 drug candidates since 2005 in collaboration with commercial partners, of which 13 have reached clinical trials.
Professor Swen Hoelder, Director of Chemistry at The Institute of Cancer Research, London, emphasized the collaboration's potential: "This exciting new collaboration is a great opportunity to combine our research capabilities and expertise in fragment-based drug discovery with Enamine's compound expertise. This focused, practical project aims to produce a well-characterized set of fluorinated fragments that can accelerate early-stage drug discovery for researchers worldwide, and that we hope will ultimately lead to the discovery of new drugs that benefit cancer patients."
The partnership leverages Enamine's position as a leading global provider of screening compounds, chemical building blocks, and drug discovery services, combining it with ICR's proven track record in translating early-stage discoveries into clinical candidates.