Projects per year
Our main research achievements were in the areas of medicinal chemistry of sulphur containing compounds (Hamilton), macrocycles (Matthews) and natural product compounds (Gibbons).
In chemical biology, our current research strengths lie in understanding of assembly of DNA and its alternative motives (Waller), protein-protein interactions (Searcey, Beekman) and epigenetics (Ganesan).
These lines of research are supported by UKRI (EPSRC (Searcey); BBSRC (Searcey, Ganesan), industrial funding (Hamilton, Ganesan), Big C (Searcey), Royal Society and British Council (Matthews, Ganesan). Ganesan was the lead of EU funded COST action Epigenetic Chemical Biology (EPICHEM).
- By using an in vivo mouse model of lung infection we demonstrated that our novel Calixarene-based glycoclusters functionalized with galactosides or fucosides provided an almost complete protection against Pseudomonas aeruginosa (Matthews).
- As part of interdisciplinary team (UCL, Southampton, Hong-Kong, UEA), Ganesan showed that NAADP signalling plays a major role in reperfusion-induced cell death and represents a potent pathway for protection against reperfusion injury.
- Searcey and Beekman discovered a highly efficient approach to the development of inhibitors of the p53/hDMX or hDM2 interaction that involves the design of small molecules in silico based upon a peptide/protein structure.
- Hamilton made significant advances in understanding the role of bacillithiol, the main thiol metabolite in many Gram-positive bacteria, including identification of its derivatives, studying mechanisms of their synthesis and analysis of genome data.
- Considerable breakthroughs were achieved in understanding structure-activity relationship of Diphyllin and its derivatives (cytotoxic natural products structurally related to the anti-cancer drug podophyllotoxin) upon human melanoma cells (Gibbons).
This research cluster is led by Professor Ganesan.
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Amino DSA analogues as payloads for antibody-drug conjugates with multiple sites for conjugation. Initial studies and solid phase synthesisM. M. D. Cominetti, M., Goddard, Z. R., Howman, C. E., O'Connell, M. A. & Searcey, M., 25 May 2021, In : Tetrahedron Letters. 72, 153058.
Research output: Contribution to journal › Article
In silico peptide-directed ligand design complements experimental peptide-directed binding for protein–protein interaction modulator discoveryHowell, L. A. & Beekman, A. M., 1 Feb 2021, In : RSC Chemical Biology. 2, 1, p. 215-219 5 p.
Research output: Contribution to journal › ArticleOpen AccessFile27 Downloads (Pure)
Peptide directed phthalocyanine-gold nanoparticles for selective photodynamic therapy of EGFR overexpressing cancersGoddard, Z. R., Beekman, A. M., Cominetti, M. M. D., O'Connell, M. A., Chambrier, I., Cook, M. J., Marin, M. J., Russell, D. A. & Searcey, M., 1 Feb 2021, In : RSC Medicinal Chemistry. 12, 2, p. 288-292 5 p.
Research output: Contribution to journal › ArticleOpen AccessFile1 Citation (Scopus)13 Downloads (Pure)