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LLAMA launch!

28 September 2015

LLAMA (Lead Likeness And Molecular Analysis) is an open access tool that was launched on Friday 25th September.

The launch coincided with a Dial-a-Molecule Challenge meeting on lead-oriented synthesis at GSK’s Stevenage site.  LLAMA allows the lead-likeness of different molecular scaffolds to be evaluated and compared.  Screening compounds based on lead-like scaffolds can provide good starting points in drug discovery. 

LLAMA is a free tool that was developed in Leeds as part of an EPSRC-funded collaboration with GSK, and is available to the synthetic chemistry community for both research and teaching.
Twitter: @llama_leeds

Developing International Links

21 September 2015

Prof Andy Wilson recently took part in a joint RSC/British Council supported Sympoisa Tour of Turkey to foster new collaborative links.

Entitled Catalysis for Sensing and Health (CASH). Prof Wilson, together with Profs Steve Bull, Tony James (both Bath) and Juyoung Yoon (EWHA Womans University) gave lectures at four top Turkish Universities together with local speakers from Bogazici University (Istanbul), Izmir Institute of Technology, Middle East Technical University and Bilkent University (both Ankara). The tour which also included a public engagement event hosted at the British Council in Izmir and reception at the British Embassy in Ankara coincided with the British council celebrating 75 years in Turkey, the International Year of Science and ongoing initiatives associated with the Newton Fund.   

Inaugural Dalton Symposium and Poster Prize

15 September 2015

The inaugural Dalton Younger Members Event (DYME@Leeds 2015) was held at the University of Leeds on 9-10th September.

This two-day conference saw national PhD and post-doctoral speakers from across the UK presenting their research in the area of inorganic chemistry.

PhD student, Jonathan Fowler from the Hardie and Willans groups at the University of Leeds, won the Dalton Transactions prize for the best poster contribution entitled "NHC Ligands in Metallo-supramolecular Chemistry: Fundamentals and Towards Carbene-Appended Cavitands".

The anticancer mechanism of a wasp venom peptide

7 September 2015

Research from the group of Dr Paul Beales has provided mechanistic insight into why a wasp venom peptide has anticancer properties.

The MP1 peptide, found in the venom of the aggressive Brazilian social wasp Polybia Paulista, is known to be able to inhibit the proliferation of, and in some cases kill, a variety of cancer cells without harming healthy cells such as red blood cells. However, until now, it was unclear why the peptide has these properties.

The natural role of this peptide is as an antibiotic, which attacks microbial membranes due to their different molecular composition compared to the wasp’s own cells. The team hypothesized that pathological changes in membrane composition were responsible for this peptide’s ability to specifically target cancer cells. It is known that PE and PS lipids, which are normally “hidden” on the inner leaflet of cell membranes become exposed to the outer membrane leaflet in many cancer cells.

In collaboration with Sao Paulo State University in Brazil and Dr Simon Connell in the School of Physics and Astronomy, this hypothesis was tested on model lipid membranes that were mainly composed of PC lipids (the major component of cell membranes) and containing neither, one of, or both PE and PS lipids. A variety of advanced biophysical spectroscopy and imaging techniques were applied to study the MP1 peptide’s interaction with these membranes. It was found that the PS lipid is required to increase the concentration of bound peptide on the membrane, whereas the PE lipid significantly increases the membrane’s susceptibility to disruption by the peptide. This facilitates the formation of large holes across the membrane that would allow vital biochemical constituents to leak from the cell and would lead to the loss of transmembrane chemical gradients. Therefore changes in the membrane composition of cancer cells form a mechanistic basis for the anticancer properties of MP1.

This work was recently published in Biophysical Journal and received significant international media attention. Coverage included the BBC website, BBC World Service, The International Business Times, The Times, The Guardian, The Independent,, IFLscience, Discover Magazine, MTV and the Huffington Post.

This is early stage, fundamental research but these findings could in future aid the development of novel chemotherapies that target changes in the membrane composition of cancer cells. This would be a novel mechanism for an anticancer drug and so be particularly useful for the development of combination therapies where multiple drugs are used simultaneously to attack different parts of cancerous cells. The MP1 peptide has evolved as a natural antibiotic and not as an anticancer agent. Therefore it could be possible, now that there is insight into its mechanism of action, to improve the selectivity and potency of this peptide to cancer cells by designing modifications within its chemical structure.

Poster Prize

7 September 2015

Last week members of the McGowan and Willans groups travelled to St Anne’s College, Oxford for the RSC Coordination and Organometallic Chemistry Discussion Group meeting.

The two day event saw both national and international speakers presenting work in the areas of coordination and organometallic chemistry, with a poster session of around 100 posters. Heba Abdelgawad from the Willans group won first prize for her poster entitled ‘Silver N-Heterocyclic Carbene Complexes as Anticancer Agents’.

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