Journal Papers

Molecularly profiled trials: toward a framework of actions for the “nil actionables”

The sequencing of tumour or blood samples is increasingly used to stratify patients into clinical trials of molecularly targeted agents, and this approach has frequently demonstrated clinical benefit for those who are deemed eligible....

Impact of Mitochondrial Targeting Antibiotics on Mitochondrial Function and Proliferation of Cancer Cells

Edward J Cochrane, James Hulit, Franz P Lagasse, Tanguy Lechertier, Brett Stevenson, Corina Tudor, Diana Trebicka, Tim Sparey, and Andrew J Ratcliffe Abstract: Some marketed antibiotics can cause mitochondria dysfunction via inhibition of the...

Targeting p300/CBP axis in lethal prostate cancer

Jonathan Welti, Adam Sharp, Nigel Brooks, Wei Yuan, Christopher McNair, Saswati N Chand, Abhijit Pal, Ines Figueiredo, Ruth Riisnaes, Bora Gurel, Jan Rekowski, Denisa Bogdan, William West, Barbara Young, Meera Raja, Amy Prosser, Jordan...

Sensitivity of Binding Free Energy Calculations to Initial Protein Crystal Structure

Miroslav Suruzhon, Michael S Bodnarchuk, Antonella Ciancetta, Russel Viner, Ian D Wall, and Jonathan W Essex Abstract: Binding free energy calculations using alchemical free energy (AFE) methods are widely considered to be the most...

High Throughput Screening: Methods, Techniques and Applications (Chapter 7)

Chapter 7. Biophysical Hit Evaluation Scott Pollack, Rupert Satchell, Juliet Morgan and Patrick J. McIntyre, Bioscience Department, Sygnature Discovery High Throughput Screening (HTS) is one of several hit identification approaches that are part of...

Derivatisation of parthenolide to address chemoresistant chronic lymphocytic leukaemia

Xingjian Li, Daniel T. Payne, Badarinath Ampolu, Nicholas Bland, Jane T. Brown, Mark J. Dutton, Catherine A. Fitton, Abigail Gulliver, Lee Hale, Daniel Hamza, Geraint Jones, Rebecca Lane, Andrew G. Leach, Louise Male, Elena...

Synthesis of a hexahydropyrrolo indole (HPI) compound library

Sabrina Nickel, Philipp Nickel, Marco Hellmert, Silvia Ernst, Robert Jewell, Christopher A. Pearce, Geraint Jones, Daniel Hamza, Markus Kaisera Abstract Scaffolds of natural products represent promising starting points for the development of focused compound...

Facile access to a heterocyclic, sp3-rich chemical scaffold via a tandem condensation/intramolecular nitrone–alkene [3+2] cycloaddition strategy

M. J. Rawling,  T. E. Storr,  W. A. Bawazir,  S. J. Cully,  W. Lewis,  M. S. I. T. Makki,  I. R. Strutt,  G. Jones,  D. Hamza  and  R. A. Stockman Abstract Scaffolds of natural...

Discovery of Narrow Spectrum Kinase Inhibitors: New Therapeutic Agents for the Treatment of COPD and Steroid-Resistant Asthma

Stuart T. Onions, Kazuhiro Ito, Catherine E. Charron, Richard J. Brown, Marie Colucci, Fritz Frickel, George Hardy, Kevin Joly, John King-Underwood, Yasuo Kizawa, Ian Knowles, P. John Murray, Andrew Novak, Anjna Rani, Garth Rapeport,...

Expansion of chemical space for collaborative lead generation and drug discovery: the European Lead Factory Perspective

Karawajczyk A., Giordanetto F., Benningshof J., Hamza D., Kalliokoski T., Pouwer K., Morgentin R., Nelson A., Müller G., Piechot A., Tzalis D. Abstract High-throughput screening (HTS) represents a major cornerstone of drug discovery. The...

Expedient synthesis of an atypical oxazolidinone compound library

Sarah J. Cully, Thomas E. Storr, Michael J. Rawling, Induka R. Abeysena, Daniel Hamza, Geraint Jones, Christopher A. Pearce, Abdul Quddus, William Lewis, Robert A. Stockman Abstract In order to address the current downturn...

In vitro and in vivo antifungal profile of a novel and long-acting inhaled azole, PC945, on Aspergillus fumigatus infection

Colley T., Alanio A., Kelly S.L., Sehra G., Kizawa Y., Warrilow A.G.S., Parker J.E., Kelly D.E., Kimura G., Anderson-Dring L., Nakaoki T., Sunose M., Onions S., Crepin D., Lagasse F., Crittall M., Shannon J.,...