Search

Your search keyword '"Berry, Neil G."' showing total 6 results
Start Over Author "Berry, Neil G." Journal proceedings of the national academy of sciences of the united states of america
6 results on '"Berry, Neil G."'

1. AWZ1066S, a highly specific anti- Wolbachia drug candidate for a short-course treatment of filariasis

Author

Hong, W. David, Benayoud, Farid, Nixon, Gemma L., Ford, Louise, Johnston, Kelly L., Clare, Rachel H., Cassidy, Andrew, Cook, Darren A. N., Siu, Amy, Shiotani, Motohiro, Webborn, Peter J. H., Kavanagh, Stefan, Aljayyoussi, Ghaith, Murphy, Emma, Steven, Andrew, Archer, John, Struever, Dominique, Frohberger, Stefan J., Ehrens, Alexandra, Hübner, Marc P., Hoerauf, Achim, Roberts, Adam P., Hubbard, Alasdair T. M., Tate, Edward W., Serwa, Remigiusz A., Leung, Suet C., Qie, Li, Berry, Neil G., Gusovsky, Fabian, Hemingway, Janet, Turner, Joseph D., Taylor, Mark J., Ward, Stephen A., and O’Neill, Paul M.

Published
2019

4. Generation of quinolone antimalarials targeting the Plasmodium falciparum mitochondrial respiratory chain for the treatment and prophylaxis of malaria

Author

Biagini, Giancarlo A., Fisher, Nicholas, Shone, Alison E., Mubaraki, Murad A., Srivastava, Abhishek, Hill, Alisdair, Antoine, Thomas, Warman, Ashley J., Davies, Jill, Pidathala, Chandrakala, Amewu, Richard K., Leung, Suet C., Sharma, Raman, Gibbons, Peter, Hong, David W., Pacorel, Bénédicte, Lawrenson, Alexandre S., Charoensutthivarakul, Sitthivut, Taylor, Lee, Berger, Olivier, Mbekeani, Alison, Stocks, Paul A., Nixon, Gemma L., Chadwick, James, Hemingway, Janet, Delves, Michael J., Sinden, Robert E., Zeeman, Anne-Marie, Kocken, Clemens H. M., Berry, Neil G., O'Neill, Paul M., and Ward, Stephen A.

Published
2012

6. Antimalarial 4(1H)-pyridones bind to the Qi site of cytochrome bc1.

Author

Capper MJ, O'Neill PM, Fisher N, Strange RW, Moss D, Ward SA, Berry NG, Lawrenson AS, Hasnain SS, Biagini GA, and Antonyuk SV

Subjects
Binding Sites, Electron Transport Complex III chemistry, Molecular Docking Simulation, Antimalarials metabolism, Electron Transport Complex III metabolism, Pyridones metabolism
Abstract

Cytochrome bc1 is a proven drug target in the prevention and treatment of malaria. The rise in drug-resistant strains of Plasmodium falciparum, the organism responsible for malaria, has generated a global effort in designing new classes of drugs. Much of the design/redesign work on overcoming this resistance has been focused on compounds that are presumed to bind the Q(o) site (one of two potential binding sites within cytochrome bc1 using the known crystal structure of this large membrane-bound macromolecular complex via in silico modeling. Cocrystallization of the cytochrome bc1 complex with the 4(1H)-pyridone class of inhibitors, GSK932121 and GW844520, that have been shown to be potent antimalarial agents in vivo, revealed that these inhibitors do not bind at the Q(o) site but bind at the Q(i )site. The discovery that these compounds bind at the Q(i) site may provide a molecular explanation for the cardiotoxicity and eventual failure of GSK932121 in phase-1 clinical trial and highlight the need for direct experimental observation of a compound bound to a target site before chemical optimization and development for clinical trials. The binding of the 4(1H)-pyridone class of inhibitors to Q(i) also explains the ability of this class to overcome parasite Q(o)-based atovaquone resistance and provides critical structural information for future design of new selective compounds with improved safety profiles.

Published
2015
Full Text
View/download PDF

Catalog

Books, media, physical & digital resources
See catalog results