S
Simon A. Osborne
Researcher at Medical Research Council Technology
Publications - 27
Citations - 1333
Simon A. Osborne is an academic researcher from Medical Research Council Technology. The author has contributed to research in topics: Plasmodium falciparum & Protein kinase A. The author has an hindex of 17, co-authored 27 publications receiving 1142 citations. Previous affiliations of Simon A. Osborne include Medical Research Council & University of Cambridge.
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Journal ArticleDOI
Subcellular discharge of a serine protease mediates release of invasive malaria parasites from host erythrocytes.
Sharon Yeoh,Rebecca A. O'Donnell,Konstantinos Koussis,Anton R. Dluzewski,Keith H. Ansell,Simon A. Osborne,Fiona Hackett,Chrislaine Withers-Martinez,Graham H. Mitchell,L. H. Bannister,Justin S. Bryans,Catherine A. Kettleborough,Michael J. Blackman +12 more
TL;DR: The presence in the malarial parasitophorous vacuole of a regulated, PfSUB1-mediated proteolytic processing event required for release of viable parasites from the host erythrocyte is revealed.
Journal ArticleDOI
Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy
Katy J. Petherick,Owen Conway,Chido Mpamhanga,Simon A. Osborne,Ahmad Kamal,Barbara Saxty,Ian G. Ganley +6 more
TL;DR: Two compounds, MRT67307 and MRT68921, potently inhibit ULK1 and ULK2 in vitro and block autophagy in cells, indicating a role for ULK 1 in the maturation of autophagosomes as well as initiation.
Journal ArticleDOI
A potent series targeting the malarial cGMP-dependent protein kinase clears infection and blocks transmission.
David A. Baker,Lindsay B. Stewart,Jonathan M. Large,Paul W. Bowyer,Keith H. Ansell,María Belén Jiménez-Díaz,Majida El Bakkouri,Majida El Bakkouri,Kristian Birchall,Koen J. Dechering,Nathalie Bouloc,P.J. Coombs,David Whalley,Denise J. Harding,Ela Smiljanic-Hurley,Mary C. Wheldon,Eloise M. Walker,Johannes T. Dessens,Maria Lafuente,Laura Sanz,Francisco-Javier Gamo,Santiago Ferrer,Raymond Hui,Raymond Hui,Teun Bousema,Iñigo Angulo-Barturen,Andy Merritt,Simon L. Croft,Winston E. Gutteridge,Catherine A. Kettleborough,Simon A. Osborne +30 more
TL;DR: An imidazopyridine series is generated that selectively targets Plasmodium falciparum PKG, inhibits blood stage parasite growth in vitro and in mice and blocks transmission to mosquitoes and warrants consideration for further development to produce an antimalarial drug.
Journal ArticleDOI
New anti-tuberculosis agents amongst known drugs.
TL;DR: Five compounds were selected as those which represent the most promising starting points for new anti-tuberculosis agents and it was demonstrated that all five were active against intracellular M. tuberculosis in a macrophage model of infection.
Journal ArticleDOI
Effective inhibitors of the essential kinase PknB and their potential as anti-mycobacterial agents.
Kathryn E.A. Lougheed,Simon A. Osborne,Barbara Saxty,David Whalley,Tim Chapman,Nathalie Bouloc,Jasveen Chugh,Timothy J. Nott,Dony Patel,Vicky L. Spivey,Catherine A. Kettleborough,Justin S. Bryans,Debra L. Taylor,Stephen J. Smerdon,Roger S. Buxton +14 more
TL;DR: A program of synthetic medicinal chemistry was conducted around one class of inhibitors and was successful in generating ATP competitive inhibitors with potency in the nanomolar range, but found no evidence that the activity of the inhibitors could be improved by weakening the cell wall.