Christine Oswald

HTA95 Predicting Evidence Requirement Implications of the EU Joint Clinical Assessment (JCA) Through a Population, Comparator, Intervention, Outcome (PICO) Simulation for Two Anticancer Investigational Medicinal Products (IMPs)

Elena Anastasaki, Nicolas Despiégel, Franziska Dirnberger, A van Engen et autres

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Structural basis for CCR6 modulation by allosteric antagonists

David Jonathan Wasilko, Brian S. Gerstenberger, Kathleen A. Farley, Wěi Li et autres

The CC chemokine receptor 6 (CCR6) is a potential target for chronic inflammatory diseases. Previously, we reported an active CCR6 structure in complex with its cognate chemokine CCL20, revealing the molecular basis of CCR6 activation. Here, we present two inactive CCR6 structures …

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Structural basis for CCR6 modulation by allosteric antagonists

David Jonathan Wasilko, Brian S. Gerstenberger, Kathleen A. Farley, Wěi Li et autres

Abstract The CC chemokine receptor 6 (CCR6) is a potential target for chronic inflammatory diseases such as psoriasis and inflammatory bowel disease. Previously, we reported an active CCR6 structure in complex with its cognate chemokine CCL20, revealing the molecular basis of CCR6 …

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Antimalarial agents. III. Mechanism of action of artesunate against Plasmodium berghei infection.

Christine Oswald, Toshio Yokoi, Kuo Hsiung Lee, Iris H. Hall et autres

The antimalarial agent, artesunate has been observed to suppress the infection growth rate of in CF mouse red blood cells. The inhibition of growth was due to a number of biochemical mechanisms. Deoxyribonucleic acid (DNA) synthesis in the was inhibited significantly by …

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Allosteric drug transport mechanism of multidrug transporter AcrB

Heng-Keat Tam, Wuen Ee Foong, Christine Oswald, Andrea Herrmann et autres

Abstract Gram-negative bacteria maintain an intrinsic resistance mechanism against entry of noxious compounds by utilizing highly efficient efflux pumps. The E. coli AcrAB-TolC drug efflux pump contains the inner membrane H + /drug antiporter AcrB comprising three functionally interdependent protomers, cycling consecutively …

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Fusidic acid binding to the allosteric deep transmembrane domain binding pocket, TM7/TM8 groove, and TM1/TM2 groove of the fully induced AcrB T protomer

Christine Oswald, H.K. Tam, Klaas M. Pos

Applying Structure-Based Drug Design Approaches to Allosteric Modulators of GPCRs

Miles Congreve, Christine Oswald, Fiona H. Marshall

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Transport of lipophilic carboxylates is mediated by transmembrane helix 2 in multidrug transporter AcrB

Christine Oswald, Heng-Keat Tam, Klaas M. Pos

The deployment of multidrug efflux pumps is a powerful defence mechanism for Gram-negative bacterial cells when exposed to antimicrobial agents. The major multidrug efflux transport system in Escherichia coli, AcrAB-TolC, is a tripartite system using the proton-motive force as an energy source. …

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Intracellular allosteric antagonism of the CCR9 receptor

Christine Oswald, Mathieu Rappas, James Kean, A.S. Dore et autres

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Crystal structure of the human CC chemokine receptor type 9 (CCR9) in complex with vercirnon

Christine Oswald, Mathieu Rappas, J. Kean, A.S. Dore et autres

Fusidic acid bound AcrB

Christine Oswald, H.K. Tam, Klaas M. Pos

Functional Stability of the Human Kappa Opioid Receptor Reconstituted in Nanodiscs Revealed by a Time-Resolved Scintillation Proximity Assay

Randi Westh Hansen, Xiaole Wang, Agnieszka Gołąb, Olivier Bornert et autres

Long-term functional stability of isolated membrane proteins is crucial for many in vitro applications used to elucidate molecular mechanisms, and used for drug screening platforms in modern pharmaceutical industry. Compared to soluble proteins, the understanding at the molecular level of membrane proteins …

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