Professor Steven Charlton's Outputs (4)

'Partial' competition of heterobivalent ligand binding may be mistaken for allosteric interactions: a comparison of different target interaction models (2014)
Journal Article
Vauquelin, G., Hall, D., & Charlton, S. (2015). 'Partial' competition of heterobivalent ligand binding may be mistaken for allosteric interactions: a comparison of different target interaction models. British Journal of Pharmacology, 172(9), 2300-2315. https://doi.org/10.1111/bph.13053

© 2014 The British Pharmacological Society. Background and Purpose Non-competitive drugs that confer allosteric modulation of orthosteric ligand binding are of increasing interest as therapeutic agents. Sought-after advantages include a ceiling level... Read More about 'Partial' competition of heterobivalent ligand binding may be mistaken for allosteric interactions: a comparison of different target interaction models.

Potent and efficacious inhibition of CXCR2 signaling by biparatopic nanobodies combining two distinct modes of action (2014)
Journal Article
Bradley, M. E., Dombrecht, B., Manini, J., Willis, J., Vlerick, D., De Taeye, S., Van den Heede, K., Roobrouck, A., Grot, E., Kent, T. C., Laeremans, T., Steffensen, S., Van Heeke, G., Brown, Z., Charlton, S. J., & Cromie, K. D. (2015). Potent and efficacious inhibition of CXCR2 signaling by biparatopic nanobodies combining two distinct modes of action. Molecular Pharmacology, 87(2), 251-262. https://doi.org/10.1124/mol.114.094821

Copyright © 2015 by The American Society for Pharmacology and Experimental Therapeutics. Chemokines and chemokine receptors are key modulators in inflammatory diseases and malignancies. Here, we describe the identification and pharmacologic character... Read More about Potent and efficacious inhibition of CXCR2 signaling by biparatopic nanobodies combining two distinct modes of action.

Observed drug-receptor association rates are governed by membrane affinity: The importance of establishing "micro-pharmacokinetic/pharmacodynamic relationships" at the β2-adrenoceptor (2014)
Journal Article
Sykes, D. A., Parry, C., Reilly, J., Wright, P., Fairhurst, R. A., & Charlton, S. J. (2014). Observed drug-receptor association rates are governed by membrane affinity: The importance of establishing "micro-pharmacokinetic/pharmacodynamic relationships" at the β2-adrenoceptor. Molecular Pharmacology, 85(4), 608-617. https://doi.org/10.1124/mol.113.090209

Current pharmacological models for determining affinity and kinetics of drugs for membrane receptors assume the interacting molecules are homogeneously distributed in the bulk aqueous phase. The phospholipid membrane can, however, provide a second co... Read More about Observed drug-receptor association rates are governed by membrane affinity: The importance of establishing "micro-pharmacokinetic/pharmacodynamic relationships" at the β2-adrenoceptor.

Investigating the molecular mechanisms through which FTY720?P causes persistent S1P1 receptor internalization (2014)
Journal Article
Sykes, D. A., Riddy, D. M., Stamp, C., Bradley, M. E., McGuiness, N., Sattikar, A., Guerini, D., Rodrigues, I., Glaenzel, A., Dowling, M. R., Mullershausen, F., & Charlton, S. J. (2014). Investigating the molecular mechanisms through which FTY720‐P causes persistent S1P1 receptor internalization. British Journal of Pharmacology, 171(21), 4797-4807. https://doi.org/10.1111/bph.12620