Outputs (25)

Analysis of sequence divergence in mammalian abcgs predicts a structural network of residues that underlies functional divergence (2021)
Journal Article
Mitchell-White, J. I., Stockner, T., Holliday, N., Briddon, S. J., & Kerr, I. D. (2021). Analysis of sequence divergence in mammalian abcgs predicts a structural network of residues that underlies functional divergence. International Journal of Molecular Sciences, 22(6), 1-16. https://doi.org/10.3390/ijms22063012

© 2021 by the authors. Licensee MDPI, Basel, Switzerland. The five members of the mammalian G subfamily of ATP-binding cassette transporters differ greatly in their substrate specificity. Four members of the subfamily are important in lipid transport... Read More about Analysis of sequence divergence in mammalian abcgs predicts a structural network of residues that underlies functional divergence.

Heterodimeric Analogues of the Potent Y1R Antagonist 1229U91, Lacking One of the Pharmacophoric C-Terminal Structures, Retain Potent Y1R Affinity and Show Improved Selectivity over Y4R (2020)
Journal Article
Richardson, R. R., Richardson, R., Groenen, M., Liu, M., Mountford, S. J., Briddon, S. J., Holliday, N. D., & Thompson, P. E. (2020). Heterodimeric Analogues of the Potent Y1R Antagonist 1229U91, Lacking One of the Pharmacophoric C-Terminal Structures, Retain Potent Y1R Affinity and Show Improved Selectivity over Y4R. Journal of Medicinal Chemistry, 63(10), 5274-5286. https://doi.org/10.1021/acs.jmedchem.0c00027

The cyclic dimeric peptide 1229U91 (GR231118) has an unusual structure and displays potent, insurmountable antagonism of the Y1 receptor. To probe the structural basis for this activity, we have prepared ring size variants and heterodimeric compounds... Read More about Heterodimeric Analogues of the Potent Y1R Antagonist 1229U91, Lacking One of the Pharmacophoric C-Terminal Structures, Retain Potent Y1R Affinity and Show Improved Selectivity over Y4R.

Red-Emitting Dibenzodiazepinone Derivatives as Fluorescent Dualsteric Probes for the Muscarinic Acetylcholine M2 Receptor (2020)
Journal Article
She, X., Pegoli, A., Gruber, C. G., Wifling, D., Carpenter, J., Hübner, H., Chen, M., Wan, J., Bernhardt, G., Gmeiner, P., Holliday, N. D., & Keller, M. (2020). Red-Emitting Dibenzodiazepinone Derivatives as Fluorescent Dualsteric Probes for the Muscarinic Acetylcholine M2 Receptor. Journal of Medicinal Chemistry, 63(8), 4133-4154. https://doi.org/10.1021/acs.jmedchem.9b02172

Fluorescently labeled dibenzodiazepinone-type muscarinic acetylcholine receptor (MR) antagonists, including dimeric ligands, were prepared using red-emitting cyanine dyes. Probes containing a fluorophore with negative charge showed high M2R affinitie... Read More about Red-Emitting Dibenzodiazepinone Derivatives as Fluorescent Dualsteric Probes for the Muscarinic Acetylcholine M2 Receptor.

The tetraspanin Tspan15 is an essential subunit of an ADAM10 scissor complex (2020)
Journal Article
Koo, C. Z., Harrison, N., Noy, P. J., Szyroka, J., Matthews, A. L., Hsia, H. E., Müller, S. A., Tüshaus, J., Goulding, J., Willis, K., Apicella, C., Cragoe, B., Davis, E., Keles, M., Malinova, A., McFarlane, T. A., Morrison, P. R., Nguyen, H. T., Sykes, M. C., Ahmed, H., …Tomlinson, M. G. (2020). The tetraspanin Tspan15 is an essential subunit of an ADAM10 scissor complex. Journal of Biological Chemistry, 295(36), 12822-12839. https://doi.org/10.1074/jbc.RA120.012601

© 2020 Koo et al. A disintegrin and metalloprotease 10 (ADAM10) is a transmembrane protein essential for embryonic development, and its dysregulation underlies disorders such as cancer, Alzheimer's disease, and inflammation. ADAM10 is a "molecular sc... Read More about The tetraspanin Tspan15 is an essential subunit of an ADAM10 scissor complex.

Application of fluorescence correlation spectroscopy to study substrate binding in styrene maleic acid lipid copolymer encapsulated ABCG2 (2020)
Journal Article
Horsey, A. J., Briggs, D. A., Holliday, N. D., Briddon, S. J., & Kerr, I. D. (2020). Application of fluorescence correlation spectroscopy to study substrate binding in styrene maleic acid lipid copolymer encapsulated ABCG2. BBA - Biomembranes, 1862(6), Article 183218. https://doi.org/10.1016/j.bbamem.2020.183218

© 2020 The Authors ABCG2 is one of a trio of human ATP binding cassette transporters that have the ability to bind and transport a diverse array of chemical substrates out of cells. This so-called “multidrug” transport has numerous physiological cons... Read More about Application of fluorescence correlation spectroscopy to study substrate binding in styrene maleic acid lipid copolymer encapsulated ABCG2.

Fluorescence Labeling of Neurotensin(8–13) via Arginine Residues Gives Molecular Tools with High Receptor Affinity (2019)
Journal Article
Bernhardt, G., Keller, M., Mahuroof, S. A., Hong Yee, V., Carpenter, J., Schindler, L., Littmann, T., Pegoli, A., Hübner, H., Gmeiner, P., & Holliday, N. D. (2020). Fluorescence Labeling of Neurotensin(8–13) via Arginine Residues Gives Molecular Tools with High Receptor Affinity. ACS Medicinal Chemistry Letters, 11, 16-22. https://doi.org/10.1021/acsmedchemlett.9b00462

Fluorescence-labeled receptor ligands have emerged as valuable molecular tools, being indispensable for studying receptor–ligand interactions by fluorescence-based techniques such as high-content imaging, fluorescence microscopy, and fluorescence pol... Read More about Fluorescence Labeling of Neurotensin(8–13) via Arginine Residues Gives Molecular Tools with High Receptor Affinity.

Tetraspanin Tspan15 is an essential subunit of an ADAM10 scissor complex (2019)
Preprint / Working Paper
Koo, C. Z., Harrison, N., Noy, P. J., Szyroka, J., Matthews, A. L., Hsia, H.-E., Mueller, S. A., Tüshaus, J., Goulding, J., Willis, K., Apicella, C., Cragoe, B., Davis, E., Keles, M., Malinova, A., McFarlane, T. A., Morrison, P. R., Sykes, M. C., Ahmed, H., Di Maio, A., …Tomlinson, M. G. (2019). Tetraspanin Tspan15 is an essential subunit of an ADAM10 scissor complex

A disintegrin and metalloprotease 10 (ADAM10) is essential for embryonic development and impacts on diseases such as cancer, Alzheimer’s and inflammatory diseases. ADAM10 is a ‘molecular scissor’ that proteolytically cleaves the extracellular region... Read More about Tetraspanin Tspan15 is an essential subunit of an ADAM10 scissor complex.

The peptide PnPP-19, a spider toxin derivative, activates μ-opioid receptors and modulates calcium channels (2018)
Journal Article
Freitas, A. C., Peigneur, S., Macedo, F. H., Menezes-Filho, J. E., Millns, P., Medeiros, L. F., Arruda, M. A., Cruz, J., Holliday, N. D., Tytgat, J., Hathway, G., & de Lima, M. E. (2018). The peptide PnPP-19, a spider toxin derivative, activates μ-opioid receptors and modulates calcium channels. Toxins, 10(1), 1-12. https://doi.org/10.3390/toxins10010043

The synthetic peptide PnPP-19 comprehends 19 amino acid residues and it represents part of the primary structure of the toxin δ-CNTX-Pn1c (PnTx2-6), isolated from the venom of the spider Phoneutria nigriventer. Behavioural tests suggest that PnPP-19... Read More about The peptide PnPP-19, a spider toxin derivative, activates μ-opioid receptors and modulates calcium channels.

Extrapyramidal side effects of antipsychotics are linked to their association kinetics at dopamine D2 receptors (2017)
Journal Article
Sykes, D. A., Moore, H., Stott, L., Holliday, N., Javitch, J. A., Lane, J. R., & Charlton, S. J. (2017). Extrapyramidal side effects of antipsychotics are linked to their association kinetics at dopamine D2 receptors. Nature Communications, 8(1), Article 763. https://doi.org/10.1038/s41467-017-00716-z

Atypical antipsychotic drugs (APDs) have been hypothesized to show reduced extrapyramidal side effects (EPS) due to their rapid dissociation from the dopamine D2 receptor. However, support for this hypothesis is limited to a relatively small number o... Read More about Extrapyramidal side effects of antipsychotics are linked to their association kinetics at dopamine D2 receptors.

Identification of a Cyanine-dye labeled peptidic ligand for Y₁R and Y₄R, based upon the Neuropeptide Y C-terminal analogue, BVD-15 (2016)
Journal Article
Liu, M., Richardson, R. R., Mountford, S. J., Zhang, L., Tempone, M. H., Herzog, H., Holliday, N. D., & Thompson, P. E. (2016). Identification of a Cyanine-dye labeled peptidic ligand for Y₁R and Y₄R, based upon the Neuropeptide Y C-terminal analogue, BVD-15. Bioconjugate Chemistry, 27(9), 2166-2175. https://doi.org/10.1021/acs.bioconjchem.6b00376

Traceable truncated Neuropeptide Y (NPY) analogues with Y₁ receptor (Y₁R) affinity and selectivity are highly desirable tools in studying receptor location, regulation, and biological functions. A range of fluorescently labeled analogues of a reporte... Read More about Identification of a Cyanine-dye labeled peptidic ligand for Y₁R and Y₄R, based upon the Neuropeptide Y C-terminal analogue, BVD-15.