All Outputs (3)

M1 muscarinic receptor activation reduces the molecular pathology and slows the progression of prion-mediated neurodegenerative disease (2022)
Journal Article
Dwomoh, L., Rossi, M., Scarpa, M., Khajehali, E., Molloy, C., Herzyk, P., …Tobin, A. B. (2022). M1 muscarinic receptor activation reduces the molecular pathology and slows the progression of prion-mediated neurodegenerative disease. Science Signaling, 15(760), 00. https://doi.org/10.1126/scisignal.abm3720

Many dementias are propagated through the spread of “prion-like” misfolded proteins. This includes prion diseases themselves (such as Creutzfeldt-Jakob disease) and Alzheimer’s disease (AD), for which no treatments are available to slow or stop progr... Read More about M1 muscarinic receptor activation reduces the molecular pathology and slows the progression of prion-mediated neurodegenerative disease.

Development of fluorescent peptide G protein-coupled receptor activation biosensors for NanoBRET characterization of intracellular allosteric modulators (2022)
Journal Article
Farmer, J. P., Mistry, S. N., Laughton, C. A., & Holliday, N. D. (2022). Development of fluorescent peptide G protein-coupled receptor activation biosensors for NanoBRET characterization of intracellular allosteric modulators. FASEB Journal, 36(11), Article e22576. https://doi.org/10.1096/fj.202201024R

G protein-coupled receptors (GPCRs) are widely therapeutically targeted, and recent advances in allosteric modulator development at these receptors offer further potential for exploitation. Intracellular allosteric modulators (IAM) represent a class... Read More about Development of fluorescent peptide G protein-coupled receptor activation biosensors for NanoBRET characterization of intracellular allosteric modulators.

Optimization of Peptide Linker-Based Fluorescent Ligands for the Histamine H1 Receptor (2022)
Journal Article
Kok, Z. Y., Stoddart, L. A., Mistry, S. J., Mocking, T. A., Vischer, H. F., Leurs, R., …Kellam, B. (2022). Optimization of Peptide Linker-Based Fluorescent Ligands for the Histamine H1 Receptor. Journal of Medicinal Chemistry, 65(12), 8258–8288. https://doi.org/10.1021/acs.jmedchem.2c00125

The histamine H1 receptor (H1R) has recently been implicated in mediating cell proliferation and cancer progression, therefore high affinity H1R-selective fluorescent ligands are desirable tools for further investigation of this behaviour in vitro an... Read More about Optimization of Peptide Linker-Based Fluorescent Ligands for the Histamine H1 Receptor.