All Outputs (3)

Multivalent approaches and beyond: novel tools for the investigation of dopamine D2 receptor pharmacology (2016)
Journal Article
Kopinathan, A., Scammells, P. J., Lane, J. R., & Capuano, B. (2016). Multivalent approaches and beyond: novel tools for the investigation of dopamine D2 receptor pharmacology. Future Medicinal Chemistry, 8(11), 1349-1372. https://doi.org/10.4155/fmc-2016-0010

The dopamine D2 receptor (D2R) has been implicated in the symptomology of disorders such as schizophrenia and Parkinson's disease. Multivalent ligands provide useful tools to investigate emerging concepts of G protein-coupled receptor drug action suc... Read More about Multivalent approaches and beyond: novel tools for the investigation of dopamine D2 receptor pharmacology.

β2-Adrenoceptors on tumor cells play a critical role in stress-enhanced metastasis in a mouse model of breast cancer (2016)
Journal Article
Chang, A., Le, C. P., Walker, A. K., Creed, S. J., Pon, C. K., Albold, S., …Sloan, E. K. (2016). β2-Adrenoceptors on tumor cells play a critical role in stress-enhanced metastasis in a mouse model of breast cancer. Brain, Behavior, and Immunity, 57, 106-115. https://doi.org/10.1016/j.bbi.2016.06.011

© 2016 The Authors Chronic stress accelerates metastasis – the main cause of death in cancer patients – through the activation of β-adrenoceptors (βARs). We have previously shown that β2AR signaling in MDA-MB-231HM breast cancer cells, facilitates in... Read More about β2-Adrenoceptors on tumor cells play a critical role in stress-enhanced metastasis in a mouse model of breast cancer.

The role of kinetic context in apparent biased agonism at GPCRs (2016)
Journal Article
Javitch, J. A., Klein Herenbrink, C., Sykes, D. A., Donthamsetti, P., Canals, M., Coudrat, T., …Lane, J. R. (2016). The role of kinetic context in apparent biased agonism at GPCRs. Nature Communications, 7, Article 10842. https://doi.org/10.1038/ncomms10842

Biased agonism describes the ability of ligands to stabilize different conformations of a GPCR linked to distinct functional outcomes and offers the prospect of designing pathway-specific drugs that avoid on-target side effects. This mechanism is usu... Read More about The role of kinetic context in apparent biased agonism at GPCRs.