Synthesis, functional and binding profile of (R)-apomorphine based homobivalent ligands targeting the dopamine D2 receptor

Shonberg, Jeremy; Lane, J. Robert; Scammells, Peter J; Capuano, Ben

doi:10.1039/c3md00154g

All Outputs (4)

A structure-activity analysis of biased agonism at the dopamine D2 receptor. (2013)
Journal Article
Shonberg, J., Herenbrink, C. K., López, L., Christopoulos, A., Scammells, P. J., Capuano, B., & Lane, J. R. (2013). A structure-activity analysis of biased agonism at the dopamine D2 receptor. Journal of Medicinal Chemistry, 56(22), 9199-9221. https://doi.org/10.1021/jm401318w

Biased agonism offers an opportunity for the medicinal chemist to discover pathway-selective ligands for GPCRs. A number of studies have suggested that biased agonism at the dopamine D2 receptor (D2R) may be advantageous for the treatment of neuropsy... Read More about A structure-activity analysis of biased agonism at the dopamine D2 receptor..

Reverse Engineering of the Selective Agonist TBPB Unveils Both Orthosteric and Allosteric Modes of Action at the M1 Muscarinic Acetylcholine Receptor (2013)
Journal Article
Keov, P., Valant, C., Devine, S. M., Lane, J. R., Scammells, P. J., Sexton, P. M., & Christopoulos, A. (2013). Reverse Engineering of the Selective Agonist TBPB Unveils Both Orthosteric and Allosteric Modes of Action at the M1 Muscarinic Acetylcholine Receptor. Molecular Pharmacology, 84(3), 425-437. https://doi.org/10.1124/mol.113.087320

Recent interest in the M1 muscarinic acetylcholine (ACh) receptor (mAChR) has led to the discovery of various selective agonists for the receptor. The novel selective agonist 1-(1′-(2-methylbenzyl)-1,4′-bipiperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-1 (... Read More about Reverse Engineering of the Selective Agonist TBPB Unveils Both Orthosteric and Allosteric Modes of Action at the M1 Muscarinic Acetylcholine Receptor.

Allosteric approaches to GPCR drug discovery (2013)
Journal Article
Lane, J. R., & Ijzerman, A. P. (2013). Allosteric approaches to GPCR drug discovery. Drug Discovery Today: Technologies, 10(2), e219-e221. https://doi.org/10.1016/j.ddtec.2013.01.006

Synthesis, functional and binding profile of (R)-apomorphine based homobivalent ligands targeting the dopamine D2 receptor (2013)
Journal Article
Shonberg, J., Lane, J. R., Scammells, P. J., & Capuano, B. (2013). Synthesis, functional and binding profile of (R)-apomorphine based homobivalent ligands targeting the dopamine D2 receptor. MedChemComm, 4(9), 1290-1296. https://doi.org/10.1039/c3md00154g

Bivalent ligands represent useful tools to investigate the phenomenon of GPCR dimerization. We synthesized bivalent ligands based on (R)-apomorphine with variations in spacer length, and assessed these compounds in functional and binding assays at th... Read More about Synthesis, functional and binding profile of (R)-apomorphine based homobivalent ligands targeting the dopamine D2 receptor.