McDonald, Iain M., Austin, Carol, Buck, Ildiko M., Dunstone, David J., Gaffen, John, Griffin, Eric, Harper, Elaine A., Hull, Robert A.D., Kalindjian, S. Barret, Linney, Ian D., Low, Caroline M.R., Patel, Dipa, Pether, Michael J., Raynor, Michelle, Roberts, Sonia P., Shaxted, Mark E., Spencer, John, Steel, Katherine I.M., Sykes, David A., Wright, Paul T. and Xun, Wei (2007) [Letter] Discovery and characterization of novel, potent, non-peptide parathyroid hormone-1 receptor antagonists. Journal of Medicinal Chemistry, 50 (20). pp. 4789-4792. ISSN 0022-2623 (Print), 1520-4804 (Online) (doi:10.1021/jm0707626)

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Abstract

A 1,3,4-benzotriazepine was identified as a suitable lead in our effort toward obtaining a non-peptide parathyroid hormone-1 receptor (PTHIR) antagonist. A process of optimization afforded derivatives displaying nanomolar PTHIR affinity, a representative example of which behaved as a PTHIR antagonist in cell-based cyclic adenosine monophosphate (cAMP) assays, with selectivity over PTH2 receptors.

Item Type:	Article
Uncontrolled Keywords:	monoclonal-antibody, protein, growth, ramps, cells, pthrp, bone, osteoprotegerin, specificity, metastasis
Subjects:	Q Science > QD Chemistry R Medicine > R Medicine (General)
Pre-2014 Departments:	School of Science
Related URLs:	Organisation
Last Modified:	14 Oct 2016 09:11
URI:	http://gala.gre.ac.uk/id/eprint/4315

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