Literature DB >> 17850061

Discovery and characterization of novel, potent, non-peptide parathyroid hormone-1 receptor antagonists.

Iain M McDonald1, Carol Austin, Ildiko M Buck, David J Dunstone, John Gaffen, Eric Griffin, Elaine A Harper, Robert A D Hull, S Barret Kalindjian, Ian D Linney, Caroline M R Low, Dipa Patel, Michael J Pether, Michelle Raynor, Sonia P Roberts, Mark E Shaxted, John Spencer, Katherine I M Steel, David A Sykes, Paul T Wright, Wei Xun.   

Abstract

A 1,3,4-benzotriazepine was identified as a suitable lead in our effort toward obtaining a non-peptide parathyroid hormone-1 receptor (PTH1R) antagonist. A process of optimization afforded derivatives displaying nanomolar PTH1R affinity, a representative example of which behaved as a PTH1R antagonist in cell-based cyclic adenosine monophosphate (cAMP) assays, with selectivity over PTH2 receptors.

Entities:  

Mesh:

Substances:

Year:  2007        PMID: 17850061     DOI: 10.1021/jm0707626

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  6 in total

1.  Actions of the small molecule ligands SW106 and AH-3960 on the type-1 parathyroid hormone receptor.

Authors:  Percy H Carter; Thomas Dean; Brijesh Bhayana; Ashok Khatri; Raj Rajur; Thomas J Gardella
Journal:  Mol Endocrinol       Date:  2015-01-13

2.  An Inverse Agonist Ligand of the PTH Receptor Partially Rescues Skeletal Defects in a Mouse Model of Jansen's Metaphyseal Chondrodysplasia.

Authors:  Hiroshi Noda; Jun Guo; Ashok Khatri; Thomas Dean; Monica Reyes; Michael Armanini; Daniel J Brooks; Janaina S Martins; Ernestina Schipani; Mary L Bouxsein; Marie B Demay; John T Potts; Harald Jüppner; Thomas J Gardella
Journal:  J Bone Miner Res       Date:  2019-12-04       Impact factor: 6.741

Review 3.  International Union of Basic and Clinical Pharmacology. XCIII. The parathyroid hormone receptors--family B G protein-coupled receptors.

Authors:  Thomas J Gardella; Jean-Pierre Vilardaga
Journal:  Pharmacol Rev       Date:  2015       Impact factor: 25.468

4.  Application of Daugulis copper-catalyzed direct arylation to the synthesis of 5-aryl benzotriazepines.

Authors:  Sirilata Yotphan; Robert G Bergman; Jonathan A Ellman
Journal:  Org Lett       Date:  2009-04-02       Impact factor: 6.005

Review 5.  Evolution of parathyroid hormone receptor family and their ligands in vertebrate.

Authors:  Jason S W On; Billy K C Chow; Leo T O Lee
Journal:  Front Endocrinol (Lausanne)       Date:  2015-03-10       Impact factor: 5.555

6.  Small Molecule Inhibited Parathyroid Hormone Mediated cAMP Response by N-Terminal Peptide Binding.

Authors:  Amit Kumar; Monika Baumann; Jochen Balbach
Journal:  Sci Rep       Date:  2016-03-02       Impact factor: 4.379

  6 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.