Literature DB >> 20161662

Human TSH receptor ligands as pharmacological probes with potential clinical application.

Susanne Neumann1, Bruce M Raaka, Marvin C Gershengorn.   

Abstract

The biologic role of thyroid-stimulating hormone (TSH; thyrotropin) as an activator (agonist) of the TSH receptor (TSHR) in the hypothalamic-pituitary-thyroid axis is well known and activation of TSHR by recombinant human TSH is used clinically in patients with thyroid cancer. TSHR ligands other than TSH could be used to probe TSHR biology in thyroidal and extrathyroidal tissues, and potentially be employed in patients. A number of different TSHR ligands have been reported, including TSH analogs, antibodies and small-molecule, drug-like compounds. In this review, we will provide an update on all these classes of TSHR agonists and antagonists but place emphasis on small-molecule ligands.

Entities:  

Year:  2009        PMID： 20161662      PMCID： PMC2819035          DOI： 10.1586/eem.09.36

Source DB:  PubMed          Journal:  Expert Rev Endocrinol Metab        ISSN： 1744-6651


  91 in total

1.  Bioengineering of human thyrotropin superactive analogs by site-directed "lysine-scanning" mutagenesis. Cooperative effects between peripheral loops.

Authors:  H Leitolf; K P Tong; M Grossmann; B D Weintraub; M W Szkudlinski
Journal:  J Biol Chem       Date:  2000-09-01       Impact factor: 5.157

2.  Small molecule biaryl FSH receptor agonists. Part 1: Lead discovery via encoded combinatorial synthesis.

Authors:  Tao Guo; Anton E P Adang; Roland E Dolle; Guizhen Dong; Dan Fitzpatrick; Peng Geng; Koc-Kan Ho; Steven G Kultgen; Ruiyan Liu; Edward McDonald; Brian F McGuinness; Kurt W Saionz; Kenneth J Valenzano; Nicole C R van Straten; Dan Xie; Maria L Webb
Journal:  Bioorg Med Chem Lett       Date:  2004-04-05       Impact factor: 2.823

Review 3.  Recent developments in constitutive receptor activity and inverse agonism, and their potential for GPCR drug discovery.

Authors:  Richard A Bond; Ad P Ijzerman
Journal:  Trends Pharmacol Sci       Date:  2006-01-06       Impact factor: 14.819

4.  Evidence that the thyrotropin receptor ectodomain contains not one, but two, cleavage sites.

Authors:  G D Chazenbalk; K Tanaka; Y Nagayama; A Kakinuma; J C Jaume; S M McLachlan; B Rapoport
Journal:  Endocrinology       Date:  1997-07       Impact factor: 4.736

5.  Evaluation of small-molecule modulators of the luteinizing hormone/choriogonadotropin and thyroid stimulating hormone receptors: structure-activity relationships and selective binding patterns.

Authors:  Susanna Moore; Holger Jaeschke; Gunnar Kleinau; Susanne Neumann; Stefano Costanzi; Jian-kang Jiang; John Childress; Bruce M Raaka; Anny Colson; Ralf Paschke; Gerd Krause; Craig J Thomas; Marvin C Gershengorn
Journal:  J Med Chem       Date:  2006-06-29       Impact factor: 7.446

6.  Thyroid-stimulating hormone restores bone volume, microarchitecture, and strength in aged ovariectomized rats.

Authors:  T Kuber Sampath; Petra Simic; Rebecca Sendak; Natasa Draca; Ann E Bowe; Stephen O'Brien; Susan C Schiavi; John M McPherson; Slobodan Vukicevic
Journal:  J Bone Miner Res       Date:  2007-06       Impact factor: 6.741

7.  The thyrotrophin hormone receptor of Graves' disease: overexpression of the extracellular domain in insect cells using recombinant baculovirus, immunoaffinity purification and analysis of autoantibody binding.

Authors:  G C Huang; M J Page; L B Nicholson; K S Collison; A M McGregor; J P Banga
Journal:  J Mol Endocrinol       Date:  1993-04       Impact factor: 5.098

8.  Expression of thyrotropin receptor on clonal osteoblast-like rat osteosarcoma cells.

Authors:  M Inoue; M Tawata; N Yokomori; T Endo; T Onaya
Journal:  Thyroid       Date:  1998-11       Impact factor: 6.568

9.  A low molecular weight agonist signals by binding to the transmembrane domain of thyroid-stimulating hormone receptor (TSHR) and luteinizing hormone/chorionic gonadotropin receptor (LHCGR).

Authors:  Holger Jäschke; Susanne Neumann; Susanna Moore; Craig J Thomas; Anny-Odile Colson; Stefano Costanzi; Gunnar Kleinau; Jian-Kang Jiang; Ralf Paschke; Bruce M Raaka; Gerd Krause; Marvin C Gershengorn
Journal:  J Biol Chem       Date:  2006-02-16       Impact factor: 5.157

10.  Thyrocyte-specific Gq/G11 deficiency impairs thyroid function and prevents goiter development.

Authors:  Jukka Kero; Kashan Ahmed; Nina Wettschureck; Sorin Tunaru; Tim Wintermantel; Erich Greiner; Günther Schütz; Stefan Offermanns
Journal:  J Clin Invest       Date:  2007-09       Impact factor: 14.808
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  10 in total

1.  Small molecule TSHR agonists and antagonists.

Authors:  S Neumann; M C Gershengorn
Journal:  Ann Endocrinol (Paris)       Date:  2011-04-20       Impact factor: 2.478

2.  History of the clinical endocrinology branch of the National Institute of Diabetes and Digestive and Kidney Diseases: impact on understanding and treatment of diseases of the thyroid gland.

Authors:  Marvin C Gershengorn
Journal:  Thyroid       Date:  2012-01-18       Impact factor: 6.568

3.  Constitutively active thyrotropin and thyrotropin-releasing hormone receptors and their inverse agonists.

Authors:  Susanne Neumann; Bruce M Raaka; Marvin C Gershengorn
Journal:  Methods Enzymol       Date:  2010       Impact factor: 1.600

4.  A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.

Authors:  Susanne Neumann; Wenwei Huang; Elena Eliseeva; Steve Titus; Craig J Thomas; Marvin C Gershengorn
Journal:  Endocrinology       Date:  2010-04-28       Impact factor: 4.736

5.  Mutations that silence constitutive signaling activity in the allosteric ligand-binding site of the thyrotropin receptor.

Authors:  Ann-Karin Haas; Gunnar Kleinau; Inna Hoyer; Susanne Neumann; Jens Furkert; Claudia Rutz; Ralf Schülein; Marvin C Gershengorn; Gerd Krause
Journal:  Cell Mol Life Sci       Date:  2010-07-22       Impact factor: 9.261

Review 6.  Novel insights on thyroid-stimulating hormone receptor signal transduction.

Authors:  Gunnar Kleinau; Susanne Neumann; Annette Grüters; Heiko Krude; Heike Biebermann
Journal:  Endocr Rev       Date:  2013-05-03       Impact factor: 19.871

Review 7.  Structural-Functional Features of the Thyrotropin Receptor: A Class A G-Protein-Coupled Receptor at Work.

Authors:  Gunnar Kleinau; Catherine L Worth; Annika Kreuchwig; Heike Biebermann; Patrick Marcinkowski; Patrick Scheerer; Gerd Krause
Journal:  Front Endocrinol (Lausanne)       Date:  2017-04-24       Impact factor: 5.555

Review 8.  Discovery and Development of Small Molecule Allosteric Modulators of Glycoprotein Hormone Receptors.

Authors:  Selvaraj G Nataraja; Henry N Yu; Stephen S Palmer
Journal:  Front Endocrinol (Lausanne)       Date:  2015-09-14       Impact factor: 5.555

9.  Molecular Insights into the Transmembrane Domain of the Thyrotropin Receptor.

Authors:  Vanessa Chantreau; Bruck Taddese; Mathilde Munier; Louis Gourdin; Daniel Henrion; Patrice Rodien; Marie Chabbert
Journal:  PLoS One       Date:  2015-11-06       Impact factor: 3.240

Review 10.  The Molecular Function and Clinical Role of Thyroid Stimulating Hormone Receptor in Cancer Cells.

Authors:  Yu-De Chu; Chau-Ting Yeh
Journal:  Cells       Date:  2020-07-20       Impact factor: 6.600
  10 in total

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