Small Molecule Ghrelin Receptor Inverse Agonists and Antagonists

2014 ◽  
Vol 57 (21) ◽  
pp. 8671-8691 ◽  
Author(s):  
Kimberly O. Cameron ◽  
Samit K. Bhattacharya ◽  
A. Katrina Loomis
Keyword(s):  
Small Molecule ◽  
Inverse Agonists ◽  
Ghrelin Receptor

Identification of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor

2012 ◽  
Vol 22 (13) ◽  
pp. 4281-4287 ◽  
Author(s):  
Daniel W. Kung ◽  
Steven B. Coffey ◽  
Ryan M. Jones ◽  
Shawn Cabral ◽  
Wenhua Jiao ◽  
...  
Keyword(s):  
Inverse Agonists ◽  
Ghrelin Receptor

scholarly journals Update in TSH Receptor Agonists and Antagonists

2012 ◽  
Vol 97 (12) ◽  
pp. 4287-4292 ◽  
Author(s):  
Marvin C. Gershengorn ◽  
Susanne Neumann
Keyword(s):  
Thyroid Function ◽  
Small Molecule ◽  
Physiological Role ◽  
Tsh Receptor ◽  
Thyroid Tumors ◽  
Inverse Agonists ◽  
Small Molecule Drug ◽  
Pathological Conditions ◽  
Receptor Agonists And Antagonists

The physiological role of the TSH receptor (TSHR) as a major regulator of thyroid function is well understood, but TSHRs are also expressed in multiple normal extrathyroidal tissues, and the physiological roles of TSHRs in these tissues are unclear. Moreover, TSHRs play a major role in several pathological conditions including hyperthyroidism, hypothyroidism, and thyroid tumors. Small molecule, “drug-like” TSHR agonists, neutral antagonists, and inverse agonists may be useful as probes of TSHR function in extrathyroidal tissues and as leads to develop drugs for several diseases of the thyroid. In this Update, we review the most recent findings regarding the development and use of these small molecule TSHR ligands.

Ghrelin Receptor Inverse Agonists: Identification of an Active Peptide Core and Its Interaction Epitopes on the Receptor

2006 ◽  
Vol 70 (3) ◽  
pp. 936-946 ◽  
Author(s):  
Birgitte Holst ◽  
Manja Lang ◽  
Erik Brandt ◽  
Anders Bach ◽  
Andrew Howard ◽  
...  
Keyword(s):  
Inverse Agonists ◽  
Ghrelin Receptor ◽  
Active Peptide ◽  
Peptide Core

Overlapping Binding Site for the Endogenous Agonist, Small-Molecule Agonists, and Ago-allosteric Modulators on the Ghrelin Receptor

2008 ◽  
Vol 75 (1) ◽  
pp. 44-59 ◽  
Author(s):  
Birgitte Holst ◽  
Thomas M. Frimurer ◽  
Jacek Mokrosinski ◽  
Tine Halkjaer ◽  
Karina B. Cullberg ◽  
...  
Keyword(s):  
Binding Site ◽  
Small Molecule ◽  
Allosteric Modulators ◽  
Ghrelin Receptor

scholarly journals Ghrelin receptor inverse agonists as a novel therapeutic approach against obesity‐related metabolic disease

2017 ◽  
Vol 19 (12) ◽  
pp. 1740-1750 ◽  
Author(s):  
Kathrin Abegg ◽  
Lara Bernasconi ◽  
Melanie Hutter ◽  
Lynda Whiting ◽  
Claudio Pietra ◽  
...  
Keyword(s):  
Metabolic Disease ◽  
Therapeutic Approach ◽  
Inverse Agonists ◽  
Ghrelin Receptor ◽  
Novel Therapeutic

Orally active ghrelin receptor inverse agonists and their actions on a rat obesity model

2015 ◽  
Vol 23 (15) ◽  
pp. 4792-4803 ◽  
Author(s):  
Bitoku Takahashi ◽  
Hideaki Funami ◽  
Takehiko Iwaki ◽  
Hiroshi Maruoka ◽  
Makoto Shibata ◽  
...  
Keyword(s):  
Inverse Agonists ◽  
Ghrelin Receptor ◽  
Orally Active

Design, Evaluation, and Comparison of Ghrelin Receptor Agonists and Inverse Agonists as Suitable Radiotracers for PET Imaging

2012 ◽  
Vol 23 (4) ◽  
pp. 771-784 ◽  
Author(s):  
Constance Chollet ◽  
Ralf Bergmann ◽  
Jens Pietzsch ◽  
Annette G. Beck-Sickinger
Keyword(s):  
Pet Imaging ◽  
Design Evaluation ◽  
Inverse Agonists ◽  
Ghrelin Receptor ◽  
Receptor Agonists

scholarly journals Small-Molecule Ghrelin Receptor Antagonists Improve Glucose Tolerance, Suppress Appetite, and Promote Weight Loss

Endocrinology ◽  
2007 ◽  
Vol 148 (11) ◽  
pp. 5175-5185 ◽  
Author(s):  
William P. Esler ◽  
Joachim Rudolph ◽  
Thomas H. Claus ◽  
Weifeng Tang ◽  
Nicole Barucci ◽  
...  
Keyword(s):  
Weight Loss ◽  
Glucose Tolerance ◽  
Small Molecule ◽  
Receptor Antagonists ◽  
Promote Weight Loss ◽  
Ghrelin Receptor ◽  
Improve Glucose Tolerance

scholarly journals Structural Optimization of Ghrelin Receptor Inverse Agonists to Improve Lipophilicity and Avoid Mechanism-Based CYP3A4 Inactivation

2015 ◽  
Vol 63 (10) ◽  
pp. 825-832 ◽  
Author(s):  
Bitoku Takahashi ◽  
Hideaki Funami ◽  
Makoto Shibata ◽  
Hiroshi Maruoka ◽  
Makoto Koyama ◽  
...  
Keyword(s):  
Structural Optimization ◽  
Inverse Agonists ◽  
Ghrelin Receptor
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