Document Detail

Patented TGR5 modulators: a review (2006 - present).
MedLine Citation:
PMID:  23039746     Owner:  NLM     Status:  MEDLINE    
INTRODUCTION: The G protein-coupled receptor TGR5 is a key player of the bile acid signaling network, and its activation has been proved to increase the glycemic control, to enhance energy expenditure and to exert anti-inflammatory actions. Accordingly, TGR5 ligands have emerged in drug discovery and preclinical appraisals as promising agents for the treatment of liver diseases, metabolic syndrome and related disorders.
AREAS COVERED: Recent advances in the field of TGR5 modulators are reviewed, with a particular attention on patent applications and peer-reviewed publications in the past 6 years.
EXPERT OPINION: Activation of TGR5 showed to protect mice from diabesity and insulin resistance, to improve liver functions, as well as to attenuate the development of atherosclerosis. However, although the efficacy of TGR5 agonists in mice is encouraging, further studies are needed to determine their potential in humans and to evaluate carefully the balance between the therapeutic benefits and adverse effects associated with the target. The development of new TGR5 selective ligands to support studies in animal models will surely facilitate the understanding of the complexity of TGR5 signaling network.
Antimo Gioiello; Emiliano Rosatelli; Roberto Nuti; Antonio Macchiarulo; Roberto Pellicciari
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Publication Detail:
Type:  Journal Article; Review     Date:  2012-10-06
Journal Detail:
Title:  Expert opinion on therapeutic patents     Volume:  22     ISSN:  1744-7674     ISO Abbreviation:  Expert Opin Ther Pat     Publication Date:  2012 Dec 
Date Detail:
Created Date:  2012-11-20     Completed Date:  2013-05-10     Revised Date:  2013-11-06    
Medline Journal Info:
Nlm Unique ID:  9516419     Medline TA:  Expert Opin Ther Pat     Country:  England    
Other Details:
Languages:  eng     Pagination:  1399-414     Citation Subset:  IM    
Dipartimento di Chimica e Tecnologia del Farmaco, University of Perugia, Via del Liceo 1, 06123 Perugia, Italy.
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MeSH Terms
Atherosclerosis / drug therapy,  metabolism
Blood Glucose / drug effects,  metabolism
Cardiovascular Agents / chemistry,  pharmacology*,  therapeutic use
Diabetes Mellitus / blood,  drug therapy,  physiopathology
Drug Design*
Hypoglycemic Agents / chemistry,  pharmacology*,  therapeutic use
Insulin / blood
Insulin Resistance
Molecular Structure
Patents as Topic*
Protein Conformation
Receptors, G-Protein-Coupled / agonists*,  chemistry,  metabolism
Structure-Activity Relationship
Reg. No./Substance:
0/Blood Glucose; 0/Cardiovascular Agents; 0/GPBAR1 protein, human; 0/Hypoglycemic Agents; 0/Insulin; 0/Ligands; 0/Receptors, G-Protein-Coupled

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