Targeting appetite and satiety in diabetes and obesity, via G protein-coupled receptors

Targeting appetite and satiety in diabetes and obesity, via G protein-coupled receptors

[Display omitted] Type 2 diabetes and obesity have reached pandemic proportions throughout the world, so much so that the World Health Organisation coined the term “Globesity” to help encapsulate the magnitude of the problem. G protein-coupled receptors (GPCRs) are highly tractable drug targets due...

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Bibliographic Details
Published in:Biochemical pharmacology Vol. 202; p. 115115
Main Authors: Piper, Noah B.C., Whitfield, Emily A., Stewart, Gregory D., Xu, Xiaomeng, Furness, Sebastian G.B.
Format: Journal Article
Language:English
Published: England Elsevier Inc 01-08-2022
Subjects:
Appetite
Diabetes
GPCR
Obesity
Review
Satiety
PP
CTR
VTA
OLETF
β-EP
PVN
Y1;2;3;4;5;6
Review
NTS
MPO
THC
GFP
NAc
NPY
Satiety
ME
AgRP
WT
DMH
Appetite
Obesity
GLP-1
MSH
CCK1R
sCT
CB(1;2)
CCK
AMY
AP
POMC
VMH
MRAP
RAMP(1;3)
PYY
ARC
GIT
MC(1;2;3;4;5)R
GPCR
Diabetes
LH
MRAP2
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Description
Summary:[Display omitted] Type 2 diabetes and obesity have reached pandemic proportions throughout the world, so much so that the World Health Organisation coined the term “Globesity” to help encapsulate the magnitude of the problem. G protein-coupled receptors (GPCRs) are highly tractable drug targets due to their wide involvement in all aspects of physiology and pathophysiology, indeed, GPCRs are the targets of approximately 30% of the currently approved drugs. GPCRs are also broadly involved in key physiologies that underlie type 2 diabetes and obesity including feeding reward, appetite and satiety, regulation of blood glucose levels, energy homeostasis and adipose function. Despite this, only two GPCRs are the target of approved pharmaceuticals for treatment of type 2 diabetes and obesity. In this review we discuss the role of these, and select other candidate GPCRs, involved in various facets of type 2 diabetic or obese pathophysiology, how they might be targeted and the potential reasons why pharmaceuticals against these targets have not progressed to clinical use. Finally, we provide a perspective on the current development pipeline of anti-obesity drugs that target GPCRs.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
ObjectType-Feature-3
content type line 23
ObjectType-Review-1
ISSN:0006-2952
1873-2968
DOI:10.1016/j.bcp.2022.115115