Abstract
G protein–coupled receptors (GPCRs) continue to be important discovery targets for the treatment of type 2 diabetes mellitus (T2DM). Many GPCRs are directly involved in the development of insulin resistance and b-cell dysfunction, and in the etiology of inflammation that can lead to obesity induced T2DM. This review summarizes the current literature describing a number of well-validated GPCR targets, but also outlines several new and promising targets for drug discovery. Wehighlight the importance of understanding the role of these receptors in the disease pathology, and their basic pharmacology, which will pave the way to the development of novel pharmacological probes that will enable these targets to fulfill their promise for the treatment of these metabolic disorders.
| Original language | English |
|---|---|
| Pages (from-to) | 39-67 |
| Number of pages | 29 |
| Journal | Pharmacological Reviews |
| Volume | 70 |
| Issue number | 1 |
| DOIs | |
| Publication status | Published - 1 Jan 2018 |
Cite this
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G protein–coupled receptors targeting insulin resistance, obesity, and type 2 diabetes mellitus. / Riddy, Darren M.; Delerive, Philippe; Summers, Roger J.; Sexton, Patrick; Langmead, Christopher J.
In: Pharmacological Reviews, Vol. 70, No. 1, 01.01.2018, p. 39-67.Research output: Contribution to journal › Review Article › Research › peer-review
TY - JOUR
T1 - G protein–coupled receptors targeting insulin resistance, obesity, and type 2 diabetes mellitus
AU - Riddy, Darren M.
AU - Delerive, Philippe
AU - Summers, Roger J.
AU - Sexton, Patrick
AU - Langmead, Christopher J.
PY - 2018/1/1
Y1 - 2018/1/1
N2 - G protein–coupled receptors (GPCRs) continue to be important discovery targets for the treatment of type 2 diabetes mellitus (T2DM). Many GPCRs are directly involved in the development of insulin resistance and b-cell dysfunction, and in the etiology of inflammation that can lead to obesity induced T2DM. This review summarizes the current literature describing a number of well-validated GPCR targets, but also outlines several new and promising targets for drug discovery. Wehighlight the importance of understanding the role of these receptors in the disease pathology, and their basic pharmacology, which will pave the way to the development of novel pharmacological probes that will enable these targets to fulfill their promise for the treatment of these metabolic disorders.
AB - G protein–coupled receptors (GPCRs) continue to be important discovery targets for the treatment of type 2 diabetes mellitus (T2DM). Many GPCRs are directly involved in the development of insulin resistance and b-cell dysfunction, and in the etiology of inflammation that can lead to obesity induced T2DM. This review summarizes the current literature describing a number of well-validated GPCR targets, but also outlines several new and promising targets for drug discovery. Wehighlight the importance of understanding the role of these receptors in the disease pathology, and their basic pharmacology, which will pave the way to the development of novel pharmacological probes that will enable these targets to fulfill their promise for the treatment of these metabolic disorders.
UR - http://www.scopus.com/inward/record.url?scp=85040020831&partnerID=8YFLogxK
U2 - 10.1124/pr.117.014373
DO - 10.1124/pr.117.014373
M3 - Review Article
VL - 70
SP - 39
EP - 67
JO - Pharmacological Reviews
JF - Pharmacological Reviews
SN - 1521-0081
IS - 1
ER -