Abstract
The metabotropic glutamate (mGlu) receptor family is a potential therapeutic target for multiple central nervous system (CNS) disorders. However, aspects of mGlu receptor signaling and their role in neural pathways remain to be fully elucidated. Novel subtype selective allosteric modulators have revealed new roles for mGlu receptors in brain health and disease, as well as expanding on previously underappreciated aspects of mGlu signaling such as biased agonism and modulation. Recent advances have improved our understanding of mGlu receptor function. Harnessing these new insights to inform drug discovery programs has the potential to lead to the design and discovery of mGlu allosteric modulators that specifically drive glutamatergic activity toward therapeutically beneficial effects and avoid on-target adverse effect liability.
| Original language | English |
|---|---|
| Pages (from-to) | 49-55 |
| Number of pages | 7 |
| Journal | Current Opinion in Pharmacology |
| Volume | 32 |
| DOIs | |
| Publication status | Published - 1 Feb 2017 |
Cite this
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Neurobiological insights and novel therapeutic opportunities for CNS disorders from mGlu receptor allosteric and biased modulation. / Hellyer, Shane; Leach, Katie; Gregory, Karen J.
In: Current Opinion in Pharmacology, Vol. 32, 01.02.2017, p. 49-55.Research output: Contribution to journal › Review Article › Research › peer-review
TY - JOUR
T1 - Neurobiological insights and novel therapeutic opportunities for CNS disorders from mGlu receptor allosteric and biased modulation
AU - Hellyer, Shane
AU - Leach, Katie
AU - Gregory, Karen J
PY - 2017/2/1
Y1 - 2017/2/1
N2 - The metabotropic glutamate (mGlu) receptor family is a potential therapeutic target for multiple central nervous system (CNS) disorders. However, aspects of mGlu receptor signaling and their role in neural pathways remain to be fully elucidated. Novel subtype selective allosteric modulators have revealed new roles for mGlu receptors in brain health and disease, as well as expanding on previously underappreciated aspects of mGlu signaling such as biased agonism and modulation. Recent advances have improved our understanding of mGlu receptor function. Harnessing these new insights to inform drug discovery programs has the potential to lead to the design and discovery of mGlu allosteric modulators that specifically drive glutamatergic activity toward therapeutically beneficial effects and avoid on-target adverse effect liability.
AB - The metabotropic glutamate (mGlu) receptor family is a potential therapeutic target for multiple central nervous system (CNS) disorders. However, aspects of mGlu receptor signaling and their role in neural pathways remain to be fully elucidated. Novel subtype selective allosteric modulators have revealed new roles for mGlu receptors in brain health and disease, as well as expanding on previously underappreciated aspects of mGlu signaling such as biased agonism and modulation. Recent advances have improved our understanding of mGlu receptor function. Harnessing these new insights to inform drug discovery programs has the potential to lead to the design and discovery of mGlu allosteric modulators that specifically drive glutamatergic activity toward therapeutically beneficial effects and avoid on-target adverse effect liability.
UR - http://www.scopus.com/inward/record.url?scp=84994761123&partnerID=8YFLogxK
U2 - 10.1016/j.coph.2016.10.007
DO - 10.1016/j.coph.2016.10.007
M3 - Review Article
VL - 32
SP - 49
EP - 55
JO - Current Opinion in Pharmacology
JF - Current Opinion in Pharmacology
SN - 1471-4892
ER -