MAS-related G protein-coupled receptors X (MRGPRX): Orphan GPCRs with potential as targets for future drugs

G Al Hamwi, YK Riedel, S Clemens… - Pharmacology & …, 2022 - Elsevier
MAS-related G protein-coupled receptors (GPCRs) of subfamily X, designated MRGPRX,
are primate-specific orphan receptors that belong to the δ-branch of rhodopsin-like, class A …

Structure, function and pharmacology of human itch GPCRs

C Cao, HJ Kang, I Singh, H Chen, C Zhang, W Ye… - Nature, 2021 - nature.com
The MRGPRX family of receptors (MRGPRX1–4) is a family of mas-related G-protein-
coupled receptors that have evolved relatively recently. Of these, MRGPRX2 and MRGPRX4 …

Illuminating the understudied GPCR-ome

S Majumdar, Y Chiu, JE Pickett, BL Roth - Drug Discovery Today, 2023 - Elsevier
G-protein-coupled receptors (GPCRs) are the target of> 30% of approved drugs. Despite
their popularity, many of the> 800 human GPCRs remain understudied. The Illuminating the …

Ligand recognition and allosteric modulation of the human MRGPRX1 receptor

Y Liu, C Cao, XP Huang, RH Gumpper… - Nature Chemical …, 2023 - nature.com
The human MAS-related G protein–coupled receptor X1 (MRGPRX1) is preferentially
expressed in the small-diameter primary sensory neurons and involved in the mediation of …

Oncostatin M can sensitize sensory neurons in inflammatory pruritus

PY Tseng, MA Hoon - Science translational medicine, 2021 - science.org
Chronic itch is a major symptom of many inflammatory skin diseases. This type of pruritus is
thought to be facilitated by cytokines that activate cutaneous nerve fibers; however, the …

Transcriptome profiling of microRNAs reveals potential mechanisms of manual therapy alleviating neuropathic pain through microRNA-547-3p-mediated Map4k4/NF …

C Yao, J Ren, R Huang, C Tang, Y Cheng, Z Lv… - Journal of …, 2022 - Springer
Background Local neuroinflammation secondary to spinal nerve compression in lumbar disk
herniation (LDH) is a key driver contributing to neuropathic pain. Manual therapy (MT), a …

Nppb neurons are sensors of mast cell-induced itch

HJ Solinski, MC Kriegbaum, PY Tseng, TW Earnest… - Cell reports, 2019 - cell.com
Itch is an unpleasant skin sensation that can be triggered by exposure to many chemicals,
including those released by mast cells. The natriuretic polypeptide b (Nppb)-expressing …

Ligand recognition and G protein coupling of the human itch receptor MRGPRX1

L Guo, Y Zhang, G Fang, L Tie, Y Zhuang, C Xue… - Nature …, 2023 - nature.com
MRGPRX1, a Mas-related GPCR (MRGPR), is a key receptor for itch perception and
targeting MRGPRX1 may have potential to treat both chronic itch and pain. Here we report …

scRNA-sequencing reveals subtype-specific transcriptomic perturbations in DRG neurons of PirtEGFPf mice in neuropathic pain condition

C Zhang, MW Hu, XW Wang, X Cui, J Liu, Q Huang… - Elife, 2022 - elifesciences.org
Functionally distinct subtypes/clusters of dorsal root ganglion (DRG) neurons may play
different roles in nerve regeneration and pain. However, details about their transcriptomic …

Activation of µ-δ opioid receptor heteromers inhibits neuropathic pain behavior in rodents

V Tiwari, SQ He, Q Huang, L Liang, F Yang, Z Chen… - Pain, 2020 - journals.lww.com
Several reports support the idea that m-and d-opioid receptors (ORs) may exist as
heterodimers in brain regions involved in pain signaling. The unique pharmacology of these …