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CryoEM structure of Gq-coupled MRGPRX4 with fospropofol bound


ABSTRACT:

SUBMITTER: Jonathan Firoze Fay 

PROVIDER: EMPIAR-11986 | biostudies-other |

REPOSITORIES: biostudies-other

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Publications

MRGPRX4 mediates phospho-drug-associated pruritus in a humanized mouse model.

Chien Daphne Chun-Che DC   Limjunyawong Nathachit N   Cao Can C   Meixiong James J   Peng Qi Q   Ho Cheng-Ying CY   Fay Jonathan F JF   Roth Bryan L BL   Dong Xinzhong X  

Science translational medicine 20240508 746


The phosphate modification of drugs is a common chemical strategy to increase solubility and allow for parenteral administration. Unfortunately, phosphate modifications often elicit treatment- or dose-limiting pruritus through an unknown mechanism. Using unbiased high-throughput drug screens, we identified the Mas-related G protein-coupled receptor X4 (MRGPRX4), a primate-specific, sensory neuron receptor previously implicated in itch, as a potential target for phosphate-modified compounds. Usin  ...[more]

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