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CryoEM structure of Gq-coupled MRGPRX1 with peptide agonist BAM8-22 & ML382


ABSTRACT:

SUBMITTER: Jonathan Firoze Fay 

PROVIDER: EMPIAR-11188 | biostudies-other |

REPOSITORIES: biostudies-other

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Publications

Ligand recognition and allosteric modulation of the human MRGPRX1 receptor.

Liu Yongfeng Y   Cao Can C   Huang Xi-Ping XP   Gumpper Ryan H RH   Rachman Moira M MM   Shih Sheng-Luen SL   Krumm Brian E BE   Zhang Shicheng S   Shoichet Brian K BK   Fay Jonathan F JF   Roth Bryan L BL  

Nature chemical biology 20221027 4


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 nociception and pruritus. Central activation of MRGPRX1 by the endogenous opioid peptide fragment BAM8-22 and its positive allosteric modulator ML382 has been shown to effectively inhibit persistent pain, making MRGPRX1 a promising target for non-opioid pain treatment. However, the activation mechanism of MRGPRX1 is still largely  ...[more]

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