PXD038292

PXD038292 is an original dataset announced via ProteomeXchange.

Title	GPR21(m5) GPR21(m5)_P6.29A GPR21(m5)_β2AR
Description	GPR21 is a class-A orphan G protein-coupled receptor (GPCR) and a potential therapeutic target for type 2 diabetes and other metabolic disorders. This receptor shows high basal activity in coupling to multiple G proteins in the absence of any known endogenous agonist or synthetic ligand. Here, we present the structures of ligand-free human GPR21 bound to heterotrimeric miniGs and miniG15 proteins, respectively. We identified an agonist-like motif in extracellular loop 2 (ECL2) that occupies the orthosteric pocket and promotes receptor activation. A side pocket that may be employed as a new ligand binding site was also uncovered.These findings will enable the design of modulators for GPR21 for understanding its signal transduction and exploring opportunity for deorphanization
HostingRepository	iProX
AnnounceDate	2022-11-23
AnnouncementXML	Submission_2023-01-03_01:48:58.455.xml
DigitalObjectIdentifier
ReviewLevel	Peer-reviewed dataset
DatasetOrigin	Original dataset
RepositorySupport	Unsupported dataset by repository
PrimarySubmitter	Ao Qi
SpeciesList	scientific name: Homo sapiens; NCBI TaxID: 9606;
ModificationList	No PTMs are included in the dataset
Instrument	Orbitrap Fusion ETD

Revision	Datetime	Status	ChangeLog Entry
0	2022-11-22 19:07:45	ID requested
⏵ 1	2023-01-03 01:48:58	announced

Dataset with its publication pending

submitter keyword: GPR21 LC-MSMS

Jie Zheng
contact affiliation	The Drug Research Center of Immunological Diseases, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
contact email	jzheng@simm.ac.cn
lab head
Ao Qi
contact affiliation	The Drug Research Center of Immunological Diseases, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
contact email	qiao21@mails.ucas.ac.cn
dataset submitter

iProX dataset URI