6li2

Crystal structure of GPR52 ligand free form with rubredoxin fusionCrystal structure of GPR52 ligand free form with rubredoxin fusion

Structural highlights

6li2 is a 1 chain structure with sequence from Clostridium pasteurianum and Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:	X-ray diffraction, Resolution 2.8Å
Ligands:	, ,
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

GPR52_HUMAN Gs-coupled receptor activated by antipsychotics reserpine leading to an increase in intracellular cAMP and its internalization (PubMed:24587241). May play a role in locomotor activity through modulation of dopamine, NMDA and ADORA2A-induced locomotor activity. These behavioral changes are accompanied by modulation of the dopamine receptor signaling pathway in striatum (PubMed:24587241). Modulates HTT level via cAMP-dependent but PKA independent mechanisms throught activation of RAB39B that translocates HTT to the endoplasmic reticulum, thus avoiding proteasome degradation (PubMed:25738228).^[1] ^[2] RUBR_CLOPA Rubredoxin is a small nonheme, iron protein lacking acid-labile sulfide. Its single Fe, chelated to 4 Cys, functions as an electron acceptor and may also stabilize the conformation of the molecule.

References

↑ Komatsu H, Maruyama M, Yao S, Shinohara T, Sakuma K, Imaichi S, Chikatsu T, Kuniyeda K, Siu FK, Peng LS, Zhuo K, Mun LS, Han TM, Matsumoto Y, Hashimoto T, Miyajima N, Itoh Y, Ogi K, Habata Y, Mori M. Anatomical transcriptome of G protein-coupled receptors leads to the identification of a novel therapeutic candidate GPR52 for psychiatric disorders. PLoS One. 2014 Feb 28;9(2):e90134. doi: 10.1371/journal.pone.0090134. eCollection, 2014. PMID:24587241 doi:http://dx.doi.org/10.1371/journal.pone.0090134
↑ Yao Y, Cui X, Al-Ramahi I, Sun X, Li B, Hou J, Difiglia M, Palacino J, Wu ZY, Ma L, Botas J, Lu B. A striatal-enriched intronic GPCR modulates huntingtin levels and toxicity. Elife. 2015 Mar 4;4. doi: 10.7554/eLife.05449. PMID:25738228 doi:http://dx.doi.org/10.7554/eLife.05449

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OCA

[1] Komatsu H, Maruyama M, Yao S, Shinohara T, Sakuma K, Imaichi S, Chikatsu T, Kuniyeda K, Siu FK, Peng LS, Zhuo K, Mun LS, Han TM, Matsumoto Y, Hashimoto T, Miyajima N, Itoh Y, Ogi K, Habata Y, Mori M. Anatomical transcriptome of G protein-coupled receptors leads to the identification of a novel therapeutic candidate GPR52 for psychiatric disorders. PLoS One. 2014 Feb 28;9(2):e90134. doi: 10.1371/journal.pone.0090134. eCollection, 2014. PMID:24587241 doi:http://dx.doi.org/10.1371/journal.pone.0090134

[2] Yao Y, Cui X, Al-Ramahi I, Sun X, Li B, Hou J, Difiglia M, Palacino J, Wu ZY, Ma L, Botas J, Lu B. A striatal-enriched intronic GPCR modulates huntingtin levels and toxicity. Elife. 2015 Mar 4;4. doi: 10.7554/eLife.05449. PMID:25738228 doi:http://dx.doi.org/10.7554/eLife.05449

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