7c6a

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Crystal structure of AT2R-BRIL and SRP2070_Fab complex

Structural highlights

7c6a is a 4 chain structure with sequence from Escherichia coli, Homo sapiens and Mus musculus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:X-ray diffraction, Resolution 3.4Å
Ligands:SAR
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Disease

AGTR2_HUMAN X-linked non-syndromic intellectual disability.

Function

C562_ECOLX Electron-transport protein of unknown function.AGTR2_HUMAN Receptor for angiotensin II. Cooperates with MTUS1 to inhibit ERK2 activation and cell proliferation.[1]

Publication Abstract from PubMed

G-protein-coupled receptors (GPCRs)-the largest family of cell-surface membrane proteins-mediate the intracellular signal transduction of many external ligands. Thus, GPCRs have become important drug targets. X-ray crystal structures of GPCRs are very useful for structure-based drug design (SBDD). Herein, we produced a new antibody (SRP2070) targeting the thermostabilised apocytochrome b562 from Escherichia coli M7W/H102I/R106L (BRIL). We found that a fragment of this antibody (SRP2070Fab) facilitated the crystallisation of the BRIL-tagged, ligand bound GPCRs, 5HT(1B) and AT(2)R. Furthermore, the electron densities of the ligands were resolved, suggesting that SPR2070Fab is versatile and adaptable for GPCR SBDD. We anticipate that this new tool will significantly accelerate structure determination of other GPCRs and the design of small molecular drugs targeting them.

The discovery of a new antibody for BRIL-fused GPCR structure determination.,Miyagi H, Asada H, Suzuki M, Takahashi Y, Yasunaga M, Suno C, Iwata S, Saito JI Sci Rep. 2020 Jul 15;10(1):11669. doi: 10.1038/s41598-020-68355-x. PMID:32669569[2]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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Citations
4 reviews cite this structure
The Angiotensin AT<sub>2</sub> Receptor: From a Binding Site to a Novel Therapeutic Target.
Steckelings et al. (2022)
3 more
7 other articles
No citations found

See Also

References

  1. ↑ Nouet S, Amzallag N, Li JM, Louis S, Seitz I, Cui TX, Alleaume AM, Di Benedetto M, Boden C, Masson M, Strosberg AD, Horiuchi M, Couraud PO, Nahmias C. Trans-inactivation of receptor tyrosine kinases by novel angiotensin II AT2 receptor-interacting protein, ATIP. J Biol Chem. 2004 Jul 9;279(28):28989-97. Epub 2004 Apr 29. PMID:15123706 doi:http://dx.doi.org/10.1074/jbc.M403880200
  2. ↑ Miyagi H, Asada H, Suzuki M, Takahashi Y, Yasunaga M, Suno C, Iwata S, Saito JI. The discovery of a new antibody for BRIL-fused GPCR structure determination. Sci Rep. 2020 Jul 15;10(1):11669. PMID:32669569 doi:10.1038/s41598-020-68355-x

Contents


PDB ID 7c6a

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OCA

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