User:Myron Williams/Sandbox 2
From Proteopedia
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| 3odu, resolution 2.50Å () | |||||||
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| Ligands: | , , | ||||||
| Gene: | CXCR4, CXCR4_HUMAN, E (Homo sapiens) | ||||||
| Activity: | Lysozyme, with EC number 3.2.1.17 | ||||||
| Related: | 3oe0, 3oe6, 3oe8, 3oe9 | ||||||
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| Resources: | FirstGlance, OCA, RCSB, PDBsum | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Contents |
The 2.5 A structure of the CXCR4 chemokine receptor in complex with small molecule antagonist IT1t
Chemokine receptors are critical regulators of cell migration in the context of immune surveillance, inflammation, and development. The G protein-coupled chemokine receptor, CXCR4, is specifically implicated in cancer metastasis and HIV-1 infection. Here, we report five independent crystal structures of CXCR4 bound to an antagonist small molecule IT1t and a cyclic peptide CVX15 at 2.5 to 3.2 angstrom resolution. All structures reveal a consistent homodimer with an interface including helices V and VI that may be involved in regulating signaling. The location and shape of the ligand-binding sites differ from other G protein-coupled receptors (GPCRs) and are closer to the extracellular surface. These structures provide new clues about the interactions between CXCR4 and its natural ligand CXCL12 and with the HIV-1 glycoprotein gp120.
Structures of the CXCR4 Chemokine GPCR with Small-Molecule and Cyclic Peptide Antagonists., Wu B, Chien EY, Mol CD, Fenalti G, Liu W, Katritch V, Abagyan R, Brooun A, Wells P, Bi FC, Hamel DJ, Kuhn P, Handel TM, Cherezov V, Stevens RC, Science. 2010 Oct 7. PMID:20929726
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
About this Structure
3odu is a 2 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA.
See Also
Reference
- Wu B, Chien EY, Mol CD, Fenalti G, Liu W, Katritch V, Abagyan R, Brooun A, Wells P, Bi FC, Hamel DJ, Kuhn P, Handel TM, Cherezov V, Stevens RC. Structures of the CXCR4 Chemokine GPCR with Small-Molecule and Cyclic Peptide Antagonists. Science. 2010 Oct 7. PMID:20929726 doi:10.1126/science.1194396
Categories: Homo sapiens | Lysozyme | ATCG3D, Accelerated Technologies Center for Gene to 3D Structure. | Cherezov, V. | Chien, E Y.T. | GPCR, GPCR Network. | Han, G W. | Katritch, V. | Liu, W. | Mol, C D. | Stevens, R C. | Wu, B. | 7tm | Accelerated technologies center for gene to 3d structure | Atcg3d | Cancer | Chemokine | Chimera | Cxcl12 | G protein-coupled receptor | Gpcr | Gpcr network | Hiv-1 co-receptor | Hydrolase | Isothiourea | Membrane protein | Protein structure initiative | Psi-2 | Psi-biology | Sdf1 | Signal transduction | Signaling protein | Singnaling protein | Structural genomic | T4l fusion | Transmembrane
