Hypoxia-Inducible factor 1 alpha inhibitor

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<StructureSection load='1h2m' size='340' side='right' caption='Structure of FIH-1 dimer (cyan, grey) complex with HIF-1 C-terminal transactivation domain (pink,), oxalylglycine, sulphate and Zn+2 ion (grey) (PDB code [[1h2m]])' scene='87/875688/Cv/1'>
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<StructureSection load='1h2m' size='340' side='right' caption='Structure of FIH-1 dimer (cyan, green) complex with HIF-1 C-terminal transactivation domain (pink, magenta), oxalylglycine, sulphate and Zn+2 ion (grey) (PDB code [[1h2m]])' scene='87/875688/Cv/1'>
== Function ==
== Function ==
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== Structural highlights ==
== Structural highlights ==
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The 3D structure of the complex between FIH-1 and the C-terminal transactivation domain of HIF-1 shows 2 interaction sites between the two proteins. The buried hydroxylation site which includes the Asn which undergoes hydroxylation and a surface interaction site <ref>PMID:12446723</ref>.
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<scene name='87/875688/Cv/2'>FIH-1 dimer complex with HIF-1 C-terminal transactivation domain</scene> (PDB code [[1h2m]]). The 3D structure of the complex between FIH-1 and the C-terminal transactivation domain of HIF-1 shows 2 interaction sites between the two proteins. The buried hydroxylation site which includes the Asn which undergoes hydroxylation and a surface interaction site <ref>PMID:12446723</ref>.
</StructureSection>
</StructureSection>

Revision as of 10:14, 23 February 2021

Structure of FIH-1 dimer (cyan, green) complex with HIF-1 C-terminal transactivation domain (pink, magenta), oxalylglycine, sulphate and Zn+2 ion (grey) (PDB code 1h2m)

Drag the structure with the mouse to rotate

3D Structures of Hypoxia-Inducible factor 1 alpha inhibitor

Updated on 23-February-2021

References

  1. ↑ Mahon PC, Hirota K, Semenza GL. FIH-1: a novel protein that interacts with HIF-1alpha and VHL to mediate repression of HIF-1 transcriptional activity. Genes Dev. 2001 Oct 15;15(20):2675-86. PMID:11641274 doi:http://dx.doi.org/10.1101/gad.924501
  2. ↑ Kiriakidis S, Henze AT, Kruszynska-Ziaja I, Skobridis K, Theodorou V, Paleolog EM, Mazzone M. Factor-inhibiting HIF-1 (FIH-1) is required for human vascular endothelial cell survival. FASEB J. 2015 Jul;29(7):2814-27. doi: 10.1096/fj.14-252379. Epub 2015 Apr 2. PMID:25837583 doi:http://dx.doi.org/10.1096/fj.14-252379
  3. ↑ Chen T, Ren Z, Ye LC, Zhou PH, Xu JM, Shi Q, Yao LQ, Zhong YS. Factor inhibiting HIF1alpha (FIH-1) functions as a tumor suppressor in human colorectal cancer by repressing HIF1alpha pathway. Cancer Biol Ther. 2015;16(2):244-52. doi: 10.1080/15384047.2014.1002346. PMID:25602156 doi:http://dx.doi.org/10.1080/15384047.2014.1002346
  4. ↑ Elkins JM, Hewitson KS, McNeill LA, Seibel JF, Schlemminger I, Pugh CW, Ratcliffe PJ, Schofield CJ. Structure of factor-inhibiting hypoxia-inducible factor (HIF) reveals mechanism of oxidative modification of HIF-1 alpha. J Biol Chem. 2003 Jan 17;278(3):1802-6. Epub 2002 Nov 21. PMID:12446723 doi:http://dx.doi.org/10.1074/jbc.C200644200

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