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4wag

From Proteopedia

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Phosphatidylinositol 4-kinase III beta crystallized with MI103 inhibitor

Structural highlights

4wag is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:	X-ray diffraction, Resolution 3.407Å
Ligands:
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

PI4KB_HUMAN Phosphorylates phosphatidylinositol (PI) in the first committed step in the production of the second messenger inositol-1,4,5,-trisphosphate (PIP). May regulate Golgi disintegration/reorganization during mitosis, possibly via its phosphorylation. Involved in Golgi-to-plasma membrane trafficking (By similarity).^[1] ^[2] ^[3]

Publication Abstract from PubMed

Phosphatidylinositol 4-kinase IIIbeta is a cellular lipid kinase pivotal to pathogenesis of various RNA viruses. These viruses hijack the enzyme in order to modify the structure of intracellular membranes and use them for the construction of functional replication machinery. Selective inhibitors of this enzyme are potential broad-spectrum antiviral agents, as inhibition of this enzyme results in the arrest of replication of PI4K IIIbeta-dependent viruses. Herein, we report a detailed study of novel selective inhibitors of PI4K IIIbeta, which exert antiviral activity against a panel of single-stranded positive-sense RNA viruses. Our crystallographic data show that the inhibitors occupy the binding site for the adenine ring of the ATP molecule and therefore prevent the phosphorylation reaction.

Highly Selective Phosphatidylinositol 4-Kinase IIIbeta Inhibitors and Structural Insight into Their Mode of Action.,Mejdrova I, Chalupska D, Kogler M, Sala M, Plackova P, Baumlova A, Hrebabecky H, Prochazkova E, Dejmek M, Guillon R, Strunin D, Weber J, Lee G, Birkus G, Mertlikova-Kaiserova H, Boura E, Nencka R J Med Chem. 2015 May 14;58(9):3767-93. doi: 10.1021/acs.jmedchem.5b00499. Epub, 2015 May 4. PMID:25897704^[4]

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

References

↑ Suzuki K, Hirano H, Okutomi K, Suzuki M, Kuga Y, Fujiwara T, Kanemoto N, Isono K, Horie M. Identification and characterization of a novel human phosphatidylinositol 4-kinase. DNA Res. 1997 Aug 31;4(4):273-80. PMID:9405935
↑ Godi A, Pertile P, Meyers R, Marra P, Di Tullio G, Iurisci C, Luini A, Corda D, De Matteis MA. ARF mediates recruitment of PtdIns-4-OH kinase-beta and stimulates synthesis of PtdIns(4,5)P2 on the Golgi complex. Nat Cell Biol. 1999 Sep;1(5):280-7. PMID:10559940 doi:http://dx.doi.org/10.1038/12993
↑ Heilmeyer LM Jr, Vereb G Jr, Vereb G, Kakuk A, Szivak I. Mammalian phosphatidylinositol 4-kinases. IUBMB Life. 2003 Feb;55(2):59-65. PMID:12749687 doi:http://dx.doi.org/10.1002/tbmb.718540873
↑ Mejdrova I, Chalupska D, Kogler M, Sala M, Plackova P, Baumlova A, Hrebabecky H, Prochazkova E, Dejmek M, Guillon R, Strunin D, Weber J, Lee G, Birkus G, Mertlikova-Kaiserova H, Boura E, Nencka R. Highly Selective Phosphatidylinositol 4-Kinase IIIbeta Inhibitors and Structural Insight into Their Mode of Action. J Med Chem. 2015 May 14;58(9):3767-93. doi: 10.1021/acs.jmedchem.5b00499. Epub, 2015 May 4. PMID:25897704 doi:http://dx.doi.org/10.1021/acs.jmedchem.5b00499

1 Structural highlights
2 Function
3 Publication Abstract from PubMed
4 See Also
5 References

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/4wag"

Categories: Homo sapiens | Large Structures | Boura E | Chalupska D

@@ Line 4: / Line 4: @@
 == Structural highlights ==
 <table><tr><td colspan='2'>[[4wag]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4WAG OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4WAG FirstGlance]. <br>
-</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=3K7:6-CHLORO-3-(3,4-DIMETHOXYPHENYL)-2-METHYLIMIDAZO[1,2-B]PYRIDAZIN-8-AMINE'>3K7</scene></td></tr>
+</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 3.407&#8491;</td></tr>
+<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=3K7:6-CHLORO-3-(3,4-DIMETHOXYPHENYL)-2-METHYLIMIDAZO[1,2-B]PYRIDAZIN-8-AMINE'>3K7</scene></td></tr>
 <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=4wag FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4wag OCA], [https://pdbe.org/4wag PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4wag RCSB], [https://www.ebi.ac.uk/pdbsum/4wag PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4wag ProSAT]</span></td></tr>
 </table>

4wag

From Proteopedia

Current revision

Phosphatidylinositol 4-kinase III beta crystallized with MI103 inhibitor

Structural highlights

Function

Publication Abstract from PubMed

See Also

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

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