4uwh: Difference between revisions

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'''Unreleased structure'''


The entry 4uwh is ON HOLD  until Paper Publication
==Discovery of (2S)-8-((3R)-3-Methylmorpholin-4-yl)-1-(3-methyl-2-oxo- butyl)-2-(trifluoromethyl)-3,4-dihydro-2H-pyrimido(1,2-a)pyrimidin-6- one: a Novel Potent and Selective Inhibitor of Vps34 for the Treatment of Solid Tumors==
<StructureSection load='4uwh' size='340' side='right'caption='[[4uwh]], [[Resolution|resolution]] 1.93&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[4uwh]] 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=4UWH OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4UWH FirstGlance]. <br>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.93&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=JXM:(8S)-9-[(2R)-2-HYDROXY-2-PHENYLETHYL]-2-(MORPHOLIN-4-YL)-8-(TRIFLUOROMETHYL)-6,7,8,9-TETRAHYDRO-4H-PYRIMIDO[1,2-A]PYRIMIDIN-4-ONE'>JXM</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</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=4uwh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4uwh OCA], [https://pdbe.org/4uwh PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4uwh RCSB], [https://www.ebi.ac.uk/pdbsum/4uwh PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4uwh ProSAT]</span></td></tr>
</table>
== Function ==
[https://www.uniprot.org/uniprot/PK3C3_HUMAN PK3C3_HUMAN] Catalytic subunit of the PI3K complex that mediates formation of phosphatidylinositol 3-phosphate which plays a key role in initiation and maturation of autophagosomes. Involved in the transport of lysosomal enzyme precursors to lysosomes. Required for the abcission step in cytokinesis. Required for transport from early to late endosomes.<ref>PMID:7628435</ref> <ref>PMID:14617358</ref> <ref>PMID:20208530</ref>


Authors: Pasquier, B., El-Ahmad, Y., Filoche-Romme, B., Dureuil, C., Fassy, F., Abecassis, P.Y., Mathieu, M., Bertrand, T., Benard, T., Barriere, C., ElBatti, S., Letallec, J.P., Sonnefraud, V., Brollo, M., Delbarre, L., Loyau, V., Pilorge, F., Bertin, L., Richepin, P., Arigon, J., Labrosse, J.R., Clement, J., Durand, F., Combet, R., Perraut, P., Leroy, V., Gay, F., Lefrancois, D., Bretin, F., Marquette, J.P., Michot, N., Caron, A., Castell, C., Schio, L., McCort, G., Goulaouic, H., Garcia-Echeverria, C.
==See Also==
 
*[[Phosphoinositide 3-kinase 3D structures|Phosphoinositide 3-kinase 3D structures]]
Description: Discovery of (2S)-8-((3R)-3-Methylmorpholin-4-yl)-1-(3-methyl-2-oxo-butyl)-2-(trifluoromethyl)-3,4-dihydro-2H-pyrimido(1,2-a)pyrimidin-6-one: a Novel Potent and Selective Inhibitor of Vps34 for the Treatment of Solid Tumors
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Abecassis PY]]
[[Category: Arigon J]]
[[Category: Barriere C]]
[[Category: Benard T]]
[[Category: Bertin L]]
[[Category: Bertrand T]]
[[Category: Bretin F]]
[[Category: Brollo M]]
[[Category: Caron A]]
[[Category: Castell C]]
[[Category: Clement J]]
[[Category: Combet R]]
[[Category: Delbarre L]]
[[Category: Durand F]]
[[Category: Dureuil C]]
[[Category: El-Ahmad Y]]
[[Category: ElBatti S]]
[[Category: Fassy F]]
[[Category: Filoche-Romme B]]
[[Category: Garcia-Echeverria C]]
[[Category: Gay F]]
[[Category: Goulaouic H]]
[[Category: Labrosse JR]]
[[Category: Lefrancois D]]
[[Category: Leroy V]]
[[Category: Letallec JP]]
[[Category: Loyau V]]
[[Category: Marquette JP]]
[[Category: Mathieu M]]
[[Category: McCort G]]
[[Category: Michot N]]
[[Category: Pasquier B]]
[[Category: Perraut P]]
[[Category: Pilorge F]]
[[Category: Richepin P]]
[[Category: Ronan B]]
[[Category: Schio L]]
[[Category: Sonnefraud V]]

Latest revision as of 10:19, 1 May 2024

Discovery of (2S)-8-((3R)-3-Methylmorpholin-4-yl)-1-(3-methyl-2-oxo- butyl)-2-(trifluoromethyl)-3,4-dihydro-2H-pyrimido(1,2-a)pyrimidin-6- one: a Novel Potent and Selective Inhibitor of Vps34 for the Treatment of Solid TumorsDiscovery of (2S)-8-((3R)-3-Methylmorpholin-4-yl)-1-(3-methyl-2-oxo- butyl)-2-(trifluoromethyl)-3,4-dihydro-2H-pyrimido(1,2-a)pyrimidin-6- one: a Novel Potent and Selective Inhibitor of Vps34 for the Treatment of Solid Tumors

Structural highlights

4uwh 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 1.93Å
Ligands:,
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

PK3C3_HUMAN Catalytic subunit of the PI3K complex that mediates formation of phosphatidylinositol 3-phosphate which plays a key role in initiation and maturation of autophagosomes. Involved in the transport of lysosomal enzyme precursors to lysosomes. Required for the abcission step in cytokinesis. Required for transport from early to late endosomes.[1] [2] [3]

See Also

References

  1. ↑ Volinia S, Dhand R, Vanhaesebroeck B, MacDougall LK, Stein R, Zvelebil MJ, Domin J, Panaretou C, Waterfield MD. A human phosphatidylinositol 3-kinase complex related to the yeast Vps34p-Vps15p protein sorting system. EMBO J. 1995 Jul 17;14(14):3339-48. PMID:7628435
  2. ↑ Stein MP, Feng Y, Cooper KL, Welford AM, Wandinger-Ness A. Human VPS34 and p150 are Rab7 interacting partners. Traffic. 2003 Nov;4(11):754-71. PMID:14617358
  3. ↑ Sagona AP, Nezis IP, Pedersen NM, Liestol K, Poulton J, Rusten TE, Skotheim RI, Raiborg C, Stenmark H. PtdIns(3)P controls cytokinesis through KIF13A-mediated recruitment of FYVE-CENT to the midbody. Nat Cell Biol. 2010 Apr;12(4):362-71. doi: 10.1038/ncb2036. Epub 2010 Mar 7. PMID:20208530 doi:http://dx.doi.org/10.1038/ncb2036

4uwh, resolution 1.93Å

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