7mi3: Difference between revisions

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<StructureSection load='7mi3' size='340' side='right'caption='[[7mi3]], [[Resolution|resolution]] 3.50&Aring;' scene=''>
<StructureSection load='7mi3' size='340' side='right'caption='[[7mi3]], [[Resolution|resolution]] 3.50&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
<table><tr><td colspan='2'>[[7mi3]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Bpt4 Bpt4]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7MI3 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7MI3 FirstGlance]. <br>
<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7MI3 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7MI3 FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ATP:ADENOSINE-5-TRIPHOSPHATE'>ATP</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=ZG7:(8S)-6-(3-bromophenoxy)-2-[1-(4-chlorophenyl)cyclopropyl]-7-hydroxypyrazolo[1,5-a]pyrimidine-3-carbonitrile'>ZG7</scene></td></tr>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Electron Microscopy, [[Resolution|Resolution]] 3.5&#8491;</td></tr>
<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">DYN1, DHC1, YKR054C ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10665 BPT4])</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ATP:ADENOSINE-5-TRIPHOSPHATE'>ATP</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=ZG7:(8S)-6-(3-bromophenoxy)-2-[1-(4-chlorophenyl)cyclopropyl]-7-hydroxypyrazolo[1,5-a]pyrimidine-3-carbonitrile'>ZG7</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=7mi3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7mi3 OCA], [https://pdbe.org/7mi3 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7mi3 RCSB], [https://www.ebi.ac.uk/pdbsum/7mi3 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7mi3 ProSAT]</span></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=7mi3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7mi3 OCA], [https://pdbe.org/7mi3 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7mi3 RCSB], [https://www.ebi.ac.uk/pdbsum/7mi3 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7mi3 ProSAT]</span></td></tr>
</table>
</table>
== Function ==
[[https://www.uniprot.org/uniprot/DYHC_YEAST DYHC_YEAST]] Cytoplasmic dynein acts as a motor for the intracellular retrograde motility of vesicles and organelles along microtubules. Dynein has ATPase activity; the force-producing power stroke is thought to occur on release of ADP. Required to maintain uniform nuclear distribution in hyphae. May play an important role in the proper orientation of the mitotic spindle into the budding daughter cell yeast. Probably required for normal progression of the cell cycle.<ref>PMID:15642746</ref> 
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
Cytoplasmic dyneins are AAA (ATPase associated with diverse cellular activities) motor proteins responsible for microtubule minus-end-directed intracellular transport. Dynein's unusually large size, four distinct nucleotide-binding sites, and conformational dynamics pose challenges for the design of potent and selective chemical inhibitors. Here we use structural approaches to develop a model for the inhibition of a well-characterized S. cerevisiae dynein construct by pyrazolo-pyrimidinone-based compounds. These data, along with functional assays of dynein motility and mutagenesis studies, suggest that the compounds inhibit dynein by engaging the regulatory ATPase sites in the AAA3 and AAA4 domains, and not by interacting with dynein's main catalytic site in the AAA1 domain. A double Walker B mutation of the AAA3 and AAA4 sites substantially reduces enzyme activity, suggesting that targeting these regulatory domains is sufficient to inhibit dynein. Our findings reveal how chemical inhibitors can be designed to disrupt allosteric communication across dynein's AAA domains.
Targeting allostery in the Dynein motor domain with small molecule inhibitors.,Santarossa CC, Mickolajczyk KJ, Steinman JB, Urnavicius L, Chen N, Hirata Y, Fukase Y, Coudray N, Ekiert DC, Bhabha G, Kapoor TM Cell Chem Biol. 2021 May 17. pii: S2451-9456(21)00217-8. doi:, 10.1016/j.chembiol.2021.04.024. PMID:34015309<ref>PMID:34015309</ref>
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 7mi3" style="background-color:#fffaf0;"></div>


==See Also==
==See Also==
*[[Dynein 3D structures|Dynein 3D structures]]
*[[Dynein 3D structures|Dynein 3D structures]]
== References ==
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
[[Category: Bpt4]]
[[Category: Large Structures]]
[[Category: Large Structures]]
[[Category: Bhabha, G]]
[[Category: Bhabha G]]
[[Category: Coudray, N]]
[[Category: Coudray N]]
[[Category: Ekiert, D C]]
[[Category: Ekiert DC]]
[[Category: Kapoor, T M]]
[[Category: Kapoor TM]]
[[Category: Santarossa, C C]]
[[Category: Santarossa CC]]
[[Category: Urnavicius, L]]
[[Category: Urnavicius L]]
[[Category: Aaa atpase]]
[[Category: Atpase inhibitor]]
[[Category: Motor protein]]
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