View source for 8b7a


==Tubulin - maytansinoid - 4 complex==
<StructureSection load='8b7a' size='340' side='right'caption='[[8b7a]], [[Resolution|resolution]] 2.25&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[8b7a]] is a 6 chain structure with sequence from [https://en.wikipedia.org/wiki/Bos_taurus Bos taurus], [https://en.wikipedia.org/wiki/Gallus_gallus Gallus gallus] and [https://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=8B7A OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8B7A 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]] 2.25&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ACP:PHOSPHOMETHYLPHOSPHONIC+ACID+ADENYLATE+ESTER'>ACP</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=GDP:GUANOSINE-5-DIPHOSPHATE'>GDP</scene>, <scene name='pdbligand=GTP:GUANOSINE-5-TRIPHOSPHATE'>GTP</scene>, <scene name='pdbligand=IMD:IMIDAZOLE'>IMD</scene>, <scene name='pdbligand=MES:2-(N-MORPHOLINO)-ETHANESULFONIC+ACID'>MES</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=Q0F:[(1~{R},2~{R},3~{S},5~{S},6~{S},16~{E},18~{E},20~{R},21~{S})-11-chloranyl-12,20-dimethoxy-2,5,9,16-tetramethyl-21-oxidanyl-8,23-bis(oxidanylidene)-4,24-dioxa-9,22-diazatetracyclo[19.3.1.1^{10,14}.0^{3,5}]hexacosa-10(26),11,13,16,18-pentaen-6-yl]+pent-4-enoate'>Q0F</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=8b7a FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8b7a OCA], [https://pdbe.org/8b7a PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8b7a RCSB], [https://www.ebi.ac.uk/pdbsum/8b7a PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8b7a ProSAT]</span></td></tr>
</table>
== Function ==
[https://www.uniprot.org/uniprot/TBB2B_BOVIN TBB2B_BOVIN] Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain (By similarity).
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
Maytansinoids are a successful class of natural and semisynthetic tubulin binders, known for their potent cytotoxic activity. Their wider application as cytotoxins and chemical probes to study tubulin dynamics has been held back by the complexity of natural product chemistry. Here we report the synthesis of long-chain derivatives and maytansinoid conjugates. We confirmed that bulky substituents do not impact their high activity or the scaffold's binding mode. These encouraging results open new avenues for the design of new maytansine-based probes.

Maytansinol Functionalization: Towards Useful Probes for Studying Microtubule Dynamics.,Boiarska Z, Perez-Pena H, Abel AC, Marzullo P, Alvarez-Bernad B, Bonato F, Santini B, Horvath D, Lucena-Agell D, Vasile F, Sironi M, Diaz JF, Prota AE, Pieraccini S, Passarella D Chemistry. 2023 Jan 24;29(5):e202203431. doi: 10.1002/chem.202203431. Epub 2022 , Dec 30. PMID:36468686<ref>PMID:36468686</ref>

From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 8b7a" style="background-color:#fffaf0;"></div>
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Bos taurus]]
[[Category: Gallus gallus]]
[[Category: Large Structures]]
[[Category: Rattus norvegicus]]
[[Category: Abel A-C]]
[[Category: Alvarez-Bernad B]]
[[Category: Boiarska Z]]
[[Category: Bonato F]]
[[Category: Diaz FJ]]
[[Category: Horvath D]]
[[Category: Lucena-Agell D]]
[[Category: Marzullo P]]
[[Category: Passarella D]]
[[Category: Perez-Pena H]]
[[Category: Piaraccini S]]
[[Category: Prota AE]]
[[Category: Santini B]]
[[Category: Sironi M]]
[[Category: Steinmetz MO]]
[[Category: Vasile F]]