Structural highlights
5gon is a 6 chain structure with sequence from Bos taurus, Gallus gallus and Rattus norvegicus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
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| Method: | X-ray diffraction, Resolution 2.48Å |
| Ligands: | , , , , , , , |
| Resources: | FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT |
Function
TBA1B_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.
Publication Abstract from PubMed
A series of chiral beta-lactam bridged analogues (3-substituted 1,4-diaryl-2-azetidinones) of combretastatin A-4 (CA-4) were synthesized asymmetrically, and their antitumor activities were evaluated in vitro and in vivo. The cocrystal structure of tubulin in complex with compound 9 was determined by X-ray crystallography, which showed that 9 binds to the same site as colchicine with similar binding mode, and the absolute configuration of its C-4 was first identified and demonstrated to be critically important for their antiproliferative activities.
Potent Antitumor Activities and Structure Basis of the Chiral beta-Lactam Bridged Analogue of Combretastatin A-4 Binding to Tubulin.,Zhou P, Liu Y, Zhou L, Zhu K, Feng K, Zhang H, Liang Y, Jiang H, Luo C, Liu M, Wang Y J Med Chem. 2016 Nov 23;59(22):10329-10334. Epub 2016 Nov 14. PMID:27805821[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Zhou P, Liu Y, Zhou L, Zhu K, Feng K, Zhang H, Liang Y, Jiang H, Luo C, Liu M, Wang Y. Potent Antitumor Activities and Structure Basis of the Chiral beta-Lactam Bridged Analogue of Combretastatin A-4 Binding to Tubulin. J Med Chem. 2016 Nov 23;59(22):10329-10334. Epub 2016 Nov 14. PMID:27805821 doi:http://dx.doi.org/10.1021/acs.jmedchem.6b01268
