5sbb

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Tubulin-maytansinoid-4c-complex

Structural highlights

5sbb 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.
Method:X-ray diffraction, Resolution 2.25Å
Ligands:5JH, ACP, CA, GDP, GOL, GTP, IMD, MES, MG
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

Maytansinol is a valuable precursor for the preparation of maytansine derivatives (known as maytansinoids). Inspired by the intriguing structure of the macrocycle and the success in targeted cancer therapy of the derivatives, we explored the maytansinol acylation reaction. As a result, we were able to obtain a series of derivatives with novel modifications of the maytansine scaffold. We characterized these molecules by docking studies, by a comprehensive biochemical evaluation, and by determination of their crystal structures in complex with tubulin. The results shed further light on the intriguing chemical behavior of maytansinoids and confirm the relevance of this peculiar scaffold in the scenario of tubulin binders.

Maytansinol Derivatives: Side Reactions as a Chance for New Tubulin Binders.,Marzullo P, Boiarska Z, Perez-Pena H, Abel AC, Alvarez-Bernad B, Lucena-Agell D, Vasile F, Sironi M, Altmann KH, Prota AE, Diaz JF, Pieraccini S, Passarella D Chemistry. 2022 Jan 10;28(2):e202103520. doi: 10.1002/chem.202103520. Epub 2021 , Nov 29. PMID:34788896[1]

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

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Citations
1 reviews cite this structure
Antibody-drug conjugates: Recent advances in payloads.
Wang et al. (2023)
0 more
1 other articles
No citations found

See Also

References

  1. ↑ Marzullo P, Boiarska Z, Pérez-Peña H, Abel AC, Álvarez-Bernad B, Lucena-Agell D, Vasile F, Sironi M, Altmann KH, Prota AE, Díaz JF, Pieraccini S, Passarella D. Maytansinol Derivatives: Side Reactions as a Chance for New Tubulin Binders. Chemistry. 2022 Jan 10;28(2):e202103520. PMID:34788896 doi:10.1002/chem.202103520

Contents


PDB ID 5sbb

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OCA

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