8b7b

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Tubulin - maytansinoid - 6 complex

Structural highlights

8b7b 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:ACP, CA, GDP, GOL, GTP, MES, MG, PX0
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

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[1]

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

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References

  1. ↑ Boiarska Z, Pérez-Peña H, Abel AC, Marzullo P, Álvarez-Bernad B, Bonato F, Santini B, Horvath D, Lucena-Agell D, Vasile F, Sironi M, Díaz JF, Prota AE, Pieraccini S, Passarella D. Maytansinol Functionalization: Towards Useful Probes for Studying Microtubule Dynamics. Chemistry. 2023 Jan 24;29(5):e202203431. PMID:36468686 doi:10.1002/chem.202203431

Contents


PDB ID 8b7b

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