Taxol((R)), an antitumor drug with significant activity, is the first microtubule stabilizing agent described in the literature. This short review of the mechanism of action of Taxol((R)) emphasizes the research done in the Horwitz' laboratory. It discusses the contribution of photoaffinity ...
et al. The biosynthetic gene cluster for the microtubule-stabilizing agents epothilones A and B from Sorangium cellulosum So ce90. Chem. Biol. 7, 97–109 (2000). CAS PubMed Google Scholar Julien, B. et al. Isolation and characterization of the epothilone biosynthetic gene cluster from ...
Paradoxically, recent studies have shown that CSCs are sensitive to inhibition of polo-like kinase 1 (PLK1)—a key regulator of the G2/M transition16,17—whereas they are highly resistant to traditional anti-mitotic drugs such as the microtubule-stabilizing agent paclitaxel4,18. Indeed, gene ...
Zampanolide covalently binds to the luminal paclitaxel site at β-tubulin N228 and H229 Labeling occurs in both tubulin dimers and microtubules Bound zampanolide models indicate interaction with the M-loop at the paclitaxel site Microtubule nucleation may proceed through both matchmaking and allosteric...
The model includes the binding site of taxol, an anti-cancer agent that acts by stabilizing microtubules. The present tubulin model gives the first structural framework for understanding microtubule polymerization and its regulation by nucleotides and anti-mitotic drugs at the molecular level. This is...
Microtubule-binding agents, such as taxanes and vinca alkaloids, are used in the treatment of cancer. The limitations of these treatments, such as resistance to therapy and the need for intravenous administration, have encouraged the development of new a
They comprise highly efficacious small-molecule components with often intercalating or microtubule-disrupting properties. A special case of an ADC is a radiopharmaceutical agent being covalently attached to an antibody. BAY 2315497 is a recent example in which the small-molecule component of the ...
Microtubule-associated proteins 1A/1B light chain 3B MAPT: Microtubule-associated protein tau ML: Mediolateral MS: Mass spectrometry NFT: Neurofibrillary tangle nTg: Nontransgenic PCR: Polymerase chain reaction p-Tau: Phosphorylated tau PV: Parvalbumin RMP: Resting membrane potential TFEB...
“R-CHOP” regimen, regardless of the patient stage39. Microtubule stabilizers and JAK inhibitors are not included in this regimen. Here, we show that the microtubule-stabilizing agent Taxol and the JAK1/2 inhibitor ruxolitinib effectively suppress the dissemination of DLBCL by impeding STAT3-driven...
R. et al. Epothilone D improves microtubule density, axonal integrity, and cognition in a transgenic mouse model of tauopathy. J. Neurosci. 30, 13861–13866 (2010). 20. Zhang, B. et al. The microtubule-stabilizing agent, epothilone D, reduces axonal dysfunction, neurotoxicity, cognitive ...