Further Insight into the Interactions of the Cytotoxic Macrolides Laulimalide and Peloruside A with Their Common Binding Site.
Alejandro Castro-Alvarez,Oriol Pineda,Jaume Vilarrasa +2 more
- 09 Feb 2018
- Vol. 3, Iss: 2, pp 1770-1782
TL;DR: Metadynamics simulations of laulimalide and peloruside A, reported for the first time, suggest that pelorusid A produces a stronger change in the M-loop, which explains the stabilization of the β1/β2 interaction.
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Abstract: The binding site of the macrolides laulimalide and peloruside A, which is different from that of the clinically useful drugs paclitaxel/taxol and ixabepilone (tax site), is known to be between two ...
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Recent Advances in the Synthetic Biology of Natural Drugs
TL;DR: A recent review as discussed by the authors provides an overview of the recent advances in the synthetic biology of natural drugs, focusing on the investigations of drugs that may be mass-produced by the pharmaceutical industry after optimization of corresponding synthetic systems.
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Function-Oriented Synthesis toward Peloruside A Analogues
Anne-Caroline Chany,Frédéric Legros,Heloua Haroun,Uday Kumar Kundu,Bohdan Biletskyi,Sergii Torlak,Monique Mathé-Allainmat,Jacques Lebreton,Aurélie Macé,Bertrand Carboni,Brigitte Renoux,Pascal Gosselin,Gilles Dujardin,Catherine Gaulon-Nourry +13 more
TL;DR: A convergent and rapid synthesis of original C2,C3-unsaturated, C11,C13-keto-enol macrocycles with a peloruside A skeleton with antiproliferative activity in the low micromolar range on NCI and MCF7 tumor cell lines is developed.
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Wangzaozin A, a potent novel microtubule stabilizer, targets both the taxane and laulimalide sites on β-tubulin through molecular dynamics simulations.
TL;DR: Wangzaozin A, an ent-kaurene diterpenoid isolated from Isodon racemosa (Hemsl) Hara, promotes the polymerization of intracellular microtubules as well as purified tubulin, which is similar to other known microtubule stabilizers as discussed by the authors .
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Combretastatins A-4 and A-1 and their derivatives: Review
Е. Р. Немцова,N. B. Morozova,A. D. Plyutinskaya,Alexey Noev,А. А. Панкратов,Peter Shegay +5 more
TL;DR: Review of the literature on combretastatins A-4 and A-1 and their derivatives covering SAR studies, mechanisms of action, clinical trials and challenges in developing effective antitumor agents.
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