生物活性

• 描述Microtubules are long cylindrical polymers composed of tubulin subunits. In cells, microtubules play an essential role in architecture and motility. For example, microtubules give shape to cells, serve as intracellular transport tracks, and act as key elements in important cellular structures such as axonemes and mitotic spindles^[3]. Microtubules act as "railways" for motor-driven intracellular transport, interact with accessory proteins to assemble into larger structures such as the mitotic spindle, and provide an organizational framework to the rest of the cell^[4]. Maytansine is a highly potent microtubule-targeted compound that induces mitotic arrest and kills tumor cells at subnanomolar concentrations^[5]. Maytansine, a potent inhibitor of mitosis and in vitro microtubule assembly, was used to demonstrate a striking difference in the mechanism by which two of the main groups of brain microtubule-associated proteins, Tau and MAP2, interact with tubulin. At the low concentrations of 0.5 to 2 mM, maytansine inhibited Tau-catalyzed tubulin assembly more effectively than it did MAP2-catalyzed assembly^[6]. Maytansine, at 6x10^-8 M, irreversibly inhibits cell division in eggs of sea urchins and clams. Maytansine causes the disappearance of a mitotic apparatus or prevents one from forming if added at early stages. Maytansine inhibits in vitro polymerization of tubulin^[7].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT02318901	-	-	Terminated(PI no longer at sig... more >>ht. Results not collected) Collapse <<	-	-
  NCT02318901	Advanced Cancer ... more >> Breast Cancer Gastric Cancer Esophageal Cancer Colorectal Cancer Collapse <<	Phase 1 Phase 2	Terminated(PI no longer at sig... more >>ht. Results not collected) Collapse <<	-	United States, Arizona ... more >> Western Regional Medical Center/Cancer Treatment Center of America Goodyear, Arizona, United States, 85338 Collapse <<
  NCT02465060	Advanced Malignant Solid Neopl... more >>asm Bladder Carcinoma Breast Carcinoma Cervical Carcinoma Colon Carcinoma Colorectal Carcinoma Endometrial Carcinoma Esophageal Carcinoma Gastric Carcinoma Glioma Head and Neck Carcinoma Kidney Carcinoma Liver and Intrahepatic Bile Duct Carcinoma Lung Carcinoma Lymphoma Malignant Uterine Neoplasm Melanoma Ovarian Carcinoma Pancreatic Carcinoma Plasma Cell Myeloma Prostate Carcinoma Rectal Carcinoma Recurrent Bladder Carcinoma Recurrent Breast Carcinoma Recurrent Cervical Carcinoma Recurrent Colon Carcinoma Recurrent Colorectal Carcinoma Recurrent Esophageal Carcinoma Recurrent Gastric Carcinoma Recurrent Glioma Recurrent Head and Neck Carcinoma Recurrent Liver Carcinoma Recurrent Lung Carcinoma Recurrent Lymphoma Recurrent Malignant Solid Neoplasm Recurrent Melanoma Recurrent Ovarian Carcinoma Recurrent Pancreatic Carcinoma Recurrent Plasma Cell Myeloma Recurrent Prostate Carcinoma Recurrent Rectal Carcinoma Recurrent Skin Carcinoma Recurrent Thyroid Gland Carcinoma Recurrent Uterine Corpus Carcinoma Refractory Lymphoma Refractory Malignant Solid Neoplasm Refractory Plasma Cell Myeloma Skin Carcinoma Thyroid Gland Carcinoma Uterine Corpus Cancer Collapse <<	Phase 2	Recruiting	-	-

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• 参考文献

• [1] Kusari S, Lamshoft M, et al. Endophytes are hidden producers of maytansine in Putterlickia roots. J Nat Prod. 2014 Dec 26;77(12):2577-84.

  [2] Tang X, Dai H, et al. Maytansine-loaded star-shaped folate-core PLA-TPGS nanoparticles enhancing anticancer activity. Am J Transl Res. 2014 Oct 11;6(5):528-37. eCollection 2014.

  [3] Melissa K Gardner,et al. Microtubule catastrophe and rescue. Curr Opin Cell Biol. 2013 Feb;25(1):14-22.

  [4] Holly V Goodson,et al. Microtubules and Microtubule-Associated Proteins. Cold Spring Harb Perspect Biol.2018 Jun 1;10(6):a022608.

  [5] Lopus M, et al. Maytansine and cellular metabolites of antibody-maytansinoid conjugates strongly suppress microtubule dynamics by binding to microtubules. Mol Cancer Ther. 2010;9(10):2689-2699.

  [6] A Fellous,et al. Effects of Tau and MAP2 on the interaction of maytansine with tubulin: inhibitory effect of maytansine on vinblastine-induced aggregation of tubulin. Cancer Res. 1985 Oct;45(10):5004-10.

  [7] Remillard S, et al. Antimitotic activity of the potent tumor inhibitor maytansine. Science. 1975;189(4207):1002-1005.

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