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CYT997的发现：一种结构新颖的口服活性微管靶向剂。

Discovery of CYT997: a structurally novel orally active microtubule targeting agent.

作者信息

Burns Christopher J, Harte Michael F, Bu Xianyong, Fantino Emmanuelle, Joffe Max, Sikanyika Harrison, Su Stephen, Tranberg C Elisabet, Wilson Neil, Charman Susan A, Shackleford David M, Wilks Andrew F

机构信息

Cytopia Research Pty Ltd, Richmond, VIC 3121, Australia.

出版信息

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4639-42. doi: 10.1016/j.bmcl.2009.06.079. Epub 2009 Jun 25.

DOI:10.1016/j.bmcl.2009.06.079
PMID:19616947
Abstract

CYT997 was discovered as a potent tubulin polymerization inhibitor possessing potent cytotoxic activity against a range of cancer cells. Details of SAR studies, pharmacokinetic investigations and synthesis of compounds leading to the discovery of CYT997 are reported.

摘要

CYT997被发现是一种有效的微管蛋白聚合抑制剂，对一系列癌细胞具有强大的细胞毒性活性。本文报道了导致CYT997发现的构效关系（SAR）研究、药代动力学研究及化合物合成的详细情况。

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1
Discovery of CYT997: a structurally novel orally active microtubule targeting agent.CYT997的发现：一种结构新颖的口服活性微管靶向剂。
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2
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引用本文的文献

1
Mitochondrial ROS accumulation inhibiting JAK2/STAT3 pathway is a critical modulator of CYT997-induced autophagy and apoptosis in gastric cancer.线粒体 ROS 积累抑制 JAK2/STAT3 通路是 CYT997 诱导胃癌自噬和凋亡的关键调节剂。
J Exp Clin Cancer Res. 2020 Jun 23;39(1):119. doi: 10.1186/s13046-020-01621-y.
2
CYT997(Lexibulin) induces apoptosis and autophagy through the activation of mutually reinforced ER stress and ROS in osteosarcoma.赛特津（Lexibulin）通过激活相互增强的内质网应激和 ROS 诱导骨肉瘤细胞发生细胞凋亡和自噬。
J Exp Clin Cancer Res. 2019 Jan 31;38(1):44. doi: 10.1186/s13046-019-1047-9.
3
Intracellular reduction in ATP levels contributes to CYT997-induced suppression of metastasis of head and neck squamous carcinoma.
细胞内 ATP 水平的降低有助于 CYT997 抑制头颈部鳞状细胞癌的转移。
J Cell Mol Med. 2019 Feb;23(2):1174-1182. doi: 10.1111/jcmm.14017. Epub 2018 Nov 18.
4
Autophagy blockade sensitizes human head and neck squamous cell carcinoma towards CYT997 through enhancing excessively high reactive oxygen species-induced apoptosis.自噬阻断通过增强过高的活性氧诱导的细胞凋亡使人类头颈部鳞状细胞癌对 CYT997 敏感。
J Mol Med (Berl). 2018 Sep;96(9):929-938. doi: 10.1007/s00109-018-1670-5. Epub 2018 Jul 18.
5
Augmentation of the anticancer activity of CYT997 in human prostate cancer by inhibiting Src activity.抑制Src 活性增强 CYT997 对人前列腺癌的抗癌活性。
J Hematol Oncol. 2017 Jun 12;10(1):118. doi: 10.1186/s13045-017-0485-0.
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Current Advances of Tubulin Inhibitors in Nanoparticle Drug Delivery and Vascular Disruption/Angiogenesis.微管蛋白抑制剂在纳米颗粒药物递送及血管破坏/血管生成方面的研究进展
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The microtubule depolymerizing agent CYT997 effectively kills acute myeloid leukemia cells via activation of caspases and inhibition of PI3K/Akt/mTOR pathway proteins.微管解聚剂CYT997通过激活半胱天冬酶和抑制PI3K/Akt/mTOR通路蛋白有效杀死急性髓性白血病细胞。
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CYT997 causes apoptosis in human multiple myeloma.CYT997 诱导人多发性骨髓瘤细胞凋亡。
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