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天然抗微管蛋白剂:3,4,5-三甲氧基苯基片段的重要性

Natural antitubulin agents: importance of 3,4,5-trimethoxyphenyl fragment.

作者信息

Negi Arvind S, Gautam Yashveer, Alam Sarfaraz, Chanda Debabrata, Luqman Suaib, Sarkar Jayanta, Khan Feroz, Konwar Rituraj

机构信息

CSIR-Central Institute of Medicinal and Aromatic Plants (CSIR-CIMAP), Kukrail Picnic Spot Road, PO CIMAP, Lucknow 226015, India.

CSIR-Central Institute of Medicinal and Aromatic Plants (CSIR-CIMAP), Kukrail Picnic Spot Road, PO CIMAP, Lucknow 226015, India.

出版信息

Bioorg Med Chem. 2015 Feb 1;23(3):373-89. doi: 10.1016/j.bmc.2014.12.027. Epub 2014 Dec 20.

DOI:10.1016/j.bmc.2014.12.027
PMID:25564377
Abstract

Microtubules are polar cytoskeletal filaments assembled from head-to-tail and comprised of lateral associations of α/β-tubulin heterodimers that play key role in various cellular processes. Because of their vital role in mitosis and various other cellular processes, microtubules have been attractive targets for several disease conditions and especially for cancer. Antitubulin is the most successful class of antimitotic agents in cancer chemotherapeutics. The target recognition of antimitotic agents as a ligand is not much explored so far. However, 3,4,5-trimethoxyphenyl fragment has been much highlighted and discussed in such type of interactions. In this review, some of the most important naturally occurring antimitotic agents and their interactions with microtubules are discussed with a special emphasis on the role of 3,4,5-trimethoxyphenyl unit. At last, some emerging naturally occurring antimitotic agents have also been tabulated.

摘要

微管是由头对头组装而成的极性细胞骨架细丝,由α/β-微管蛋白异二聚体的侧向缔合组成,在各种细胞过程中起关键作用。由于它们在有丝分裂和各种其他细胞过程中起着至关重要的作用,微管已成为多种疾病状况尤其是癌症的有吸引力的靶点。抗微管蛋白是癌症化疗中最成功的一类抗有丝分裂剂。到目前为止,作为配体的抗有丝分裂剂的靶点识别研究得还不多。然而,3,4,5-三甲氧基苯基片段在这类相互作用中受到了很多关注和讨论。在这篇综述中,讨论了一些最重要的天然抗有丝分裂剂及其与微管的相互作用,并特别强调了3,4,5-三甲氧基苯基单元的作用。最后,还列出了一些新出现的天然抗有丝分裂剂。

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