tubulysins 的化学和生物学：具有抗耐药性癌症活性的抗有丝分裂四肽。
Chemistry and biology of tubulysins: antimitotic tetrapeptides with activity against drug resistant cancers.
机构信息
University of Minnesota, Medicinal Chemistry, 8-101 Weaver Densford Hall, 308 Harvard Street S.E, Minneapolis, Minnesota 55455, USA.
出版信息
Nat Prod Rep. 2015 May;32(5):654-62. doi: 10.1039/c4np00036f.
Since their first report in 2000, tubulysins have sparked great interest for development as anti-cancer agents due to their exceptionally potent antiproliferative activity. Progress in the discovery and development of tubulysins, especially tubulysin conjugates, has quickly advanced despite limitations in their availability from Nature. In this Highlight, the key research on the isolation and structure determination, biosynthesis, bioactivity, structure-activity relationships (SAR), synthesis, and conjugates of tubulysins is presented.
自 2000 年首次报道以来，由于其具有异常强大的抗增殖活性，tubulysins 作为抗癌药物引起了极大的兴趣。尽管自然界中 tubulysins 的供应有限，但 tubulysins 的发现和开发，特别是 tubulysin 缀合物的开发，进展迅速。在这篇综述中，介绍了 tubulysins 的分离与结构测定、生物合成、生物活性、构效关系(SAR)、合成以及缀合物的关键研究。
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