期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 43, 期 22, 页码 4212-4218出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm000168v
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资金
- NCI NIH HHS [R01 CA40081, R29 CA619178] Funding Source: Medline
- NIGMS NIH HHS [T32 GM145304] Funding Source: Medline
Synthetic and naturally occurring didemnins are potent and specific inhibitors of protein synthesis in vitro. Structure-activity analysis indicates a requirement for the intact macrocycle; however, the smaller ring size represented by the didemnin analogue, tamandarin A, is equipotent to didemnin B. Replacement of the N,O-dimethyltyrosine by a N-methylphenylalanine or N-methylleucine residue is also well-tolerated. The rank order for inhibition of protein synthesis in vitro appears to be retained in MCF-7 cells, albeit at much higher potency. This increase in potency is explained for the first time by data indicating that MCF-7 cells can accumulate didemnin B up to 2-3 orders of magnitude compared to the growth medium.
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