波瑞霉素可抑制酿酒酵母的一种细胞周期蛋白依赖性激酶（CDK），即Cdc28/Cln2。

Borrelidin inhibits a cyclin-dependent kinase (CDK), Cdc28/Cln2, of Saccharomyces cerevisiae.

作者信息

Tsuchiya E, Yukawa M, Miyakawa T, Kimura K I, Takahashi H

机构信息

Department of Molecular Biotechnology, Graduate School of Advanced Sciences of Matter, Hiroshima University, Japan.

出版信息

J Antibiot (Tokyo). 2001 Jan;54(1):84-90. doi: 10.7164/antibiotics.54.84.

DOI:10.7164/antibiotics.54.84

PMID:11269718

Abstract

We identified borrrelidin, a member of macrolide antibiotic, as an inhibitor of a cyclin-dependent kinase of the budding yeast, Cdc28/Cln2. A 50% inhibition concentration (IC50) of borrelidin for Cdc28/Cln2 was 24 microM. In addition, borrelidin arrests both haploid and diploid cells in G1 phase at the point indistinguishable from that of alpha-mating pheromone, at concentrations not affecting the gross protein synthesis. Although the inhibition of CDK activity may not be a solo cause of the G1 arrest, our results indicate that borrelidin is a potential lead compound for developing novel CDK inhibitors of higher eukaryotes.

摘要

我们鉴定出大环内酯类抗生素成员博来霉素是芽殖酵母细胞周期蛋白依赖性激酶Cdc28/Cln2的抑制剂。博来霉素对Cdc28/Cln2的50%抑制浓度（IC50）为24微摩尔。此外，在不影响总蛋白质合成的浓度下，博来霉素可将单倍体细胞和二倍体细胞阻滞在G1期，其阻滞点与α-交配信息素的阻滞点无法区分。虽然抑制CDK活性可能不是G1期阻滞的唯一原因，但我们的结果表明，博来霉素是开发高等真核生物新型CDK抑制剂的潜在先导化合物。