Synthesis of cyclic di-nucleotidic acids as potential inhibitors targeting diguanylate cyclase

Synthesis of cyclic di-nucleotidic acids as potential inhibitors targeting diguanylate cyclase
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DOI:
10.1016/j.bmc.2010.07.068
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发表时间:
2010-09-15
影响因子:
3.5
通讯作者:
Lam, Yulin
Lam, Yulin
中科院分区:
医学3区
文献类型:
--
作者:
Ching, Shi Min;Tan, Wan Jun;Lam, Yulin

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合成了包括c-di-GMP在内的5个环二核苷酸类似物,并对其在集胞藻双鸟苷酸环化酶Slr 1143上的生物活性进行了评价。优化了一种新的高效液相色谱法,该方法能够以良好的分离度分离化合物和产物峰,并应用于化合物的分析。结果表明,环二肌苷酸1b对Slr 1143的抑制作用强于c-di-GMP,是一种潜在的生物膜形成抑制剂。(c)2010爱思唯尔有限公司保留所有权利。
Five analogs of cyclic di-nucleotidic acid including c-di-GMP were synthesized and evaluated for their biological activities on Slr1143, a diguanylate cyclase of Synechocystis sp. Slr1143 was overexpressed from the recombinant plasmid which contained the gene of interest and subsequently purified by affinity chromatography. A new HPLC method capable of separating the compound and product peaks with good resolution was optimized and applied to the analysis of the compounds. Results obtained show that cyclic di-inosinylic acid 1b demonstrates a stronger inhibition on Slr1143 than c-di-GMP and is a potential inhibitor for biofilm formation. (c) 2010 Elsevier Ltd. All rights reserved.