β-Lactams from the Ocean.
β-Lactams from the Ocean.
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作者：
这篇文章的标题既是一个陈述，也是一个问题。β-内酰胺类抗生素（包括青霉素、头孢菌素和碳青霉烯类）的发现改变了现代医学，这些抗生素大部分（如果不是全部的话）是陆地真菌和细菌的次级代谢产物。抗生素β-内酰胺是细菌细胞壁生物合成的必需酶。此外，β-内酰胺作为酶抑制剂的能力具有如此大的医学价值，以致于水解降解β-内酰胺的酶（β-内酰胺酶）的抑制剂具有同等的价值。鉴于β-内酰胺环的这种特权地位，因此令人失望的是，海洋次级代谢产物中该环的例证很少。可能有生物活性的海洋β-内酰胺存在，只是还没有遇到。在这份报告中，我们提出了第二种解释：β-内酰胺在海洋环境中确保生态优势的价值可能会受到其与群体感应β-内酯结构相似性的影响。β-内酰胺和β-内酯之间的空间和反应性相似性代表了将新结构和新酶靶点相关联以发现引人注目的生物活性的开箱即用的机会。
The title of this essay is as much a question as it is a statement. The discovery of the β-lactam antibiotics—including penicillins, cephalosporins, and carbapenems—as largely (if not exclusively) secondary metabolites of terrestrial fungi and bacteria, transformed modern medicine. The antibiotic β-lactams inactivate essential enzymes of bacterial cell-wall biosynthesis. Moreover, the ability of the β-lactams to function as enzyme inhibitors is of such great medical value, that inhibitors of the enzymes which degrade hydrolytically the β-lactams, the β-lactamases, have equal value. Given this privileged status for the β-lactam ring, it is therefore a disappointment that the exemplification of this ring in marine secondary metabolites is sparse. It may be that biologically active marine β-lactams are there, and simply have yet to be encountered. In this report, we posit a second explanation: that the value of the β-lactam to secure an ecological advantage in the marine environment might be compromised by its close structural similarity to the β-lactones of quorum sensing. The steric and reactivity similarities between the β-lactams and the β-lactones represent an outside-of-the-box opportunity for correlating new structures and new enzyme targets for the discovery of compelling biological activities.
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影响因子：
2.9
作者：
Patrick GJ;Fang L;Schaefer J;Singh S;Bowman GR;Wencewicz TA
通讯作者：
Wencewicz TA
Fsa2 和 Phm7 的晶体结构催化[4 2] 木贼黄素和磷酸马黄素生物合成中具有反向立体选择性的环加成反应
影响因子：
4.1
作者：
Chi C;Wang Z;Liu T;Zhang Z;Zhou H;Li A;Jin H;Jia H;Yin F;Yang D;Ma M
通讯作者：
Ma M
影响因子：
5.2
作者：
Delago A;Gregor R;Dubinsky L;Dandela R;Hendler A;Krief P;Rayo J;Aharoni A;Meijler MM
通讯作者：
Meijler MM
影响因子：
3.4
作者：
通讯作者：
--
影响因子：
3.7
作者：
Koyama N;Tokura Y;Münch D;Sahl HG;Schneider T;Shibagaki Y;Ikeda H;Tomoda H
通讯作者：
Tomoda H