Inside Cover: The Catalytic Mechanism of the Marine-Derived Macrocyclase PatGmac (Chem. Eur. J. 37/2016)
Inside Cover: The Catalytic Mechanism of the Marine-Derived Macrocyclase PatGmac (Chem. Eur. J. 37/2016)
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内封面：海洋来源的大环化酶 PatGmac 的催化机制（Chem. Eur. J. 37/2016）
DOI：
10.1002/chem.201603742
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发表时间：
2016
期刊：
影响因子：
--
通讯作者：
Brás N
中科院分区：
文献类型：
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作者：
Brás N
环肽是一类具有高治疗潜力的化合物。它们具有非常有前途的生物活性，如抗肿瘤和抗病毒（包括抗HIV）活性。然而，迄今为止，通过合成方法有效地生产这些化合物还没有实现，这激发了对肽的大环化的生物方法的研究。采用量子力学/分子力学（QM/MM）方法研究了由海绵共生体（Lissoclinum patella）合成的PatG大环化酶（PatGmac）的催化机理. PatGmac可以环化多种肽，仅需要识别信号序列（AYDG）。因此，这种酶可能是大规模生产具有治疗和生物技术应用的高兴趣环肽的关键，并吸引人们进一步关注水下世界的巨大潜力。更多信息可参见MJ拉莫斯等人的论文全文（第13089页）。
Cyclic peptides are a class of compounds with high therapeutic potential. They possess very promising bioactivities, such as antitumor and antiviral (including anti-HIV) activity. However, effective production of these compounds by synthetic approaches have not been achieved to date, which motivates the study of biological methods of macrocyclization of peptides. A quantum mechanics/molecular mechanics (QM/MM) study was used to unveil the atomistic portrait and energy profile of the catalytic mechanism of PatG macrocyclase (PatGmac), which is synthesized by an obligate symbiont of a sea sponge (Lissoclinum patella). PatGmac can cyclize a variety of peptides requiring only a recognition signal sequence (AYDG). This enzyme may thus hold the key to producing high-interest cyclic peptides with therapeutic and biotechnological applications on large scale and attract further attention to the immense potential of the underwater world. More information can be found in the Full Paper by MJ Ramos et al. on page 13089 ff.