本文主要研究内容
作者（2019）在《Establishing the structure-activity relationship of teixobactin》一文中研究指出：In 2015, a new antimicrobial peptide agent was discovered, termed teixobactin. Over the past few years,the structure-activity relationship of teixobactin has been extensively studied. Here, the updated studies have been summarized to provide structure-activity relationship established to date. It can be seen that position 1, 2, 5 and 6 of teixobactin are not tolerant of diversion from the native amino acids.In positions 7 and 11, native amino acids give the highest activity but there is tolerance for other amino acids. Positions 3, 4, 9 and 10 are very tolerant of substitution while maintaining good potency and a broad activity spectrum. Activity does not depend on absolute stereochemistry, but on the relative stereochemistry and positions 1, 4, 5, and 8 must contain D-amino acids. The ring and tail structure are necessary for activity, macrolactone and lactam rings are both acceptable. Some teixobactin analogues show greater activity than native teixobactin. All conducted animal studies show positive results with no animal deaths.
Abstract
In 2015, a new antimicrobial peptide agent was discovered, termed teixobactin. Over the past few years,the structure-activity relationship of teixobactin has been extensively studied. Here, the updated studies have been summarized to provide structure-activity relationship established to date. It can be seen that position 1, 2, 5 and 6 of teixobactin are not tolerant of diversion from the native amino acids.In positions 7 and 11, native amino acids give the highest activity but there is tolerance for other amino acids. Positions 3, 4, 9 and 10 are very tolerant of substitution while maintaining good potency and a broad activity spectrum. Activity does not depend on absolute stereochemistry, but on the relative stereochemistry and positions 1, 4, 5, and 8 must contain D-amino acids. The ring and tail structure are necessary for activity, macrolactone and lactam rings are both acceptable. Some teixobactin analogues show greater activity than native teixobactin. All conducted animal studies show positive results with no animal deaths.
论文参考文献
[1].Synthesis and biological activities of(E)-β-farnesene analogues containing 1,2,3-thiadiazole[J]. Jing-Peng Zhang,Yao-Guo Qin,Ya-Wen Dong,Dun-Lun Song,Hong-Xia Duan,Xin-Ling Yang. Chinese Chemical Letters.2017(02)[2].Preparation of 4-and 6-desphenyl analogues of(-)-clausenamide and alternative synthesis of(+)-epi-clausenamide[J]. Jian Jun Xue,Yu Mei Zhou,Xiao Ming Yu~* Institute of Materia Medica,Chinese Academy of Medical Sciences & Peking Union Medical College,Beijing 100050,China. Chinese Chemical Letters.2011(11)[3].Synthesis and antitumor activity of novel salvicine analogues[J]. Fei Deng~(a,*),Jin Jian Lu~a,Hong Ying Liu~b,Li Ping Lin~a,Jian Ding~a, Jin Sheng Zhang~a a State Key Laboratory of Drug Research,Shanghai Institute of Materia Medica,Chinese Academy of Sciences,Shanghai 201203,China b College of Life Sciences,Northwest A & F University,Yangling 712100,China. Chinese Chemical Letters.2011(01)[4].Synthesis and Antitumor Activity of Tanshinone Analogues[J]. 阿吉艾克拜尔·艾萨,吕伟,蔡俊超. Chinese Journal of Chemistry.2003(07)[5].First synthesis and in vitro biological assessment of isosideroxylin,6,8-dimethylgenistein and their analogues as nitric oxide production inhibition agents[J]. Jong-Woon Jung,Kongara Damodar,Jin-Kyung Kim,Jong-Gab Jun. Chinese Chemical Letters.2017(05)[6].Synthesis and fungicidal activity of novel strobilurin analogues containing substituted N-phenylpyrimidin-2-amines[J]. Hui Chao Li~(a,b),Bao Shan Chai~b,Zhi Nian Li~b,Ji Chun Yang~b,Chang Ling Liu~(b,*) a Liaoning University,Shenyang 110036,China b Shenyang Research Institute of Chemical Industry,Shenyang 110021,China. Chinese Chemical Letters.2009(11)[7].An Efficient Synthesis and Screening of Osteostatin analogues by Using Pooling Strategy[J]. De Xin WANG; Rui HAN; Hong Yan LIU; Lei HUANG; Jun FU(Institute of Materia Medica. Chinese Academy of Medical Sciencesand Peking Union Medical College, Beijing 100050). Chinese Chemical Letters.1999(10)[8].Synthesis of novel analogues of zanamivir as neuraminidase inhibitors[J]. Rui Sheng Xiong~a,Qing Jie Zhao~a,Hang Hang Zhu~b,Zheng Liu~c, Ya Bing Wei~b,Jing Shan Shen~(a,c,*) a Shanghai Institute of Materia Medica,Chinese Academy of Sciences,Shanghai 201203,China b College of Materials Science and Engineering,Nanjing University of Technology,Nanjing 210009,China c Topharman Shanghai Co.,Ltd.,Shanghai 201209,China. Chinese Chemical Letters.2010(11)[9].Rheological properties of salt-tolerant HPAM solutions with ultrahigh molecular weight[J]. 张敏革,张吕鸿,姜斌,李鑫钢. Journal of Central South University of Technology.2008(S1)[10].High yield synthesis of cyclic analogues of antibacterial peptides P-113 by Sortase A-mediated ligation and their conformation studies[J]. Zhi-Meng Wu,Shao-Zhong Liu,Xiao-Zhong Cheng,Xin-Rui Zhao,Hao-Fei Hong. Chinese Chemical Letters.2017(03)
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：Establishing the structure-activity relationship of teixobactin论文
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