globalchange  > 气候变化与战略
DOI: 10.1073/pnas.1806900115
论文题名:
Kinetically guided radical-based synthesis of C(sp3)−C(sp3) linkages on DNA
作者: Wang J.; Lundberg H.; Asai S.; Martín-Acosta P.; Chen J.S.; Brown S.; Farrell W.; Dushin R.G.; O’Donnell C.J.; Ratnayake A.S.; Richardson P.; Liu Z.; Qin T.; Blackmond D.G.; Baran P.S.
刊名: Proceedings of the National Academy of Sciences of the United States of America
ISSN: 0027-8424
出版年: 2018
卷: 115, 期:28
起始页码: E6404
结束页码: E6410
语种: 英语
英文关键词: Combinatorial chemistr ; DNA-encoded libraries ; Kinetic analysis ; Organic synthesis ; Radical reactions
Scopus关键词: DNA ; transcription factor Sp3 ; DNA ; Article ; chemical bond ; chemical structure ; combinatorial chemistry ; DNA cross linking ; DNA library ; genetic transcription and translation ; genetic variability ; kinetics ; priority journal ; radical reaction ; synthesis ; chemistry ; gene library ; molecular model ; DNA ; Gene Library ; Kinetics ; Models, Molecular
英文摘要: DNA-encoded libraries (DEL)-based discovery platforms have re cently been widely adopted in the pharmaceutical industry, mainl due to their powerful diversity and incredible number of mole cules. In the two decades since their disclosure, great strides hav been made to expand the toolbox of reaction modes that are com patible with the idiosyncratic aqueous, dilute, and DNA-sensitiv parameters of this system. However, construction of highly impor tant C(sp3)−C(sp3) linkages on DNA through cross-coupling remain unexplored. In this article, we describe a systematic approach t translating standard organic reactions to a DEL setting throug the tactical combination of kinetic analysis and empirical screenin with information captured from data mining. To exemplify thi model, implementation of the Giese addition to forge high valu C–C bonds on DNA was studied, which represents a radical-base synthesis in DEL. © 2018 National Academy of Sciences. All rights reserved.
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资源类型: 期刊论文
标识符: http://119.78.100.158/handle/2HF3EXSE/163695
Appears in Collections:气候变化与战略

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作者单位: Wang, J., Department of Chemistry, Scripps Research Institute, La Jolla, CA 92037, United States; Lundberg, H., Department of Chemistry, Scripps Research Institute, La Jolla, CA 92037, United States; Asai, S., Department of Chemistry, Scripps Research Institute, La Jolla, CA 92037, United States; Martín-Acosta, P., Department of Chemistry, Scripps Research Institute, La Jolla, CA 92037, United States; Chen, J.S., Department of Chemistry, Scripps Research Institute, La Jolla, CA 92037, United States; Brown, S., Natural Products Laboratory, Worldwide Medicinal Chemistry, Pfizer Worldwide Research and Development, Groton, CT 06340, United States; Farrell, W., Department of Chemistry, La Jolla Laboratories, Pfizer Inc., San Diego, CA 92121, United States; Dushin, R.G., Natural Products Laboratory, Worldwide Medicinal Chemistry, Pfizer Worldwide Research and Development, Groton, CT 06340, United States; O’Donnell, C.J., Natural Products Laboratory, Worldwide Medicinal Chemistry, Pfizer Worldwide Research and Development, Groton, CT 06340, United States; Ratnayake, A.S., Natural Products Laboratory, Worldwide Medicinal Chemistry, Pfizer Worldwide Research and Development, Groton, CT 06340, United States; Richardson, P., Department of Chemistry, La Jolla Laboratories, Pfizer Inc., San Diego, CA 92121, United States; Liu, Z., Tianjin Key Laboratory of Pharmaceutical Green Synthesis Technology, Asymchem Laboratories (Tianjin) Co., Ltd., Tianjin, 300457, China; Qin, T., Department of Chemistry, Scripps Research Institute, La Jolla, CA 92037, United States; Blackmond, D.G., Department of Chemistry, Scripps Research Institute, La Jolla, CA 92037, United States; Baran, P.S., Department of Chemistry, Scripps Research Institute, La Jolla, CA 92037, United States

Recommended Citation:
Wang J.,Lundberg H.,Asai S.,et al. Kinetically guided radical-based synthesis of C(sp3)−C(sp3) linkages on DNA[J]. Proceedings of the National Academy of Sciences of the United States of America,2018-01-01,115(28)
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