气候变化领域集成服务门户(CCPortal): Kinetically guided radical-based synthesis of C(sp3)−C(sp3) linkages on DNA

CCPortal

DOI	10.1073/pnas.1806900115
	Kinetically guided radical-based synthesis of C(sp3)−C(sp3) linkages on DNA
	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.
发表日期	2018
ISSN	0027-8424
起始页码	E6404
结束页码	E6410
卷号	115 期号:28
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.
英文关键词	Combinatorial chemistr; DNA-encoded libraries; Kinetic analysis; Organic synthesis; Radical reactions
语种	英语
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
来源期刊	Proceedings of the National Academy of Sciences of the United States of America
文献类型	期刊论文
条目标识符	http://gcip.llas.ac.cn/handle/2XKMVOVA/160498
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 Resear...
推荐引用方式 GB/T 7714	Wang J.,Lundberg H.,Asai S.,et al. Kinetically guided radical-based synthesis of C(sp3)−C(sp3) linkages on DNA[J],2018,115(28).
APA	Wang J..,Lundberg H..,Asai S..,Martín-Acosta P..,Chen J.S..,...&Baran P.S..(2018).Kinetically guided radical-based synthesis of C(sp3)−C(sp3) linkages on DNA.Proceedings of the National Academy of Sciences of the United States of America,115(28).
MLA	Wang J.,et al."Kinetically guided radical-based synthesis of C(sp3)−C(sp3) linkages on DNA".Proceedings of the National Academy of Sciences of the United States of America 115.28(2018).