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【25th.Oct.】DNA编码化合物库(DNA Encoded Library)研讨会 —DEL构建新技术及在新药研发中的应用

2018-10-24


时间:10月25日(周四)下午14:00 - 16:00
地点: 化学楼A楼528会议室
邀请人: 陈刚 特别研究员

14:00-15:00  DNA Encoded Library Platform for Drug Discovery
陆晓杰   博士  上海药物所研究员


陆晓杰   (Xiaojie Lu)
Principal investigator,  Shanghai Institute of Materia Medica CAS
Email: xjlu@simm.ac.cn

教育背景和研究经历:
Dr. Lu Xiaojie   received his bachelor degree in chemistry from Nanjing University in 2005. He moved to Boston for his PhD at Brandeis University to work on new asymmetric peroxidation and amination reactions employing modified Cinchona alkaloids organic catalysts for the synthesis of chiral peroxide natural products under the guidance of Professor Deng Li. 


In 2010, he joined GlaxoSmithKline for early stage drug discovery at molecular research department in Boston. As a research investigator, he has been working on designing and developing DNA encoded chemical libraries to identify small molecule ligands for biologically interesting targets, which could potentially be advanced to drug candidates. In May 2016, Dr. Lu was awarded GSK associate fellow. Since July 2017, he has joined the Shanghai Institute of Materia Medica CAS as the principal investigator.  


His research interest mainly focuses on small molecule and peptide drug discovery by applying multiple technologies together including DNA-encoded library technology, computer-aided and natural products drug discovery to tackle the undruggable challenge therapeutic targets .
Email: xjlu@simm.ac.cn


报告摘要
DNA-encoded library technology is a cutting-edge technology for hit identification of biological targets of interest. It provides both an ultra-high-throughput and a cost-efficient tool for the discovery of small molecules that bind to protein targets of pharmaceutical interest. 


The success of ELT relies heavily on the chemical diversity accessed through DNA-Encoded Library (DEL) synthesis. Although progress has been made for some commonly employed reactions in medicinal chemistry, there is still a large need for additional on-DNA reactions with a wide range of synthetic regents for ELT library synthesis. 


This seminar summarized recent on-DNA reaction development progress and discussed the future challenges and opportunities in DNA encoded chemistry. The case study and future direction of technology development in DEL will also be discussed. 


 




15:00-15:30  Forging Csp3-Csp3 and Csp3-Csp2 Bonds in DEL-Format
王  杰 博士    美国Scripps 研究所(Phil S. Baran教授 课题组)博士后



王 杰    (Jie Wang) 
美国Scripps研究所 博士后(合作导师:Phil S. Baran教授)
Email: jiewang@scripps.edu


教育背景和研究经历:
2015 – present Postdoctoral Associate     Advisor: Professor Phil S. Baran     The Scripps Research Institute, San Diego, California, USA  
2014 – 2015  Research Associate     Advisor: Professor Guo-Qiang Lin     Shanghai Institute of Organic Chemistry, Shanghai, China 
2009 – 2014  Ph.D. Student in Organic Chemistry    Advisor: Professor Guo-Qiang Lin     Shanghai Institute of Organic Chemistry, Shanghai, China 
2005 – 2009  B.S. Student in General Chemistry     Nanjing University, Nanjing, Jiangsu, China


报告摘要
Decarboxylative cross-coupling has been the subject of recent investigation in our lab. Our ability to harness the carboxylic acid functional group for cross-coupling has resulted in new strategies and tactics in making sp3-enriched medicinally relevant structures and complex molecules. 


Amongst our accomplishments in this area, transformations forging both Csp3-Csp3 and Csp3-Csp2 bonds have been successfully applied to DNA-encoded library development, which could significantly expand the chemical space available to DNA-encoded libraries. 


We expect this new technology will have a great impact on the field of drug discovery allowing for facile access to a plethora of new chemical entities.




15:30-16:00  A Biocompatible SOF4 based SuFEx Chemistry For DEL
刘  烽 博士     美国Scripps研究所 (K. B. Sharpless 教授 课题组)访问学者



刘烽   (Feng Liu)
美国Scripps研究所 访问学者(合作导师:K. B. Sharpless 教授)
Email:liufeng@sit.edu.cn


教育背景和研究经历:

1998年-2002年, 南开大学化学系 获得学士学位,导师:尤英才 教授
2002年-2007年, 中国科学院上海有机所 获得有机化学博士学位,导师:马大为 研究员
2008年-至今, 上海应用技术大学香料香精技术与工程学院 副教授
2012年-2014年, 复旦大学化学系 博士后 
2017年-2018年, 美国Scripps研究所 访问学者(合作导师:K. B. Sharpless 教授)


报告摘要
In this report, a biocompatible SOF4-based SuFEx reactions are developed. Beginning from iminosulfur oxydifluorides (R-N=SOF2), the reaction with primary amines gave sulfamides (8 examples, up to 98%) while the reaction with secondary amines furnished sulfuramidimidoyl fluoride products (8 examples, up to 97%) under mild aqueous condition. 


Likewise, phenols react with Ar-N=SOF2 to produce sulfurofluoridoimidates (9 examples, up to 99%), which can be further modified by nucleophiles to form asymmetric and trisubstituted products at the sulfur(VI) center with versatile S-N and S-O connectivity (9 examples, up to 94%). 


Finally, SuFEx bioconjugation of R-N=SOF2 to either single-stranded DNA or to BSA protein support the development of these reactions as a useful contribution to DEL chemistry and bioconjugation strategies.




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