【25th.Oct.】DNA編碼化合物庫(kù)（DNA Encoded Library）研討會(huì) —DEL構(gòu)建新技術(shù)及在新藥研發(fā)中的應(yīng)用
日期：2018-10-25
閱讀：1590
時(shí)間：10月25日（周四）下午14:00 - 16:00
地點(diǎn)： 化學(xué)樓A樓528會(huì)議室
邀請(qǐng)人： 陳剛 特別研究員
14:00-15:00? DNA Encoded Library Platform for Drug Discovery
陸曉杰? ?博士? 上海藥物所研究員
陸曉杰? ?(Xiaojie Lu)
Principal investigator,? Shanghai Institute of Materia Medica CAS
Email: [email protected]
教育背景和研究經(jīng)歷:
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: [email protected]
報(bào)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.?
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15:00-15:30? Forging Csp3-Csp3 and Csp3-Csp2 Bonds in DEL-Format
王? 杰 博士? ? 美國(guó)Scripps 研究所（Phil S. Baran教授 課題組）博士后
王 杰?? ?（Jie Wang）?
美國(guó)Scripps研究所 博士后（合作導(dǎo)師：Phil S. Baran教授）
Email: [email protected]
教育背景和研究經(jīng)歷:
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
報(bào)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
劉? 烽 博士? ? ?美國(guó)Scripps研究所 （K. B. Sharpless 教授 課題組）訪問(wèn)學(xué)者
劉烽? ?（Feng Liu）
美國(guó)Scripps研究所 訪問(wèn)學(xué)者（合作導(dǎo)師：K. B. Sharpless 教授）
Email:[email protected]
教育背景和研究經(jīng)歷:
1998年-2002年, 南開大學(xué)化學(xué)系 獲得學(xué)士學(xué)位，導(dǎo)師：尤英才 教授
2002年-2007年, 中國(guó)科學(xué)院上海有機(jī)所 獲得有機(jī)化學(xué)博士學(xué)位，導(dǎo)師：馬大為 研究員
2008年-至今, 上海應(yīng)用技術(shù)大學(xué)香料香精技術(shù)與工程學(xué)院 副教授
2012年-2014年, 復(fù)旦大學(xué)化學(xué)系 博士后?
2017年-2018年, 美國(guó)Scripps研究所 訪問(wèn)學(xué)者（合作導(dǎo)師：K. B. Sharpless 教授）
報(bào)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.
