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全球视野下的PROTAC:第19届圣地亚哥生物制药年会分享

2021-10-20
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2021年10月2日 09:00 上午 太平洋时间(美国和加拿大),第19届圣地亚哥生物制药年会(The 19th AnnualSan Diego BioPharma Conference)网络大会召开,pg电子官网国际研发服务部执行副总裁戴学东博士参加并做了PROTAC相关的主题演讲,我们整理戴博士的部分PPT进行分享。

演讲者信息
About Presenter

戴学东博士

pg电子官网国际研发服务部执行副总裁
美国麻省理工大学有机化学博士,博士后,深耕于中枢神经系统疾病、传染病和肿瘤疾病化学药物的研发20余载,对药物发现过程中包括苗头化合物的确定及优化,以及成功发展到高质量的临床候选化合物有着深刻的理解和丰富的实践经验。戴学东博士参与主持研发的药物有已上市药物,如Horizant®/Regnite®;临床药物,如JNJ-75276617;临床候选化合物,如Arbaclofen Placarbil,XP21279,XP23829等。

Dr. Xuedong Dai

ExecutiveVP and Head of IDSU (International Discovery Service Unit) at Medicilon,obtained his Ph.D. in organic chemistry at MIT. He is a senior-level expertwith over 20 years of experience focusing on small molecule drug discovery anddevelopment in CNS, infectious disease, and oncology therapy areas. He has deepunderstanding and practical knowledge of drug discovery process, including leadidentification, optimization, and development of high quality clinicalcandidate molecules. Prior to Medicilon, Dr. Dai worked at Janssen, HDBiosciences, GSK, and Xenoportwith a demonstrated successful track record ofprogram leadership and made significant contributions to medicinal chemistryprograms that led to the marketed drug Horizant®/Regnite® and several otherclinical candidates (JNJ-75276617, arbaclofen placarbil, XP21279, and XP23829).

pg电子官网国际研发服务部
Medicilon International Discovery Service Unit

pg电子官网国际研发服务部是pg电子官网一站式生物医药临床前研发服务平台的重要组成部分,使命是持续助力药企的国际化,向全球药物研发客户提供高质高效高性价比的合成化学、药物设计、以及新药候选化合物服务,以满足客户在临床前新药研究的各个化学领域的研发需求,缩短药物研发的周期,降低药物研发的成本。
目前,pg电子官网国际研发服务部拥有丰富海外留学工作背景的管理团队和实验人员、世界先进水平的合成实验室、分析实验室、和配套的高端仪器设备。为了给客户提供更优质的服务,国际研发服务部紧跟药物设计以及合成的新进展和新技术,如人工智能/机器学习(AI/ML),蛋白降解靶向嵌合体(PROTAC),高活性药物及抗体药物偶联物(ADC),惰性碳氢键直接官能团化,光致氧化还原反应,以及流动化学等。

The mission of Medicilon International Discovery Service Unit is to provide high quality, efficient and cost-effective synthetic chemistry, drug design, and new drug candidate compound services to global pharmaceutical companies.  We are stride to meet the research and development needs of the clients in various chemical fields of pre-clinical new drug research, shorten the cycle of drug R&D, and reduce the cost of drug R&D.

Medicilon International Discovery Service Unit has a management team and lab personnel with a rich background of studying abroad, a world-leading synthesis and analysis laboratory with installed state-of-the-art instruments and equipment.  In order to provide clients with better services, the International Discovery Service Unit keeps up with new developments and new technologies in drug design and synthesis, such as artificial intelligence/machine learning (AI/ML), proteolysis targeting chimera (PROTAC), antibody-drug conjugates (ADC), direct functionalization of inert carbon-hydrogen bonds, photoredox reactions, and flow chemistry, etc.

pg电子官网会议报告
Medicilon conference presentation

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以上为部分PPT分享

PROTAC技术平台
Medicilon PROTAC Platform

pg电子官网PROTAC药物发现技术平台汇总了当前流行的热门的靶标蛋白配体;建立了广泛的热门靶向蛋白高度亲和力小分子及小分子片段化合物库(TPSM),广泛的E3连接酶,高度亲和力的小分子及小分子片段(E3SM);建立了linker系统,包括收集大量具有广泛多样性的双官能团连接体(BF-Linker)。这些积累的化合物库可以帮助快速高效的合成大量高活性PROTAC双特异性小分子,极大地提高采用PROTAC技术进行的药物研发过程。除了快速合成之外,我们同时建立和完善的PROTAC生物筛选与测试平台,后续发展到临床前所有阶段。

Proteolysis Targeting Chimeras (PROTACs) are interesting biology as achemical knock-down approach in a fast and reversible way. Medicilon has established a wide range of popular target proteins withhigh affinity small molecules and small molecule fragment compound libraries, awide range of E3 ligases, and high affinity small molecules and small moleculefragments. We offer these services in any format you like;we can only do the chemical synthesis part for you, only the in vitro and/or invivo part, or we can offer a fully combined package.

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