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全球視野下的PROTAC:第19屆聖地亞哥生物製藥年會分享

2021-10-20
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2021年10月2日 09:00 上午 太平洋時間(美國和加拿大),第19屆聖地亞哥生物製藥年會(The 19th AnnualSan Diego BioPharma Conference)網絡大會召開,hjc黄金城國際研發服務部執行副總裁戴學東博士參加並做了PROTAC相關的主題演講,我們整理戴博士的部分PPT進行分享。

演講者信息
About Presenter

戴學東博士

hjc黄金城國際研發服務部執行副總裁
美國麻省理工大學有機化學博士,博士後,深耕於中樞神經係統疾病、傳染病和腫瘤疾病化學藥物的研發20餘載,對藥物發現過程中包括苗頭化合物的確定及優化,以及成功發展到高質量的臨床候選化合物有著深刻的理解和豐富的實踐經驗。戴學東博士參與主持研發的藥物有已上市藥物,如Horizant®/Regnite®;臨床藥物,如JNJ-75276617;臨床候選化合物,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).

hjc黄金城國際研發服務部
Medicilon International Discovery Service Unit

hjc黄金城國際研發服務部是hjc黄金城一站式生物醫藥臨床前研發服務平台的重要組成部分,使命是持續助力藥企的國際化,向全球藥物研發客戶提供高質高效高性價比的合成化學、藥物設計、以及新藥候選化合物服務,以滿足客戶在臨床前新藥研究的各個化學領域的研發需求,縮短藥物研發的周期,降低藥物研發的成本。
目前,hjc黄金城國際研發服務部擁有豐富海外留學工作背景的管理團隊和實驗人員、世界先進水平的合成實驗室、分析實驗室、和配套的高端儀器設備。為了給客戶提供更優質的服務,國際研發服務部緊跟藥物設計以及合成的新進展和新技術,如人工智能/機器學習(AI/ML),蛋白降解靶向嵌合體(PROTAC),高活性藥物及抗體藥物偶聯物(ADC),惰性碳氫鍵直接官能團化,光致氧化還原反應,以及流動化學等。

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.

hjc黄金城會議報告
Medicilon conference presentation

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以上為部分PPT分享

PROTAC技術平台
Medicilon PROTAC Platform

hjc黄金城PROTAC藥物發現技術平台匯總了當前流行的熱門的靶標蛋白配體;建立了廣泛的熱門靶向蛋白高度親和力小分子及小分子片段化合物庫(TPSM),廣泛的E3連接酶,高度親和力的小分子及小分子片段(E3SM);建立了linker係統,包括收集大量具有廣泛多樣性的雙官能團連接體(BF-Linker)。這些積累的化合物庫可以幫助快速高效的合成大量高活性PROTAC雙特異性小分子,極大地提高采用PROTAC技術進行的藥物研發過程。除了快速合成之外,我們同時建立和完善的PROTAC生物篩選與測試平台,後續發展到臨床前所有階段。

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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