单击化学是指与高热力学力量快速完成的反应,以高收率产生单个产品。4通过使用可点击部分进行功能化,从药物中得出的单击探针通过单击探针和相关疾病模型中选择的记者之间的选择性反应实现结合。In previous work, we demonstrated that this strategy can be used to identify drug targets and off-targets, visualise the cellular localization of the probe and measure target engagement of non-derivatised drug compounds.5 In the same study, different click reactions were compared and the inverse electron demand Diels Alder (IEDDA) reaction between a trans-cyclooctene (TCO) and a tetrazine was identified as the most efficient.在我们的点击探针策略中,IEDDA反应的出色性能归因于其无与伦比的动力学。6TCO与四嗪的选择性和高反应性,结合其在水溶液中的延长稳定性,使其成为非常有吸引力的单击部分。尽管如此,TCO是一个疏水群。连接到药物时,它可能会影响点击探针的物理化学特性以及药物的药理特性。在这种情况下,几个研究小组已经做出了相当大的努力,以开发出具有疏水性降低的新的跨环烯衍生物(例如oxotco)7或更快的动力学(例如STCO,DTCO).8,9
核酸的研究合成第6节(主席:Kathie Seley-Radtk E)9:35-9:50 OP4 - Malgorzata Honcharenko,Karolinska Institutet一种新颖的方法,是一种合成寡核苷酸多核苷酸多核苷酸的新方法Peyrottes,蒙彼利埃大学,CNRS碳碳和氯核苷磷酸类似物作为恶性疟原虫抑制疟原虫的新型化学型10:15-10:30 OP6 - Robert Britton,Robert Britton,Simon Fraser University,快速,灵活,柔性,可稳定的,可伸缩的核心合成,the tea coffee teacoy 10:30:30:30:55 55 55 55 55 55(55 55) Asanuma)10:55-11:20 IL8 - 塞奇·范·卡伦伯格(Serge van Calenbergh),根特大学结核素类似物与重要的Human and Fivestock疾病相似的原生动物病原体11:25-11:40 OP7 - Nicholas Chim,Nicholas Chim,加利福尼亚大学,最大程度地融合了最有效的TRYMASE TRYMASE TRYMASE TRYMASE TRYMASE TRIMPSINGS TRIMPTIONT, 11:45-12:00 OP8 - Michal Hocek,捷克科学学院酶合成基础改性RNA与工程DNA聚合酶基础修饰的RNA 12:00-13:30午餐,海报II II次,第8届海报(主席:FUMI NAGATSUGI:FUMI NAGATSUGI)13:30-13:30-13:55 IL9 - ROGERSTRASES基于Rogerstrified Artrins on Artnified Artnifirent on strutt on strutt on strutt rocority rogation intriptiation寡核苷酸ES 14:00-14:15 OP9 - 加利福尼亚大学的Dong Wang,圣地亚哥分校的结构基础,是通过Cel-lular RNA聚合酶14:20-14:20-14:35 OP10-Michiko Kimoto,Xenolis Pte的转录遗传字母识别的遗传字母。Ltd. Six-Letter DNA Aptamer Generation as an Antibody Alternative 14:40-16:00 Coffee, tea Recruitment/Discussion session Session 9 (Chair: Ramon Erit ja) 16:00-16:25 IL10 – Kazuo Nagasawa, Tokyo University of Agriculture and Technology Control of functions of dynamically formed high-order nucleic acids by polyoxazole compounds 16:30-16:45 OP11 – M. Carmen Galan, University of Bristol Small molecule G-quadruplex ligands are antibacterial candidates for Gram- nega- tive bacteria 16:50-17:05 OP12 – Shigeori Takenaka, Kyushu Institute of Technology Double-strand structuring of oligo-thymine by cyclic bis-naphthalene diimide Session 10 (主席:Takehiko Wada)17:10-17:25 OP13 - Vyacheslav V. Massey University University结构的结构引导抑制癌症DNA-Mutating酶Apobec 3A 17:30-17:30-17:55 IL11 - Zlatko Janeba,Iocb purague pare