报告时间：4月24日（星期五）上午10:00
报告地点：bw必威西汉姆联官网-霍普金斯大学中美中心 匡亚明报告厅
报告题目：Small Electrochemical Sensors and Single Cells: Zeptomoles Milliseconds and the Nature of Reality in Exocytosis
报告人：Dr. Andrew G Ewing
瑞典University of Gothenburg和Chalmers University of Technology双聘教授
美国科学促进会会士
英国皇家化学会会士
瑞典科学院院士
《Analytical Chemistry》副主编
报告摘要：
The chemokine receptors, CCR5 and CXCR4, are the primary co-receptors responsible for mediating HIV-1 cell entry. Small molecules that modulate these receptors utilize a fundamentally different approach for controlling viral replication than most other classes of antiretroviral agents in that they act on host factors, rather than viral enzymes. While CCR5 entry inhibitors that demonstrate clinical efficacy against HIV have now become available (Maraviroc), the development of CXCR4 entry inhibitors is currently at a more nascent stage. Due to the ability of HIV to switch between CCR5 and CXCR4 entry co-receptors, the availability of a CXCR4 entry inhibitor that could be used in combination with Maraviroc or other ARVs could prove to be important in prolonging the effectiveness of HIV therapies in patients. Unfortunately, the complexities associated with the multiple CXCR4 signaling pathways (which include, inter alia, expression of survival and proliferation genes, as well as induction of chemotaxis) create a major challenge for identifying efficacious compounds that also possess a safety profile suitable for dosing every day of a patient’s life. Alternatively, exploitation of selective aspects of the CXCR4 signaling pathways can be used for other important medical applications, such as hematopoetic stem cell mobilization and chemosensitization.
My lab has discovered a series of CXCR4 modulators that, depending on their their binding profiles, can act as either an antagonist or an inverse agonist. In addition, we have discovered a series of dual tropic antagonists that simultaneously block HIV entry through both CXCR4 and CCR5. In this presentation I will discuss some of the issues and challenges associated with the development of these series.
欢迎本感兴趣的同学和老师们参加！
