New Directions in Small Molecule Drug Discovery - Greenlee, Chair

描述(由申请人提供)：本提案旨在请求支持将于2010年4月20-25日在加拿大不列颠哥伦比亚省举行的题为小分子药物发现新方向的Keystone研讨会，该会议由William J.Greenlee，George Hartman和Anna K.Mapp组织。这次会议的目的是强调在发现小分子候选药物方面令人兴奋的新机会，包括：1.小分子的新靶点，包括破坏蛋白质-蛋白质相互作用，受体和酶的变构调节，以及与转录因子的直接相互作用。2.发现新的小分子先导的使能技术，包括面向多样性的筛选、片段筛选和亲和力筛选。3.最成功的基于结构的设计方法，以优化引线。会议的一个焦点将是基于结构的设计在发现治疗丙型肝炎病毒感染(蛋白酶抑制剂)和癌症(蛋白激酶抑制剂)的治疗药物方面的成功应用。包括首次披露第二阶段临床候选对象的会议将说明基于结构的设计在药物发现中的成功应用。同时举行的计算机辅助药物设计会议将大大增加跨学科互动的机会，该会议将与本次会议分享四个会议和一个主旨。 与公共卫生相关：小分子候选药物的成功发现导致了满足主要医疗需求的新的令人兴奋的药物。小分子药物发现的费用和风险不断增加，突显出需要新的方法和技术来提高候选药物的成功率，减少他们在开发过程中的消耗。这次关于小分子药物发现新方向的第一次Keystone研讨会会议将集中讨论有助于确定成功的小分子药物候选药物的新方法和使能技术。

DESCRIPTION (provided by applicant): This proposal is to request support for a Keystone Symposia meeting entitled New Directions in Small Molecule Drug Discovery, organized by William J. Greenlee, George Hartman and Anna K. Mapp, which will be held in British Columbia, Canada from April 20 - 25, 2010. The purpose of this meeting is to highlight exciting new opportunities in the discovery of small molecule drug candidates, including the following: 1. Novel targets for small molecules, including disruption of protein-protein interactions, allosteric modulation of receptors and enzymes, and direct interactions with transcription factors. 2. Enabling technologies for the discovery of new small molecule leads, including diversity-oriented screening, fragment screening, and affinity screening. 3. the most successful structure-based design approaches to the optimization of leads. A focus of the conference will be successful applications structure-based design in the discovery of therapeutics for the treatment of HCV infection (protease inhibitors) and cancer (protein kinase inhibitors). A session comprising first-time disclosures of Phase 2 clinical candidates will illustrate successful applications of structure-based design in drug discovery. Opportunities for interdisciplinary interactions will be significantly enhanced by the concurrent meeting on Computer-Aided Drug Design, which will share four sessions and a keynote with this meeting. PUBLIC HEALTH RELEVANCE: Successful discovery of small molecule drug candidates has led to new and exciting medicines that address major medical needs. The increasing expense and risk in small molecule drug discovery has highlighted the need for new approaches and technologies that can improve the success rate of drug candidates and reduce their attrition in development. This first Keystone Symposia meeting on New Directions in Small Molecule Drug Discovery will focus on new approaches and enabling technologies that will contribute to the identification of successful small molecule drug candidates.