New Directions in Small Molecule Drug Discovery - Greenlee, Chair

小分子药物发现的新方向 - Greenlee，主席

• 批准号: 7916023
• 负责人: ANDREW D ROBERTSON
• 金额: $ 0.8万
• 依托单位: KEYSTONE SYMPOSIA
• 依托单位国家: 美国
• 财政年份: 2010
• 资助国家: 美国
• 起止时间: 2010-04-15 至 2011-03-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7916023
• 关键词: Address; Affinity; British Columbia; Canada; Clinical; Computer Assisted; Development; Disclosure; Drug Design; Enzymes; Hepatitis C; Malignant Neoplasms; Medical; Medicine; Phase; Protease Inhibitor; Protein Kinase Inhibitors; Risk; Screening procedure; Structure; Technology; Therapeutic; Time; base; design; drug candidate; drug discovery; improved; meetings; novel; novel strategies; protein kinase inhibitor; protein protein interaction; public health relevance; receptor; small molecule; success; symposium; transcription factor

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.

描述（由申请人提供）：本提案请求支持由William J. Greenlee， George Hartman和Anna K. Mapp组织的题为“小分子药物发现新方向”的Keystone专题会议，该会议将于2010年4月20日至25日在加拿大不列颠哥伦比亚省举行。本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，包括以下方面：小分子的新靶点，包括蛋白质相互作用的破坏，受体和酶的变构调节，以及与转录因子的直接相互作用。2. 支持发现新小分子先导物的技术，包括多样性筛选、片段筛选和亲和筛选。3. 最成功的基于结构的设计方法来优化引线。会议的一个重点将是基于结构的设计在发现治疗HCV感染（蛋白酶抑制剂）和癌症（蛋白激酶抑制剂）的治疗方法中的成功应用。第二阶段临床候选药物的首次披露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题演讲。