CHEMICAL SCREENING AND OPTIMIZATION FACILITY - "STRUCTURE ACTIVITY RELATIONSHIPS"

化学筛选和优化设施 - “结构活性关系”

• 批准号: 10274476
• 负责人: LEYI GONG
• 金额: $ 96.73万
• 依托单位: SRI INTERNATIONAL
• 依托单位国家: 美国
• 财政年份: 2020
• 资助国家: 美国
• 起止时间: 2020-09-24 至 2022-09-23
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/10274476
• 关键词: Affinity; Biochemical; Biological; Biological Assay; Biological Availability; Cells; Chemicals; Contraceptive Agents; Contraceptive methods; Development; Female Contraceptive Agents; Freedom; Generations; Lead; Ligands; Male Contraceptive Agents; Methods; Mission; Molecular; National Institute of Child Health and Human Development; Oogenesis; Outcome; Ovulation; Permeability; Pharmaceutical Chemistry; Pharmacology; Play; Process; Production; Property; Protein Isoforms; Recombinant Proteins; Research; Research Support; Role; Safety; Services; Sperm Maturation; Spermatogenesis; Structure-Activity Relationship; Woman; X-Ray Crystallography; assay development; computational chemistry; design; drug development; high throughput screening; in silico; men; preclinical evaluation; recombinant peptide; screening; small molecule

The Contraception Research Branch (CRB) within the Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) supports research to develop compounds that can disrupt oogenesis, spermatogenesis, normal ovulation, sperm maturation and/or function affording safe and effective contraceptives that can be implemented for men and/or women. The Chemical Screening and Optimization Facility (CSOF) is designed to fulfill a unique role by identifying, optimizing, and conducting small scale production of molecular agents that achieve a contraceptive effect. The CSOF provides overall project management and the capabilities to support these objectives pursuant to development of new contraceptive methods: these include, but are not limited to, the generation of recombinant peptides and proteins, assay development, high throughput screening (HTS), x-ray crystallography, computational chemistry, medicinal chemistry, and pharmacology. Compounds identified and optimized by the CSOF will be prepared under non-Good Manufacturing Practices (non-GMP) for further preclinical evaluation. The CSOF plays a critical role in the drug development mission of the CRB.

尤尼斯·肯尼迪·施莱佛国家研究所避孕研究分支（CRB） 儿童健康和人类发展（NICHD）支持研究开发化合物， 卵子发生、精子发生、正常排卵、精子成熟和/或功能提供 可供男性和/或女性使用的安全有效的避孕药具。 化学 筛选和优化设施（CSOF）的目的是履行一个独特的作用， 鉴定、优化和进行小规模生产分子试剂， 避孕效果 CSOF提供全面的项目管理和能力， 通过开发新的避孕方法来支持这些目标：这些方法包括， 但不限于重组肽和蛋白质的产生，分析开发， 高通量筛选（HTS），X射线晶体学，计算化学，医学 化学和药理学。 由CSOF鉴定和优化的化合物将在以下条件下制备： 用于进一步临床前评价的非药品生产质量管理规范（非GMP）。 的 CSOF在CRB的药物开发使命中发挥着关键作用。