Mass Spectrometer for Small Molecule Drug Development

描述(由申请人提供)：此共享仪器应用程序用于AB Sciex Triple Quad 4500三重四极质谱计，以取代过时的共享液相色谱质谱计。田纳西大学健康科学中心药学院和医学院的主要研究工作是针对未得到满足的医疗需求开发新的分子实体。申请的仪器支持9名研究人员的14个研究项目(10个由美国国立卫生研究院资助)，重点是小分子药物的发现和开发。有针对性的适应症包括各种癌症类型、结核病、辐射损伤和其他疾病的治疗。早期药物发现和先导优化的关键评估包括先导化合物的化学和代谢稳定性、生物制药和药代动力学特性的调查。所要求的仪器将用于小分子药物的定量 支持这些研究的生物矩阵候选人。由于其与其他LC-MS/MS设备相比具有较高的灵敏度，它将允许可靠地定量高效力候选药物的通常较低的药理活性浓度。

DESCRIPTION (provided by applicant): This shared instrumentation application is for an AB Sciex Triple Quad 4500 triple quadrupole mass spectrometer as replacement for an outdated shared liquid chromatography-mass spectrometry instrument. Major research efforts at the University of Tennessee Health Science Center Colleges of Pharmacy and Medicine are directed towards the development of new molecular entities for unmet medical needs. The requested instruments supports 9 investigators with 14 research projects (10 NIH-supported) focused on small molecule drug discovery and development. Targeted indications include the treatments of a variety of cancer types, tuberculosis, radiation injury, and other conditions. Crucial assessments in early drug discovery and lead optimization include the investigation of the lead compounds' chemical and metabolic stability, biopharmaceutical and pharmacokinetic properties. The requested instrument will be utilized for the quantification of small molecule drug candidates in biologic matrices in support of these studies. Due to its high sensitivity compared to other LC-MS/MS equipment, it will allow the reliable quantification of the usually low pharmacologically active concentrations of highly potent drug candidates.