Phamacology Core

药理学核心设施将负责实验的设计、执行和分析 内容涉及代谢稳定性、I//VO毒性、药代动力学和体内抗癌疗效。 由本计划项目拨款(PPG)产生的化合物。此外，他们还将维护细胞系， 动物资源，以及支持这些功能的设备。预计这四个项目都将 PPG可能需要该核心设施提供的服务。此外，核心将为 作为德克萨斯大学西南医学中心(UTSWMC)综合癌症成员的资源 需要协助进行药理检测的中心。因为这里没有其他设施可以 在活体环境中深入分析新的小分子的行为，创造这样的 共享资源有可能影响转译癌症研究的未来发展，请访问 UTSWMC。核心设施提供的服务将包括：化合物的体外筛选 广泛的肿瘤小组；单个化合物的体外代谢稳定性的表征 必要时对代谢物进行鉴定；对其溶解性、血浆蛋白结合力和 化合物的体外吸收特性.体内最大耐受剂量和最大耐受量的测定 毒性的初步评估.化合物在小型啮齿动物模型中的分布评估 (药代动力学)；发展小鼠异种移植或其他适当的模型以评估 体内复合药效。药理学核心设施将与PPG化学家密切合作，以完善 单个化合物的结构，以便有利于体内最佳疗效的特性将被最大化。 迫切需要新的疗法来对抗癌症，在2005年，癌症造成了50多万人死亡 死亡。该计划项目赠款(PPG)的总体目标是发现和表征合成的、小型的 可能对治疗这种疾病有效的分子化合物。药理学核心设施 将在动物身上进行化合物浓度、毒性和有效性的体外和体内测量 模特们。核心的总体目标是以这种方式指导PPG项目的化学合成工作 在癌症患者中产生了最有可能获得临床成功的新分子。

The Pharmacology Core facility will be responsible for the design, execution, and analysis of experiments that address metabolic stability, general in i//Vo toxicity, pharmacokinetics, and in vivo efficacy of anti-cancer compounds generated by this Program Project Grant (PPG). In addition, they will maintain the cell lines, animal resources, and equipment that support these functions. It is anticipated that all four projects of this PPG may potentially have need for the services provided by this Core facility. In addition, the Core will serve as a resourcefor members of the UT Southwestern Medical Center (UTSWMC) Comprehensive Cancer Center needing assistance with pharmacological assays. Since there are no other facilities here that can provide in-depth analysis of the behavior of novel small molecules in an in vivo setting, the creation of such a shared resource has the potential to impact the future development of translational cancer research at UTSWMC. The services provided by the Core facility will include: in vitro screening of compounds against a broad tumor panel; characterization of the metabolic stability of individual compounds in vitro and identification of metabolites as necessary; assessment of the solubility, plasma protein binding, and absorption characteristics of compounds in vitro; determination of the maximum in vivo tolerated dose and a preliminary assessment of toxicity; assessment of the distribution of compounds in small rodent models (pharmacokinetics); and development of mouse xenograft or other appropriate models for assessment of compound efficacy in vivo. The Pharmacology Core facility will work closely with PPG chemists to refine the structure of individual compounds so that characteristics that favor optimal efficacy in vivo will be maximized. There is an urgent need for new therapeutics to fight cancer, which in 2005 was responsible for over 500,000 deaths. The overall goal of this Program Project grant (PPG) is to discover and characterize synthetic, small molecule compounds that may be effective in the treatment of this disease. The Pharmacology Core facility will perform in vitro and in vivo measurements of compound concentration, toxicity, and efficacy in animal models. The overall goal of the Core is to guide chemical synthesis efforts of PPG projects in such a way that novel molecules with the best chance of clinical success in cancer patients are generated.