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中文摘要
翻译
描述(由申请人提供):该设备补助金要求资金购买等温滴定微量热仪(ITC),用于测定配体受体解离常数和热力学参数,由NIH资助的化学,药物化学,生物化学,分子生物学和生物物理学研究人员组成。这些研究人员参与了NIH资助的研究,这些研究涉及潜在药物靶点的小分子的设计和合成,或利用小分子配体研究与各种疾病相关的生物学过程。他们的研究涉及男性避孕药、肺结核、炭疽、心力衰竭、癌症、致癌作用和艾滋病毒等不同领域。目前,明尼苏达大学双城校区没有ITC仪器,该校区在生物医学研究方面处于全国领先地位。许多抑制剂通过非特异性熵相互作用(即去溶剂化)获得其亲和力,而非特异性氢键和货车范德华相互作用(表现为焓)。因此,了解相关的热力学特征是至关重要的。治疗和药物发现研究所(ITDD)将维护仪器并提供ITC的用户培训,费用由药物化学系支付。
英文摘要
DESCRIPTION (provided by applicant): This equipment grant is requesting funds for the purchase of an isothermal titration microcalorimeter (ITC) for the determination of ligand receptor dissociation constants and thermodynamic parameters by a group of very productive NIH-funded researchers in chemistry, medicinal chemistry, biochemistry, molecular biology, and biophysics. These investigators are involved in NIH funded research that deals either with the design and synthesis of small molecules for potential drug targets or the utilization of small molecule ligands to study biological processes associated with various diseases. Their research addresses such diverse areas as male contraceptives, tuberculosis, anthrax, heart failure, cancer, carcinogenesis, and HIV. Presently, there is no available ITC instrument at the University of Minnesota-Twin Cities campus, which is a leader nationally in biomedical research. Many inhibitors derive their affinity by non- specific entropic interactions (i.e. desolvation) rater than specific hydrogen-bonding and van der Waal interactions that is manifested in the enthalpy. Thus, knowledge of the relative thermodynamic signature is vitally important. The Institute of Therapeutics and Drug Discovery (ITDD) will maintain the instrument and provide user training of the ITC, which will be paid for by the Department of Medicinal Chemistry.
期刊论文(9)
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DOI: 10.1039/d0ma00608d
发表时间: 2020-12-01
期刊: Materials advances
影响因子: 5
作者: [Rodriguez RS, Szlag VM, Reineke TM, Haynes CL]
通讯作者: Haynes CL
Optimization of rifamycins to overcome intrinsic resistance of nontuberculous mycobacteria to improve treatment of NTM lung disease
Overcoming Pyrazinamide Resistance with Pyrazinoate-Cephalosporin Conjugates
  • 批准号:
    10088387
  • 项目类别:
  • 资助金额:
    $19.17万
  • 财政年份:
    2020
  • 负责人:
    Courtney C Aldrich
  • 依托单位:
Overcoming Pyrazinamide Resistance with Pyrazinoate-Cephalosporin Conjugates
  • 批准号:
    9895968
  • 项目类别:
  • 资助金额:
    $22.96万
  • 财政年份:
    2020
  • 负责人:
    Courtney C Aldrich
  • 依托单位:
Targeting Biotin Metabolism in Mycobacterium Tuberculosis
  • 批准号:
    10322125
  • 项目类别:
  • 资助金额:
    $77.99万
  • 财政年份:
    2019
  • 负责人:
    Courtney C Aldrich
  • 依托单位:
海外基金