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中文摘要
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描述(由申请人提供):这项设备赠款正在申请资金,用于购买等温滴定微量热计(ITC),用于由NIH资助的一群在化学、药物化学、生物化学、分子生物学和生物物理学领域非常有成效的研究人员测定配体受体解离常数和热力学参数。这些研究人员参与了美国国立卫生研究院资助的研究,这些研究要么涉及潜在药物靶标的小分子的设计和合成,要么涉及利用小分子配体研究与各种疾病相关的生物过程。他们的研究涉及男性避孕药、结核病、炭疽病、心力衰竭、癌症、致癌和艾滋病毒等不同领域。目前,在全国生物医学研究领域处于领先地位的明尼苏达大学双子城分校没有可用的ITC仪器。许多抑制剂的亲和力是通过比特定氢键和范德华相互作用更快的非特定熵相互作用(即去溶)来获得的,范德华相互作用表现在热焓中。因此,相对热力学特征的知识是至关重要的。治疗和药物发现研究所(ITDD)将维护该仪器,并提供ITC的用户培训,费用将由药物化学系支付。
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