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STRUCTURE OF HUMAN DNA REPAIR PROTEIN AGT

STRUCTURE OF HUMAN DNA REPAIR PROTEIN AGT
人类 DNA 修复蛋白 AGT 的结构
批准号:
6119513
负责人:
DOUGLAS S DANIELS
金额:
$0.0万
依托单位:
依托单位国家:
美国
项目类别:
财政年份:
1999
资助国家:
美国
项目状态:
已结题
起止时间:
1999-03-01 至 2000-04-14

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中文摘要
翻译
o -6-烷基鸟嘌呤-DNA烷基转移酶(AGT)是一种DNA修复酶
英文摘要
O-6-Alkylguanine-DNA alkyltransferase (AGT) is a DNA repair protein which corrects promutagenic O-6-methylguanine lesions in DNA by removing the alkyl group from the guanyl moiety. In this reaction, the alkyl group is transferred to a cysteine residue in the active site of AGT, inactivating it. Elevated activity of AGT is responsible for resistance of tumor cells to cancer chemotherapies involving DNA alkylation such as chloroethylnitrosoureas (CENUs). Therefore, inactivation of AGT effectively potentiates current alkylation chemotherapies. One AGT inhibitor, o-6-benzylguanine, is currently in phase II studies as such a potentiation therapy. To begin a program of structure-based drug design using AGT, the inhibitors O-6-benyzlguanine (BG) and O-6-(3-iodobenzyl)guanine (IBG) were synthesized. AGT was cocrystallized with BG and IBG. Diffraction data from the AGT-BG complex was collected to 2.3 E at a synchotron source. Currently, heavy metal derivatives of the complex are being pursued. The structure of the AGT-BG complex will then be used to improve existing inhibitors and generate novel ones by complementation to the active site.
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Inhibition of c-Myc: Max dimerization by beta-peptides
  • 批准号:
    6994955
  • 项目类别:
  • 资助金额:
    $4.99万
  • 财政年份:
    2006
  • 负责人:
    DOUGLAS S DANIELS
  • 依托单位:
Inhibition of c-Myc: Max dimerization by beta-peptides
  • 批准号:
    7101025
  • 项目类别:
  • 资助金额:
    $5.2万
  • 财政年份:
    2005
  • 负责人:
    DOUGLAS S DANIELS
  • 依托单位:
STRUCTURE OF HUMAN DNA REPAIR PROTEIN AGT
  • 批准号:
    6976202
  • 项目类别:
  • 资助金额:
    $0.06万
  • 财政年份:
    2004
  • 负责人:
    DOUGLAS S DANIELS
  • 依托单位:
ANTI FUNGAL DRUG DESIGN CANDIDA ALBICANS DUTPASE
  • 批准号:
    6119559
  • 项目类别:
  • 资助金额:
    $0.0万
  • 财政年份:
    1999
  • 负责人:
    DOUGLAS S DANIELS
  • 依托单位:
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