A BROMOENOL LACTONE SUICIDE SUBSTRATE INACTIVATES GROUP VIA PHOSPHOLIPASE A2
溴烯醇内酯自杀底物通过磷脂酶 A2 灭活基团
基本信息
- 批准号:7721511
- 负责人:
- 金额:$ 0.44万
- 依托单位:
- 依托单位国家:美国
- 项目类别:
- 财政年份:2008
- 资助国家:美国
- 起止时间:2008-02-01 至 2009-01-31
- 项目状态:已结题
- 来源:
- 关键词:6-(bromomethylene)tetrahydro-3-(1-naphthaleneyl)-2H-pyran-2-oneActive SitesAlkylationAmino AcidsBiological ProcessComputer Retrieval of Information on Scientific Projects DatabaseConsensus SequenceDependenceDistantEnzymesFundingGrantHydrolysisIncubatedIndividualInstitutionKeto AcidsLipaseLysophospholipidsModificationNonesterified Fatty AcidsPeptidesPhospholipase A2PhospholipidsResearchResearch PersonnelResourcesSerineSourceSpecificitySulfhydryl CompoundsUnited States National Institutes of Healtharachidonateinhibitor/antagonistsuicide substratesthioether
项目摘要
This subproject is one of many research subprojects utilizing the
resources provided by a Center grant funded by NIH/NCRR. The subproject and
investigator (PI) may have received primary funding from another NIH source,
and thus could be represented in other CRISP entries. The institution listed is
for the Center, which is not necessarily the institution for the investigator.
Phospholipases A2 (PLA2) comprise a superfamily of enzymes that hydrolyze phospholipids to a free fatty acid, e.g., arachidonate, and a 2-lysophospholipid. Dissecting their individual functions has relied in large part on pharmacological inhibitors that discriminate among PLA2. Group VIA PLA2 (iPLA2) has a GTSTG serine lipase consensus sequence, and studies with a bromoenol lactone (BEL) suicide substrate inhibitor have been taken to suggest that iPLA2 participates in a wide variety of biological processes. Such conclusions presume inhibitor specificity. Inhibition by BEL requires its hydrolysis by and results in uncharacterized covalent modification(s) of iPLA2. We performed mass spectrometric analyses of proteolytic digests of BEL-treated iPLA2 to identify modifications associated with loss of activity. The GTSTG active site and large flanking regions of sequence are not modified by BEL treatment, but most iPLA2 Cys residues are alkylated at various BEL concentrations to form a thioether linkage to a BEL keto acid hydrolysis product. Synthetic Cys-containing peptides are alkylated when incubated with iPLA2 and BEL, which reflects iPLA2-catalyzed BEL hydrolysis to a diffusible bromomethyl keto acid product that reacts with distant thiols. The BEL concentration dependence of Cys651 alkylation closely parallels that of loss of iPLA2 activity. No amino acid residues other than Cys were found to be modified, suggesting that Cys alkylation is the covalent modification of iPLA2 responsible for loss of activity, and the alkylating species appears to be a diffusible hydrolysis product of BEL rather than a tethered acyl-enzyme intermediate.
这个子项目是众多研究子项目之一
项目成果
期刊论文数量(0)
专著数量(0)
科研奖励数量(0)
会议论文数量(0)
专利数量(0)
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HAOWEI SONG其他文献
HAOWEI SONG的其他文献
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{{ truncateString('HAOWEI SONG', 18)}}的其他基金
ALGORITHMS FOR AUTOMATIC PROCESSING OF DATA FROM MASS SPECTROMETRIC ANALYSES
自动处理质谱分析数据的算法
- 批准号:
8361390 - 财政年份:2011
- 资助金额:
$ 0.44万 - 项目类别:
EVIDENCE FOR PROTEOLYTIC PROCESSING AND STIMULATED ORGANELLE REDISTRIBUTION
蛋白水解加工和刺激细胞器重新分布的证据
- 批准号:
8168828 - 财政年份:2010
- 资助金额:
$ 0.44万 - 项目类别:
ALGORITHMS FOR AUTOMATIC PROCESSING OF DATA FROM MASS SPECTROMETRIC ANALYSES
自动处理质谱分析数据的算法
- 批准号:
8168786 - 财政年份:2010
- 资助金额:
$ 0.44万 - 项目类别:
MODULATION OF THE REGULATORY ACTIVITY OF BACTERIAL TWO-COMPONENT SYSTEMS BY SLY
SLY 对细菌二组分系统调节活性的调节
- 批准号:
8168776 - 财政年份:2010
- 资助金额:
$ 0.44万 - 项目类别:
MODULATION OF THE REGULATORY ACTIVITY OF BACTERIAL TWO-COMPONENT SYSTEMS BY SLY
SLY 对细菌二组分系统调节活性的调节
- 批准号:
7954025 - 财政年份:2009
- 资助金额:
$ 0.44万 - 项目类别:
ALGORITHM FOR PROCESSING RAW MASS SPECTROMETRIC DATA TO IDENTIFY AND QUANTITATE
处理原始质谱数据以进行识别和定量的算法
- 批准号:
7953990 - 财政年份:2009
- 资助金额:
$ 0.44万 - 项目类别:
ALGORITHMS FOR AUTOMATIC PROCESSING OF DATA FROM MASS SPECTROMETRIC ANALYSES
自动处理质谱分析数据的算法
- 批准号:
7954035 - 财政年份:2009
- 资助金额:
$ 0.44万 - 项目类别:
EFFECTS OF BIOLOGICAL OXIDANTS ON THE CATALYTIC ACTIVITY AND STRUCTURE OF GROUP
生物氧化剂对催化活性和基团结构的影响
- 批准号:
7721510 - 财政年份:2008
- 资助金额:
$ 0.44万 - 项目类别:
N-TERMINAL PROCESSING OF IPLA2B AND OF POT CLEAVAGE SITES OF APP CONSTRUCTS
IPLA2B 和 APP 构建体的 Pot 裂解位点的 N 端处理
- 批准号:
7355244 - 财政年份:2006
- 资助金额:
$ 0.44万 - 项目类别:
BROMOENOL LACTONE SUICIDE SUBSTR INACTIVATES IPLA2B BY GENERATING A DIFF
溴烯醇内酯自杀底物通过产生差异使 IPLA2B 失活
- 批准号:
7355273 - 财政年份:2006
- 资助金额:
$ 0.44万 - 项目类别:
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