FUNCTIONAL STUDIES OF HUMAN AND SOYBEAN LIPOXYGENASE
FUNCTIONAL STUDIES OF HUMAN AND SOYBEAN LIPOXYGENASE
批准号:
6386709
负责人:
Theodore R Holman
金额:
$10.46万
依托单位国家:
美国
项目类别:
财政年份:
1997
资助国家:
美国
项目状态:
已结题
起止时间:
1997-05-01 至 2002-04-30
中文摘要
描述:脂氧合酶(LO)是催化
将分子氧引入含1,4-顺,顺-戊二烯的脂肪族
酸,并广泛分布于整个植物和动物王国。
这种酶的活性与植物的发芽、人类的生长和发育有关。
哮喘和关节炎。 酶的活性部位含有一个必需的
铁原子 已经提出了两种不同的LO催化机制。
第一个涉及一个自由基为基础的机制,其中活性位点铁
离子将亚油酸(LA)的1,4-二烯氧化成脂肪酸自由基。
第二种机制使用三价铁来促进
通过协调所得的碳酸化作用,
有机金属中间体 因此,这两种机制的关键区别在于
是铁中心的作用以及它如何激活质子提取。
这项建议涉及光谱和动力学研究,目的是
研究了活性中心铁的结构和功能,
大豆和人脂氧合酶。 此外,一些活跃的网站
突变体的设计,以影响电子结构的铁及其
将研究反应性。 光谱技术(例如,EPR,MCD,
EXAFS)将用于确定铁配位和/或
电子环境。 这些研究将与动力学相关
调查,解决结构变化对
反应性以及pH、粘度和同位素的影响
替代品
所获得的信息将用于确定一个统一的理论,
Fe中心的结构与催化氧化作用
反应.
英文摘要
DESCRIPTION: Lipoxygenases (LOs) are enzymes that catalyze the
incorporation of dioxygen into 1,4-cis,cis-pentadiene containing fatty
acids, and are widely distributed throughout the plant and animal kingdoms.
The activity of the enzyme has been implicated in plant germination, human
asthma and arthritis. The active site of the enzyme contains an essential
iron atom. Two distinct mechanisms for LO catalysis have been proposed.
The first involves a radical based mechanism in which the active site ferric
ion oxidizes the 1,4-diene of linoleic acid (LA) to a fatty acid radical.
The second mechanism uses the ferric iron to facilitate de-protonation of
the substrate by coordinating the resulting carbonation to form an
organometallic intermediate. Thus, the key difference in the two mechanisms
is the role of the iron center and how it activates the proton abstraction.
This proposal involves spectroscopic and kinetic studies aimed at
investigating the structure and function of the active site iron in both
soybean and human lipoxygenases. In addition, a number of active site
mutants designed to affect the electronic structure of the iron and its
reactivity will be studied. Spectroscopic techniques (e.g., EPR, MCD,
EXAFS) will be used to determine the changes in the iron coordination and/or
electronic environment. These studies will be correlated to kinetic
investigations that address the effect of the structural changes on
reactivity as well as the effects of pH, viscosity and isotopic
substitutions.
The information obtained will be used to determine a unified theory of the
structure and function of the Fe center in catalyzing the oxidation
reactions.
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DOI:
10.1371/journal.pone.0104094
发表时间:
2014
期刊:
PloS one
影响因子:
3.7
作者:
[Jameson JB 2nd, Kantz A, Schultz L, Kalyanaraman C, Jacobson MP, Maloney DJ, Jadhav A, Simeonov A, Holman TR]
通讯作者:
Holman TR
Azole Antifungal Sensitivity of Sterol 14α-Demethylase (CYP51) and CYP5218 from Malassezia globosa.
来自球形马拉色菌的甾醇 14α-脱甲基酶 (CYP51) 和 CYP5218 的唑类抗真菌敏感性。
DOI:
10.1038/srep27690
发表时间:
2016
期刊:
Scientific reports
影响因子:
4.6
作者:
[Warrilow,AndrewGS, Price,ClaireL, Parker,JosieE, Rolley,NicolaJ, Smyrniotis,ChristopherJ, Hughes,DavidD, Thoss,Vera, Nes,WDavid, Kelly,DianeE, Holman,TheodoreR, Kelly,StevenL]
通讯作者:
Kelly,StevenL
Spectroscopic characterization of soybean lipoxygenase-1 mutants: the role of second coordination sphere residues in the regulation of enzyme activity.
大豆脂氧合酶-1突变体的光谱表征:第二配位球残基在酶活性调节中的作用。
DOI:
10.1021/bi027380g
发表时间:
2003
期刊:
Biochemistry
影响因子:
2.9
作者:
[Schenk,Gerhard, Neidig,MichaelL, Zhou,Jing, Holman,TheodoreR, Solomon,EdwardI]
通讯作者:
Solomon,EdwardI
Structural and functional characterization of second-coordination sphere mutants of soybean lipoxygenase-1.
大豆脂氧合酶-1第二配位球突变体的结构和功能表征。
DOI:
10.1021/bi002893d
发表时间:
2001
期刊:
Biochemistry
影响因子:
2.9
作者:
[Tomchick,DR, Phan,P, Cymborowski,M, Minor,W, Holman,TR]
通讯作者:
Holman,TR
Evidence for downregulation of calcium signaling proteins in advanced mouse adenocarcinoma.
晚期小鼠腺癌中钙信号蛋白下调的证据。
DOI:
10.1002/pros.20207
发表时间:
2005
期刊:
The Prostate.
影响因子:
--
作者:
[Ruddat,ViolaC, Whitman,Stephanie, Klein,RussellD, Fischer,SusanM, Holman,TheodoreR]
通讯作者:
Holman,TheodoreR
共 14 条
Discovery of 12/15-lipoxygenase therapeutics for Alzheimer's disease
-
批准号:10427370
-
项目类别:
-
资助金额:$53.44万
-
财政年份:2018
-
负责人:Theodore R Holman
-
依托单位:
Discovery of 12/15-lipoxygenase therapeutics for Alzheimer's disease
-
批准号:9789803
-
项目类别:
-
资助金额:$55.27万
-
财政年份:2018
-
负责人:Theodore R Holman
-
依托单位:
Discovery of 12/15-Lipoxygenase Inhibitors for Alzheimer's Disease
-
批准号:9763402
-
项目类别:
-
资助金额:$19.59万
-
财政年份:2018
-
负责人:Theodore R Holman
-
依托单位:
Discovery of Potent 12-Lipoxygenase Inhibitors of Platelet Activation
-
批准号:8746993
-
项目类别:
-
资助金额:$49.65万
-
财政年份:2014
-
负责人:Theodore R Holman
-
依托单位:
Discovery of Potent 12-Lipoxygenase Inhibitors of Platelet Activation
-
批准号:9151693
-
项目类别:
-
资助金额:$45.94万
-
财政年份:2014
-
负责人:Theodore R Holman
-
依托单位:
Development of Potent/Selective Lipoxygenase Therapeutics Against Stroke Injury
-
批准号:8632065
-
项目类别:
-
资助金额:$56.08万
-
财政年份:2013
-
负责人:Theodore R Holman
-
依托单位:
Functional and inhibitory studies of human lipoxygenase
-
批准号:7820039
-
项目类别:
-
资助金额:$56.95万
-
财政年份:2009
-
负责人:Theodore R Holman
-
依托单位:
High Throughput and Virtual Screening for Human 12-LO, 15-LO-1, and 15-LO-2 Inhib
-
批准号:7368412
-
项目类别:
-
资助金额:$2.5万
-
财政年份:2007
-
负责人:Theodore R Holman
-
依托单位:
NCRR: UCSC Acquisition of a Thermo Electron LTQ-Mass Spectrometer
-
批准号:7046277
-
项目类别:
-
资助金额:$36.85万
-
财政年份:2006
-
负责人:Theodore R Holman
-
依托单位:
THERMO ELECTRON LTQ-FT MASS SPECTROMETER
-
批准号:7335010
-
项目类别:
-
资助金额:$36.85万
-
财政年份:2006
-
负责人:Theodore R Holman
-
依托单位:
FUNCTIONAL STUDIES OF HUMAN AND SOYBEAN LIPOXYGENASE
-
批准号:2910348
-
项目类别:
-
资助金额:$9.85万
-
财政年份:1997
-
负责人:Theodore R Holman
-
依托单位:
Functional and inhibitory studies of human lipoxygenase
-
批准号:8366611
-
项目类别:
-
资助金额:$4.76万
-
财政年份:1997
-
负责人:Theodore R Holman
-
依托单位:
Functional and inhibitory studies of human lipoxygenase
-
批准号:8298691
-
项目类别:
-
资助金额:$2.1万
-
财政年份:1997
-
负责人:Theodore R Holman
-
依托单位:
FUNCTIONAL STUDIES OF HUMAN AND SOYBEAN LIPOXYGENASE
-
批准号:2024604
-
项目类别:
-
资助金额:$9.29万
-
财政年份:1997
-
负责人:Theodore R Holman
-
依托单位:
Functional and inhibitory studies of human lipoxygenase
-
批准号:7919704
-
项目类别:
-
资助金额:$1.51万
-
财政年份:1997
-
负责人:Theodore R Holman
-
依托单位:
Functional and Inhibitory Studies of Human Lipoxygenase
-
批准号:6895773
-
项目类别:
-
资助金额:$28.12万
-
财政年份:1997
-
负责人:Theodore R Holman
-
依托单位:
Functional and inhibitory studies of human lipoxygenase
-
批准号:7743078
-
项目类别:
-
资助金额:$34.06万
-
财政年份:1997
-
负责人:Theodore R Holman
-
依托单位:
Functional and inhibitory studies of human lipoxygenase
-
批准号:7996025
-
项目类别:
-
资助金额:$29.17万
-
财政年份:1997
-
负责人:Theodore R Holman
-
依托单位:
Functional and Inhibitory Studies of Human Lipoxygenase
-
批准号:6640284
-
项目类别:
-
资助金额:$29.8万
-
财政年份:1997
-
负责人:Theodore R Holman
-
依托单位:
Functional and Inhibitory Studies of Human Lipoxygenase
-
批准号:6751914
-
项目类别:
-
资助金额:$29.8万
-
财政年份:1997
-
负责人:Theodore R Holman
-
依托单位:
海外基金