HTS for Small Molecule Modulators of RGS Proteins
RGS 蛋白小分子调节剂的 HTS
基本信息
- 批准号:7188563
- 负责人:
- 金额:$ 4.88万
- 依托单位:
- 依托单位国家:美国
- 项目类别:
- 财政年份:2006
- 资助国家:美国
- 起止时间:2006-02-01 至 2008-01-31
- 项目状态:已结题
- 来源:
- 关键词:AccelerationAcidsAffinityBindingBiochemicalBiological AssayCalmodulinCell ProliferationCell physiologyCellsCellular AssayChemicalsCommercial SourcesCyclic AMPDependenceDevelopmentDiseaseDrug Delivery SystemsEvaluationFamilyFlow CytometryG-Protein-Coupled ReceptorsGTP-Binding Protein RegulatorsGTP-Binding ProteinsGuanosine DiphosphateGuanosine Triphosphate PhosphohydrolasesLaboratoriesLeadLibrariesLipid BindingLysophospholipidsMeasurementMeasuresMediatingMethodsNeoplasm MetastasisNucleotidesParkinson DiseasePhosphatidic AcidPlayProteinsQuantitative Structure-Activity RelationshipRGS ProteinsRoleSchizophreniaScreening procedureSecond Messenger SystemsSignal TransductionSiteSourceStructureSystemTechniquesTestingTherapeutic AgentsWorkbasehigh throughput screeninginhibitor/antagonistlysophosphatidic acidmouse Gdi2 proteinnovelnovel therapeuticspharmacophoreprotein functionprotein protein interactionsecond messengersmall moleculesmall molecule librariestool
项目摘要
DESCRIPTION (provided by applicant): Regulators of G-protein signaling (RGS) proteins are important modulators of signals initiated through G- protein coupled receptors (GPCRs). The action of RGS proteins is the acceleration of the deactivation of G- protein signals through modulation of G? subunit GTPase activity, which causes a termination of signal. While GPCRs have been classical drug targets, many cellular processes can be modulated by altering the action of RGS proteins. I propose to measure the interaction affinity of a variety of RGS proteins for their effector proteins (i.e. G?) using a novel high throughput flow cytometric method. With these parameters established, a library of diverse chemical compounds (~35,000) will be screened to identify modulators of RGS activity using the high throughput flow cytometric method. Once modulators are identified, complete quantitative structure-activity relationships will be evaluated and additional similar compounds will be characterized in both biochemical and cell-based assays. The use of these pharmacological modulators would provide utility for studying various disease in which RGS proteins could play a role, including Parkinson's disease (RGS9), Schizophrenia (RGS4), as well as cell proliferation and metastasis (LARG).
描述(由申请人提供):G蛋白信号传导调节剂(RGS)蛋白是通过G蛋白偶联受体(GPCR)启动的信号的重要调节剂。RGS蛋白的作用是通过调节G蛋白信号加速G蛋白信号的失活。亚基GT3活性,其导致信号的终止。虽然GPCR是经典的药物靶标,但许多细胞过程可以通过改变RGS蛋白的作用来调节。我建议测量的相互作用亲和力的各种RGS蛋白的效应蛋白(即G?)使用新的高通量流式细胞术方法。在建立这些参数的情况下,将使用高通量流式细胞术方法筛选不同化合物(约35,000种)的文库以鉴定RGS活性的调节剂。一旦确定了调节剂,将评估完整的定量结构-活性关系,并在生物化学和基于细胞的测定中表征其他类似化合物。这些药理学调节剂的使用将为研究RGS蛋白可发挥作用的各种疾病提供效用,包括帕金森病(RGS 9)、精神分裂症(RGS 4)以及细胞增殖和转移(LARG)。
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)
数据更新时间:{{ journalArticles.updateTime }}
{{
item.title }}
{{ item.translation_title }}
- DOI:
{{ item.doi }} - 发表时间:
{{ item.publish_year }} - 期刊:
- 影响因子:{{ item.factor }}
- 作者:
{{ item.authors }} - 通讯作者:
{{ item.author }}
数据更新时间:{{ journalArticles.updateTime }}
{{ item.title }}
- 作者:
{{ item.author }}
数据更新时间:{{ monograph.updateTime }}
{{ item.title }}
- 作者:
{{ item.author }}
数据更新时间:{{ sciAawards.updateTime }}
{{ item.title }}
- 作者:
{{ item.author }}
数据更新时间:{{ conferencePapers.updateTime }}
{{ item.title }}
- 作者:
{{ item.author }}
数据更新时间:{{ patent.updateTime }}
David L. Roman其他文献
The Concise Guide to PHARMACOLOGY 2023/24: Introduction and Other Protein Targets
药理学简明指南 2023/24:简介和其他蛋白质靶点
- DOI:
- 发表时间:
2023 - 期刊:
- 影响因子:7.3
- 作者:
S. Alexander;E. Kelly;A. Mathie;John A. Peters;E. Veale;J. Armstrong;O. Buneman;E. Faccenda;S. Harding;Michael Spedding;J. Cidlowski;Doriano Fabbro;Anthony P Davenport;Jörg Striessnig;J. Davies;K. Ahlers;Mohammed Alqinyah;T. Arumugam;Christopher R Bodle;Josephine Buo Dagner;B. Chakravarti;S. P. Choudhuri;Kirk M. Druey;R. Fisher;Kyle J Gerber;J. Hepler;S. Hooks;Havish S. Kantheti;Behirda Karaj;Somayeh Layeghi;Jae‐Kyung Lee;Zili Luo;Kirill Martemyanov;Luke D. Mascarenhas;Harrison J. McNabb;Carolina Montañez;Osita W. Ogujiofor;H. Phan;David L. Roman;Vincent S. Shaw;Benita Sjogren;C. Sobey;Mackenzie M. Spicer;Katherine E Squires;Laurie Sutton;Menbere Y Wendimu;Thomas M. Wilkie;Keqiang Xie;Qian Zhang;Yalda Zolghadri - 通讯作者:
Yalda Zolghadri
College of Pharmacy.
药学院。
- DOI:
- 发表时间:
- 期刊:
- 影响因子:0
- 作者:
D. Letendre;Gary Milavetz;Mary E. Ray;David L. Roman;Susan S. Vos - 通讯作者:
Susan S. Vos
Regulator of G Protein Signaling 17 as a Negative Modulator of GPCR Signaling in Multiple Human Cancers
- DOI:
10.1208/s12248-016-9894-1 - 发表时间:
2016-02-29 - 期刊:
- 影响因子:3.700
- 作者:
Michael P. Hayes;David L. Roman - 通讯作者:
David L. Roman
David L. Roman的其他文献
{{
item.title }}
{{ item.translation_title }}
- DOI:
{{ item.doi }} - 发表时间:
{{ item.publish_year }} - 期刊:
- 影响因子:{{ item.factor }}
- 作者:
{{ item.authors }} - 通讯作者:
{{ item.author }}
{{ truncateString('David L. Roman', 18)}}的其他基金
Predoctoral Training in the Pharmacological Sciences
药理学博士前培训
- 批准号:
10347969 - 财政年份:2022
- 资助金额:
$ 4.88万 - 项目类别:
Predoctoral Training in the Pharmacological Sciences
药理学博士前培训
- 批准号:
10621722 - 财政年份:2022
- 资助金额:
$ 4.88万 - 项目类别:
Non-opioids for inflammatory pain: Adenylyl cyclase 1 as a novel target
非阿片类药物治疗炎性疼痛:腺苷酸环化酶 1 作为新靶点
- 批准号:
10397712 - 财政年份:2021
- 资助金额:
$ 4.88万 - 项目类别:
Non-Opioids for Inflammatory Pain: Adenylyl Cyclase 1 as a Novel Target
非阿片类药物治疗炎症性疼痛:腺苷酸环化酶 1 作为新靶点
- 批准号:
10525509 - 财政年份:2021
- 资助金额:
$ 4.88万 - 项目类别:
Non-Opioids for Inflammatory Pain: Adenylyl Cyclase 1 as a Novel Target
非阿片类药物治疗炎症性疼痛:腺苷酸环化酶 1 作为新靶点
- 批准号:
10405130 - 财政年份:2021
- 资助金额:
$ 4.88万 - 项目类别:
Biochemical and Cell-Based HTS Assays for RGS17 Inhibitors
RGS17 抑制剂的生化和基于细胞的 HTS 测定
- 批准号:
8626364 - 财政年份:2012
- 资助金额:
$ 4.88万 - 项目类别:
Biochemical and Cell-Based HTS Assays for RGS17 Inhibitors
RGS17 抑制剂的生化和基于细胞的 HTS 测定
- 批准号:
8462940 - 财政年份:2012
- 资助金额:
$ 4.88万 - 项目类别:
Biochemical and Cell-Based HTS Assays for RGS17 Inhibitors
RGS17 抑制剂的生化和基于细胞的 HTS 测定
- 批准号:
8242653 - 财政年份:2012
- 资助金额:
$ 4.88万 - 项目类别:
HTS for Small Molecule Modulators of RGS Proteins
RGS 蛋白小分子调节剂的 HTS
- 批准号:
7054988 - 财政年份:2006
- 资助金额:
$ 4.88万 - 项目类别:
相似国自然基金
具有抗癌活性的天然产物金霉酸(Aureolic acids)全合成与选择性构建2-脱氧糖苷键
- 批准号:22007039
- 批准年份:2020
- 资助金额:24.0 万元
- 项目类别:青年科学基金项目
海洋放线菌来源聚酮类化合物Pteridic acids生物合成机制研究
- 批准号:
- 批准年份:2019
- 资助金额:10.0 万元
- 项目类别:省市级项目
手性Lewis Acids催化的分子内串联1,5-氢迁移/环合反应及其在构建结构多样性手性含氮杂环化合物中的应用
- 批准号:21372217
- 批准年份:2013
- 资助金额:80.0 万元
- 项目类别:面上项目
对空气稳定的新型的有机金属Lewis Acids催化剂制备、表征与应用研究
- 批准号:21172061
- 批准年份:2011
- 资助金额:30.0 万元
- 项目类别:面上项目
钛及含钛Lewis acids促臭氧/过氧化氢体系氧化性能的广普性、高效性及其机制
- 批准号:21176225
- 批准年份:2011
- 资助金额:60.0 万元
- 项目类别:面上项目
基于Zip Nucleic Acids引物对高度降解和低拷贝DNA检材的STR分型研究
- 批准号:81072511
- 批准年份:2010
- 资助金额:31.0 万元
- 项目类别:面上项目
海洋天然产物Makaluvic acids 的全合成及其对南海鱼虱存活的影响
- 批准号:30660215
- 批准年份:2006
- 资助金额:21.0 万元
- 项目类别:地区科学基金项目
相似海外基金
Lipid nanoparticle-mediated Inhalation delivery of anti-viral nucleic acids
脂质纳米颗粒介导的抗病毒核酸的吸入递送
- 批准号:
502577 - 财政年份:2024
- 资助金额:
$ 4.88万 - 项目类别:
CAREER: Highly Rapid and Sensitive Nanomechanoelectrical Detection of Nucleic Acids
职业:高度快速、灵敏的核酸纳米机电检测
- 批准号:
2338857 - 财政年份:2024
- 资助金额:
$ 4.88万 - 项目类别:
Continuing Grant
Double Incorporation of Non-Canonical Amino Acids in an Animal and its Application for Precise and Independent Optical Control of Two Target Genes
动物体内非规范氨基酸的双重掺入及其在两个靶基因精确独立光学控制中的应用
- 批准号:
BB/Y006380/1 - 财政年份:2024
- 资助金额:
$ 4.88万 - 项目类别:
Research Grant
Quantifying L-amino acids in Ryugu to constrain the source of L-amino acids in life on Earth
量化 Ryugu 中的 L-氨基酸以限制地球生命中 L-氨基酸的来源
- 批准号:
24K17112 - 财政年份:2024
- 资助金额:
$ 4.88万 - 项目类别:
Grant-in-Aid for Early-Career Scientists
Synthetic analogues based on metabolites of omega-3 fatty acids protect mitochondria in aging hearts
基于 omega-3 脂肪酸代谢物的合成类似物可保护衰老心脏中的线粒体
- 批准号:
477891 - 财政年份:2023
- 资助金额:
$ 4.88万 - 项目类别:
Operating Grants
Metabolomic profiles of responders and non-responders to an omega-3 fatty acids supplementation.
对 omega-3 脂肪酸补充剂有反应和无反应者的代谢组学特征。
- 批准号:
495594 - 财政年份:2023
- 资助金额:
$ 4.88万 - 项目类别:
Molecular recognition and enantioselective reaction of amino acids
氨基酸的分子识别和对映选择性反应
- 批准号:
23K04668 - 财政年份:2023
- 资助金额:
$ 4.88万 - 项目类别:
Grant-in-Aid for Scientific Research (C)
Integrated understanding and manipulation of hypoxic cellular functions by artificial nucleic acids with hypoxia-accumulating properties
具有缺氧累积特性的人工核酸对缺氧细胞功能的综合理解和操纵
- 批准号:
23H02086 - 财政年份:2023
- 资助金额:
$ 4.88万 - 项目类别:
Grant-in-Aid for Scientific Research (B)
Basic research toward therapeutic strategies for stress-induced chronic pain with non-natural amino acids
非天然氨基酸治疗应激性慢性疼痛策略的基础研究
- 批准号:
23K06918 - 财政年份:2023
- 资助金额:
$ 4.88万 - 项目类别:
Grant-in-Aid for Scientific Research (C)
Molecular mechanisms how arrestins that modulate localization of glucose transporters are phosphorylated in response to amino acids
调节葡萄糖转运蛋白定位的抑制蛋白如何响应氨基酸而被磷酸化的分子机制
- 批准号:
23K05758 - 财政年份:2023
- 资助金额:
$ 4.88万 - 项目类别:
Grant-in-Aid for Scientific Research (C)