A fluorescence-based high-throughput assay for the discovery of exchange protein directly activated by cyclic AMP (EPAC) antagonists
about
Exchange protein directly activated by cAMP encoded by the mammalian rapgef3 gene: Structure, function and therapeuticsRecent advances in the discovery of small molecules targeting exchange proteins directly activated by cAMP (EPAC).5-Cyano-6-oxo-1,6-dihydro-pyrimidines as potent antagonists targeting exchange proteins directly activated by cAMP.A novel EPAC-specific inhibitor suppresses pancreatic cancer cell migration and invasionIsoform-specific antagonists of exchange proteins directly activated by cAMPIdentification of a tetrahydroquinoline analog as a pharmacological inhibitor of the cAMP-binding protein Epac.Cyclic AMP sensor EPAC proteins and energy homeostasis.The future of EPAC-targeted therapies: agonism versus antagonismBiochemical and pharmacological characterizations of ESI-09 based EPAC inhibitors: defining the ESI-09 "therapeutic window".Identification and characterization of small molecules as potent and specific EPAC2 antagonists.Identification of a Novel, Small Molecule Partial Agonist for the Cyclic AMP Sensor, EPAC1.Structure-Activity Relationship Studies of Substituted 2-(Isoxazol-3-yl)-2-oxo-N'-phenyl-acetohydrazonoyl Cyanide Analogues: Identification of Potent Exchange Proteins Directly Activated by cAMP (EPAC) Antagonists.Efficient Synthesis of ESI-09, A Novel Non-cyclic Nucleotide EPAC AntagonistCritical role for Epac1 in inflammatory pain controlled by GRK2-mediated phosphorylation of Epac1.Functionalized N,N-Diphenylamines as Potent and Selective EPAC2 Inhibitors.Identification and validation of modulators of exchange protein activated by cAMP (Epac) activity: structure-function implications for Epac activation and inhibition.Epac proteins: specific ligands and role in cardiac remodelling.A-kinase anchoring proteins: cAMP compartmentalization in neurodegenerative and obstructive pulmonary diseases.Exchange proteins directly activated by cAMP (EPACs): Emerging therapeutic targets.Lithium and an EPAC-specific inhibitor ESI-09 synergistically suppress pancreatic cancer cell proliferation and survival.A cell-based, quantitative and isoform-specific assay for exchange proteins directly activated by cAMP.Structure-activity relationships of 2-substituted phenyl-N-phenyl-2-oxoacetohydrazonoyl cyanides as novel antagonists of exchange proteins directly activated by cAMP (EPACs).FRET-based binding assay between a fluorescent cAMP analogue and a cyclic nucleotide-binding domain tagged with a CFP.The Potential of a Novel Class of EPAC-Selective Agonists to Combat Cardiovascular Inflammation.Structure-Activity Relationship Studies with Tetrahydroquinoline Analogs as EPAC Inhibitors.Identification of novel 2-(benzo[d]isoxazol-3-yl)-2-oxo-N-phenylacetohydrazonoyl cyanide analoguesas potent EPAC antagonists.Intracellular cAMP Sensor EPAC: Physiology, Pathophysiology, and Therapeutics Development.
P2860
Q28608179-157FC8BD-7846-4215-B953-40039A3BF1BCQ30405298-79C12DF3-2A8E-4156-B258-C17AF3060BA1Q34274771-945FDF3C-ADC1-4F3E-AC24-C41876830CCDQ34306163-2400CAED-8D93-49C5-8A46-02BC2CFB922CQ34307662-6B919F09-2D03-4CA6-B31F-C5B43E14C137Q34310769-CDF9011B-392F-4E83-87E3-66700C49D2FEQ34385094-65DED850-0A25-4CFC-8774-7AEC18C33CB1Q34465923-FC815355-1D5E-4B4C-8CD2-66A6128292E6Q34467944-AB796551-46C8-449F-9B3E-D1D28D587224Q34535973-EA091671-6259-4372-9212-939008E25EECQ36319044-4BAA4221-CCDC-42AC-97CA-A25CD7D61B48Q36624204-6A9998C2-0350-4ACF-B4FC-747E9B6B6ED8Q36634333-67F56709-764A-4991-BD9C-48B745E7A7A3Q36710634-48DDA921-5B2C-40CA-8E43-E3D35156165DQ36902839-0268083B-BEFB-4265-87B1-B8065E2CCBF4Q37653245-61035A28-6C48-4374-A77A-979294B75342Q38197308-953C893A-1E28-4F2D-8148-278626B9E0C0Q38240756-918A29D2-E4A2-41EF-AE14-FE36E73867DDQ38747476-1DB74812-C801-4FFA-9EB8-39942A755288Q38802133-A044DBEC-6E5D-4DDD-987F-1064B366A19DQ41108182-69E6C08F-86E9-4F74-BD1E-E8A91D357746Q47443813-F6BEB607-5FC2-4E8D-8DDB-743C5CC89D5BQ48057277-F1772A89-F1E8-4DCA-8062-85D4A544BBCBQ48172039-5BE8569B-9181-4A2F-9FD4-A4020B13C516Q49497128-93FC9990-338D-4745-A7E0-2677C010C08DQ51063407-37DBA23F-2457-4B97-9198-21B1D6D7553CQ52656382-B9C1380E-0B04-4E92-9FA5-E516FE0E9633
P2860
A fluorescence-based high-throughput assay for the discovery of exchange protein directly activated by cyclic AMP (EPAC) antagonists
description
2012 nî lūn-bûn
@nan
2012 թուականին հրատարակուած գիտական յօդուած
@hyw
2012 թվականին հրատարակված գիտական հոդված
@hy
2012年の論文
@ja
2012年論文
@yue
2012年論文
@zh-hant
2012年論文
@zh-hk
2012年論文
@zh-mo
2012年論文
@zh-tw
2012年论文
@wuu
name
A fluorescence-based high-thro ...... cyclic AMP (EPAC) antagonists
@ast
A fluorescence-based high-thro ...... cyclic AMP (EPAC) antagonists
@en
A fluorescence-based high-thro ...... cyclic AMP (EPAC) antagonists
@nl
type
label
A fluorescence-based high-thro ...... cyclic AMP (EPAC) antagonists
@ast
A fluorescence-based high-thro ...... cyclic AMP (EPAC) antagonists
@en
A fluorescence-based high-thro ...... cyclic AMP (EPAC) antagonists
@nl
prefLabel
A fluorescence-based high-thro ...... cyclic AMP (EPAC) antagonists
@ast
A fluorescence-based high-thro ...... cyclic AMP (EPAC) antagonists
@en
A fluorescence-based high-thro ...... cyclic AMP (EPAC) antagonists
@nl
P2093
P2860
P1433
P1476
A fluorescence-based high-thro ...... cyclic AMP (EPAC) antagonists
@en
P2093
Fang C Mei
Tamara Tsalkova
Xiaodong Cheng
P2860
P304
P356
10.1371/JOURNAL.PONE.0030441
P407
P577
2012-01-01T00:00:00Z