Search Results - "Tsalkova, Tamara"
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Epac and PKA: a tale of two intracellular cAMP receptors
Published in Acta biochimica et biophysica Sinica (01-07-2008)“…cAMP‐mediated signaling pathways regulate a multitude of important biological processes under both physiological and pathological conditions, including…”
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A novel EPAC-specific inhibitor suppresses pancreatic cancer cell migration and invasion
Published in Molecular pharmacology (01-01-2013)“…Exchange protein directly activated by cAMP (EPAC) and cAMP-dependent protein kinase (PKA) are two intracellular receptors that mediate the effects of the…”
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Isoform-specific antagonists of exchange proteins directly activated by cAMP
Published in Proceedings of the National Academy of Sciences - PNAS (06-11-2012)“…The major physiological effects of cAMP in mammalian cells are transduced by two ubiquitously expressed intracellular cAMP receptors, protein kinase A (PKA)…”
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A fluorescence-based high-throughput assay for the discovery of exchange protein directly activated by cyclic AMP (EPAC) antagonists
Published in PloS one (19-01-2012)“…The discovery, more than ten years ago, of exchange proteins directly activated by cAMP (EPAC) as a new family of intracellular cAMP receptors revolutionized…”
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Identification and Characterization of Small Molecules as Potent and Specific EPAC2 Antagonists
Published in Journal of medicinal chemistry (14-02-2013)“…EPAC1 and EPAC2, two isoforms of exchange proteins directly activated by cAMP (EPAC), respond to the second messenger cAMP and regulate a wide variety of…”
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Stimulation of Proglucagon Gene Expression by Human GPR119 in Enteroendocrine L-cell Line GLUTag
Published in Molecular endocrinology (Baltimore, Md.) (01-08-2013)“…GPR119 is a G protein-coupled receptor expressed on enteroendocrine L-cells that synthesize and secrete the incretin hormone glucagon-like peptide-1 (GLP-1)…”
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Mechanism of Interactions of α-Naphthoflavone with Cytochrome P450 3A4 Explored with an Engineered Enzyme Bearing a Fluorescent Probe
Published in Biochemistry (Easton) (09-01-2007)“…Design of a partially cysteine-depleted C98S/C239S/C377S/C468A cytochrome P450 3A4 mutant designated CYP3A4(C58,C64) allowed site-directed incorporation of…”
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Structural analyses of a constitutively active mutant of exchange protein directly activated by cAMP
Published in PloS one (26-11-2012)“…Exchange proteins directly activated by cAMP (EPACs) are important allosteric regulators of cAMP-mediated signal transduction pathways. To understand the…”
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Effect of glutathione on homo- and heterotropic cooperativity in cytochrome P450 3A4
Published in Archives of biochemistry and biophysics (15-03-2008)“…Glutathione (GSH) exerted a profound effect on the oxidation of 7-benzyloxy-4-(trifluoromethyl)coumarin (BFC) and 7-benzyloxyquinoline (BQ) by human liver…”
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Mechanism of Intracellular cAMP Sensor Epac2 Activation
Published in The Journal of biological chemistry (01-05-2011)“…Epac2, a guanine nucleotide exchange factor, regulates a wide variety of intracellular processes in response to second messenger cAMP. In this study, we have…”
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Mechanism of Epac Activation
Published in The Journal of biological chemistry (28-08-2009)“…Epac2 is a member of the family of exchange proteins directly activated by cAMP (Epac). Our previous studies suggest a model of Epac activation in which cAMP…”
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Developing Pharmacological Probes Targeting exchange protein directly activated by cAMP
Published in The FASEB journal (01-04-2013)“…Abstract only Cyclic adenosine monophosphate (cAMP), a prototypical second messenger, regulates a myriad of important biological processes under both…”
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5-Cyano-6-oxo-1,6-dihydro-pyrimidines as potent antagonists targeting exchange proteins directly activated by cAMP
Published in Bioorganic & medicinal chemistry letters (15-06-2012)“…Exchange proteins directly activated by cAMP (Epac) are a family of guanine nucleotide exchange factors that regulate a wide variety of intracellular processes…”
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Truncations at the NH2 Terminus of Rhodanese Destabilize the Enzyme and Decrease Its Heterologous Expression
Published in The Journal of biological chemistry (23-10-1998)“…Rhodanese mutants containing sequential NH2-terminal deletions were constructed to test the distinct contributions of this region of the protein to expression,…”
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A Fluorescence-Based High-Throughput Assay for the Discovery of Exchange Protein Directly Activated by Cyclic AMP
Published in PloS one (19-01-2012)“…Background The discovery, more than ten years ago, of exchange proteins directly activated by cAMP (EPAC) as a new family of intracellular cAMP receptors…”
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Mechanism of intracellular cAMP sensor Epac2 activation: cAMP-induced conformational changes identified by amide hydrogen/deuterium exchange mass spectrometry (DXMS)
Published in The Journal of biological chemistry (20-05-2011)“…Epac2, a guanine nucleotide exchange factor, regulates a wide variety of intracellular processes in response to second messenger cAMP. In this study, we have…”
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Conformational States of Exchange Protein Directly Activated by cAMP (EPAC1) Revealed by Ensemble Modeling and Integrative Structural Biology
Published in Cells (Basel, Switzerland) (21-12-2019)“…Exchange proteins directly activated by cAMP (EPAC1 and EPAC2) are important allosteric regulators of cAMP-mediated signal transduction pathways. To understand…”
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Mechanism of Epac Activation: STRUCTURAL AND FUNCTIONAL ANALYSES OF Epac2 HINGE MUTANTS WITH CONSTITUTIVE AND REDUCED ACTIVITIES
Published in The Journal of biological chemistry (28-08-2009)“…Epac2 is a member of the family of exchange proteins directly activated by cAMP (Epac). Our previous studies suggest a model of Epac activation in which cAMP…”
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Exchange protein directly activated by cyclic AMP isoform 2 is not a direct target of sulfonylurea drugs
Published in Assay and drug development technologies (01-02-2011)“…It has been reported by Zhang et al. that antidiabetic sulfonylurea drugs promote insulin secretion by directly binding to exchange protein directly activated…”
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