4f7z | pdb_00004f7z

Conformational dynamics of exchange protein directly activated by cAMP

spinqualitylabelsall models 4f7z, resolution 2.60Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 4f7z is a 1 chain structure with sequence from Mus musculus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: GOL Gene: Rapgef4, Cgef2, Epac2 (Mus musculus) Resources: FirstGlance, OCA, RCSB, PDBsum Function [RPGF4_MOUSE] Guanine nucleotide exchange factor (GEF) for RAP1A, RAP1B and RAP2A small GTPases that is activated by binding cAMP. Seems not to activate RAB3A. Involved in cAMP-dependent, PKA-independent exocytosis through interaction with RIMS2. Publication Abstract from PubMed Exchange proteins directly activated by cAMP (EPACs) are important allosteric regulators of cAMP-mediated signal transduction pathways. To understand the molecular mechanism of EPAC activation, we have combined site-directed mutagenesis, X-ray crystallography, and peptide amide hydrogen/deuterium exchange mass spectrometry (DXMS) to probe the structural and conformational dynamics of EPAC2-F435G, a constitutively active EPAC2 mutant. Our study demonstrates that conformational dynamics plays a critical role in cAMP-induced EPAC activation. A glycine mutation at 435 position shifts the equilibrium of conformational dynamics towards the extended active conformation. Structural analyses of a constitutively active mutant of exchange protein directly activated by cAMP.,White MA, Li S, Tsalkova T, Mei FC, Liu T, Woods VL Jr, Cheng X PLoS One. 2012;7(11):e49932. doi: 10.1371/journal.pone.0049932. Epub 2012 Nov 26. PMID:23189173 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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