background:
The activation of RaP1 by cAMP is independent of PKA and is mediated by recently discovered family of guanine nucleotide exchange factors (GEFs) called cAMP-GEFs or Epacs. The Epac signaling therefore represents a novel mechanism for cAMP signaling with in the cAMP cascade. There are 2 members of the Epac family, Epac1 and Epac 2. Both proteins are multidomain proteins containing an autoinhibitory cAMP-binding domain that inhibits the catalytic region and a DEP domain (dishevelled, Egl-10 and pleckstrin homology domain) targeting the membrane anchors. EPAC2 has an additional cAMP-binding site in its N-terminus that binds cAMP with low affinity. EPAC1 mRNA is broadly expressed, with particularly high levels occurring in the thyroid, ovary, kidney and certain brain regions, whereas expression of EPAC2 mRNA appears to be restricted to the brain and adrenal glands. Epac 1 and Epac 2 also interact with light chain 2 (LC2) or MAP1A that serves as a scaffolding structure to stabilize the signal transduction complex. The Epac 1-selective antibodies were generated against unique antigenic sequences form near N-terminus and between RasGEFN and Ras GEF domains. The antibodies to Epac 1are affinity purified over immobilized antigen based chromatography.
Function:
Guanine nucleotide exchange factor (GEF) for RAP1A and RAP2A small GTPases that is activated by binding cAMP. Through simultaneous binding of PDE3B to RAPGEF3 and PIK3R6 is assembled in a signaling complex in which it activates the PI3K gamma complex and which is involved in angiogenesis.
Subunit:
Interacts with PDE3B.
Subcellular Location:
Endomembrane system
Tissue Specificity:
Widely expressed with highest levels in adult kidney, heart, thyroid and brain, and fetal kidney.
Similarity:
Contains 1 cyclic nucleotide-binding domain.
Contains 1 DEP domain.
Contains 1 N-terminal Ras-GEF domain.
Contains 1 Ras-GEF domain.
Database links:
Entrez Gene: 10411 Human
Entrez Gene: 223864 Mouse
Entrez Gene: 59326 Rat
Omim: 606057 Human
SwissProt: O95398 Human
SwissProt: Q8VCC8 Mouse
SwissProt: Q9Z1C8 Rat
Unigene: 8578 Human
Unigene: 42899 Rat
Important Note:
This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications.
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