title: Structure and functional roles of Epac2 (Rapgef4).
abstract: Epac (exchange protein activated by cyclic-AMP) 2 is a direct target of 3'-5'-cyclic adenosine monophosphate (cAMP) and is involved in cAMP-mediated signal transduction through activation of the Ras-like small GTPase Rap. Crystallographic analyses revealed that activation of Epac2 by cAMP is accompanied by dynamic structural changes. Epac2 is expressed mainly in brain, neuroendocrine and endocrine tissues, and is involved in diverse cellular functions in the tissues. In this review, we summarize the structure and function of Epac2. We also discuss the physiological and pathophysiological roles of Epac2, and the possibility of Epac2 as a therapeutic target.
authors.affiliation: Division of Diabetes and Endocrinology, Kobe University Graduate School of Medicine, Kobe, Japan; Division of Molecular and Metabolic Medicine, Kobe University Graduate School of Medicine, Kobe, Japan.
authors.forename: Kenji
authors.initials: K
authors.lastname: Sugawara
authors.affiliation: Division of Molecular and Metabolic Medicine, Kobe University Graduate School of Medicine, Kobe, Japan.
authors.forename: Tadao
authors.initials: T
authors.lastname: Shibasaki
authors.affiliation: Division of Molecular and Metabolic Medicine, Kobe University Graduate School of Medicine, Kobe, Japan.
authors.forename: Harumi
authors.initials: H
authors.lastname: Takahashi
authors.affiliation: Division of Molecular and Metabolic Medicine, Kobe University Graduate School of Medicine, Kobe, Japan. Electronic address: seino@med.kobe-u.ac.jp.
authors.forename: Susumu
authors.initials: S
authors.lastname: Seino
mesh_terms: D000818:Animals; D001921:Brain / Q000378:metabolism; D000242:Cyclic AMP / Q000378:metabolism*; D004703:Endocrine System / Q000378:metabolism; D020662:Guanine Nucleotide Exchange Factors / Q000737:chemistry* / Q000378:metabolism*; D006801:Humans; D009206:Myocardium / Q000378:metabolism; D011487:Protein Conformation; D015398:Signal Transduction; D018631:ras Proteins / Q000378:metabolism
chemical_list: D020662:Guanine Nucleotide Exchange Factors; C442864:RAPGEF4 protein, human; D000242:Cyclic AMP; D018631:ras Proteins
keywords: Epac2; Rap; cAMP