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Synthesis, Molecular Modelling Studies and Biological Evaluation of New Oxoeicosanoid Receptor 1 Agonists by Tomasz Maciej Stepniewski; Mariona Torrens-Fontanals; Ismael Rodríguez-Espigares; Toni Giorgino; Karoline G. Primdahl; Anders Vik; Yngve Stenstrøm; Jana Selent; Trond Vidar Hansen is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Synthesis, Molecular Modelling Studies and Biological Evaluation of New Oxoeicosanoid Receptor 1 Agonists about?
The oxoeicosanoid receptor 1 (OXER1) is a member of the G-protein coupled receptors (GPCR) family, and is involved in inflammatory processes and oncogenesis. As such it is an attractive target for pharmacological intervention. The present study aimed to shed light on the molecular fundaments of OXER1 modulation using chemical probes structurally related to the natural agonist 5-oxo-ETE. In a first step, 5-oxo-ETE and its closely related derivatives (5-oxo-EPE and 4-oxo-DHA) were obtained by conducting concise and high-yielding syntheses. The biological activity of obtained compounds was assessed in terms of potency (EC) and efficacy (E) for arrestin recruitment. Finally, molecular modelling and simulation were used to explore binding characteristics of 5-oxo-ETE and derivatives with the aim to rationalize biological activity. Our data suggest that the tested 5-oxo-ETE derivatives (i) insert quickly into the membrane, (ii) access the receptor via transmembrane helices (TMs) 5 and 6 from the membrane side and (iii) drive potency and efficacy by differential interaction with TM5 and 7. Most importantly, we found that the methyl ester of 5-oxo-ETE (1a) showed even a higher maximum resp
Who reads Synthesis, Molecular Modelling Studies and Biological Evaluation of New Oxoeicosanoid Receptor 1 Agonists?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Tomasz Maciej Stepniewski; Mariona Torrens-Fontanals; Ismael Rodríguez-Espigares; Toni Giorgino; Karoline G. Primdahl; Anders Vik; Yngve Stenstrøm; Jana Selent; Trond Vidar Hansen
- Publisher
- Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)
- Published
- 2018
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)