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International Journal of Molecular Medicine
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Print ISSN: 1107-3756 Online ISSN: 1791-244X
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October 2008 Volume 22 Issue 4

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International Journal of Molecular Medicine

International Journal of Molecular Medicine

International Journal of Molecular Medicine is an international journal devoted to molecular mechanisms of human disease.

International Journal of Oncology

International Journal of Oncology

International Journal of Oncology is an international journal devoted to oncology research and cancer treatment.

Molecular Medicine Reports

Molecular Medicine Reports

Covers molecular medicine topics such as pharmacology, pathology, genetics, neuroscience, infectious diseases, molecular cardiology, and molecular surgery.

Oncology Reports

Oncology Reports

Oncology Reports is an international journal devoted to fundamental and applied research in Oncology.

Experimental and Therapeutic Medicine

Experimental and Therapeutic Medicine

Experimental and Therapeutic Medicine is an international journal devoted to laboratory and clinical medicine.

Oncology Letters

Oncology Letters

Oncology Letters is an international journal devoted to Experimental and Clinical Oncology.

Biomedical Reports

Biomedical Reports

Explores a wide range of biological and medical fields, including pharmacology, genetics, microbiology, neuroscience, and molecular cardiology.

Molecular and Clinical Oncology

Molecular and Clinical Oncology

International journal addressing all aspects of oncology research, from tumorigenesis and oncogenes to chemotherapy and metastasis.

World Academy of Sciences Journal

World Academy of Sciences Journal

Multidisciplinary open-access journal spanning biochemistry, genetics, neuroscience, environmental health, and synthetic biology.

International Journal of Functional Nutrition

International Journal of Functional Nutrition

Open-access journal combining biochemistry, pharmacology, immunology, and genetics to advance health through functional nutrition.

International Journal of Epigenetics

International Journal of Epigenetics

Publishes open-access research on using epigenetics to advance understanding and treatment of human disease.

Medicine International

Medicine International

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Article

Evaluation of novel cyclic analogues of apelin

  • Authors:
    • Juri Hamada
    • Junko Kimura
    • Junji Ishida
    • Takeo Kohda
    • Setsuo Morishita
    • Shigeyasu Ichihara
    • Akiyoshi Fukamizu

  • View Affiliations / Copyright

    Affiliations: Ankhs Incorporated, Tsukuba Industrial Liaison and Cooperative Research Center, University of Tsukuba, Tsukuba, Ibaraki 305-8577, Japan
  • Pages: 547-552
    |
    Published online on: October 1, 2008
       https://doi.org/10.3892/ijmm_00000054
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Abstract

Apelin regulates various cell signaling processes through interaction with its specific cell-surface receptor, APJ, which is a member of a seven transmembrane G protein-coupled receptor superfamily. To develop a novel apelin analogue, we synthesized cyclic analogues of minimal apelin fragment RPRLSHKGPMPF (apelin-12), and evaluated their bioactivities in a recombinant human APJ-expressed cell line. Three cyclic analogues were synthesized: cyclo apelin-12 (C1) in combination with amino-terminal to carboxy-terminal, cyclourea apelin-12 (C3) in combination with amino-terminal and amino acid side chain at positions 7, and cyclic apelin-12 (C4) in combination with amino acid side chain at positions 7 to carboxy-terminal. All cyclic analogues exhibited dose-dependent inhibitory effects against forskolin-induced cyclic adenosine monophosphate (cAMP) accumulation, and the maximal effects were almost abolished by pertussis toxin (PTx) treatment. Moreover, they could modulate the intracellular signaling pathways composed of Akt and extracellular signal-regulated kinase 1/2 (ERK1/2) serine/threonine protein kinases in PTx-sensitive manner. This is the first approach to apply cyclization on apelin, and these results provide the basis for the development of drug-like apelin analogues.

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Copy and paste a formatted citation
Spandidos Publications style
Hamada J, Kimura J, Ishida J, Kohda T, Morishita S, Ichihara S and Fukamizu A: Evaluation of novel cyclic analogues of apelin. Int J Mol Med 22: 547-552, 2008.
APA
Hamada, J., Kimura, J., Ishida, J., Kohda, T., Morishita, S., Ichihara, S., & Fukamizu, A. (2008). Evaluation of novel cyclic analogues of apelin. International Journal of Molecular Medicine, 22, 547-552. https://doi.org/10.3892/ijmm_00000054
MLA
Hamada, J., Kimura, J., Ishida, J., Kohda, T., Morishita, S., Ichihara, S., Fukamizu, A."Evaluation of novel cyclic analogues of apelin". International Journal of Molecular Medicine 22.4 (2008): 547-552.
Chicago
Hamada, J., Kimura, J., Ishida, J., Kohda, T., Morishita, S., Ichihara, S., Fukamizu, A."Evaluation of novel cyclic analogues of apelin". International Journal of Molecular Medicine 22, no. 4 (2008): 547-552. https://doi.org/10.3892/ijmm_00000054
Copy and paste a formatted citation
x
Spandidos Publications style
Hamada J, Kimura J, Ishida J, Kohda T, Morishita S, Ichihara S and Fukamizu A: Evaluation of novel cyclic analogues of apelin. Int J Mol Med 22: 547-552, 2008.
APA
Hamada, J., Kimura, J., Ishida, J., Kohda, T., Morishita, S., Ichihara, S., & Fukamizu, A. (2008). Evaluation of novel cyclic analogues of apelin. International Journal of Molecular Medicine, 22, 547-552. https://doi.org/10.3892/ijmm_00000054
MLA
Hamada, J., Kimura, J., Ishida, J., Kohda, T., Morishita, S., Ichihara, S., Fukamizu, A."Evaluation of novel cyclic analogues of apelin". International Journal of Molecular Medicine 22.4 (2008): 547-552.
Chicago
Hamada, J., Kimura, J., Ishida, J., Kohda, T., Morishita, S., Ichihara, S., Fukamizu, A."Evaluation of novel cyclic analogues of apelin". International Journal of Molecular Medicine 22, no. 4 (2008): 547-552. https://doi.org/10.3892/ijmm_00000054
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