Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review

99mTc-Hydrazinonicotinamide-aminohexanoic acid-Lys40-exendin-4

Kam Leung  1
In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004.
[updated ].
Affiliations
Free Books & Documents
Review

99mTc-Hydrazinonicotinamide-aminohexanoic acid-Lys40-exendin-4

Kam Leung.
Free Books & Documents

Excerpt

Glucagon-like peptide-1 (GLP-1, 30 amino acids) is secreted from enteroendocrine cells of the distal small intestine in response to food ingestion (1). GLP-1 plays an important role in glucose metabolism and homeostasis. It inhibits gastric emptying, glucagon secretion, and glucose production (2). In addition, it induces insulin release from the pancreatic β-cells as well as their proliferation. The GLP-1 receptor has been identified in normal tissues such as the pancreas, stomach, brain, and lung, and it has been shown to be highly overexpressed in human insulinomas and gastrinomas (3). In insulinomas, GLP-1 receptor density is considerably greater, and the GLP-1 receptor is more frequently observed than somatostatin receptors.

Exendin-4 is a GLP-1 analog with 39 amino acids isolated from the venom of the Gila monster (Heloderma suspectum) (4). Exendin-4 and GLP-1 share a 53% amino acid sequence homology. Exendin-4 is a more potent and longer-lasting GLP-1 receptor agonist than GLP-1. Exendin-4 is resistant to cleavage by dipeptidyl peptidase IV, whereas the first two N-terminal amino acids of GLP-1 are rapidly cleaved. Exenatide, a synthetic version of exendin-4, is the first GLP-1 mimetic recently approved by the United States Food and Drug Administration (FDA) for use in select patients with type 2 diabetes (5). 99mTc-Hydrazinonicotinamide-aminohexanoic acid-Lys40-exendin-4 ([Lys40(Ahx-HYNIC-99mTc)NH2]-exendin-4) is being developed for single-photon emission computed tomography (SPECT) imaging of the GLP-1 receptor (6).

PubMed Disclaimer

Similar articles

  • 111In-Diethylenetriaminepentaacetic acid-aminohexanoic acid-Lys40-exendin-4.
    Leung K. Leung K. 2007 Jan 17 [updated 2012 Jan 30]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. 2007 Jan 17 [updated 2012 Jan 30]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. PMID: 20641774 Free Books & Documents. Review.
  • 68Ga-1,4,7,10-Tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid-aminohexanoic acid-Lys40-exendin-4.
    Leung K. Leung K. 2012 Jan 30 [updated 2012 Apr 26]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. 2012 Jan 30 [updated 2012 Apr 26]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. PMID: 22553890 Free Books & Documents. Review.
  • 111In-Diethylenetriaminepentaacetic acid-Lys40-exendin-3.
    Leung K. Leung K. 2010 Aug 20 [updated 2010 Nov 3]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. 2010 Aug 20 [updated 2010 Nov 3]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. PMID: 21061499 Free Books & Documents. Review.
  • VivoTag-S 750-(S)-2-amino-4-pentynoic acid12-exendin-4.
    Leung K. Leung K. 2011 Nov 1 [updated 2012 Jan 5]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. 2011 Nov 1 [updated 2012 Jan 5]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. PMID: 22238793 Free Books & Documents. Review.
  • 68Ga-1,4,7,10-Tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid-Lys40-exendin-3.
    Leung K. Leung K. 2010 Aug 20 [updated 2010 Nov 3]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. 2010 Aug 20 [updated 2010 Nov 3]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. PMID: 21061498 Free Books & Documents. Review.
See all similar articles

References

    1. Theodorakis M.J., Carlson O., Michopoulos S., Doyle M.E., Juhaszova M., Petraki K., Egan J.M. Human duodenal enteroendocrine cells: source of both incretin peptides, GLP-1 and GIP. . Am J Physiol Endocrinol Metab. 2006;290(3):E550–9. - PubMed
    1. Doyle M.E., Egan J.M. Glucagon-like peptide-1. . Recent Prog Horm Res. 2001;56:377–99. - PubMed
    1. Reubi J.C., Waser B. Concomitant expression of several peptide receptors in neuroendocrine tumours: molecular basis for in vivo multireceptor tumour targeting. . Eur J Nucl Med Mol Imaging. 2003;30(5):781–93. - PubMed
    1. Meier J.J., Nauck M.A. Glucagon-like peptide 1(GLP-1) in biology and pathology. . Diabetes Metab Res Rev. 2005;21(2):91–117. - PubMed
    1. Nielsen L.L., Young A.A., Parkes D.G. Pharmacology of exenatide (synthetic exendin-4): a potential therapeutic for improved glycemic control of type 2 diabetes. . Regul Pept. 2004;117(2):77–88. - PubMed

LinkOut - more resources