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

4-[18F]Fluorobenzoyl-C2A domain of synaptotagmin I-glutathione- S-transferase

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

4-[18F]Fluorobenzoyl-C2A domain of synaptotagmin I-glutathione- S-transferase

Kam Leung.
Free Books & Documents

Excerpt

Apoptosis (programmed cell death) plays an important role in the pathophysiology of many diseases, such as cancer, neurodegenerative disorders, vascular disorders, atherosclerosis, and chronic hepatitis, as well as in the biology of normal cells, such as epithelial cells and immune cells (1). During apoptosis, there is rapid redistribution of phosphatidylserine (PS) from the inner membrane leaflet to the outer membrane leaflet, exposing the anionic head group of PS. PS is also accessible for annexin V (or annexin A5) binding in necrosis because of disruption of the plasma membrane. Annexin V, a 36-kDa protein, binds to PS with high affinity (Kd = 7 nM). Annexin V has been radiolabeled with 123I and 99mTc for single-photon emission computed tomography imaging and with 124I for positron emission tomography (PET) (2-4). Annexin V has been successfully labeled with 18F (18F-labeled annexin V (4-[18F]FBA)) and is currently being developed as a PET agent for imaging apoptosis as well as necrosis (5, 6). Cy5.5-Annexin V has been evaluated as an optical probe in small animals. Annexin V-CLIO-Cy5.5 (AnxCLIO-Cy5.5) is a multimodal agent that consists of CLIO nanoparticles labeled with annexin V and Cy5.5 (7).

Synaptotagmins are integral membrane proteins of synaptic vesicles with calcium ion (Ca2+) binding domains (8). The C2A domain of synaptotagmin I (Syt1) binds two to three Ca2+ ions and also binds anionic phospholipids including PS. Calcium binding to Syt1 participates in triggering neurotransmitter release at the synapse. Davletov et al. (9) showed that C2A-glutathione-S-transferase (C2A-GST) fusion protein binds specifically Ca2+ and anionic phospholipids. 99mTc-Labeled C2A-GST (99mTc-C2A-GST) has been shown to target apoptotic cells in acute myocardial infarction and tumor models in vivo in animal studies (10-14). Wang et al. (15) prepared 4-[18F]fluorobenzoyl-C2A-GST (4-[18F]FB-C2A-GST) as a PET agent for imaging of apoptotic cells.

PubMed Disclaimer

Similar articles

  • Annexin A5-Gd-micelles-Cy5.5.
    Leung K. Leung K. 2011 Feb 27 [updated 2011 Apr 27]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. 2011 Feb 27 [updated 2011 Apr 27]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. PMID: 21542558 Free Books & Documents. Review.
  • Annexin V-cross-linked iron oxide-Cy5.5.
    Leung K. Leung K. 2006 Jul 27 [updated 2008 Mar 28]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. 2006 Jul 27 [updated 2008 Mar 28]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. PMID: 20641674 Free Books & Documents. Review.
  • 111In-Labeled annexin A5-polyethylene glycol–coated core-cross-linked polymeric micelle-Cy7.
    Leung K. Leung K. 2011 Nov 30 [updated 2012 Jan 19]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. 2011 Nov 30 [updated 2012 Jan 19]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. PMID: 22279634 Free Books & Documents. Review.
  • Annexin A5-quantum dot-DTPA-gadolinium.
    Leung K. Leung K. 2007 Mar 16 [updated 2008 Mar 27]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. 2007 Mar 16 [updated 2008 Mar 27]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. PMID: 20641423 Free Books & Documents. Review.
  • 4-[18F]Fluorobenzoyl-annexin V.
    Leung K. Leung K. 2006 Feb 7 [updated 2008 Mar 27]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. 2006 Feb 7 [updated 2008 Mar 27]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. PMID: 20641449 Free Books & Documents. Review.
See all similar articles

References

    1. Thompson C.B. Apoptosis in the pathogenesis and treatment of disease. . Science. 1995;267(5203):1456–62. - PubMed
    1. Blankenberg F.G. Recent advances in the imaging of programmed cell death. . Curr Pharm Des. 2004;10(13):1457–67. - PubMed
    1. Keen H.G., Dekker B.A., Disley L., Hastings D., Lyons S., Reader A.J., Ottewell P., Watson A., Zweit J. Imaging apoptosis in vivo using 124I-annexin V and PET. . Nucl Med Biol. 2005;32(4):395–402. - PubMed
    1. Lahorte C., Slegers G., Philippe J., Van de Wiele C., Dierckx R.A. Synthesis and in vitro evaluation of 123I-labelled human recombinant annexin V. . Biomol Eng. 2001;17(2):51–3. - PubMed
    1. Toretsky J., Levenson A., Weinberg I.N., Tait J.F., Uren A., Mease R.C. Preparation of F-18 labeled annexin V: a potential PET radiopharmaceutical for imaging cell death. . Nucl Med Biol. 2004;31(6):747–52. - PubMed

LinkOut - more resources