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Advances in Brief

Noninvasive Imaging of αvβ3 Integrin Expression Using 18F-labeled RGD-containing Glycopeptide and Positron Emission Tomography

Roland Haubner, Hans-Jürgen Wester, Wolfgang A. Weber, Christian Mang, Sibylle I. Ziegler, Simon L. Goodman, Reingard Senekowitsch-Schmidtke, Horst Kessler and Markus Schwaiger
Roland Haubner
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Hans-Jürgen Wester
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Wolfgang A. Weber
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Christian Mang
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Sibylle I. Ziegler
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Simon L. Goodman
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Reingard Senekowitsch-Schmidtke
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Horst Kessler
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Markus Schwaiger
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DOI:  Published March 2001
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    Fig. 1.

    Schematic structure of [18F]Galacto-RGD. The glycopeptide shows the characteristic βII’-turn with d-Phe in the i+1 position and the RGD site in a “kinked” conformation responsible for the αvβ3 selectivity.

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    Fig. 2.

    Comparison of the biodistribution data of [18F]Galacto-RGD in melanoma M21 (▪)- and M21-L (▵)-bearing nude mice. Error bars, 1 SD. For some data points, error bars are not visible because the SD is smaller than the size of the symbol.

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    Fig. 3.

    Transaxial small animal PET images of nude mice bearing human melanoma xenografts. Images were acquired 90 min after injection of approximately 5.5 MBq of [18F]Galacto-RGD. The top left image shows selective accumulation of the tracer in the αvβ3-positve (M21) tumor on the left flank. In contrast, no focal tracer accumulation is visible in the αvβ3-negative (M21-L) control tumor (bottom left image). The three images on the right were obtained from serial [18F]Galacto-RGD PET studies in one mouse. These illustrate the dose-dependent blockade of tracer uptake by the αv-selective cyclic pentapeptide cyclo(-Arg-Gly-Asp-d-Phe-Val-).

Tables

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  • Table 1

    Biodistribution data for [18F]Galacto-RGD in melanoma-bearing nude mice and osteosarcoma-bearing mice

    Values are given as % ID/g ± SD.
    Time p.i. (min)Osteosarcoma (αvβ3 positive)Melanoma M21 (αvβ3 positive)Melanoma M21-L (negative control)
    Blood
     102.58 ± 0.412.93 ± 0.534.70a
     600.27 ± 0.060.18 ± 0.060.26 ± 0.06
     1200.13 ± 0.030.05 ± 0.010.13 ± 0.07
    Serum
     105.25 ± 0.335.65 ± 0.898.71
     600.50 ± 0.120.34 ± 0.110.49 ± 0.11
     1200.19 ± 0.040.09 ± 0.010.22 ± 0.10
    Liver
     105.47 ± 0.115.64 ± 2.276.40
     602.94 ± 0.271.85 ± 0.392.07 ± 0.20
     1201.97 ± 0.271.25 ± 0.051.79 ± 0.58
    Kidneys
     108.67 ± 0.528.48 ± 0.8410.82
     603.11 ± 0.601.86 ± 0.102.24 ± 0.21
     1202.21 ± 0.461.52 ± 0.101.86 ± 0.46
    Muscle
     100.80 ± 0.131.13 ± 0.181.44
     600.32 ± 0.060.21 ± 0.020.21 ± 0.03
     1200.28 ± 0.020.15 ± 0.020.18 ± 0.03
    Spleen
     102.54 ± 0.072.10 ± 0.452.39
     601.54 ± 0.220.69 ± 0.100.77 ± 0.02
     1201.20 ± 0.040.64 ± 0.090.73 ± 0.14
    Heart
     101.94 ± 0.051.85 ± 0.242.02
     600.51 ± 0.070.28 ± 0.050.34 ± 0.02
     1200.63 ± 0.410.19 ± 0.040.29 ± 0.06
    Tumor
     102.88 ± 0.323.90 ± 1.361.88
     601.33 ± 0.201.56 ± 0.150.42 ± 0.09
     1201.68 ± 0.491.49 ± 0.100.44 ± 0.24
    Lung
     103.43 ± 0.243.64 ± 0.524.84
     601.10 ± 0.180.76 ± 0.090.83 ± 0.08
     1200.72 ± 0.150.53 ± 0.050.71 ± 0.24
    Femur
     101.22 ± 0.041.51 ± 0.341.46
     600.54 ± 0.110.34 ± 0.050.44 ± 0.06
     1200.51 ± 0.020.33 ± 0.020.50 ± 0.10
    Colon
     103.77 ± 0.161.74 ± 0.551.68
     602.27 ± 1.230.57 ± 0.040.70 ± 0.19
     1201.59 ± 0.463.53 ± 0.440.76 ± 0.27
    Brain
     100.14 ± 0.010.19 ± 0.040.19
     600.06 ± 0.010.05 ± 0.010.05 ± 0.01
     1200.05 ± 0.010.04 ± 0.010.05 ± 0.01
    • a Data for this time point result from one mouse.

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Cancer Research: 61 (5)
March 2001
Volume 61, Issue 5
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Noninvasive Imaging of αvβ3 Integrin Expression Using 18F-labeled RGD-containing Glycopeptide and Positron Emission Tomography
Roland Haubner, Hans-Jürgen Wester, Wolfgang A. Weber, Christian Mang, Sibylle I. Ziegler, Simon L. Goodman, Reingard Senekowitsch-Schmidtke, Horst Kessler and Markus Schwaiger
Cancer Res March 3 2001 (61) (5) 1781-1785;

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Noninvasive Imaging of αvβ3 Integrin Expression Using 18F-labeled RGD-containing Glycopeptide and Positron Emission Tomography
Roland Haubner, Hans-Jürgen Wester, Wolfgang A. Weber, Christian Mang, Sibylle I. Ziegler, Simon L. Goodman, Reingard Senekowitsch-Schmidtke, Horst Kessler and Markus Schwaiger
Cancer Res March 3 2001 (61) (5) 1781-1785;
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