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<script type="text/javascript" src="/corehtml/pmc/jatsreader/ptpmc_3.22/js/jr.boots.min.js"> </script><title>99mTc-Regioselectively addressable functionalized template-[cyclo-(Arg-Gly-Asp-d-Phe-Lys)]4 - Molecular Imaging and Contrast Agent Database (MICAD) - NCBI Bookshelf</title>
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<meta name="citation_title" content="99mTc-Regioselectively addressable functionalized template-[cyclo-(Arg-Gly-Asp-d-Phe-Lys)]4">
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<meta name="citation_author" content="Kam Leung">
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<meta name="DC.Contributor" content="Kam Leung">
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<meta name="og:description" content="Integrins are a family of heterodimeric glycoproteins on cell surfaces that mediate diverse biological events involving cell–cell and cell–matrix interactions (1). Integrins consist of an α and a β subunit and are important for cell adhesion and signal transduction. The αvβ3 integrin is the most prominent receptor affecting tumor growth, tumor invasiveness, metastasis, tumor-induced angiogenesis, inflammation, osteoporosis, and rheumatoid arthritis (2-7). Expression of the αvβ3 integrin is strong on tumor cells and activated endothelial cells, whereas expression is weak on resting endothelial cells and most normal tissues. Antagonists of αvβ3 are being studied as anti-tumor and anti-angiogenic agents, and agonists of αvβ3 are being studied as angiogenic agents for coronary angiogenesis (6, 8, 9). A peptide sequence consisting of Arg-Gly-Asp (RGD) has been identified as a recognition motif used by extracellular matrix proteins (vitronectin, fibrinogen, laminin, and collagen) to bind to a variety of integrins, including αvβ3. Various radiolabeled antagonists have been introduced to image tumors and tumor angiogenesis (10).">
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id="jr-fip-info-p"><a id="jr-fip-prev" class="wsprkl btn" title="Jump to previuos match">◀</a><button id="jr-fip-matches">no matches yet</button><a id="jr-fip-next" class="wsprkl btn" title="Jump to next match">▶</a></nav></nav></div><div id="jr-epub-interstitial" class="hidden"></div><div id="jr-content"><article data-type="main"><div class="main-content lit-style" itemscope="itemscope" itemtype="http://schema.org/CreativeWork"><div class="meta-content fm-sec"><div class="fm-sec"><h1 id="_NBK24598_"><span class="title" itemprop="name"><sup>99m</sup>Tc-Regioselectively addressable functionalized template-[cyclo-(Arg-Gly-Asp-<span class="small-caps">d</span>-Phe-Lys)]<sub>4</sub></span></h1><div itemprop="alternativeHeadline" class="subtitle whole_rhythm"><sup>99m</sup>Tc-RAFT-c(-RGDfK-)<sub>4</sub></div><p class="contribs">Leung K.</p><p class="fm-aai"><a href="#_NBK24598_pubdet_">Publication Details</a></p></div></div><div class="jig-ncbiinpagenav body-content whole_rhythm" data-jigconfig="allHeadingLevels: ['h2'],smoothScroll: false" itemprop="text"><div class="iconblock whole_rhythm clearfix ten_col table-wrap" id="figRAFTRGD99mTcT1"><a href="/books/NBK24598/table/RAFT-RGD99mTc.T1/?report=objectonly" target="object" title="Table" class="img_link icnblk_img" rid-ob="figobRAFTRGD99mTcT1"><img class="small-thumb" src="/corehtml/pmc/css/bookshelf/2.26/img/table-icon.gif" alt="Table Icon" /></a><div class="icnblk_cntnt"><h4 id="RAFT-RGD99mTc.T1"><a href="/books/NBK24598/table/RAFT-RGD99mTc.T1/?report=objectonly" target="object" rid-ob="figobRAFTRGD99mTcT1">Table</a></h4><p class="float-caption no_bottom_margin">
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<i>In vitro</i>
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Rodents
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</p></div></div><div id="RAFT-RGD99mTc.Background"><h2 id="_RAFT-RGD99mTc_Background_">Background</h2><p>[<a href="/sites/entrez?Db=pubmed&Cmd=DetailsSearch&Term=RAFT+RGD" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>Integrins are a family of heterodimeric glycoproteins on cell surfaces that mediate diverse biological events involving cell–cell and cell–matrix interactions (<a class="bibr" href="#RAFT-RGD99mTc.REF.1" rid="RAFT-RGD99mTc.REF.1">1</a>). Integrins consist of an α and a β subunit and are important for cell adhesion and signal transduction. The α<sub>v</sub>β<sub>3</sub> integrin is the most prominent receptor affecting tumor growth, tumor invasiveness, metastasis, tumor-induced angiogenesis, inflammation, osteoporosis, and rheumatoid arthritis (<a href="#RAFT-RGD99mTc.REF.2">2-7</a>). Expression of the α<sub>v</sub>β<sub>3</sub> integrin is strong on tumor cells and activated endothelial cells, whereas expression is weak on resting endothelial cells and most normal tissues. Antagonists of α<sub>v</sub>β<sub>3</sub> are being studied as anti-tumor and anti-angiogenic agents, and agonists of α<sub>v</sub>β<sub>3</sub> are being studied as angiogenic agents for coronary angiogenesis (<a class="bibr" href="#RAFT-RGD99mTc.REF.6" rid="RAFT-RGD99mTc.REF.6">6</a>, <a class="bibr" href="#RAFT-RGD99mTc.REF.8" rid="RAFT-RGD99mTc.REF.8">8</a>, <a class="bibr" href="#RAFT-RGD99mTc.REF.9" rid="RAFT-RGD99mTc.REF.9">9</a>). A peptide sequence consisting of Arg-Gly-Asp (RGD) has been identified as a recognition motif used by extracellular matrix proteins (vitronectin, fibrinogen, laminin, and collagen) to bind to a variety of integrins, including α<sub>v</sub>β<sub>3</sub>. Various radiolabeled antagonists have been introduced to image tumors and tumor angiogenesis (<a class="bibr" href="#RAFT-RGD99mTc.REF.10" rid="RAFT-RGD99mTc.REF.10">10</a>).</p><p>Most of the cyclic RGD peptides are composed of five amino acids. Haubner et al. (<a class="bibr" href="#RAFT-RGD99mTc.REF.11" rid="RAFT-RGD99mTc.REF.11">11</a>) reported that various cyclic RGD peptides exhibit selective inhibition of binding to the α<sub>v</sub>β<sub>3</sub> integrin (50% inhibition concentration (IC<sub>50</sub>) = 7–40 nM) but not to the α<sub>v</sub>β<sub>5</sub> (IC<sub>50</sub> = 600–4,000 nM) or α<sub>IIb</sub>β<sub>3</sub> (IC<sub>50</sub> = 700–5,000 nM) integrins. Various radiolabeled cyclic RGD peptides have been found to have high accumulation in tumors in nude mice (<a class="bibr" href="#RAFT-RGD99mTc.REF.12" rid="RAFT-RGD99mTc.REF.12">12</a>). Hydrazinonicotinic acid (HYNIC) is a coupling agent for <sup>99m</sup>Tc-labeling of peptides that can achieve high specific activities without affecting the receptor-binding ability of the amino acid sequence. <sup>99m</sup>Tc is bound to the hydrazine group, and other coordination sites could be occupied by one or more coligands. Liu et al. (<a class="bibr" href="#RAFT-RGD99mTc.REF.13" rid="RAFT-RGD99mTc.REF.13">13</a>) reported the success of radiolabeling the cyclo(Arg-Gly-Asp-<span class="small-caps">d</span>-Phe-Lys) (c(RGDfK)) tetramer linked by glutamic acid and conjugated with HYNIC, which displayed high tumor accumulation in nude mice bearing human tumor xenografts. Boturyn et al. (<a class="bibr" href="#RAFT-RGD99mTc.REF.14" rid="RAFT-RGD99mTc.REF.14">14</a>) generated a versatile molecular regioselectively addressable functionalized template (RAFT) platform with a cyclic decapeptide [c(-Lys(Boc)-Lys(Alloc)-Lys(Boc)-Pro-Gly-Lys(Boc)-Lys(Alloc)-Lys(Boc)-Pro-Gly-)] that had two attachment sides. The upper side is linked to four copies of the c(RGDfK) peptide for integrin α<sub>v</sub>β<sub>3</sub> targeting, and the bottom side is linked to <sup>99m</sup>Tc for single-photon emission computed tomography (SPECT) imaging or other labels for other imaging modalities. Sancey et al. (<a class="bibr" href="#RAFT-RGD99mTc.REF.15" rid="RAFT-RGD99mTc.REF.15">15</a>) reported that <sup>99m</sup>Tc-RAFT-c(-RGDfK-)<sub>4</sub> efficiently accumulated into tumors in mice. <sup>99m</sup>Tc-RAFT-c(-RGDfK-)<sub>4</sub> is an integrin-targeted molecular imaging agent developed for imaging of tumor vasculature and tumor angiogenesis.</p></div><div id="RAFT-RGD99mTc.Synthesis"><h2 id="_RAFT-RGD99mTc_Synthesis_">Synthesis</h2><p>[<a href="/sites/entrez?Db=pubmed&Cmd=DetailsSearch&Term=RAFT+RGD+synthesis" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>Boturyn et al. (<a class="bibr" href="#RAFT-RGD99mTc.REF.14" rid="RAFT-RGD99mTc.REF.14">14</a>) described a detailed synthesis of RAFT-c(-RGDfK-)<sub>4</sub> by solid-phase peptide synthesis. Radiolabeling of RAFT-c(-RGDfK-)<sub>4</sub> was performed by heating 2.2–3 GBq (59–81 mCi) <sup>99m</sup>Tc in a commercially available IsoLink kit at 100°C for 20 min (<a class="bibr" href="#RAFT-RGD99mTc.REF.15" rid="RAFT-RGD99mTc.REF.15">15</a>). The peptide was added to one third of the mixture after neutralization with HCl; the mixture was then incubated at 60°C for 20 min. <sup>99m</sup>Tc-RAFT-c(-RGDfK-)<sub>4</sub> had a radiochemical purity of >95%. <sup>99m</sup>Tc-RAFT-c(-RADfK-) (non-specific control) and <sup>99m</sup>Tc-c(RGDfK) (specific control) were radiolabeled similarly.</p></div><div id="RAFT-RGD99mTc.In_Vitro_Studies_Tes"><h2 id="_RAFT-RGD99mTc_In_Vitro_Studies_Tes_"><i>In Vitro</i> Studies: Testing in Cells and Tissues</h2><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=RAFT+RGD+AND%20in%20vitro" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>Boturyn et al. (<a class="bibr" href="#RAFT-RGD99mTc.REF.14" rid="RAFT-RGD99mTc.REF.14">14</a>) reported that RAFT-c(-RGDfK-)<sub>4</sub> inhibited CHO3a cell adhesion to vitronectin (IC<sub>50</sub> = 0.5 ± 0.05 μM). RAFT-c(-RGDfK-)<sub>4</sub> was internalized into the cells as observed with fluorescence microscopy. Sancey et al. (<a class="bibr" href="#RAFT-RGD99mTc.REF.15" rid="RAFT-RGD99mTc.REF.15">15</a>) performed <i>in vitro</i> blood distribution pattern analyses of <sup>99m</sup>Tc-RAFT-c(-RGDfK-)<sub>4</sub> and <sup>9m</sup>Tc-RAFT-c(-RADfK-) in human blood. After incubation at room temperature for 60 min, 42% and 15% of <sup>99m</sup>Tc-RAFT-c(-RGDfK-)<sub>4</sub> bound to globulins and cells, respectively. On the other hand, only 8% and 10% of <sup>99m</sup>Tc-RAFT-c(-RADfK-) bound to globulins and cells, respectively.</p></div><div id="RAFT-RGD99mTc.Animal_Studies"><h2 id="_RAFT-RGD99mTc_Animal_Studies_">Animal Studies</h2><div id="RAFT-RGD99mTc.Rodents"><h3>Rodents</h3><p>[<a href="/sites/entrez?Db=pubmed&Cmd=DetailsSearch&Term=RAFT+RGD+AND+rodentia" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>Sancey et al. (<a class="bibr" href="#RAFT-RGD99mTc.REF.15" rid="RAFT-RGD99mTc.REF.15">15</a>) performed biodistribution studies of <sup>99m</sup>Tc-RAFT-c(-RGDfK-)<sub>4</sub>, <sup>99m</sup>Tc-RAFT-c(-RADfK-)<sub>4</sub> (non-specific control), and <sup>99m</sup>Tc-c(RGDfK) (specific control) in mice bearing B16-F0 or TS/A-pc tumors. TS/A-pc tumor cells exhibited a higher level of α<sub>v</sub>β<sub>3</sub> expression than B16-F0 tumor cells. At 60 min after injection, <sup>99m</sup>Tc-RAFT-c(-RGDfK-)<sub>4</sub> tumor uptake (% injected dose per gram (ID/g)) was higher than that of <sup>99m</sup>Tc-c(RGDfK) and <sup>99m</sup>Tc-RAFT-c(-RADfK-)<sub>4</sub> in B16-F0 (2.4 ± 0.5, 1.6 ± 0.4, 1.0 ± 0.1, respectively) and in TS/A-pc tumors (2.7 ± 0.8, 1.9 ± 0.4, 0.7 ± 0.1, respectively). Liver and kidney exhibited the highest uptake. <sup>99m</sup>Tc-c(RGDfK) and <sup>99m</sup>Tc-RAFT-c(-RGDfK-)<sub>4</sub> tumor/muscle ratios were 2.4 ± 0.5 and 3.3 ± 0.7 (<i>P</i> = 0.02), respectively, in B16-F0 tumors and 3.2 ± 0.8 and 2.7 ± 0.3 (<i>P</i> = 0.2), respectively, in TS/A-pc tumors. Planar SPECT images showed that tumor/muscle activity ratios of <sup>99m</sup>Tc-c(RGDfK) and <sup>99m</sup>Tc-RAFT-c(-RGDfK-)<sub>4</sub> were not statistically different in mice bearing B16-F0 tumors (2.5 ± 0.8 <i>versus</i> 2.2 ± 0.5) and in mice bearing TS/A-pc tumors (2.8 ± 0.5 <i>versus</i> 2.7 ± 0.5). These ratios were significantly higher than those observed with <sup>99m</sup>Tc-RAFT-c(-RADfK-)<sub>4</sub> (<i>P</i> < 0.0002). Immunohistochemical and autoradiographic studies indicated that <sup>99m</sup>Tc-RAFT-c(-RGDfK-)<sub>4</sub> intratumoral uptake preferentially occurred in angiogenic areas. Quantification of transverse slices obtained from SPECT images indicated that similar tumor/muscle ratios were obtained with <sup>99m</sup>Tc-c(RGDfK) and <sup>99m</sup>Tc-RAFT-c(-RGDfK-)<sub>4</sub> in B16-F0 tumors (2.8 ± 0.9 <i>versus</i> 2.3 ± 0.4) and in TS/A-pc tumors (4.1 ± 0.7 <i>versus</i> 4.1 ± 0.8). There was a significant difference between the <sup>99m</sup>Tc-RAFT-c(-RGDfK-)<sub>4</sub> tumor/muscle ratio in B16-F0 and in TS/A-pc tumors (2.3 ± 0.4 <i>versus</i> 4.1 ± 0.8; <i>P</i> < 0.01) whereas this difference did not reach statistical significance with <sup>99m</sup>Tc-c(RGDfK) (2.8 ± 0.9 <i>versus</i> 4.1 ± 0.7; <i>P</i> = 0.06). The <sup>99m</sup>Tc-c(RGDfK) and <sup>99m</sup>Tc-RAFT-c(-RGDfK-)<sub>4</sub> tumor/muscle ratios that were observed in both B16-F0 and TS/A-pc tumors were significantly higher (<i>P</i> < 0.05) than those obtained with <sup>99m</sup>Tc-RAFT-c(-RADfK-)<sub>4</sub> (1.2 ± 0.3 and 1.7 ± 0.1, respectively). No blocking study was performed.</p></div><div id="RAFT-RGD99mTc.Other_NonPrimate_Mam"><h3>Other Non-Primate Mammals</h3><p>[<a href="/sites/entrez?Db=pubmed&Cmd=DetailsSearch&Term=RAFT+RGD+AND+(dog%20or%20pig%20or%20sheep%20or%20rabbit)" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>No publication is currently available.</p></div><div id="RAFT-RGD99mTc.NonHuman_Primates"><h3>Non-Human Primates</h3><p>[<a href="/sites/entrez?Db=pubmed&Cmd=DetailsSearch&Term=RAFT+RGD+AND+(primate%20not%20human)" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>No publication is currently available.</p></div></div><div id="RAFT-RGD99mTc.Human_Studies"><h2 id="_RAFT-RGD99mTc_Human_Studies_">Human Studies</h2><p>[<a href="/sites/entrez?Db=pubmed&Cmd=DetailsSearch&Term=RAFT+RGD+AND+human" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>No publication is currently available.</p></div><div id="RAFT-RGD99mTc.references"><h2 id="_RAFT-RGD99mTc_references_">References</h2><dl class="temp-labeled-list"><dl class="bkr_refwrap"><dt>1.</dt><dd><div class="bk_ref" id="RAFT-RGD99mTc.REF.1">Hynes R.O. Integrins: versatility, modulation, and signaling in cell adhesion. <span><span class="ref-journal">Cell. </span>1992;<span class="ref-vol">
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</span>(3):561–5.</span> [<a href="/pmc/articles/PMC2410157/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC2410157</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/14760364" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 14760364</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>3.</dt><dd><div class="bk_ref" id="RAFT-RGD99mTc.REF.3">Varner J.A. , Cheresh D.A. Tumor angiogenesis and the role of vascular cell integrin alphavbeta3. <span><span class="ref-journal">Important Adv Oncol. </span>1996:69–87.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/8791129" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 8791129</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>4.</dt><dd><div class="bk_ref" id="RAFT-RGD99mTc.REF.4">Wilder R.L. Integrin alpha V beta 3 as a target for treatment of rheumatoid arthritis and related rheumatic diseases. <strong>Suppl 2</strong><span><span class="ref-journal">Ann Rheum Dis. </span>2002;<span class="ref-vol">
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</span>(2):123–31.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/12558065" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 12558065</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>7.</dt><dd><div class="bk_ref" id="RAFT-RGD99mTc.REF.7">Ruegg C. , Dormond O. , Foletti A. Suppression of tumor angiogenesis through the inhibition of integrin function and signaling in endothelial cells: which side to target? <span><span class="ref-journal">Endothelium. </span>2002;<span class="ref-vol">
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</span>(2):326–36.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/11216533" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 11216533</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>12.</dt><dd><div class="bk_ref" id="RAFT-RGD99mTc.REF.12">Chen X. , Park R. , Shahinian A.H. , Tohme M. , Khankaldyyan V. , Bozorgzadeh M.H. , Bading J.R. , Moats R. , Laug W.E. , Conti P.S. 18F-labeled RGD peptide: initial evaluation for imaging brain tumor angiogenesis. <span><span class="ref-journal">Nucl Med Biol. </span>2004;<span class="ref-vol">
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<strong>31</strong>
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</span>(2):179–89.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/15013483" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 15013483</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>13.</dt><dd><div class="bk_ref" id="RAFT-RGD99mTc.REF.13">Liu S. , Hsieh W.Y. , Jiang Y. , Kim Y.S. , Sreerama S.G. , Chen X. , Jia B. , Wang F. Evaluation of a (99m)Tc-labeled cyclic RGD tetramer for noninvasive imaging integrin alpha(v)beta3-positive breast cancer. <span><span class="ref-journal">Bioconjug Chem. </span>2007;<span class="ref-vol">
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<strong>18</strong>
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</span>(2):438–46.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/17341108" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 17341108</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>14.</dt><dd><div class="bk_ref" id="RAFT-RGD99mTc.REF.14">Boturyn D. , Coll J.L. , Garanger E. , Favrot M.C. , Dumy P. Template assembled cyclopeptides as multimeric system for integrin targeting and endocytosis. <span><span class="ref-journal">J Am Chem Soc. </span>2004;<span class="ref-vol">
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<strong>126</strong>
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</span>(18):5730–9.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/15125666" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 15125666</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>15.</dt><dd><div class="bk_ref" id="RAFT-RGD99mTc.REF.15">Sancey L. , Ardisson V. , Riou L.M. , Ahmadi M. , Marti-Batlle D. , Boturyn D. , Dumy P. , Fagret D. , Ghezzi C. , Vuillez J.P. In vivo imaging of tumour angiogenesis in mice with the alpha(v)beta (3) integrin-targeted tracer (99m)Tc-RAFT-RGD. <span><span class="ref-journal">Eur J Nucl Med Mol Imaging. </span>2007;<span class="ref-vol">
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<strong>34</strong>
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</span>(12):2037–47.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/17674000" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 17674000</span></a>]</div></dd></dl></dl></div><div id="bk_toc_contnr"></div></div></div><div class="fm-sec"><h2 id="_NBK24598_pubdet_">Publication Details</h2><h3>Author Information and Affiliations</h3><div class="contrib half_rhythm"><span itemprop="author">Kam Leung</span>, PhD<div class="affiliation small">
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National Center for Biotechnology Information, NLM, NIH, Bethesda, MD,
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<span class="before-email-separator"></span><span class="email-label">Email: </span><a href="mailto:dev@null" data-email="vog.hin.mln.ibcn@dacim" class="oemail">vog.hin.mln.ibcn@dacim</a>
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</div></div><h3>Publication History</h3><p class="small">Created: <span itemprop="datePublished">February 9, 2008</span>; Last Update: <span itemprop="dateModified">May 8, 2008</span>.</p><h3>Copyright</h3><div><div class="half_rhythm"><a href="/books/about/copyright/">Copyright Notice</a></div></div><h3>Publisher</h3><p><a href="http://www.ncbi.nlm.nih.gov/" ref="pagearea=page-banner&targetsite=external&targetcat=link&targettype=publisher">National Center for Biotechnology Information (US)</a>, Bethesda (MD)</p><h3>NLM Citation</h3><p>Leung K. 99mTc-Regioselectively addressable functionalized template-[cyclo-(Arg-Gly-Asp-d-Phe-Lys)]4. 2008 Feb 9 [Updated 2008 May 8]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013. <span class="bk_cite_avail"></span></p></div><div class="small-screen-prev"><a href="/books/n/micad/Litorin99mTc/?report=reader"><svg xmlns="http://www.w3.org/2000/svg" viewBox="0 0 100 100" preserveAspectRatio="none"><path d="M75,30 c-80,60 -80,0 0,60 c-30,-60 -30,0 0,-60"></path><text x="20" y="28" textLength="60" style="font-size:25px">Prev</text></svg></a></div><div class="small-screen-next"><a href="/books/n/micad/SDF1alpha99mTc/?report=reader"><svg xmlns="http://www.w3.org/2000/svg" viewBox="0 0 100 100" preserveAspectRatio="none"><path d="M25,30c80,60 80,0 0,60 c30,-60 30,0 0,-60"></path><text x="20" y="28" textLength="60" style="font-size:25px">Next</text></svg></a></div></article><article data-type="table-wrap" id="figobRAFTRGD99mTcT1"><div id="RAFT-RGD99mTc.T1" class="table"><p class="large-table-link" style="display:none"><span class="right"><a href="/books/NBK24598/table/RAFT-RGD99mTc.T1/?report=objectonly" target="object">View in own window</a></span></p><div class="large_tbl" id="__RAFT-RGD99mTc.T1_lrgtbl__"><table><tbody><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Chemical name:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><sup>99m</sup>Tc-Regioselectively addressable functionalized template-[cyclo-(Arg-Gly-Asp-<span class="small-caps">d</span>-Phe-Lys)]<sub>4</sub></td><td rowspan="2" colspan="1" style="text-align:left;vertical-align:middle;"></td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Abbreviated name:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><sup>99m</sup>Tc-RAFT-c(-RGDfK-)<sub>4</sub>, <sup>99m</sup>Tc-RAFT-RGD</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Synonym:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"></td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Agent Category:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Peptide</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Target:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Integrin α<sub>v</sub>β<sub>3</sub></td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Target Category:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Receptor-ligand binding</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Method of detection:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Single-photon emission computed tomography (SPECT), planar gamma imaging</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Source of signal:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><sup>99m</sup>Tc</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Activation:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">No</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Studies:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">
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<ul class="simple-list"><li class="half_rhythm"><div>
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<img alt="Checkbox" src="/corehtml/pmc/css/bookshelf/2.26/img/studies.checkbox.png" />
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<i>In vitro</i>
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</div></li></ul>
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<ul class="simple-list"><li class="half_rhythm"><div>
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<img alt="Checkbox" src="/corehtml/pmc/css/bookshelf/2.26/img/studies.checkbox.png" /> Rodents
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</div></li></ul>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Click on <a href="/entrez/viewer.fcgi?db=protein&val=4504763" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">protein</a>, <a href="/entrez/viewer.fcgi?db=nucleotide&val=40217844" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">nucleotide</a> (RefSeq), and <a href="/entrez/query.fcgi?db=gene&cmd=Retrieve&dopt=full_report&list_uids=3685" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">gene</a> for more information about integrin α<sub>v</sub>β<sub>3</sub>.</td></tr></tbody></table></div></div></article></div><div id="jr-scripts"><script src="/corehtml/pmc/jatsreader/ptpmc_3.22/js/libs.min.js"> </script><script src="/corehtml/pmc/jatsreader/ptpmc_3.22/js/jr.min.js"> </script></div></div>
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