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<div class="pre-content"><div><div class="bk_prnt"><p class="small">NCBI Bookshelf. A service of the National Library of Medicine, National Institutes of Health.</p><p>Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013. </p></div><div class="iconblock clearfix whole_rhythm no_top_margin bk_noprnt"><a class="img_link icnblk_img" title="Table of Contents Page" href="/books/n/micad/"><img class="source-thumb" src="/corehtml/pmc/pmcgifs/bookshelf/thumbs/th-micad-lrg.png" alt="Cover of Molecular Imaging and Contrast Agent Database (MICAD)" height="100px" width="80px" /></a><div class="icnblk_cntnt eight_col"><h2>Molecular Imaging and Contrast Agent Database (MICAD) [Internet].</h2><a data-jig="ncbitoggler" href="#__NBK23461_dtls__">Show details</a><div style="display:none" class="ui-widget" id="__NBK23461_dtls__"><div>Bethesda (MD): <a href="https://www.ncbi.nlm.nih.gov/" ref="pagearea=page-banner&targetsite=external&targetcat=link&targettype=publisher">National Center for Biotechnology Information (US)</a>; 2004-2013.</div></div><div class="half_rhythm"><ul class="inline_list"><li style="margin-right:1em"><a class="bk_cntns" href="/books/n/micad/">Contents</a></li></ul></div><div class="bk_noprnt"><form method="get" action="/books/n/micad/" id="bk_srch"><div class="bk_search"><label for="bk_term" class="offscreen_noflow">Search term</label><input type="text" title="Search this book" id="bk_term" name="term" value="" data-jig="ncbiclearbutton" /> <input type="submit" class="jig-ncbibutton" value="Search this book" submit="false" style="padding: 0.1em 0.4em;" /></div></form></div></div><div class="icnblk_cntnt two_col"><div class="pagination bk_noprnt"><a class="active page_link prev" href="/books/n/micad/MAb14C5-DOTA-111In/" title="Previous page in this title">< Prev</a><a class="active page_link next" href="/books/n/micad/TA138-111In/" title="Next page in this title">Next ></a></div></div></div></div></div>
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<div class="main-content lit-style" itemscope="itemscope" itemtype="http://schema.org/CreativeWork"><div class="meta-content fm-sec"><h1 id="_NBK23461_"><span class="title" itemprop="name"><sup>111</sup>In-Streptavidin-biotinylated α-melanocyte-stimulating hormone 2.0 bacteriophage</span></h1><div itemprop="alternativeHeadline" class="subtitle whole_rhythm"><sup>111</sup>In-SA-α-MSH2.0 phage</div><p class="contrib-group"><span itemprop="author">Kenneth T. Cheng</span>, PhD.</p><a data-jig="ncbitoggler" href="#__NBK23461_ai__" style="border:0;text-decoration:none">Author Information and Affiliations</a><div style="display:none" class="ui-widget" id="__NBK23461_ai__"><div class="contrib half_rhythm"><span itemprop="author">Kenneth T. Cheng</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></div><p class="small">Created: <span itemprop="datePublished">March 28, 2007</span>; Last Update: <span itemprop="dateModified">May 5, 2008</span>.</p></div><div class="jig-ncbiinpagenav body-content whole_rhythm" data-jigconfig="allHeadingLevels: ['h2'],smoothScroll: false" itemprop="text"><div id="MSHSA111In.T1" class="table"><p class="large-table-link" style="display:none"><span class="right"><a href="/books/NBK23461/table/MSHSA111In.T1/?report=objectonly" target="object">View in own window</a></span></p><div class="large_tbl" id="__MSHSA111In.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>
|
||
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><sup>111</sup>In-Streptavidin-biotinylated α-melanocyte-stimulating hormone 2.0 bacteriophage</td><td rowspan="9" colspan="1" style="text-align:left;vertical-align:middle;"></td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
|
||
<b>Abbreviated name:</b>
|
||
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><sup>111</sup>In-SA-α-MSH2.0 phage</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
|
||
<b>Synonym:</b>
|
||
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Pretargeted <sup>111</sup>In-MSH bacteriophage</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
|
||
<b>Agent Category:</b>
|
||
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Bacteriophage</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
|
||
<b>Target:</b>
|
||
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Melanocortin-1 (MC-1) receptor</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
|
||
<b>Target Category:</b>
|
||
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Receptor binding</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
|
||
<b>Method of detection:</b>
|
||
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Single-photon emission computed tomography (SPECT) or gamma planar imaging</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
|
||
<b>Source of signal/contrast:</b>
|
||
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><sup>111</sup>In</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
|
||
<b>Activation:</b>
|
||
</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;">
|
||
<b>Studies:</b>
|
||
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">
|
||
<ul class="simple-list"><li class="half_rhythm"><div>
|
||
<img alt="Checkbox" src="/corehtml/pmc/css/bookshelf/2.26/img/studies.checkbox.png" />
|
||
<i>In vitro</i>
|
||
|
||
</div></li></ul>
|
||
<ul class="simple-list"><li class="half_rhythm"><div>
|
||
<img alt="Checkbox" src="/corehtml/pmc/css/bookshelf/2.26/img/studies.checkbox.png" /> Rodents
|
||
</div></li></ul>
|
||
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Click on <a href="/entrez/viewer.fcgi?db=protein&val=27477129" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">protein</a>, <a href="/entrez/viewer.fcgi?db=nucleotide&val=27477128" 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=4157" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">gene</a> for more information about the melanocortin-1 receptor.</td></tr></tbody></table></div></div><div id="MSHSA111In.Background"><h2 id="_MSHSA111In_Background_">Background</h2><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=%28111In-SA-MSH2.0%20phage%29%20OR%20%28pretargeted%20bivalent%20bacteriophage%29" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p><sup>111</sup>In-Streptavidin-biotinylated α-melanocyte-stimulating hormone (MSH) 2.,0 bacteriophage (<sup>111</sup>In-SA-α-MSH2.0 phage) is a two-step melanoma pretargeting and imaging system developed as a single-photon emission computed tomography (SPECT) imaging probe for primary and metastatic melanoma (<a class="bk_pop" href="#MSHSA111In.REF.1">1</a>). This system uses a biotinylated α-MSH2.0 (bio-MSH2.0) targeting phage combined with <i>in vivo</i> labeling by <sup>111</sup>In-streptavidin (<sup>111</sup>In-SA).</p><p>Malignant melanoma is the sixth most common cancer in the United States (<a class="bk_pop" href="#MSHSA111In.REF.2">2</a>). Early diagnosis and prompt surgical removal comprise the best approach for treatment (<a class="bk_pop" href="#MSHSA111In.REF.3">3</a>). The melanocortin (MC) system is the best characterized neuropeptide network of the skin, and it is involved in pigmentation regulation, cortisol production, and many other physiological processes (<a class="bk_pop" href="#MSHSA111In.REF.4">4</a>). Most cutaneous cell types express MC receptors, proopiomelanocortin (POMC), and prohormone convertases, and they also release MCs. Five MC receptors (MC-1 to MC-5) have been cloned and characterized as receptors that belong to the G-protein−coupled receptor superfamily. MSHs (α-, β-, and γ-MSH) are derived from POMC by the proteolytic action of prohormone convertases. α-MSH (Ac-Ser<sup>1</sup>-Tyr<sup>2</sup>-Ser<sup>3</sup>-Met<sup>4</sup>-Glu<sup>5</sup>-His<sup>6</sup>-Phe<sup>7</sup>-Arg<sup>8</sup>-Trp<sup>9</sup>-Gly<sup>10</sup>-Lys<sup>11</sup>-Pro<sup>12</sup>-Val<sup>13</sup>-NH<sub>2</sub>), composed of 13 amino acids, is the most potent naturally occurring melanotropic peptide (<a class="bk_pop" href="#MSHSA111In.REF.5">5</a>). The biological effects of α-MSH are mediated <i>via</i> MC receptors.</p><p>Although positron emission tomography imaging with [<sup>18</sup>F]fluoro-2-deoxy-2-<span class="small-caps">d</span>-glucose <a href="/books/n/micad/FDG/">([<sup>18</sup>F]FDG</a>) is effective in the detection of melanoma, it is not melanoma-specific and some melanoma cells do not take up [<sup>18</sup>F]FDG (<a class="bk_pop" href="#MSHSA111In.REF.6">6</a>, <a class="bk_pop" href="#MSHSA111In.REF.7">7</a>). Radiolabeled α-MSH peptide analogs have been shown to specifically bind to MC-1 receptors that are overexpressed on human and mouse melanoma cells (<a class="bk_pop" href="#MSHSA111In.REF.6">6</a>, <a class="bk_pop" href="#MSHSA111In.REF.8">8-11</a>). To improve the <i>in vivo</i> pharmacokinetics of these radiolabeled peptides, different α-MSH analogs have been designed and studied (<a class="bk_pop" href="#MSHSA111In.REF.12">12</a>, <a class="bk_pop" href="#MSHSA111In.REF.13">13</a>). Bacteriophage display (phage display) is a combinatorial chemistry technique that uses a population of filamentous bacteriophage particles genetically modified to display a library of proteins and peptides on their surface (<a class="bk_pop" href="#MSHSA111In.REF.14">14</a>, <a class="bk_pop" href="#MSHSA111In.REF.15">15</a>). This technique has been used for the discovery of new and unique molecular imaging peptides (<a class="bk_pop" href="#MSHSA111In.REF.16">16</a>). These phage display–derived peptides can have binding properties different from chemically synthesized peptides because the conformational structures of phage peptides are affected by the microenvironment created by the surface of the phage particle (<a class="bk_pop" href="#MSHSA111In.REF.1">1</a>). Instead of using the isolated peptides, Newton et al. (<a class="bk_pop" href="#MSHSA111In.REF.1">1</a>) suggested that imaging tags can be directly added to phage particles without significant effects on their peptide binding properties. However, these very high molecular weight phage particles are generally cleared by the reticuloendothelial system <i>in vivo</i>. To circumvent this problem, Newton et al. (<a class="bk_pop" href="#MSHSA111In.REF.1">1</a>) prepared an α-MSH2.0 peptide analog from the phage display library and proposed the use of a two-step biotin-SA pretargeting system to allow for clearance of unlabeled phage particles before injection of the <sup>111</sup>In imaging label.</p></div><div id="MSHSA111In.Synthesis"><h2 id="_MSHSA111In_Synthesis_">Synthesis</h2><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=pretargeted%20bivalent%20bacteriophage" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>The α-MSH2.0 phage was generated by use of the fUSE5 vector, which contained phage with modified coat protein III and displayed up to 5 copies of a fused peptide on the tip of the phage particle (<a class="bk_pop" href="#MSHSA111In.REF.1">1</a>). Affinity selection of phage constructs was performed through multiple rounds of washing and multiplication. Briefly, the fUSE5 vector was digested with the <i>SFi</i>I restriction endonuclease. Equal molar amounts of sense and antisense phosphorylated DNA oligonucleotides were hybridized. A room-temperature DNA ligation reaction was performed for insertion of the hybridized DNA into the fUSE5 vector. <i>Escherichia coli</i> K91 Blue Kan cells were electroporated in the presence of the ligated vector. The proper DNA sequence was verified by DNA sequencing, and the amplified phage was precipitated. The phage particle concentrations in virions were determined spectrophotometrically.</p><p>Biotinylation of the phage particle was conducted by adding commercially available NHS-PEO<sub>4</sub>-biotin to the phage suspension at a 1,000-fold molar excess relative to the phage particles (<a class="bk_pop" href="#MSHSA111In.REF.1">1</a>). The mixture was rotated at room temperature for 2 h. The reaction was stopped with ethanolamine (pH 9.0) and was rotated at room temperature for 1 h. The free biotin was removed from bio-MSH2.0 by dialysis. <sup>111</sup>In-SA was prepared by first attaching diethylenetriaminepentaacetic acid (DTPA) to SA molecules. This was performed by mixing 2-(4-isothiocyanatobenzyl)-DTPA in carbonate buffer (pH 9.5) with SA suspension at a 50-fold molar excess of DTPA. The mixture was rotated overnight at 4ºC. After removal of excess DTPA, DTPA-SA was radiolabeled with <sup>111</sup>In by incubation with <sup>111</sup>In chloride in 10 mM <i>N</i>-(2-hydroxyethyl)piperazine-<i>N'</i>-(2-ethanesulfonic acid (HEPES, pH 7.0) at 37ºC for 1.5 h. Free <sup>111</sup>In was removed by Zeba Desalt Spin Columns. The specific activity and radiochemical purity of <sup>111</sup>In-SA were not reported.</p></div><div id="MSHSA111In.In_Vitro_Studies_Tes"><h2 id="_MSHSA111In_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=%28pretargeted%20bivalent%20bacteriophage%29%20AND%20in%20vitro" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>Newton et al. (<a class="bk_pop" href="#MSHSA111In.REF.1">1</a>) conducted phage sequencing to confirm that the MSH2.0 phage clone contained a modified α-MSH sequence. MSH2.0 lacked 3 nonessential amino acids at the amino terminus of the α-MSH sequence and contained a linker peptide between it and the phage coat protein III (NH<sub>2</sub>-AMEHFRWGRPVGSGSGSGSVWYAG-coat protein III). The phase clones were then probed with an anti–α-MSH antibody to determine whether the peptide sequences were accessible and reactive with the MC-1 receptor. The phage particle dot blot assay showed that the α-MSH sequence on the MSH2.0 phage clone was immunoreactive. A micropanning assay with B16/F1 mouse melanoma cells was performed to test the specific binding of MSH2.0 phage. The results indicated specific binding of MSH2.0 peptide to B16/F1 cells. There was no significant alteration of phage binding <i>in vitro</i> with the addition of PEO<sub>4</sub>-biotin to the surface of the phage particle.</p><p>The DTPA-SA complex was prepared with >90% labeling efficiency (<a class="bk_pop" href="#MSHSA111In.REF.1">1</a>). An <i>in vitro</i> stability test showed that <sup>111</sup>In-SA retained 100% labeling activity in phosphate-buffered saline and HEPES for at least 24 h at 25ºC and 37ºC. <sup>111</sup>In-SA retained ~80% activity when incubated in mouse serum for 24 h.</p></div><div id="MSHSA111In.Animal_Studies"><h2 id="_MSHSA111In_Animal_Studies_">Animal Studies</h2><div id="MSHSA111In.Rodents"><h3>Rodents</h3><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=%28pretargeted%20bivalent%20bacteriophage%29%20AND%20rodentia" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>Newton et al. (<a class="bk_pop" href="#MSHSA111In.REF.1">1</a>) conducted biodistribution studies of the pretargeted bio-MSH2.0 followed by <sup>111</sup>In-SA in mice bearing B16/F1 mouse melanoma (0.05–0.1 g s.c. tumors). Each mouse received an i.v. injection of 5 × 10<sup>12</sup> virions of bio-MSH2.0. After 4 h, an i.v. injection of 1.85 MBq (0.05 mCi) <sup>111</sup>In-SA was administered. <sup>111</sup>In-SA radioactivity was primarily cleared by the urinary and hepatobiliary systems. The initial tumor radioactivity of ~2.5% injected dose per g (% ID/g; <i>n</i> = 3) appeared to be attributable to the tumor blood volume. After 24 h, there was actual radioactivity retention of 1.0 ± 0.1% ID/g and the tumor/muscle and tumor/blood ratios were 17.5 ± 3.7 and 2.0 ± 0.2, respectively. In comparison, the tumor radioactivity of <sup>111</sup>In-SA alone without bio-MSH2.0 was 0.4 ± 0.1% ID/g at 24 h. The biotinylated nonspecific wild-type phage tumor radioactivity level was 1.8-fold less than that of bio-MSH2.0 at 24 h. This suggested that the <i>in vivo</i> targeting of <sup>111</sup>In-SA-α-MSH2.0 phage to the tumor was mediated by α-MSH peptide. Coinjection of bio-MSH2.0 with 100 μg of [NIe<sup>4</sup>,<span class="small-caps">d</span>-Phe<sup>7</sup>]α-MSH (NDP), a potent protease-resistant peptide analog of α-MSH, decreased the tumor radioactivity retention of bio-MSH2.0 by 2.4 ± 0.4-fold. The authors suggested that this demonstrated the specificity of binding for the bio-MSH2.0 phage <i>in vivo</i>.</p><p>SPECT imaging of <sup>111</sup>In-SA–α-MSH2.0 phage was performed in mice bearing B16/F1 mouse melanoma (<a class="bk_pop" href="#MSHSA111In.REF.1">1</a>). Each mouse received 5 × 10<sup>12</sup> virions of bio-MSH2.0 and then 7.4 MBq (0.2 mCi) of <sup>111</sup>In-SA. The study clearly demonstrated the accumulation of <sup>111</sup>In-SA radioactivity within the tumor. The mice were euthanized 4 h after injection. The tumor radioactivity level at 4 h was 5.2 ± 0.8% ID/g, which was higher than the biodistribution study value of 0.9 ± 0.3% ID/g. The authors suggested that the higher value in the imaging study was attributable to the higher dose of <sup>111</sup>In-SA administered in the study.</p></div><div id="MSHSA111In.Other_NonPrimate_Mam"><h3>Other Non-Primate Mammals</h3><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=%28pretargeted%20bivalent%20bacteriophage%29%20AND%20%28dog%20OR%20rabbit%20OR%20pig%20OR%20sheep%29" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>No publication is currently available.</p></div><div id="MSHSA111In.NonHuman_Primates"><h3>Non-Human Primates</h3><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=%28pretargeted%20bivalent%20bacteriophage%29%20AND%20%28primate%20NOT%20human%29" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>No publication is currently available.</p></div></div><div id="MSHSA111In.Human_Studies"><h2 id="_MSHSA111In_Human_Studies_">Human Studies</h2><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=%28pretargeted%20bivalent%20bacteriophage%29%20AND%20human" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>No publication is currently available.</p></div><div id="MSHSA111In.NIH_Support"><h2 id="_MSHSA111In_NIH_Support_">NIH Support</h2><p>NIH P50 CA103130-01.</p></div><div id="MSHSA111In.references"><h2 id="_MSHSA111In_references_">References</h2><dl class="temp-labeled-list"><dt>1.</dt><dd><div class="bk_ref" id="MSHSA111In.REF.1">Newton J.R. , Miao Y. , Deutscher S.L. , Quinn T.P. Melanoma imaging with pretargeted bivalent bacteriophage. <span><span class="ref-journal">J Nucl Med. </span>2007;<span class="ref-vol">
|
||
<strong>48</strong>
|
||
</span>(3):429–36.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/17332621" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 17332621</span></a>]</div></dd><dt>2.</dt><dd><div class="bk_ref" id="MSHSA111In.REF.2">Miao Y. , Benwell K. , Quinn T.P. 99mTc- and 111In-labeled alpha-melanocyte-stimulating hormone peptides as imaging probes for primary and pulmonary metastatic melanoma detection. <span><span class="ref-journal">J Nucl Med. </span>2007;<span class="ref-vol">
|
||
<strong>48</strong>
|
||
</span>(1):73–80.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/17204701" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 17204701</span></a>]</div></dd><dt>3.</dt><dd><div class="bk_ref" id="MSHSA111In.REF.3">Miao Y. , Hylarides M. , Fisher D.R. , Shelton T. , Moore H. , Wester D.W. , Fritzberg A.R. , Winkelmann C.T. , Hoffman T. , Quinn T.P. Melanoma therapy via peptide-targeted {alpha}-radiation. <span><span class="ref-journal">Clin Cancer Res. </span>2005;<span class="ref-vol">
|
||
<strong>11</strong>
|
||
</span>(15):5616–21.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/16061880" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 16061880</span></a>]</div></dd><dt>4.</dt><dd><div class="bk_ref" id="MSHSA111In.REF.4">Bohm M. , Luger T.A. , Tobin D.J. , Garcia-Borron J.C. Melanocortin receptor ligands: new horizons for skin biology and clinical dermatology. <span><span class="ref-journal">J Invest Dermatol. </span>2006;<span class="ref-vol">
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||
<strong>126</strong>
|
||
</span>(9):1966–75.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/16912693" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 16912693</span></a>]</div></dd><dt>5.</dt><dd><div class="bk_ref" id="MSHSA111In.REF.5">Catania A. , Airaghi L. , Garofalo L. , Cutuli M. , Lipton J.M. The neuropeptide alpha-MSH in HIV infection and other disorders in humans. <span><span class="ref-journal">Ann N Y Acad Sci. </span>1998;<span class="ref-vol">
|
||
<strong>840</strong>
|
||
</span>:848–56.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/9629310" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 9629310</span></a>]</div></dd><dt>6.</dt><dd><div class="bk_ref" id="MSHSA111In.REF.6">Weiner R.E. , Thakur M.L. Radiolabeled peptides in oncology: role in diagnosis and treatment. <span><span class="ref-journal">BioDrugs. </span>2005;<span class="ref-vol">
|
||
<strong>19</strong>
|
||
</span>(3):145–63.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/15984900" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 15984900</span></a>]</div></dd><dt>7.</dt><dd><div class="bk_ref" id="MSHSA111In.REF.7">Dimitrakopoulou-Strauss A. , Strauss L.G. , Burger C. Quantitative PET studies in pretreated melanoma patients: a comparison of 6-[18F]fluoro-L-dopa with 18F-FDG and (15)O-water using compartment and noncompartment analysis. <span><span class="ref-journal">J Nucl Med. </span>2001;<span class="ref-vol">
|
||
<strong>42</strong>
|
||
</span>(2):248–56.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/11216523" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 11216523</span></a>]</div></dd><dt>8.</dt><dd><div class="bk_ref" id="MSHSA111In.REF.8">Tatro J.B. , Reichlin S. Specific receptors for alpha-melanocyte-stimulating hormone are widely distributed in tissues of rodents. <span><span class="ref-journal">Endocrinology. </span>1987;<span class="ref-vol">
|
||
<strong>121</strong>
|
||
</span>(5):1900–7.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/2822378" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 2822378</span></a>]</div></dd><dt>9.</dt><dd><div class="bk_ref" id="MSHSA111In.REF.9">Siegrist W. , Solca F. , Stutz S. , Giuffre L. , Carrel S. , Girard J. , Eberle A.N. Characterization of receptors for alpha-melanocyte-stimulating hormone on human melanoma cells. <span><span class="ref-journal">Cancer Res. </span>1989;<span class="ref-vol">
|
||
<strong>49</strong>
|
||
</span>(22):6352–8.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/2804981" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 2804981</span></a>]</div></dd><dt>10.</dt><dd><div class="bk_ref" id="MSHSA111In.REF.10">Miao Y. , Whitener D. , Feng W. , Owen N.K. , Chen J. , Quinn T.P. Evaluation of the human melanoma targeting properties of radiolabeled alpha-melanocyte stimulating hormone peptide analogues. <span><span class="ref-journal">Bioconjug Chem. </span>2003;<span class="ref-vol">
|
||
<strong>14</strong>
|
||
</span>(6):1177–84.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/14624632" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 14624632</span></a>]</div></dd><dt>11.</dt><dd><div class="bk_ref" id="MSHSA111In.REF.11">Chen J. , Cheng Z. , Owen N.K. , Hoffman T.J. , Miao Y. , Jurisson S.S. , Quinn T.P. Evaluation of an (111)In-DOTA-rhenium cyclized alpha-MSH analog: a novel cyclic-peptide analog with improved tumor-targeting properties. <span><span class="ref-journal">J Nucl Med. </span>2001;<span class="ref-vol">
|
||
<strong>42</strong>
|
||
</span>(12):1847–55.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/11752084" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 11752084</span></a>]</div></dd><dt>12.</dt><dd><div class="bk_ref" id="MSHSA111In.REF.12">Froidevaux S. , Calame-Christe M. , Tanner H. , Eberle A.N. Melanoma targeting with DOTA-alpha-melanocyte-stimulating hormone analogs: structural parameters affecting tumor uptake and kidney uptake. <span><span class="ref-journal">J Nucl Med. </span>2005;<span class="ref-vol">
|
||
<strong>46</strong>
|
||
</span>(5):887–95.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/15872364" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 15872364</span></a>]</div></dd><dt>13.</dt><dd><div class="bk_ref" id="MSHSA111In.REF.13">Miao Y. , Owen N.K. , Whitener D. , Gallazzi F. , Hoffman T.J. , Quinn T.P. In vivo evaluation of 188Re-labeled alpha-melanocyte stimulating hormone peptide analogs for melanoma therapy. <span><span class="ref-journal">Int J Cancer. </span>2002;<span class="ref-vol">
|
||
<strong>101</strong>
|
||
</span>(5):480–7.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/12216078" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 12216078</span></a>]</div></dd><dt>14.</dt><dd><div class="bk_ref" id="MSHSA111In.REF.14">Smith G.P. Filamentous fusion phage: novel expression vectors that display cloned antigens on the virion surface. <span><span class="ref-journal">Science. </span>1985;<span class="ref-vol">
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||
<strong>228</strong>
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</span>(4705):1315–7.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/4001944" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 4001944</span></a>]</div></dd><dt>15.</dt><dd><div class="bk_ref" id="MSHSA111In.REF.15">Koscielska K. , Kiczak L. , Kasztura M. , Wesolowska O. , Otlewski J. Phage display of proteins. <span><span class="ref-journal">Acta Biochim Pol. </span>1998;<span class="ref-vol">
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<strong>45</strong>
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</span>(3):705–20.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/9918498" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 9918498</span></a>]</div></dd><dt>16.</dt><dd><div class="bk_ref" id="MSHSA111In.REF.16">Chen X. , Sievers E. , Hou Y. , Park R. , Tohme M. , Bart R. , Bremner R. , Bading J.R. , Conti P.S. Integrin alpha v beta 3-targeted imaging of lung cancer. <span><span class="ref-journal">Neoplasia. </span>2005;<span class="ref-vol">
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<strong>7</strong>
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</span>(3):271–9.</span> [<a href="/pmc/articles/PMC1501139/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC1501139</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/15799827" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 15799827</span></a>]</div></dd></dl></div><div id="bk_toc_contnr"></div></div></div>
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<div class="post-content"><div><div class="half_rhythm"><a href="/books/about/copyright/">Copyright Notice</a></div><div class="small"><span class="label">Bookshelf ID: NBK23461</span><span class="label">PMID: <a href="https://pubmed.ncbi.nlm.nih.gov/20641660" title="PubMed record of this page" ref="pagearea=meta&targetsite=entrez&targetcat=link&targettype=pubmed">20641660</a></span></div><div style="margin-top:2em" class="bk_noprnt"><a class="bk_cntns" href="/books/n/micad/">Contents</a><div class="pagination bk_noprnt"><a class="active page_link prev" href="/books/n/micad/MAb14C5-DOTA-111In/" title="Previous page in this title">< Prev</a><a class="active page_link next" href="/books/n/micad/TA138-111In/" title="Next page in this title">Next ></a></div></div></div></div>
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<div xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance"></div><div class="portlet"><div class="portlet_head"><div class="portlet_title"><h3><span>Views</span></h3></div><a name="Shutter" sid="1" href="#" class="portlet_shutter" title="Show/hide content" remembercollapsed="true" pgsec_name="PDF_download" id="Shutter"></a></div><div class="portlet_content"><ul xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="simple-list"><li><a href="/books/NBK23461/?report=reader">PubReader</a></li><li><a href="/books/NBK23461/?report=printable">Print View</a></li><li><a data-jig="ncbidialog" href="#_ncbi_dlg_citbx_NBK23461" data-jigconfig="width:400,modal:true">Cite this Page</a><div id="_ncbi_dlg_citbx_NBK23461" style="display:none" title="Cite this Page"><div class="bk_tt">Cheng KT. 111In-Streptavidin-biotinylated α-melanocyte-stimulating hormone 2.0 bacteriophage. 2007 Mar 28 [Updated 2008 May 5]. 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></div></div></li><li><a href="/books/NBK23461/pdf/Bookshelf_NBK23461.pdf">PDF version of this page</a> (388K)</li><li><a href="/books/n/micad/toc/bin/micad.csv">MICAD summary (CSV file)</a></li></ul></div></div><div class="portlet"><div class="portlet_head"><div class="portlet_title"><h3><span>In this page</span></h3></div><a name="Shutter" sid="1" href="#" class="portlet_shutter" title="Show/hide content" remembercollapsed="true" pgsec_name="page-toc" id="Shutter"></a></div><div class="portlet_content"><ul xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="simple-list"><li><a href="#MSHSA111In.Background" ref="log$=inpage&link_id=inpage">Background</a></li><li><a href="#MSHSA111In.Synthesis" ref="log$=inpage&link_id=inpage">Synthesis</a></li><li><a href="#MSHSA111In.In_Vitro_Studies_Tes" ref="log$=inpage&link_id=inpage"><i>In Vitro</i> Studies: Testing in Cells and Tissues</a></li><li><a href="#MSHSA111In.Animal_Studies" ref="log$=inpage&link_id=inpage">Animal Studies</a></li><li><a href="#MSHSA111In.Human_Studies" ref="log$=inpage&link_id=inpage">Human Studies</a></li><li><a href="#MSHSA111In.NIH_Support" ref="log$=inpage&link_id=inpage">NIH Support</a></li><li><a href="#MSHSA111In.references" ref="log$=inpage&link_id=inpage">References</a></li></ul></div></div><div class="portlet"><div class="portlet_head"><div class="portlet_title"><h3><span>Search MICAD</span></h3></div><a name="Shutter" sid="1" href="#" class="portlet_shutter" title="Show/hide content" remembercollapsed="true" pgsec_name="source-application" id="Shutter"></a></div><div class="portlet_content"><form xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" name="frmSearch" method="get" action="/books/NBK5330/" id="frmSearch"><script type="text/javascript" src="/corehtml/pmc//js/bookshelf/micad.js">/**/</script><label class="offscreen_noflow" for="txtfield">Search term</label><input id="txtfield" type="text" name="f1_term" size="22" onKeyPress="KeyPress('micad',event,'/books/NBK5330/','')" /><button name="f1_search" type="submit">Go</button><button onclick="this.form.reset();" type="reset">Clear</button><p><b>Limit my Search:</b></p><div class="clearfix"><label for="detection">Method of detection:</label><div class="right"><select name="detection" id="detection" style="width:200px"><option value="" selected="selected">Any</option><option value="(MRI OR "Magnetic resonance imaging" OR MRS)">MRI</option><option value="Multimodal">Multimodal imaging</option><option value="Optical">Optical imaging</option><option value="PET">PET</option><option value="Photoacoustic">Photoacoustic imaging</option><option value="(SPECT OR planar)">SPECT</option><option value="Ultrasound">Ultrasound</option><option value="(x-ray OR ct)">X-ray, CT</option></select></div></div><div class="clearfix"><label for="signal">Source of signal/contrast:</label><div class="right"><select name="signal" id="signal" style="width:200px"><option value="" selected="selected">Any</option><optgroup label="MRI agents"><option value="(Copper OR Cu)">Copper</option><option value="(Europium OR Eu3+)">Europium</option><option value="(Fluorine OR 19F)">Fluorine</option><option value="(Gadolinium OR Gd3+)">Gadolinium</option><option value=""Hyperpolarized 13C"">Hyperpolarized 13C</option><option value=""Iron oxide"">Iron oxide</option><option value=""Nitroxide radicals"">Nitroxide radicals</option><option value="(Oxygen OR 17O)">Oxygen</option><option value="Thulium">Thulium</option></optgroup><optgroup label="Multimodal agents"><option value="((Gadolinium OR Gd3+) AND Optical)">Gadolinium and optical</option><option value="((Gadolinium OR Gd3+) AND (Gold OR Au))">Gadolinium and Gold</option><option value="("Iron oxide" AND (64Cu OR 124I OR 111In))">Iron oxide and
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radionuclides</option><option value="(Perfluorocarbon AND (Europium OR Eu3+))">Perfluorocarbon and
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europium</option><option value="(166Ho OR 67Ga OR 68Ga OR 123I OR 124I OR 125I)">Radionuclides</option></optgroup><optgroup label="Optical agents"><option value="("Fluorescent dyes" OR protein)">Fluorescent dyes or proteins</option><option value=""Luminescent agents"">Luminescent agents</option><option value="(Metals OR Metal OR Gold OR Au)">Metals (Au)</option><option value="Nanotubes">Nanotubes</option><option value=""Quantum dots"">Quantum dots</option></optgroup><optgroup label="PET radionuclides"><option value="("Arsenic 74" OR 74As)">Arsenic-74</option><option value="("Bromine 76" OR 76Br)">Bromine-76</option><option value="("Carbon 11" OR 11C)">Carbon-11</option><option value="(Copper-60 OR Copper-61 OR Copper-62 OR Copper-64 OR 60Cu OR 61Cu OR 62Cu OR 64Cu)">Copper-60, 61, 62, 64</option><option value="("Fluorine 18" OR 18F)">Fluorine-18</option><option value="(Gallium-68 OR 68Ga)">Gallium-68</option><option value="("Iodine 124" OR 124I)">Iodine-124</option><option value="("Nitrogen 13" OR 13N)">Nitrogen-13</option><option value="("Yttrium 86" OR 86Y)">Yttrium-86</option><option value="("Zirconium 89" OR 89Zr)">Zirconium-89</option></optgroup><optgroup label="Photoacoustic agents"><option value="(Gold OR Au)">Gold</option><option value="("Indocyanine green" OR ICG)">Indocyanine green</option></optgroup><optgroup label="SPECT radionuclides"><option value="(Gallium-67 OR 67Ga)">Gallium-67</option><option value="("Indium 111" OR 111In)">Indium-111</option><option value="("Iodine 123" OR "Iodine 125" OR "Iodine 131" OR 123I OR 125I OR 131I)">Iodine-123, 125, 131</option><option value="("Lutetium 177" OR 177Lu)">Lutetium-177</option><option value="(Rhenium OR 186Re OR 188Re)">Rhenium</option><option value="("Technetium 99m" OR 99mTc)">Technetium-99m</option><option value="("Tellurium 125m" OR 125mTe)">Tellurium-125m</option></optgroup><optgroup label="Ultrasound agents"><option value="Microbubbles">Microbubbles</option><option value="Nanobubbles">Nanobubbles</option></optgroup><optgroup label="X-ray and CT agents"><option value="(Bismuth OR Bi)">Bismuth</option><option value="(Gold OR Au)">Gold</option><option value="Iodine">Iodine</option></optgroup></select></div></div><div class="clearfix"><label for="agent">Agent Category:</label><div class="right"><select name="agent" id="agent" style="width:200px"><option value="" selected="selected">Any</option><option value="(antibody OR trastuzumab OR immunoglobulin)">Antibodies</option><option value="(bacteria OR bacteriophage OR coli)">Bacteria</option><option value="cell">Cells</option><option value="(compound OR "amino acid" OR "folic acid" OR "cage molecule" OR carbohydrate OR copolymers OR polymer OR "small molecule" OR macromolecule OR triiodobenzoate OR estradiol OR glycosaminoglycan)">Compounds</option><option value="ligand">Ligands</option><option value="(lipid OR liposome OR liposomes">Lipids</option><option value="metal">Metal</option><option value="(nanoparticle OR nanoparticles OR nanotubes OR "iron oxide")">Nanoparticles</option><option value="(siRNA OR "nucleic acid" OR oligonucleotide)">Nucleic acids</option><option value="peptide">Peptides</option><option value="polyeptide">Polyeptides</option><option value="(protein OR albumin OR chemokin OR immunoprotein OR luciferase OR albumin)">Proteins</option><option value="(virus OR adenovirus)">Viruses</option></select></div></div><div class="clearfix"><label for="target">Target Category:</label><div class="right"><select name="target" id="target" style="width:200px"><option value="" selected="selected">Any</option><option value="acceptor">Acceptors</option><option value=""adhesion molecule"">Adhesion molecules</option><option value="(antigen OR antibody-antigen)">Antigens</option><option value="(enzyme OR enzymes OR enzyme-substrate)">Enzymes</option><option value="(lipids OR lipophilic cation)">Lipids</option><option value="(receptor OR receptors OR receptor-ligand OR receptor-antibody OR antibody-receptor)">Receptors</option><option value="transporter">Transporters</option><option value="non-targeted">Non-targeted</option><option value=""nucleic acid"">Nucleic acids</option><option value="(non-targeted OR "unknown binding site")">Others</option></select></div></div><div><input id="__micad_btn_1" type="radio" name="stage" value="vitro" /><label for="__micad_btn_1"><i>In vitro</i></label><input id="__micad_btn_2" type="radio" name="stage" value="rodents" /><label for="__micad_btn_2">Rodents</label><input id="__micad_btn_3" type="radio" name="stage" value="mammals" /><label for="__micad_btn_3">Non-primate non-rodent mammals</label><br /><input id="__micad_btn_4" type="radio" name="stage" value="primates" /><label for="__micad_btn_4">Non-human primates</label><input id="__micad_btn_5" type="radio" name="stage" value="humans" /><label for="__micad_btn_5">Humans</label><input id="__micad_btn_6" type="radio" name="stage" value="any" checked="checked" /><label for="__micad_btn_6">Any</label></div></form><form xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" name="frmGo" method="get" action="javascript:alert('frmGo:_@action_was_not_set')" id="frmGo"><input name="term" value="." type="hidden" /></form></div></div><div class="portlet"><div class="portlet_head"><div class="portlet_title"><h3><span>Related information</span></h3></div><a name="Shutter" sid="1" href="#" class="portlet_shutter" title="Show/hide content" remembercollapsed="true" pgsec_name="discovery_db_links" id="Shutter"></a></div><div class="portlet_content"><ul><li class="brieflinkpopper"><a class="brieflinkpopperctrl" href="/books/?Db=pmc&DbFrom=books&Cmd=Link&LinkName=books_pmc_refs&IdsFromResult=1510676" ref="log$=recordlinks">PMC</a><div class="brieflinkpop offscreen_noflow">PubMed Central citations</div></li><li class="brieflinkpopper"><a class="brieflinkpopperctrl" href="/books/?Db=pubmed&DbFrom=books&Cmd=Link&LinkName=books_pubmed_refs&IdsFromResult=1510676" ref="log$=recordlinks">PubMed</a><div class="brieflinkpop offscreen_noflow">Links to PubMed</div></li></ul></div></div><div class="portlet"><div class="portlet_head"><div class="portlet_title"><h3><span>Similar articles in PubMed</span></h3></div><a name="Shutter" sid="1" href="#" class="portlet_shutter" title="Show/hide content" remembercollapsed="true" pgsec_name="PBooksDiscovery_RA" id="Shutter"></a></div><div class="portlet_content"><ul><li class="brieflinkpopper two_line"><a class="brieflinkpopperctrl" href="/pubmed/20641798" ref="ordinalpos=1&linkpos=1&log$=relatedreviews&logdbfrom=pubmed"><span xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="invert">Review</span> (111)In-DOTA-Re(Cys(3,4,10),d-Phe(7),Arg(11))αMSH(3-13).</a><span class="source">[Molecular Imaging and Contrast...]</span><div class="brieflinkpop 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(64)Cu-[Ac-NIe-Asp-His-d-Phe-Arg-Trp-Gly-Lys(1,4,7,10-Tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid)-NH(2)].</a><span class="source">[Molecular Imaging and Contrast...]</span><div class="brieflinkpop offscreen_noflow"><span xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="invert">Review</span> (64)Cu-[Ac-NIe-Asp-His-d-Phe-Arg-Trp-Gly-Lys(1,4,7,10-Tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid)-NH(2)].<div class="brieflinkpopdesc"><em xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="author">Cheng KT, Gambhir S, Cheng Z. </em><em xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="cit">Molecular Imaging and Contrast Agent Database (MICAD). 2004</em></div></div></li></ul><a class="seemore" href="/sites/entrez?db=pubmed&cmd=link&linkname=pubmed_pubmed_reviews&uid=20641660" 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