Breast Tumor Targeting in Mice Bearing 4T1 Tumor with Labeled CXCR4 Antagonist Analogue
Chemokine receptor belongs to G-protein-coupled cell-surface receptors. CXCR4 as a chemokine receptor is over-expressed in many type of solid tumors and metastasis in which breast tumor is one of them. A CXCR4 targeted peptide was prepared and labeled with 99m Tc. Subsequently, receptor binding inte...
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| Veröffentlicht in: | International journal of peptide research and therapeutics 2021-12, Vol.27 (4), p.2449-2457 |
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| creator | Mikaeili, Azadeh Erfani, Mostafa Goudarzi, Mostafa Sabzevari, Omid |
| description | Chemokine receptor belongs to G-protein-coupled cell-surface receptors. CXCR4 as a chemokine receptor is over-expressed in many type of solid tumors and metastasis in which breast tumor is one of them. A CXCR4 targeted peptide was prepared and labeled with
99m
Tc. Subsequently, receptor binding internalization, in vivo tumor uptake and biodistribution were assessed. The receptor binding internalization rate was evaluated using 4T1 breast tumor cells. BALB/c female mice bearing 4T1 tumors were employed for investigation of radioconjugate biodistribution. Radioconjugate was obtained with labeling yield of > 95%. The highest achieved specific activity was 123 MBq/nmol. The in vitro cell uptake test resulted specific internalization into 4T1 cells (average of 1.90 ± 0.12% of total add at 2 h). Animal biodistribution data showed tumor uptake of 1.18 ± 0.11% ID/g after 30 min post injection. Our findings demonstrated that the labeled peptide can be a suitable candidate for breast tumors imaging. |
| doi_str_mv | 10.1007/s10989-021-10264-2 |
| format | Article |
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99m
Tc. Subsequently, receptor binding internalization, in vivo tumor uptake and biodistribution were assessed. The receptor binding internalization rate was evaluated using 4T1 breast tumor cells. BALB/c female mice bearing 4T1 tumors were employed for investigation of radioconjugate biodistribution. Radioconjugate was obtained with labeling yield of > 95%. The highest achieved specific activity was 123 MBq/nmol. The in vitro cell uptake test resulted specific internalization into 4T1 cells (average of 1.90 ± 0.12% of total add at 2 h). Animal biodistribution data showed tumor uptake of 1.18 ± 0.11% ID/g after 30 min post injection. Our findings demonstrated that the labeled peptide can be a suitable candidate for breast tumors imaging.</description><identifier>ISSN: 1573-3149</identifier><identifier>EISSN: 1573-3904</identifier><identifier>DOI: 10.1007/s10989-021-10264-2</identifier><language>eng</language><publisher>Dordrecht: Springer Netherlands</publisher><subject>Animal Anatomy ; Biochemistry ; Biodistribution ; Biomedical and Life Sciences ; Breast cancer ; Cell surface ; Chemokine receptors ; Chemokines ; CXCR4 protein ; G protein-coupled receptors ; Histology ; Internalization ; Life Sciences ; Metastases ; Molecular Medicine ; Morphology ; Peptides ; Pharmaceutical Sciences/Technology ; Pharmacology/Toxicology ; Polymer Sciences ; Solid tumors ; Tumor cells ; Tumors</subject><ispartof>International journal of peptide research and therapeutics, 2021-12, Vol.27 (4), p.2449-2457</ispartof><rights>The Author(s), under exclusive licence to Springer Nature B.V. 2021</rights><rights>The Author(s), under exclusive licence to Springer Nature B.V. 2021.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c319t-d824939a754599330dbe93f28a2a178cd051d5df48834dc1ced5c6439e541c8c3</citedby><cites>FETCH-LOGICAL-c319t-d824939a754599330dbe93f28a2a178cd051d5df48834dc1ced5c6439e541c8c3</cites><orcidid>0000-0002-5674-1575</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://link.springer.com/content/pdf/10.1007/s10989-021-10264-2$$EPDF$$P50$$Gspringer$$H</linktopdf><linktohtml>$$Uhttps://link.springer.com/10.1007/s10989-021-10264-2$$EHTML$$P50$$Gspringer$$H</linktohtml><link.rule.ids>314,776,780,27901,27902,41464,42533,51294</link.rule.ids></links><search><creatorcontrib>Mikaeili, Azadeh</creatorcontrib><creatorcontrib>Erfani, Mostafa</creatorcontrib><creatorcontrib>Goudarzi, Mostafa</creatorcontrib><creatorcontrib>Sabzevari, Omid</creatorcontrib><title>Breast Tumor Targeting in Mice Bearing 4T1 Tumor with Labeled CXCR4 Antagonist Analogue</title><title>International journal of peptide research and therapeutics</title><addtitle>Int J Pept Res Ther</addtitle><description>Chemokine receptor belongs to G-protein-coupled cell-surface receptors. CXCR4 as a chemokine receptor is over-expressed in many type of solid tumors and metastasis in which breast tumor is one of them. A CXCR4 targeted peptide was prepared and labeled with
99m
Tc. Subsequently, receptor binding internalization, in vivo tumor uptake and biodistribution were assessed. The receptor binding internalization rate was evaluated using 4T1 breast tumor cells. BALB/c female mice bearing 4T1 tumors were employed for investigation of radioconjugate biodistribution. Radioconjugate was obtained with labeling yield of > 95%. The highest achieved specific activity was 123 MBq/nmol. The in vitro cell uptake test resulted specific internalization into 4T1 cells (average of 1.90 ± 0.12% of total add at 2 h). Animal biodistribution data showed tumor uptake of 1.18 ± 0.11% ID/g after 30 min post injection. Our findings demonstrated that the labeled peptide can be a suitable candidate for breast tumors imaging.</description><subject>Animal Anatomy</subject><subject>Biochemistry</subject><subject>Biodistribution</subject><subject>Biomedical and Life Sciences</subject><subject>Breast cancer</subject><subject>Cell surface</subject><subject>Chemokine receptors</subject><subject>Chemokines</subject><subject>CXCR4 protein</subject><subject>G protein-coupled receptors</subject><subject>Histology</subject><subject>Internalization</subject><subject>Life Sciences</subject><subject>Metastases</subject><subject>Molecular Medicine</subject><subject>Morphology</subject><subject>Peptides</subject><subject>Pharmaceutical Sciences/Technology</subject><subject>Pharmacology/Toxicology</subject><subject>Polymer Sciences</subject><subject>Solid tumors</subject><subject>Tumor cells</subject><subject>Tumors</subject><issn>1573-3149</issn><issn>1573-3904</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2021</creationdate><recordtype>article</recordtype><sourceid>BENPR</sourceid><recordid>eNp9kF1LwzAUhoMoOKd_wKuA19GcfKzJ5Sx-wUSQit6FLElrx9bOpEX893Z24p1X5xx43pfDg9A50EugNLtKQLXShDIgQNlMEHaAJiAzTrim4vB3B6GP0UlKK0oly4BO0Ot1DDZ1uOg3bcSFjVXo6qbCdYMfaxfwdbBxd4sC9sxn3b3jhV2GdfA4f8ufBZ43na3aph565o1dt1UfTtFRadcpnO3nFL3c3hT5PVk83T3k8wVxHHRHvGJCc20zKaTWnFO_DJqXTFlmIVPOUwle-lIoxYV34IKXbia4DlKAU45P0cXYu43tRx9SZ1ZtH4cnkmFSs2ymtJYDxUbKxTalGEqzjfXGxi8D1OwEmlGgGQSaH4GGDSE-htJ2pyDEv-p_Ut86IHFE</recordid><startdate>20211201</startdate><enddate>20211201</enddate><creator>Mikaeili, Azadeh</creator><creator>Erfani, Mostafa</creator><creator>Goudarzi, Mostafa</creator><creator>Sabzevari, Omid</creator><general>Springer Netherlands</general><general>Springer Nature B.V</general><scope>AAYXX</scope><scope>CITATION</scope><scope>3V.</scope><scope>7X7</scope><scope>7XB</scope><scope>88A</scope><scope>88I</scope><scope>8AO</scope><scope>8FE</scope><scope>8FH</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>AZQEC</scope><scope>BBNVY</scope><scope>BENPR</scope><scope>BHPHI</scope><scope>CCPQU</scope><scope>DWQXO</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>GNUQQ</scope><scope>HCIFZ</scope><scope>K9.</scope><scope>LK8</scope><scope>M0S</scope><scope>M2P</scope><scope>M7P</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>Q9U</scope><orcidid>https://orcid.org/0000-0002-5674-1575</orcidid></search><sort><creationdate>20211201</creationdate><title>Breast Tumor Targeting in Mice Bearing 4T1 Tumor with Labeled CXCR4 Antagonist Analogue</title><author>Mikaeili, Azadeh ; Erfani, Mostafa ; Goudarzi, Mostafa ; Sabzevari, Omid</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c319t-d824939a754599330dbe93f28a2a178cd051d5df48834dc1ced5c6439e541c8c3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2021</creationdate><topic>Animal Anatomy</topic><topic>Biochemistry</topic><topic>Biodistribution</topic><topic>Biomedical and Life Sciences</topic><topic>Breast cancer</topic><topic>Cell surface</topic><topic>Chemokine receptors</topic><topic>Chemokines</topic><topic>CXCR4 protein</topic><topic>G protein-coupled receptors</topic><topic>Histology</topic><topic>Internalization</topic><topic>Life Sciences</topic><topic>Metastases</topic><topic>Molecular Medicine</topic><topic>Morphology</topic><topic>Peptides</topic><topic>Pharmaceutical Sciences/Technology</topic><topic>Pharmacology/Toxicology</topic><topic>Polymer Sciences</topic><topic>Solid tumors</topic><topic>Tumor cells</topic><topic>Tumors</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Mikaeili, Azadeh</creatorcontrib><creatorcontrib>Erfani, Mostafa</creatorcontrib><creatorcontrib>Goudarzi, Mostafa</creatorcontrib><creatorcontrib>Sabzevari, Omid</creatorcontrib><collection>CrossRef</collection><collection>ProQuest Central (Corporate)</collection><collection>Health & Medical Collection</collection><collection>ProQuest Central (purchase pre-March 2016)</collection><collection>Biology Database (Alumni Edition)</collection><collection>Science Database (Alumni Edition)</collection><collection>ProQuest Pharma Collection</collection><collection>ProQuest SciTech Collection</collection><collection>ProQuest Natural Science Collection</collection><collection>Hospital Premium Collection</collection><collection>Hospital Premium Collection (Alumni Edition)</collection><collection>ProQuest Central (Alumni) (purchase pre-March 2016)</collection><collection>ProQuest Central (Alumni Edition)</collection><collection>ProQuest Central UK/Ireland</collection><collection>ProQuest Central Essentials</collection><collection>Biological Science Collection</collection><collection>ProQuest Central</collection><collection>Natural Science Collection</collection><collection>ProQuest One Community College</collection><collection>ProQuest Central Korea</collection><collection>Health Research Premium Collection</collection><collection>Health Research Premium Collection (Alumni)</collection><collection>ProQuest Central Student</collection><collection>SciTech Premium Collection</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>ProQuest Biological Science Collection</collection><collection>Health & Medical Collection (Alumni Edition)</collection><collection>Science Database</collection><collection>Biological Science Database</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><collection>ProQuest Central Basic</collection><jtitle>International journal of peptide research and therapeutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Mikaeili, Azadeh</au><au>Erfani, Mostafa</au><au>Goudarzi, Mostafa</au><au>Sabzevari, Omid</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Breast Tumor Targeting in Mice Bearing 4T1 Tumor with Labeled CXCR4 Antagonist Analogue</atitle><jtitle>International journal of peptide research and therapeutics</jtitle><stitle>Int J Pept Res Ther</stitle><date>2021-12-01</date><risdate>2021</risdate><volume>27</volume><issue>4</issue><spage>2449</spage><epage>2457</epage><pages>2449-2457</pages><issn>1573-3149</issn><eissn>1573-3904</eissn><abstract>Chemokine receptor belongs to G-protein-coupled cell-surface receptors. CXCR4 as a chemokine receptor is over-expressed in many type of solid tumors and metastasis in which breast tumor is one of them. A CXCR4 targeted peptide was prepared and labeled with
99m
Tc. Subsequently, receptor binding internalization, in vivo tumor uptake and biodistribution were assessed. The receptor binding internalization rate was evaluated using 4T1 breast tumor cells. BALB/c female mice bearing 4T1 tumors were employed for investigation of radioconjugate biodistribution. Radioconjugate was obtained with labeling yield of > 95%. The highest achieved specific activity was 123 MBq/nmol. The in vitro cell uptake test resulted specific internalization into 4T1 cells (average of 1.90 ± 0.12% of total add at 2 h). Animal biodistribution data showed tumor uptake of 1.18 ± 0.11% ID/g after 30 min post injection. Our findings demonstrated that the labeled peptide can be a suitable candidate for breast tumors imaging.</abstract><cop>Dordrecht</cop><pub>Springer Netherlands</pub><doi>10.1007/s10989-021-10264-2</doi><tpages>9</tpages><orcidid>https://orcid.org/0000-0002-5674-1575</orcidid></addata></record> |
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| subjects | Animal Anatomy Biochemistry Biodistribution Biomedical and Life Sciences Breast cancer Cell surface Chemokine receptors Chemokines CXCR4 protein G protein-coupled receptors Histology Internalization Life Sciences Metastases Molecular Medicine Morphology Peptides Pharmaceutical Sciences/Technology Pharmacology/Toxicology Polymer Sciences Solid tumors Tumor cells Tumors |
| title | Breast Tumor Targeting in Mice Bearing 4T1 Tumor with Labeled CXCR4 Antagonist Analogue |
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