68Ga-labelled NOTA-RGD-GE11 peptide for dual integrin and EGFR-targeted tumour imaging
Multiple peptide receptors are co-expressed in many types of cancers. Arg-Gly-Asp (RGD) and GE11 peptides specifically target integrin αVβ3 and EGFR, respectively. Recently, we designed and synthesized a heterodimer peptide NOTA-c(RGDyK)-GE11 (NOTA-RGD-GE11). The aim of this study was to investigate...
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| Veröffentlicht in: | Nuclear medicine and biology 2019-01, Vol.68-69, p.22-30 |
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| creator | Chen, Chien-Jen Chan, Chen-Hsin Lin, Kun-Liang Chen, Jyun-Hong Tseng, Chun-Hao Wang, Ping-Yen Chien, Chuan-Yi Yu, Hung-Man Lin, Wuu-Jyh |
| description | Multiple peptide receptors are co-expressed in many types of cancers. Arg-Gly-Asp (RGD) and GE11 peptides specifically target integrin αVβ3 and EGFR, respectively. Recently, we designed and synthesized a heterodimer peptide NOTA-c(RGDyK)-GE11 (NOTA-RGD-GE11). The aim of this study was to investigate the characteristics of NOTA-RGD-GE11 for dual receptor imaging.
NOTA-RGD-GE11 heterodimer was labelled with 68Ga. The dual receptor binding affinity was investigated by antibody competition binding assay. The in vitro and in vivo characteristics of [68Ga]Ga-NOTA-RGD-GE11 were investigated and compared with that of monomeric peptides [68Ga]Ga-NOTA-RGD and [68Ga]Ga-NOTA-GE11.
NOTA-RGD-GE11 had binding affinities with both integrin αVβ3 and EGFR. The dual receptor targeting property of [68Ga]Ga-NOTA-RGD-GE11 was validated by blocking studies in a NCI-H292 tumour model. [68Ga]Ga-NOTA-RGD-GE11 showed higher tumour uptake than [68Ga]Ga-NOTA-RGD and [68Ga]Ga-NOTA-GE11 in biodistribution and PET/CT imaging studies.
The dual receptor targeting and enhanced tumour uptake of [68Ga]Ga-NOTA-RGD-GE11 warrant its further investigation for dual integrin αVβ3 and EGFR-targeted tumour imaging. |
| doi_str_mv | 10.1016/j.nucmedbio.2018.11.003 |
| format | Article |
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NOTA-RGD-GE11 heterodimer was labelled with 68Ga. The dual receptor binding affinity was investigated by antibody competition binding assay. The in vitro and in vivo characteristics of [68Ga]Ga-NOTA-RGD-GE11 were investigated and compared with that of monomeric peptides [68Ga]Ga-NOTA-RGD and [68Ga]Ga-NOTA-GE11.
NOTA-RGD-GE11 had binding affinities with both integrin αVβ3 and EGFR. The dual receptor targeting property of [68Ga]Ga-NOTA-RGD-GE11 was validated by blocking studies in a NCI-H292 tumour model. [68Ga]Ga-NOTA-RGD-GE11 showed higher tumour uptake than [68Ga]Ga-NOTA-RGD and [68Ga]Ga-NOTA-GE11 in biodistribution and PET/CT imaging studies.
The dual receptor targeting and enhanced tumour uptake of [68Ga]Ga-NOTA-RGD-GE11 warrant its further investigation for dual integrin αVβ3 and EGFR-targeted tumour imaging.</description><identifier>ISSN: 0969-8051</identifier><identifier>EISSN: 1872-9614</identifier><identifier>DOI: 10.1016/j.nucmedbio.2018.11.003</identifier><language>eng</language><publisher>Oxford: Elsevier Inc</publisher><subject>Affinity ; Antibodies ; Binding ; Computed tomography ; EGFR ; Epidermal growth factor receptors ; Ga-68 ; Heterodimer peptide ; Imaging ; In vivo methods and tests ; Integrin αVβ3 ; Investigations ; Peptides ; PET imaging ; Positron emission ; Receptors ; Tomography ; Tumors</subject><ispartof>Nuclear medicine and biology, 2019-01, Vol.68-69, p.22-30</ispartof><rights>2018 Elsevier Inc.</rights><rights>Copyright Elsevier BV Jan/Feb 2019</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c2210-7570acf06b6be55f855d92489d8d56eceee32e807730c58bed7da2f7c76268453</citedby><cites>FETCH-LOGICAL-c2210-7570acf06b6be55f855d92489d8d56eceee32e807730c58bed7da2f7c76268453</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0969805118302592$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids></links><search><creatorcontrib>Chen, Chien-Jen</creatorcontrib><creatorcontrib>Chan, Chen-Hsin</creatorcontrib><creatorcontrib>Lin, Kun-Liang</creatorcontrib><creatorcontrib>Chen, Jyun-Hong</creatorcontrib><creatorcontrib>Tseng, Chun-Hao</creatorcontrib><creatorcontrib>Wang, Ping-Yen</creatorcontrib><creatorcontrib>Chien, Chuan-Yi</creatorcontrib><creatorcontrib>Yu, Hung-Man</creatorcontrib><creatorcontrib>Lin, Wuu-Jyh</creatorcontrib><title>68Ga-labelled NOTA-RGD-GE11 peptide for dual integrin and EGFR-targeted tumour imaging</title><title>Nuclear medicine and biology</title><description>Multiple peptide receptors are co-expressed in many types of cancers. Arg-Gly-Asp (RGD) and GE11 peptides specifically target integrin αVβ3 and EGFR, respectively. Recently, we designed and synthesized a heterodimer peptide NOTA-c(RGDyK)-GE11 (NOTA-RGD-GE11). The aim of this study was to investigate the characteristics of NOTA-RGD-GE11 for dual receptor imaging.
NOTA-RGD-GE11 heterodimer was labelled with 68Ga. The dual receptor binding affinity was investigated by antibody competition binding assay. The in vitro and in vivo characteristics of [68Ga]Ga-NOTA-RGD-GE11 were investigated and compared with that of monomeric peptides [68Ga]Ga-NOTA-RGD and [68Ga]Ga-NOTA-GE11.
NOTA-RGD-GE11 had binding affinities with both integrin αVβ3 and EGFR. The dual receptor targeting property of [68Ga]Ga-NOTA-RGD-GE11 was validated by blocking studies in a NCI-H292 tumour model. [68Ga]Ga-NOTA-RGD-GE11 showed higher tumour uptake than [68Ga]Ga-NOTA-RGD and [68Ga]Ga-NOTA-GE11 in biodistribution and PET/CT imaging studies.
The dual receptor targeting and enhanced tumour uptake of [68Ga]Ga-NOTA-RGD-GE11 warrant its further investigation for dual integrin αVβ3 and EGFR-targeted tumour imaging.</description><subject>Affinity</subject><subject>Antibodies</subject><subject>Binding</subject><subject>Computed tomography</subject><subject>EGFR</subject><subject>Epidermal growth factor receptors</subject><subject>Ga-68</subject><subject>Heterodimer peptide</subject><subject>Imaging</subject><subject>In vivo methods and tests</subject><subject>Integrin αVβ3</subject><subject>Investigations</subject><subject>Peptides</subject><subject>PET imaging</subject><subject>Positron emission</subject><subject>Receptors</subject><subject>Tomography</subject><subject>Tumors</subject><issn>0969-8051</issn><issn>1872-9614</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2019</creationdate><recordtype>article</recordtype><recordid>eNqFkE1r3DAURUVoINM0vyGGbLqRo6exPrwc0hm3EDoQkmyFLD0PGjy2K9mF_PsqTOmim6ze5tzLu4eQW2AlMJD3x3JY3Al9G8aSM9AlQMnY-oKsQCtOawnVJ7JitaypZgKuyOeUjiwnK2Ar8ip1Y2lvW-x79MXP_fOGPjXfaLMFKCac5uCx6MZY-MX2RRhmPMQwFHbwxbbZPdHZxgPOOTkvp3GJRTjZQxgOX8hlZ_uEN3_vNXnZbZ8fvtPHffPjYfNIHefAqBKKWdcx2coWhei0EL7mla699kKiQ8Q1R82UWjMndIteecs75ZTkUldifU2-nnunOP5aMM3mFJLLW-yA45IMB1HXWitgGb37Dz3mh4f8neGcqwoqXqtMqTPl4phSxM5MMW-KbwaYefdtjuafb_Pu2wCY7DsnN-ck5r2_A0aTXMDBoQ8R3Wz8GD7s-AMGYIp5</recordid><startdate>201901</startdate><enddate>201901</enddate><creator>Chen, Chien-Jen</creator><creator>Chan, Chen-Hsin</creator><creator>Lin, Kun-Liang</creator><creator>Chen, Jyun-Hong</creator><creator>Tseng, Chun-Hao</creator><creator>Wang, Ping-Yen</creator><creator>Chien, Chuan-Yi</creator><creator>Yu, Hung-Man</creator><creator>Lin, Wuu-Jyh</creator><general>Elsevier Inc</general><general>Elsevier BV</general><scope>AAYXX</scope><scope>CITATION</scope><scope>7QO</scope><scope>7QP</scope><scope>7TK</scope><scope>7TM</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>201901</creationdate><title>68Ga-labelled NOTA-RGD-GE11 peptide for dual integrin and EGFR-targeted tumour imaging</title><author>Chen, Chien-Jen ; Chan, Chen-Hsin ; Lin, Kun-Liang ; Chen, Jyun-Hong ; Tseng, Chun-Hao ; Wang, Ping-Yen ; Chien, Chuan-Yi ; Yu, Hung-Man ; Lin, Wuu-Jyh</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c2210-7570acf06b6be55f855d92489d8d56eceee32e807730c58bed7da2f7c76268453</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2019</creationdate><topic>Affinity</topic><topic>Antibodies</topic><topic>Binding</topic><topic>Computed tomography</topic><topic>EGFR</topic><topic>Epidermal growth factor receptors</topic><topic>Ga-68</topic><topic>Heterodimer peptide</topic><topic>Imaging</topic><topic>In vivo methods and tests</topic><topic>Integrin αVβ3</topic><topic>Investigations</topic><topic>Peptides</topic><topic>PET imaging</topic><topic>Positron emission</topic><topic>Receptors</topic><topic>Tomography</topic><topic>Tumors</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Chen, Chien-Jen</creatorcontrib><creatorcontrib>Chan, Chen-Hsin</creatorcontrib><creatorcontrib>Lin, Kun-Liang</creatorcontrib><creatorcontrib>Chen, Jyun-Hong</creatorcontrib><creatorcontrib>Tseng, Chun-Hao</creatorcontrib><creatorcontrib>Wang, Ping-Yen</creatorcontrib><creatorcontrib>Chien, Chuan-Yi</creatorcontrib><creatorcontrib>Yu, Hung-Man</creatorcontrib><creatorcontrib>Lin, Wuu-Jyh</creatorcontrib><collection>CrossRef</collection><collection>Biotechnology Research Abstracts</collection><collection>Calcium & Calcified Tissue Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>Nucleic Acids Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Nuclear medicine and biology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Chen, Chien-Jen</au><au>Chan, Chen-Hsin</au><au>Lin, Kun-Liang</au><au>Chen, Jyun-Hong</au><au>Tseng, Chun-Hao</au><au>Wang, Ping-Yen</au><au>Chien, Chuan-Yi</au><au>Yu, Hung-Man</au><au>Lin, Wuu-Jyh</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>68Ga-labelled NOTA-RGD-GE11 peptide for dual integrin and EGFR-targeted tumour imaging</atitle><jtitle>Nuclear medicine and biology</jtitle><date>2019-01</date><risdate>2019</risdate><volume>68-69</volume><spage>22</spage><epage>30</epage><pages>22-30</pages><issn>0969-8051</issn><eissn>1872-9614</eissn><abstract>Multiple peptide receptors are co-expressed in many types of cancers. Arg-Gly-Asp (RGD) and GE11 peptides specifically target integrin αVβ3 and EGFR, respectively. Recently, we designed and synthesized a heterodimer peptide NOTA-c(RGDyK)-GE11 (NOTA-RGD-GE11). The aim of this study was to investigate the characteristics of NOTA-RGD-GE11 for dual receptor imaging.
NOTA-RGD-GE11 heterodimer was labelled with 68Ga. The dual receptor binding affinity was investigated by antibody competition binding assay. The in vitro and in vivo characteristics of [68Ga]Ga-NOTA-RGD-GE11 were investigated and compared with that of monomeric peptides [68Ga]Ga-NOTA-RGD and [68Ga]Ga-NOTA-GE11.
NOTA-RGD-GE11 had binding affinities with both integrin αVβ3 and EGFR. The dual receptor targeting property of [68Ga]Ga-NOTA-RGD-GE11 was validated by blocking studies in a NCI-H292 tumour model. [68Ga]Ga-NOTA-RGD-GE11 showed higher tumour uptake than [68Ga]Ga-NOTA-RGD and [68Ga]Ga-NOTA-GE11 in biodistribution and PET/CT imaging studies.
The dual receptor targeting and enhanced tumour uptake of [68Ga]Ga-NOTA-RGD-GE11 warrant its further investigation for dual integrin αVβ3 and EGFR-targeted tumour imaging.</abstract><cop>Oxford</cop><pub>Elsevier Inc</pub><doi>10.1016/j.nucmedbio.2018.11.003</doi><tpages>9</tpages></addata></record> |
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| subjects | Affinity Antibodies Binding Computed tomography EGFR Epidermal growth factor receptors Ga-68 Heterodimer peptide Imaging In vivo methods and tests Integrin αVβ3 Investigations Peptides PET imaging Positron emission Receptors Tomography Tumors |
| title | 68Ga-labelled NOTA-RGD-GE11 peptide for dual integrin and EGFR-targeted tumour imaging |
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