Targeting integrin αvβ6 with gallium-68 tris (hydroxypyridinone) based PET probes
Expression of the cellular transmembrane receptor αvβ6 integrin is mostly restricted to malignant epithelial cells in a wide variety of carcinomas, including pancreatic and others derived from epithelial tissues. Thus, this protein is considered an attractive target for tumour imaging and therapy. T...
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| Veröffentlicht in: | Dalton transactions : an international journal of inorganic chemistry 2022-08, Vol.51 (34), p.12796-1283 |
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| container_title | Dalton transactions : an international journal of inorganic chemistry |
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| creator | Floresta, Giuseppe Memdouh, Siham Pham, Truc Ma, Michelle T Blower, Philip J Hider, Robert C Abbate, Vincenzo Cilibrizzi, Agostino |
| description | Expression of the cellular transmembrane receptor αvβ6 integrin is mostly restricted to malignant epithelial cells in a wide variety of carcinomas, including pancreatic and others derived from epithelial tissues. Thus, this protein is considered an attractive target for tumour imaging and therapy. Two different
68
Ga hexadentate tris (3,4-hydroxypyridinone) (THP) chelators were produced in this study and coupled to the αvβ6 integrin-selective peptide
cyclo
(FRGDLAFp(NMe)K)
via
NHS chemistry. Radiolabelling experiments confirmed a high radiochemical yield of the two PET probes. In addition, cellular binding studies showed high binding affinities in the nanomolar range. The two integrin αvβ6-peptide-THP synthesized and radiolabeled in this study will facilitate
in vivo
monitoring of transmembrane receptor αvβ6 integrin by using the advantage of THP chemistry for rapid, efficient and stable gallium chelation.
Two
68
Ga-radiolabeled integrin αvβ6-peptide-THPs to enable
in vivo
monitoring of the transmembrane receptor αvβ6 integrin, by taking advantage of THP chemistry for rapid, efficient and stable gallium chelation. |
| doi_str_mv | 10.1039/d2dt00980c |
| format | Article |
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68
Ga hexadentate tris (3,4-hydroxypyridinone) (THP) chelators were produced in this study and coupled to the αvβ6 integrin-selective peptide
cyclo
(FRGDLAFp(NMe)K)
via
NHS chemistry. Radiolabelling experiments confirmed a high radiochemical yield of the two PET probes. In addition, cellular binding studies showed high binding affinities in the nanomolar range. The two integrin αvβ6-peptide-THP synthesized and radiolabeled in this study will facilitate
in vivo
monitoring of transmembrane receptor αvβ6 integrin by using the advantage of THP chemistry for rapid, efficient and stable gallium chelation.
Two
68
Ga-radiolabeled integrin αvβ6-peptide-THPs to enable
in vivo
monitoring of the transmembrane receptor αvβ6 integrin, by taking advantage of THP chemistry for rapid, efficient and stable gallium chelation.</description><identifier>ISSN: 1477-9226</identifier><identifier>EISSN: 1477-9234</identifier><identifier>DOI: 10.1039/d2dt00980c</identifier><identifier>PMID: 35972045</identifier><language>eng</language><publisher>England: Royal Society of Chemistry</publisher><subject>Antigens, Neoplasm - metabolism ; Binding ; Chelating Agents ; Chelation ; Chemistry ; Epithelium ; Gallium isotopes ; Gallium Radioisotopes ; In vivo methods and tests ; Integrin alphaVbeta3 - metabolism ; Integrins ; Peptides - metabolism ; Positron-Emission Tomography - methods ; Radiochemistry ; Radiolabelling ; Receptors ; Tissue Distribution</subject><ispartof>Dalton transactions : an international journal of inorganic chemistry, 2022-08, Vol.51 (34), p.12796-1283</ispartof><rights>Copyright Royal Society of Chemistry 2022</rights><rights>This journal is © The Royal Society of Chemistry 2022 The Royal Society of Chemistry</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c343c-29db87dd97a0010b391885bbb3401298fe8fc2268826c4560f5b7c599e9d2ace3</citedby><cites>FETCH-LOGICAL-c343c-29db87dd97a0010b391885bbb3401298fe8fc2268826c4560f5b7c599e9d2ace3</cites><orcidid>0000-0002-0668-1260 ; 0000-0002-3300-0520 ; 0000-0001-6290-1590 ; 0000-0002-3349-7346 ; 0000-0003-4510-3639 ; 0000-0002-9711-5183</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>230,314,780,784,885,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/35972045$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Floresta, Giuseppe</creatorcontrib><creatorcontrib>Memdouh, Siham</creatorcontrib><creatorcontrib>Pham, Truc</creatorcontrib><creatorcontrib>Ma, Michelle T</creatorcontrib><creatorcontrib>Blower, Philip J</creatorcontrib><creatorcontrib>Hider, Robert C</creatorcontrib><creatorcontrib>Abbate, Vincenzo</creatorcontrib><creatorcontrib>Cilibrizzi, Agostino</creatorcontrib><title>Targeting integrin αvβ6 with gallium-68 tris (hydroxypyridinone) based PET probes</title><title>Dalton transactions : an international journal of inorganic chemistry</title><addtitle>Dalton Trans</addtitle><description>Expression of the cellular transmembrane receptor αvβ6 integrin is mostly restricted to malignant epithelial cells in a wide variety of carcinomas, including pancreatic and others derived from epithelial tissues. Thus, this protein is considered an attractive target for tumour imaging and therapy. Two different
68
Ga hexadentate tris (3,4-hydroxypyridinone) (THP) chelators were produced in this study and coupled to the αvβ6 integrin-selective peptide
cyclo
(FRGDLAFp(NMe)K)
via
NHS chemistry. Radiolabelling experiments confirmed a high radiochemical yield of the two PET probes. In addition, cellular binding studies showed high binding affinities in the nanomolar range. The two integrin αvβ6-peptide-THP synthesized and radiolabeled in this study will facilitate
in vivo
monitoring of transmembrane receptor αvβ6 integrin by using the advantage of THP chemistry for rapid, efficient and stable gallium chelation.
Two
68
Ga-radiolabeled integrin αvβ6-peptide-THPs to enable
in vivo
monitoring of the transmembrane receptor αvβ6 integrin, by taking advantage of THP chemistry for rapid, efficient and stable gallium chelation.</description><subject>Antigens, Neoplasm - metabolism</subject><subject>Binding</subject><subject>Chelating Agents</subject><subject>Chelation</subject><subject>Chemistry</subject><subject>Epithelium</subject><subject>Gallium isotopes</subject><subject>Gallium Radioisotopes</subject><subject>In vivo methods and tests</subject><subject>Integrin alphaVbeta3 - metabolism</subject><subject>Integrins</subject><subject>Peptides - metabolism</subject><subject>Positron-Emission Tomography - methods</subject><subject>Radiochemistry</subject><subject>Radiolabelling</subject><subject>Receptors</subject><subject>Tissue Distribution</subject><issn>1477-9226</issn><issn>1477-9234</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2022</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpVkUtLAzEUhYMovjfulYAbFUaTm3kkG0HqEwQF6zrkNdNIO1OTqdqfpT_E3-RoterqXjgf5x7uQWiLkkNKmDiyYFtCBCdmAa3StCgSASxdnO-Qr6C1GB8IASAZLKMVlokCSJqtoru-CpVrfV1hX7euCr7G769P7285fvbtAFdqOPSTUZJz3AYf8d5gakPzMh1Pg7e-bmq3j7WKzuLbsz4eh0a7uIGWSjWMbvN7rqP787N-7zK5vrm46p1cJ4alzCQgrOaFtaJQhFCimaCcZ1prlhIKgpeOl6YLzznkJs1yUma6MJkQTlhQxrF1dDzzHU_0yFnj6jaooRwHP1JhKhvl5X-l9gNZNU9SpJAVnHYGu98GoXmcuNjKh2YS6i6zhILmJAUO0FEHM8qEJsbgyvkFSuRnAfIUTvtfBfQ6eOdvpjn68_EO2J4BIZq5-tsg-wDSXIxB</recordid><startdate>20220830</startdate><enddate>20220830</enddate><creator>Floresta, Giuseppe</creator><creator>Memdouh, Siham</creator><creator>Pham, Truc</creator><creator>Ma, Michelle T</creator><creator>Blower, Philip J</creator><creator>Hider, Robert C</creator><creator>Abbate, Vincenzo</creator><creator>Cilibrizzi, Agostino</creator><general>Royal Society of Chemistry</general><general>The Royal Society of Chemistry</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7SR</scope><scope>7U5</scope><scope>8BQ</scope><scope>8FD</scope><scope>JG9</scope><scope>L7M</scope><scope>5PM</scope><orcidid>https://orcid.org/0000-0002-0668-1260</orcidid><orcidid>https://orcid.org/0000-0002-3300-0520</orcidid><orcidid>https://orcid.org/0000-0001-6290-1590</orcidid><orcidid>https://orcid.org/0000-0002-3349-7346</orcidid><orcidid>https://orcid.org/0000-0003-4510-3639</orcidid><orcidid>https://orcid.org/0000-0002-9711-5183</orcidid></search><sort><creationdate>20220830</creationdate><title>Targeting integrin αvβ6 with gallium-68 tris (hydroxypyridinone) based PET probes</title><author>Floresta, Giuseppe ; Memdouh, Siham ; Pham, Truc ; Ma, Michelle T ; Blower, Philip J ; Hider, Robert C ; Abbate, Vincenzo ; Cilibrizzi, Agostino</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c343c-29db87dd97a0010b391885bbb3401298fe8fc2268826c4560f5b7c599e9d2ace3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2022</creationdate><topic>Antigens, Neoplasm - metabolism</topic><topic>Binding</topic><topic>Chelating Agents</topic><topic>Chelation</topic><topic>Chemistry</topic><topic>Epithelium</topic><topic>Gallium isotopes</topic><topic>Gallium Radioisotopes</topic><topic>In vivo methods and tests</topic><topic>Integrin alphaVbeta3 - metabolism</topic><topic>Integrins</topic><topic>Peptides - metabolism</topic><topic>Positron-Emission Tomography - methods</topic><topic>Radiochemistry</topic><topic>Radiolabelling</topic><topic>Receptors</topic><topic>Tissue Distribution</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Floresta, Giuseppe</creatorcontrib><creatorcontrib>Memdouh, Siham</creatorcontrib><creatorcontrib>Pham, Truc</creatorcontrib><creatorcontrib>Ma, Michelle T</creatorcontrib><creatorcontrib>Blower, Philip J</creatorcontrib><creatorcontrib>Hider, Robert C</creatorcontrib><creatorcontrib>Abbate, Vincenzo</creatorcontrib><creatorcontrib>Cilibrizzi, Agostino</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Engineered Materials Abstracts</collection><collection>Solid State and Superconductivity Abstracts</collection><collection>METADEX</collection><collection>Technology Research Database</collection><collection>Materials Research Database</collection><collection>Advanced Technologies Database with Aerospace</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>Dalton transactions : an international journal of inorganic chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Floresta, Giuseppe</au><au>Memdouh, Siham</au><au>Pham, Truc</au><au>Ma, Michelle T</au><au>Blower, Philip J</au><au>Hider, Robert C</au><au>Abbate, Vincenzo</au><au>Cilibrizzi, Agostino</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Targeting integrin αvβ6 with gallium-68 tris (hydroxypyridinone) based PET probes</atitle><jtitle>Dalton transactions : an international journal of inorganic chemistry</jtitle><addtitle>Dalton Trans</addtitle><date>2022-08-30</date><risdate>2022</risdate><volume>51</volume><issue>34</issue><spage>12796</spage><epage>1283</epage><pages>12796-1283</pages><issn>1477-9226</issn><eissn>1477-9234</eissn><abstract>Expression of the cellular transmembrane receptor αvβ6 integrin is mostly restricted to malignant epithelial cells in a wide variety of carcinomas, including pancreatic and others derived from epithelial tissues. Thus, this protein is considered an attractive target for tumour imaging and therapy. Two different
68
Ga hexadentate tris (3,4-hydroxypyridinone) (THP) chelators were produced in this study and coupled to the αvβ6 integrin-selective peptide
cyclo
(FRGDLAFp(NMe)K)
via
NHS chemistry. Radiolabelling experiments confirmed a high radiochemical yield of the two PET probes. In addition, cellular binding studies showed high binding affinities in the nanomolar range. The two integrin αvβ6-peptide-THP synthesized and radiolabeled in this study will facilitate
in vivo
monitoring of transmembrane receptor αvβ6 integrin by using the advantage of THP chemistry for rapid, efficient and stable gallium chelation.
Two
68
Ga-radiolabeled integrin αvβ6-peptide-THPs to enable
in vivo
monitoring of the transmembrane receptor αvβ6 integrin, by taking advantage of THP chemistry for rapid, efficient and stable gallium chelation.</abstract><cop>England</cop><pub>Royal Society of Chemistry</pub><pmid>35972045</pmid><doi>10.1039/d2dt00980c</doi><tpages>8</tpages><orcidid>https://orcid.org/0000-0002-0668-1260</orcidid><orcidid>https://orcid.org/0000-0002-3300-0520</orcidid><orcidid>https://orcid.org/0000-0001-6290-1590</orcidid><orcidid>https://orcid.org/0000-0002-3349-7346</orcidid><orcidid>https://orcid.org/0000-0003-4510-3639</orcidid><orcidid>https://orcid.org/0000-0002-9711-5183</orcidid><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext |
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| ispartof | Dalton transactions : an international journal of inorganic chemistry, 2022-08, Vol.51 (34), p.12796-1283 |
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| language | eng |
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| source | MEDLINE; Royal Society Of Chemistry Journals 2008-; Alma/SFX Local Collection |
| subjects | Antigens, Neoplasm - metabolism Binding Chelating Agents Chelation Chemistry Epithelium Gallium isotopes Gallium Radioisotopes In vivo methods and tests Integrin alphaVbeta3 - metabolism Integrins Peptides - metabolism Positron-Emission Tomography - methods Radiochemistry Radiolabelling Receptors Tissue Distribution |
| title | Targeting integrin αvβ6 with gallium-68 tris (hydroxypyridinone) based PET probes |
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