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Positron EmissionnTomography Imaging of NeurotensinnReceptor-Positive Tumors with 68Ga-Labeled Antagonists:nThe Chelate Makes the Difference Again 神经紧张素受体阳性肿瘤与&lt；sup>68</sup&gt； ga标记拮抗剂的正电子发射成像：螯合剂再次起作用

Figshare Pub Date : 2021-06-09 DOI: 10.1021/acs.jmedchem.1c00523.s003

Emma Renard (8212299), Mathieu Moreau (178352), Pierre-Simon Bellaye (3457178), Mélanie Guillemin (10948554), Bertrand Collin (6109697), Aurélie Prignon (3630916), Franck Denat (839548), Victor Goncalves (839547)

{"title":"Positron EmissionnTomography Imaging of NeurotensinnReceptor-Positive Tumors with 68Ga-Labeled Antagonists:nThe Chelate Makes the Difference Again","authors":"Emma Renard (8212299), Mathieu Moreau (178352), Pierre-Simon Bellaye (3457178), Mélanie Guillemin (10948554), Bertrand Collin (6109697), Aurélie Prignon (3630916), Franck Denat (839548), Victor Goncalves (839547)","doi":"10.1021/acs.jmedchem.1c00523.s003","DOIUrl":"https://doi.org/10.1021/acs.jmedchem.1c00523.s003","url":null,"abstract":"Neurotensin receptor 1 (NTS1) is involved in the developmentnand progression of numerous cancers, which makes it an interestingntarget for the development of diagnostic and therapeutic agents. Ansmall molecule NTS1 antagonist, named [177Lu]Lu-IPN01087,nis currently evaluated in phase I/II clinical trials for the targetedntherapy of neurotensin receptor-positive cancers. In this study, wensynthesized seven compounds based on the structure of NTS1 antagonists, bearing different chelating agents, and radiolabelednthem with gallium-68 for PET imaging. These compounds were evaluated in vitro and in vivo in mice bearing anHT-29 xenograft. The compound [68Ga]Ga-bisNODAGA-16 showed a promising biodistribution profile with mainlynsignal in tumor (4.917 ± 0.776%ID/g, 2 h post-injection). Itsnrapid clearance from healthy tissues led to high tumor-to-organ ratios,nresulting in highly contrasted PET images. These results were confirmednon subcutaneous xenografts of AsPC-1 tumor cells, a model of NTS1-positive human pancreatic adenocarcinoma.","PeriodicalId":522661,"journal":{"name":"Figshare","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-06-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147901254","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

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