{"entity": "researcher", "timestamp": "2026-08-20T20:46:42.213Z", "family": "Lundmark", "given": "Fanny", "initials": "F", "orcid": "0000-0002-9153-2832", "affiliations": ["Department of Medicinal Chemistry, Uppsala University, 751 83 Uppsala, Sweden."], "links": {"self": {"href": "https://publications-affiliated.scilifelab.se/researcher/c6690e6a499c48e98f5c7f6038bb463c.json"}, "display": {"href": "https://publications-affiliated.scilifelab.se/researcher/c6690e6a499c48e98f5c7f6038bb463c"}}, "publications": [{"entity": "publication", "iuid": "cfb53aa09f7b4a359bf70b8e34652e7f", "links": {"self": {"href": "https://publications-affiliated.scilifelab.se/publication/cfb53aa09f7b4a359bf70b8e34652e7f.json"}, "display": {"href": "https://publications-affiliated.scilifelab.se/publication/cfb53aa09f7b4a359bf70b8e34652e7f"}}, "title": "The GRPR Antagonist [99mTc]Tc-maSSS-PEG2-RM26 towards Phase I Clinical Trial: Kit Preparation, Characterization and Toxicity.", "authors": [{"family": "Abouzayed", "given": "Ayman", "initials": "A"}, {"family": "Borin", "given": "Jesper", "initials": "J"}, {"family": "Lundmark", "given": "Fanny", "initials": "F", "orcid": "0000-0002-9153-2832", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/c6690e6a499c48e98f5c7f6038bb463c.json"}}, {"family": "Rybina", "given": "Anastasiya", "initials": "A"}, {"family": "Hober", "given": "Sophia", "initials": "S", "orcid": "0000-0003-0605-8417", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/4a1bdfd8500c4dbea343132bc0d8e44c.json"}}, {"family": "Zelchan", "given": "Roman", "initials": "R"}, {"family": "Tolmachev", "given": "Vladimir", "initials": "V", "orcid": "0000-0002-6122-1734", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/896ae9fae8b74251afe11b4354c62794.json"}}, {"family": "Chernov", "given": "Vladimir", "initials": "V"}, {"family": "Orlova", "given": "Anna", "initials": "A", "orcid": "0000-0001-6120-2683", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/1c374f429702489494c05f84f298b4b7.json"}}], "type": "journal article", "published": "2023-05-02", "journal": {"title": "Diagnostics (Basel)", "issn": "2075-4418", "volume": "13", "issue": "9", "issn-l": null}, "abstract": "Gastrin-releasing peptide receptors (GRPRs) are overexpressed in the majority of primary prostate tumors and in prostatic lymph node and bone metastases. Several GRPR antagonists were developed for SPECT and PET imaging of prostate cancer. We previously reported a preclinical evaluation of the GRPR antagonist [99mTc]Tc-maSSS-PEG2-RM26 (based on [D-Phe6, Sta13, Leu14-NH2]BBN(6-14)) which bound to GRPR with high affinity and had a favorable biodistribution profile in tumor-bearing animal models. In this study, we aimed to prepare and test kits for prospective use in an early-phase clinical study. The kits were prepared to allow for a one-pot single-step radiolabeling with technetium-99m pertechnetate. The kit vials were tested for sterility and labeling efficacy. The radiolabeled by using the kit GRPR antagonist was evaluated in vitro for binding specificity to GRPR on PC-3 cells (GRPR-positive). In vivo, the toxicity of the kit constituents was evaluated in rats. The labeling efficacy of the kits stored at 4 \u00b0C was monitored for 18 months. The biological properties of [99mTc]Tc-maSSS-PEG2-RM26, which were obtained after this period, were examined both in vitro and in vivo. The one-pot (gluconic acid, ethylenediaminetetraacetic acid, stannous chloride, and maSSS-PEG2-RM26) single-step radiolabeling with technetium-99m was successful with high radiochemical yields (>97%) and high molar activities (16-24 MBq/nmol). The radiolabeled peptide maintained its binding properties to GRPR. The kit constituents were sterile and non-toxic when tested in living subjects. In conclusion, the prepared kit is considered safe in animal models and can be further evaluated for use in clinics.", "doi": "10.3390/diagnostics13091611", "pmid": "37175001", "labels": [], "xrefs": [{"db": "pmc", "key": "PMC10178091"}, {"db": "pii", "key": "diagnostics13091611"}], "notes": [], "created": "2026-08-20T13:40:30.341Z", "modified": "2026-08-20T13:40:30.454Z"}, {"entity": "publication", "iuid": "53a49c26113a49c7b81046171f734e46", "links": {"self": {"href": "https://publications-affiliated.scilifelab.se/publication/53a49c26113a49c7b81046171f734e46.json"}, "display": {"href": "https://publications-affiliated.scilifelab.se/publication/53a49c26113a49c7b81046171f734e46"}}, "title": "Heterodimeric Radiotracer Targeting PSMA and GRPR for Imaging of Prostate Cancer-Optimization of the Affinity towards PSMA by Linker Modification in Murine Model.", "authors": [{"family": "Lundmark", "given": "Fanny", "initials": "F", "orcid": "0000-0002-9153-2832", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/c6690e6a499c48e98f5c7f6038bb463c.json"}}, {"family": "Abouzayed", "given": "Ayman", "initials": "A"}, {"family": "Mitran", "given": "Bogdan", "initials": "B"}, {"family": "Rinne", "given": "Sara S", "initials": "SS"}, {"family": "Varasteh", "given": "Zohreh", "initials": "Z"}, {"family": "Larhed", "given": "Mats", "initials": "M", "orcid": "0000-0001-6258-0635", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/225695195abc4233bd141e6858e72e7f.json"}}, {"family": "Tolmachev", "given": "Vladimir", "initials": "V", "orcid": "0000-0002-6122-1734", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/896ae9fae8b74251afe11b4354c62794.json"}}, {"family": "Rosenstr\u00f6m", "given": "Ulrika", "initials": "U", "orcid": "0000-0002-0817-8140", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/ec6820fcb786475d85969630b0b3860b.json"}}, {"family": "Orlova", "given": "Anna", "initials": "A", "orcid": "0000-0001-6120-2683", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/1c374f429702489494c05f84f298b4b7.json"}}], "type": "journal article", "published": "2020-07-01", "journal": {"title": "Pharmaceutics", "issn": "1999-4923", "volume": "12", "issue": "7", "issn-l": null}, "abstract": "Prostate-specific membrane antigen (PSMA) and gastrin-releasing peptide receptor (GRPR) are promising targets for molecular imaging of prostate cancer (PCa) lesions. Due to the heterogenic overexpression of PSMA and GRPR in PCa, a heterodimeric radiotracer with the ability to bind to both targets could be beneficial. Recently, our group reported the novel heterodimer BQ7800 consisting of a urea-based PSMA inhibitor, the peptide-based GRPR antagonist RM26 and NOTA chelator. The study reported herein, aimed to improve the affinity of BQ7800 towards PSMA by changing the composition of the two linkers connecting the PSMA- and GRPR-targeting motifs. Three novel heterodimeric analogues were synthesized by incorporation of phenylalanine in the functional linker of the PSMA-binding motif and/or shortening the PEG-linker coupled to RM26. The heterodimers were labeled with indium-111 and evaluated in vitro. In the competitive binding assay, BQ7812, featuring phenylalanine and shorter PEG-linker, demonstrated a nine-fold improved affinity towards PSMA. In the in vivo biodistribution study of [111In]In-BQ7812 in PC3-pip tumor-bearing mice (PSMA and GRPR positive), the activity uptake was two-fold higher in the tumor and three-fold higher in kidneys than for [111In]In-BQ7800. Herein, we showed that the affinity of a bispecific PSMA/GRPR heterodimer towards PSMA could be improved by linker modification.", "doi": "10.3390/pharmaceutics12070614", "pmid": "32630176", "labels": [], "xrefs": [{"db": "pmc", "key": "PMC7408065"}, {"db": "pii", "key": "pharmaceutics12070614"}], "notes": [], "created": "2026-08-20T13:42:59.018Z", "modified": "2026-08-20T13:42:59.116Z"}]}