{"entity": "researcher", "timestamp": "2026-08-22T06:57:44.509Z", "family": "Rinne", "given": "Sara S", "initials": "SS", "orcid": "0000-0003-2141-3982", "affiliations": ["Department of Medicinal Chemistry, Uppsala University, 751 23 Uppsala, Sweden."], "links": {"self": {"href": "https://publications-affiliated.scilifelab.se/researcher/3aea3edd98b441c98bb527b1e0c911f5.json"}, "display": {"href": "https://publications-affiliated.scilifelab.se/researcher/3aea3edd98b441c98bb527b1e0c911f5"}}, "publications": [{"entity": "publication", "iuid": "d51c553d17cd4f96bfb300dc715cb1f3", "links": {"self": {"href": "https://publications-affiliated.scilifelab.se/publication/d51c553d17cd4f96bfb300dc715cb1f3.json"}, "display": {"href": "https://publications-affiliated.scilifelab.se/publication/d51c553d17cd4f96bfb300dc715cb1f3"}}, "title": "Phase I Trial of [99mTc]Tc-maSSS-PEG2-RM26, a Bombesin Analogue Antagonistic to Gastrin-Releasing Peptide Receptors (GRPRs), for SPECT Imaging of GRPR Expression in Malignant Tumors.", "authors": [{"family": "Chernov", "given": "Vladimir", "initials": "V"}, {"family": "Rybina", "given": "Anastasiya", "initials": "A"}, {"family": "Zelchan", "given": "Roman", "initials": "R"}, {"family": "Medvedeva", "given": "Anna", "initials": "A"}, {"family": "Bragina", "given": "Olga", "initials": "O"}, {"family": "Lushnikova", "given": "Nadejda", "initials": "N"}, {"family": "Doroshenko", "given": "Artem", "initials": "A"}, {"family": "Usynin", "given": "Evgeniy", "initials": "E"}, {"family": "Tashireva", "given": "Liubov", "initials": "L", "orcid": "0000-0003-2061-8417", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/e462c38bfd8846588156097b5602341a.json"}}, {"family": "Vtorushin", "given": "Sergey", "initials": "S"}, {"family": "Abouzayed", "given": "Ayman", "initials": "A"}, {"family": "Rinne", "given": "Sara S", "initials": "SS", "orcid": "0000-0003-2141-3982", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/3aea3edd98b441c98bb527b1e0c911f5.json"}}, {"family": "S\u00f6rensen", "given": "Jens", "initials": "J"}, {"family": "Tolmachev", "given": "Vladimir", "initials": "V", "orcid": "0000-0002-6122-1734", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/896ae9fae8b74251afe11b4354c62794.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": "2023-03-07", "journal": {"title": "Cancers (Basel)", "issn": "2072-6694", "volume": "15", "issue": "6", "issn-l": "2072-6694"}, "abstract": "The gastrin-releasing peptide receptor (GRPR) is overexpressed in prostate cancer (PCa) and in hormone-driven breast cancer (BCa). The aim of this phase I clinical trial was to evaluate safety, biodistribution, and dosimetry after the administration of the recently developed GRPR-targeting antagonistic bombesin analogue [99mTc]Tc-maSSS-PEG2-RM26 in PCa and BCa patients. Planar and whole-body SPECT/CT imaging was performed in six PCa patients and seven BCa patients 2, 4, 6, and 24 h post the intravenous administration of 40 \u00b5g of [99mTc]Tc-maSSS-PEG2-RM26 (600-700 MBq). No adverse events or pathological changes were observed. The rapid blood clearance of [99mTc]Tc-maSSS-PEG2-RM26 was observed with predominantly hepatobiliary excretion. The effective doses were 0.0053 \u00b1 0.0007 for male patients and 0.008 \u00b1 0.003 mSv/MBq for female patients. The accumulation of [99mTc]Tc-maSSS-PEG2-RM26 in tumors was observed in four out of six PCa and in seven out of seven BCa patients. In four BCa patients, a high uptake of the agent into the axillary lymph nodes was detected. Immunohistochemistry revealed positive GRPR expression in 60% of primary PCa, 71.4% of BCa tumors, and 50% of examined BCa lymph nodes. In conclusion, a single administration of [99mTc]Tc-maSSS-PEG2-RM26 was safe and well tolerated. [99mTc]Tc-maSSS-PEG2-RM26 SPECT may be useful for tumor detection in PCa and BCa patients, pending further studies.", "doi": "10.3390/cancers15061631", "pmid": "36980517", "labels": [], "xrefs": [{"db": "pmc", "key": "PMC10046460"}, {"db": "pii", "key": "cancers15061631"}], "notes": [], "created": "2026-08-21T13:01:52.506Z", "modified": "2026-08-21T13:01:52.564Z"}, {"entity": "publication", "iuid": "4141afd0a66b44d183c7467bdf4893e1", "links": {"self": {"href": "https://publications-affiliated.scilifelab.se/publication/4141afd0a66b44d183c7467bdf4893e1.json"}, "display": {"href": "https://publications-affiliated.scilifelab.se/publication/4141afd0a66b44d183c7467bdf4893e1"}}, "title": "Feasibility of Co-Targeting HER3 and EpCAM Using Seribantumab and DARPin-Toxin Fusion in a Pancreatic Cancer Xenograft Model.", "authors": [{"family": "Xu", "given": "Tianqi", "initials": "T", "orcid": "0000-0002-1826-4093", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/688f685bf3474e72bfab58e1fa2035b9.json"}}, {"family": "Schulga", "given": "Alexey", "initials": "A", "orcid": "0000-0003-3425-0828", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/45b1c8e5447c41bbb93e61706377a0c7.json"}}, {"family": "Konovalova", "given": "Elena", "initials": "E"}, {"family": "Rinne", "given": "Sara S", "initials": "SS", "orcid": "0000-0003-2141-3982", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/3aea3edd98b441c98bb527b1e0c911f5.json"}}, {"family": "Zhang", "given": "Hongchao", "initials": "H"}, {"family": "Vorontsova", "given": "Olga", "initials": "O"}, {"family": "Orlova", "given": "Anna", "initials": "A", "orcid": "0000-0001-6120-2683", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/1c374f429702489494c05f84f298b4b7.json"}}, {"family": "Deyev", "given": "Sergey M", "initials": "SM", "orcid": "0000-0002-3952-0631", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/fb88df2aaa8a46a5957370b9258e2834.json"}}, {"family": "Tolmachev", "given": "Vladimir", "initials": "V", "orcid": "0000-0002-6122-1734", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/896ae9fae8b74251afe11b4354c62794.json"}}, {"family": "Vorobyeva", "given": "Anzhelika", "initials": "A", "orcid": "0000-0002-4778-3909", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/99703faa11ab4c19aff2f426f61c3134.json"}}], "type": "journal article", "published": "2023-02-02", "journal": {"title": "Int J Mol Sci", "issn": "1422-0067", "volume": "24", "issue": "3", "issn-l": null}, "abstract": "Pancreatic cancer (PC) is one of the most aggressive malignancies. A combination of targeted therapies could increase the therapeutic efficacy in tumors with heterogeneous target expression. Overexpression of the human epidermal growth factor receptor type 3 (HER3) and the epithelial cell adhesion molecule (EpCAM) in up to 40% and 30% of PCs, respectively, is associated with poor prognosis and highlights the relevance of these targets. Designed ankyrin repeat protein (DARPin) Ec1 fused with the low immunogenic bacterial toxin LoPE provides specific and potent cytotoxicity against EpCAM-expressing cancer cells. Here, we investigated whether the co-targeting of HER3 using the monoclonal antibody seribantumab (MM-121) and of EpCAM using Ec1-LoPE would improve the therapeutic efficacy in comparison to the individual agents. Radiolabeled 99mTc(CO)3-Ec1-LoPE showed specific binding with rapid internalization in EpCAM-expressing PC cells. MM-121 did not interfere with the binding of Ec1-LoPE to EpCAM. Evaluation of cytotoxicity indicated synergism between Ec1-LoPE and MM-121 in vitro. An experimental therapy study using Ec1-LoPE and MM-121 in mice bearing EpCAM- and HER3-expressing BxPC3 xenografts demonstrated the feasibility of the therapy. Further development of the co-targeting approach using HER3 and EpCAM could therefore be justified.", "doi": "10.3390/ijms24032838", "pmid": "36769161", "labels": [], "xrefs": [{"db": "pmc", "key": "PMC9917732"}, {"db": "pii", "key": "ijms24032838"}], "notes": [], "created": "2026-08-21T13:03:41.482Z", "modified": "2026-08-21T13:03:41.558Z"}, {"entity": "publication", "iuid": "1852cc0e29424ee29e476c7454700498", "links": {"self": {"href": "https://publications-affiliated.scilifelab.se/publication/1852cc0e29424ee29e476c7454700498.json"}, "display": {"href": "https://publications-affiliated.scilifelab.se/publication/1852cc0e29424ee29e476c7454700498"}}, "title": "Preclinical Characterisation of PSMA/GRPR-Targeting Heterodimer [68Ga]Ga-BQ7812 for PET Diagnostic Imaging of Prostate Cancer: A Step towards Clinical Translation.", "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": "Rinne", "given": "Sara S", "initials": "SS", "orcid": "0000-0003-2141-3982", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/3aea3edd98b441c98bb527b1e0c911f5.json"}}, {"family": "Timofeev", "given": "Vasiliy", "initials": "V"}, {"family": "Sipkina", "given": "Nadezhda", "initials": "N"}, {"family": "Naan", "given": "Maria", "initials": "M"}, {"family": "Kirichenko", "given": "Anastasia", "initials": "A"}, {"family": "Vasyutina", "given": "Maria", "initials": "M"}, {"family": "Ryzhkova", "given": "Daria", "initials": "D"}, {"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": "2023-01-10", "journal": {"title": "Cancers (Basel)", "issn": "2072-6694", "volume": "15", "issue": "2", "issn-l": "2072-6694"}, "abstract": "The development of radioligands targeting prostate-specific membrane antigen (PSMA) and gastrin-releasing peptide receptor (GRPR) has shown promising results for the imaging and therapy of prostate cancer. However, studies have shown that tumors and metastases can express such targets heterogeneously. To overcome this issue and to improve protein binding, radioligands with the ability to bind both PSMA and GRPR have been developed. Herein, we present the preclinical characterization of [68Ga]Ga-BQ7812; a PSMA/GRPR-targeting radioligand for the diagnostic PET imaging of prostate cancer. This study aimed to evaluate [68Ga]Ga-BQ7812 to promote the translation of such imaging probes into the clinic. [68Ga]Ga-BQ7812 demonstrated rapid and specific binding to both targets in a PSMA/GRPR-expressing PC3-pip cell line. Results from the biodistribution study in PC3-pip xenografted mice showed specific binding to both targets, with the highest activity uptake at 1 h pi in tumor (PSMA+/GRPR+, 10.4 \u00b1 1.0% IA/g), kidneys (PSMA+, 45 \u00b1 16% IA/g), and pancreas (GRPR+, 5.6 \u00b1 0.7% IA/g). At 3h pi, increased tumour-to-organ ratios could be seen due to higher retention in the tumor compared with other PSMA or GRPR-expressing organs. These results, together with low toxicity and an acceptable estimated dosimetry profile (total effective dose = 0.0083 mSv/MBq), support the clinical translation of [68Ga]Ga-BQ7812 and represent a step towards its first clinical trial.", "doi": "10.3390/cancers15020442", "pmid": "36672390", "labels": [], "xrefs": [{"db": "pmc", "key": "PMC9856709"}, {"db": "pii", "key": "cancers15020442"}], "notes": [], "created": "2026-08-21T13:01:49.532Z", "modified": "2026-08-21T13:01:49.611Z"}, {"entity": "publication", "iuid": "5f65ced79c3b40ea96ee5e9e78ca4d73", "links": {"self": {"href": "https://publications-affiliated.scilifelab.se/publication/5f65ced79c3b40ea96ee5e9e78ca4d73.json"}, "display": {"href": "https://publications-affiliated.scilifelab.se/publication/5f65ced79c3b40ea96ee5e9e78ca4d73"}}, "title": "Targeting Tumor Cells Overexpressing the Human Epidermal Growth Factor Receptor 3 with Potent Drug Conjugates Based on Affibody Molecules.", "authors": [{"family": "Rinne", "given": "Sara S", "initials": "SS", "orcid": "0000-0003-2141-3982", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/3aea3edd98b441c98bb527b1e0c911f5.json"}}, {"family": "Yin", "given": "Wen", "initials": "W"}, {"family": "Borras", "given": "Anna Mestre", "initials": "AM"}, {"family": "Abouzayed", "given": "Ayman", "initials": "A"}, {"family": "Leitao", "given": "Charles Dahlsson", "initials": "CD"}, {"family": "Vorobyeva", "given": "Anzhelika", "initials": "A", "orcid": "0000-0002-4778-3909", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/99703faa11ab4c19aff2f426f61c3134.json"}}, {"family": "L\u00f6fblom", "given": "John", "initials": "J", "orcid": "0000-0001-9423-0541", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/bf8479d43c1c45efb85ba0c0da634aeb.json"}}, {"family": "St\u00e5hl", "given": "Stefan", "initials": "S"}, {"family": "Orlova", "given": "Anna", "initials": "A", "orcid": "0000-0001-6120-2683", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/1c374f429702489494c05f84f298b4b7.json"}}, {"family": "Gr\u00e4slund", "given": "Torbj\u00f6rn", "initials": "T", "orcid": "0000-0002-5391-600X", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/afff2431691348539334ab0e86158505.json"}}], "type": "journal article", "published": "2022-05-31", "journal": {"title": "Biomedicines", "issn": "2227-9059", "volume": "10", "issue": "6", "issn-l": null}, "abstract": "Increasing evidence suggests that therapy targeting the human epidermal growth factor receptor 3 (HER3) could be a viable route for targeted cancer therapy. Here, we studied a novel drug conjugate, ZHER3-ABD-mcDM1, consisting of a HER3-targeting affibody molecule, coupled to the cytotoxic tubulin polymerization inhibitor DM1, and an albumin-binding domain for in vivo half-life extension. ZHER3-ABD-mcDM1 showed a strong affinity to the extracellular domain of HER3 (KD 6 nM), and an even stronger affinity (KD 0.2 nM) to the HER3-overexpressing pancreatic carcinoma cell line, BxPC-3. The drug conjugate showed a potent cytotoxic effect on BxPC-3 cells with an IC50 value of 7 nM. Evaluation of a radiolabeled version, [99mTc]Tc-ZHER3-ABD-mcDM1, showed a relatively high rate of internalization, with a 27% internalized fraction after 8 h. Further in vivo evaluation showed that it could target BxPC-3 (pancreatic carcinoma) and DU145 (prostate carcinoma) xenografts in mice, with an uptake peaking at 6.3 \u00b1 0.4% IA/g at 6 h post-injection for the BxPC-3 xenografts. The general biodistribution showed uptake in the liver, lung, salivary gland, stomach, and small intestine, organs known to express murine ErbB3 naturally. The results from the study show that ZHER3-ABD-mcDM1 is a highly potent and selective drug conjugate with the ability to specifically target HER3 overexpressing cells. Further pre-clinical and clinical development is discussed.", "doi": "10.3390/biomedicines10061293", "pmid": "35740315", "labels": [], "xrefs": [{"db": "pmc", "key": "PMC9219639"}, {"db": "pii", "key": "biomedicines10061293"}], "notes": [], "created": "2026-08-21T13:01:13.994Z", "modified": "2026-08-21T13:01:14.186Z"}, {"entity": "publication", "iuid": "902371870cc242af89bd143bb81d8aa3", "links": {"self": {"href": "https://publications-affiliated.scilifelab.se/publication/902371870cc242af89bd143bb81d8aa3.json"}, "display": {"href": "https://publications-affiliated.scilifelab.se/publication/902371870cc242af89bd143bb81d8aa3"}}, "title": "Design, Synthesis, and Evaluation of Linker-Optimised PSMA-Targeting Radioligands.", "authors": [{"family": "Lundmark", "given": "Fanny", "initials": "F", "orcid": "0000-0002-9153-2832", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/c6690e6a499c48e98f5c7f6038bb463c.json"}}, {"family": "Olanders", "given": "Gustav", "initials": "G"}, {"family": "Rinne", "given": "Sara Sophie", "initials": "SS", "orcid": "0000-0003-2141-3982", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/3aea3edd98b441c98bb527b1e0c911f5.json"}}, {"family": "Abouzayed", "given": "Ayman", "initials": "A"}, {"family": "Orlova", "given": "Anna", "initials": "A", "orcid": "0000-0001-6120-2683", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/1c374f429702489494c05f84f298b4b7.json"}}, {"family": "Rosenstr\u00f6m", "given": "Ulrika", "initials": "U", "orcid": "0000-0002-0817-8140", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/ec6820fcb786475d85969630b0b3860b.json"}}], "type": "journal article", "published": "2022-05-20", "journal": {"title": "Pharmaceutics", "issn": "1999-4923", "volume": "14", "issue": "5", "issn-l": null}, "abstract": "Prostate-specific membrane antigen (PSMA) is overexpressed in the majority of prostate cancer cells and is considered to be an important target for the molecular imaging and therapy of prostate cancer. Herein, we present the design, synthesis, and evaluation of 11 PSMA-binding radioligands with modified linker structures, focusing on the relationship between molecular structure and targeting properties. The linker design was based on 2-naphthyl-L-alanine-tranexamic acid, the linker structure of PSMA-617. X-ray crystal-structure analysis of PSMA and structure-based design were used to generate the linker modifications, suggesting that substitution of tranexamic acid could lead to interactions with Phe546, Trp541, and Arg43 within the binding cavity. After synthesis through SPPS, analogues were labelled with indium-111 and evaluated in vitro for their specific binding, affinity, and cellular retention. Selected compounds were further evaluated in vivo in PSMA-expressing tumour-bearing mice. Based on the results, 2-naphthyl-L-alanine appears to be crucial for good targeting properties, whereas tranexamic acid could be replaced by other substituents. [111In]In-BQ7859, consisting of a 2-naphthyl-L-alanine-L-tyrosine linker, demonstrated favourable targeting properties. The substitution of tranexamic acid for L-tyrosine in the linker led to an improved tumour-to-blood ratio, highlighting [111In]In-BQ7859 as a promising PSMA-targeting radioligand.", "doi": "10.3390/pharmaceutics14051098", "pmid": "35631684", "labels": [], "xrefs": [{"db": "pmc", "key": "PMC9147442"}, {"db": "pii", "key": "pharmaceutics14051098"}], "notes": [], "created": "2026-08-21T13:04:57.129Z", "modified": "2026-08-21T13:04:57.201Z"}, {"entity": "publication", "iuid": "c79424bdacc14f898c66b0a94fcae8c8", "links": {"self": {"href": "https://publications-affiliated.scilifelab.se/publication/c79424bdacc14f898c66b0a94fcae8c8.json"}, "display": {"href": "https://publications-affiliated.scilifelab.se/publication/c79424bdacc14f898c66b0a94fcae8c8"}}, "title": "HER3 PET Imaging: 68Ga-Labeled Affibody Molecules Provide Superior HER3 Contrast to 89Zr-Labeled Antibody and Antibody-Fragment-Based Tracers.", "authors": [{"family": "Rinne", "given": "Sara S", "initials": "SS", "orcid": "0000-0003-2141-3982", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/3aea3edd98b441c98bb527b1e0c911f5.json"}}, {"family": "Leitao", "given": "Charles Dahlsson", "initials": "CD"}, {"family": "Abouzayed", "given": "Ayman", "initials": "A"}, {"family": "Vorobyeva", "given": "Anzhelika", "initials": "A", "orcid": "0000-0002-4778-3909", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/99703faa11ab4c19aff2f426f61c3134.json"}}, {"family": "Tolmachev", "given": "Vladimir", "initials": "V", "orcid": "0000-0002-6122-1734", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/896ae9fae8b74251afe11b4354c62794.json"}}, {"family": "St\u00e5hl", "given": "Stefan", "initials": "S"}, {"family": "L\u00f6fblom", "given": "John", "initials": "J", "orcid": "0000-0001-9423-0541", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/bf8479d43c1c45efb85ba0c0da634aeb.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": "2021-09-24", "journal": {"title": "Cancers (Basel)", "issn": "2072-6694", "volume": "13", "issue": "19", "issn-l": "2072-6694"}, "abstract": "HER3 (human epidermal growth factor receptor type 3) is a challenging target for diagnostic radionuclide molecular imaging due to the relatively modest overexpression in tumors and substantial expression in healthy organs. In this study, we compared four HER3-targeting PET tracers based on different types of targeting molecules in a preclinical model: the 89Zr-labeled therapeutic antibody seribantumab, a seribantumab-derived F(ab)2-fragment labeled with 89Zr and 68Ga, and the 68Ga-labeled affibody molecule [68Ga]Ga-ZHER3. The novel conjugates were radiolabeled and characterized in vitro using HER3-expressing BxPC-3 and DU145 human cancer cells. Biodistribution was studied using Balb/c nu/nu mice bearing BxPC-3 xenografts. HER3-negative RAMOS xenografts were used to demonstrate binding specificity in vivo. Autoradiography was conducted on the excised tumors. nanoPET/CT imaging was performed. New conjugates specifically bound to HER3 in vitro and in vivo. [68Ga]Ga-DFO-seribantumab-F(ab')2 was considered unsuitable for imaging due to the low stability and high uptake in normal organs. The highest tumor-to-non-tumor contrast with [89Zr]Zr-DFO-seribantumab and [89Zr]Zr-DFO-seribantumab-F(ab')2 was achieved at 96 h and 48 h pi, respectively. Despite lower tumor uptake, [68Ga]Ga-ZHER3 provided the best imaging contrast due to the fastest clearance from blood and normal organs. The results of our study suggest that affibody-based tracers are more suitable for PET imaging of HER3 expression than antibody- and antibody-fragment-based tracers.", "doi": "10.3390/cancers13194791", "pmid": "34638277", "labels": [], "xrefs": [{"db": "pmc", "key": "PMC8508546"}, {"db": "pii", "key": "cancers13194791"}], "notes": [], "created": "2026-08-21T13:01:47.341Z", "modified": "2026-08-21T13:01:47.376Z"}, {"entity": "publication", "iuid": "f34c53feced64382a61689e6e503325f", "links": {"self": {"href": "https://publications-affiliated.scilifelab.se/publication/f34c53feced64382a61689e6e503325f.json"}, "display": {"href": "https://publications-affiliated.scilifelab.se/publication/f34c53feced64382a61689e6e503325f"}}, "title": "Influence of the Position and Composition of Radiometals and Radioiodine Labels on Imaging of Epcam Expression in Prostate Cancer Model Using the DARPin Ec1.", "authors": [{"family": "Deyev", "given": "Sergey M", "initials": "SM", "orcid": "0000-0002-3952-0631", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/fb88df2aaa8a46a5957370b9258e2834.json"}}, {"family": "Xu", "given": "Tianqi", "initials": "T", "orcid": "0000-0002-1826-4093", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/688f685bf3474e72bfab58e1fa2035b9.json"}}, {"family": "Liu", "given": "Yongsheng", "initials": "Y", "orcid": "0000-0001-5871-5779", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/a53363bbcb5b414681ee46ac22b65230.json"}}, {"family": "Schulga", "given": "Alexey", "initials": "A", "orcid": "0000-0003-3425-0828", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/45b1c8e5447c41bbb93e61706377a0c7.json"}}, {"family": "Konovalova", "given": "Elena", "initials": "E"}, {"family": "Garousi", "given": "Javad", "initials": "J"}, {"family": "Rinne", "given": "Sara S", "initials": "SS", "orcid": "0000-0003-2141-3982", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/3aea3edd98b441c98bb527b1e0c911f5.json"}}, {"family": "Larkina", "given": "Maria", "initials": "M", "orcid": "0000-0003-1176-2441", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/557c8a9c8b2142a7a88d6211335d24e4.json"}}, {"family": "Ding", "given": "Haozhong", "initials": "H", "orcid": "0000-0003-1093-8222", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/3ee6fb5a9b694c1d8a40cc41e9d16146.json"}}, {"family": "Gr\u00e4slund", "given": "Torbj\u00f6rn", "initials": "T", "orcid": "0000-0002-5391-600X", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/afff2431691348539334ab0e86158505.json"}}, {"family": "Orlova", "given": "Anna", "initials": "A", "orcid": "0000-0001-6120-2683", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/1c374f429702489494c05f84f298b4b7.json"}}, {"family": "Tolmachev", "given": "Vladimir", "initials": "V", "orcid": "0000-0002-6122-1734", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/896ae9fae8b74251afe11b4354c62794.json"}}, {"family": "Vorobyeva", "given": "Anzhelika", "initials": "A", "orcid": "0000-0002-4778-3909", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/99703faa11ab4c19aff2f426f61c3134.json"}}], "type": "journal article", "published": "2021-07-17", "journal": {"title": "Cancers (Basel)", "issn": "2072-6694", "volume": "13", "issue": "14", "issn-l": "2072-6694"}, "abstract": "The epithelial cell adhesion molecule (EpCAM) is intensively overexpressed in 40-60% of prostate cancer (PCa) cases and can be used as a target for the delivery of drugs and toxins. The designed ankyrin repeat protein (DARPin) Ec1 has a high affinity to EpCAM (68 pM) and a small size (18 kDa). Radiolabeled Ec1 might be used as a companion diagnostic for the selection of PCa patients for therapy. The study aimed to investigate the influence of radiolabel position (N- or C-terminal) and composition on the targeting and imaging properties of Ec1. Two variants, having an N- or C-terminal cysteine, were produced, site-specifically conjugated to a DOTA chelator and labeled with cobalt-57, gallium-68 or indium-111. Site-specific radioiodination was performed using ((4-hydroxyphenyl)-ethyl)maleimide (HPEM). Biodistribution of eight radiolabeled Ec1-probes was measured in nude mice bearing PCa DU145 xenografts. In all cases, positioning of a label at the C-terminus provided the best tumor-to-organ ratios. The non-residualizing [125I]I-HPEM label provided the highest tumor-to-muscle and tumor-to-bone ratios and is more suitable for EpCAM imaging in early-stage PCa. Among the radiometals, indium-111 provided the highest tumor-to-blood, tumor-to-lung and tumor-to-liver ratios and could be used at late-stage PCa. In conclusion, label position and composition are important for the DARPin Ec1.", "doi": "10.3390/cancers13143589", "pmid": "34298801", "labels": [], "xrefs": [{"db": "pmc", "key": "PMC8304184"}, {"db": "pii", "key": "cancers13143589"}], "notes": [], "created": "2026-08-21T13:01:42.532Z", "modified": "2026-08-21T13:01:42.881Z"}, {"entity": "publication", "iuid": "d5d154bc13a24a57b39fbd903f6d2e4b", "links": {"self": {"href": "https://publications-affiliated.scilifelab.se/publication/d5d154bc13a24a57b39fbd903f6d2e4b.json"}, "display": {"href": "https://publications-affiliated.scilifelab.se/publication/d5d154bc13a24a57b39fbd903f6d2e4b"}}, "title": "PET and SPECT Imaging of the EGFR Family (RTK Class I) in Oncology.", "authors": [{"family": "Rinne", "given": "Sara S", "initials": "SS", "orcid": "0000-0003-2141-3982", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/3aea3edd98b441c98bb527b1e0c911f5.json"}}, {"family": "Orlova", "given": "Anna", "initials": "A", "orcid": "0000-0001-6120-2683", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/1c374f429702489494c05f84f298b4b7.json"}}, {"family": "Tolmachev", "given": "Vladimir", "initials": "V", "orcid": "0000-0002-6122-1734", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/896ae9fae8b74251afe11b4354c62794.json"}}], "type": "journal article", "published": "2021-04-01", "journal": {"title": "Int J Mol Sci", "issn": "1422-0067", "volume": "22", "issue": "7", "issn-l": null}, "abstract": "The human epidermal growth factor receptor family (EGFR-family, other designations: HER family, RTK Class I) is strongly linked to oncogenic transformation. Its members are frequently overexpressed in cancer and have become attractive targets for cancer therapy. To ensure effective patient care, potential responders to HER-targeted therapy need to be identified. Radionuclide molecular imaging can be a key asset for the detection of overexpression of EGFR-family members. It meets the need for repeatable whole-body assessment of the molecular disease profile, solving problems of heterogeneity and expression alterations over time. Tracer development is a multifactorial process. The optimal tracer design depends on the application and the particular challenges of the molecular target (target expression in tumors, endogenous expression in healthy tissue, accessibility). We have herein summarized the recent preclinical and clinical data on agents for Positron Emission Tomography (PET) and Single Photon Emission Tomography (SPECT) imaging of EGFR-family receptors in oncology. Antibody-based tracers are still extensively investigated. However, their dominance starts to be challenged by a number of tracers based on different classes of targeting proteins. Among these, engineered scaffold proteins (ESP) and single domain antibodies (sdAb) show highly encouraging results in clinical studies marking a noticeable trend towards the use of smaller sized agents for HER imaging.", "doi": "10.3390/ijms22073663", "pmid": "33915894", "labels": [], "xrefs": [{"db": "pmc", "key": "PMC8036874"}, {"db": "pii", "key": "ijms22073663"}], "notes": [], "created": "2026-08-21T13:03:18.625Z", "modified": "2026-08-21T13:03:18.688Z"}, {"entity": "publication", "iuid": "7c4c340c7b2248789c648fbbb1c2ef0e", "links": {"self": {"href": "https://publications-affiliated.scilifelab.se/publication/7c4c340c7b2248789c648fbbb1c2ef0e.json"}, "display": {"href": "https://publications-affiliated.scilifelab.se/publication/7c4c340c7b2248789c648fbbb1c2ef0e"}}, "title": "Preclinical Evaluation of the Copper-64 Labeled GRPR-Antagonist RM26 in Comparison with the Cobalt-55 Labeled Counterpart for PET-Imaging of Prostate Cancer.", "authors": [{"family": "Baun", "given": "Christina", "initials": "C", "orcid": "0000-0002-5199-9200", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/484f3234a1a143c38b832f22c73d1d59.json"}}, {"family": "Mitran", "given": "Bogdan", "initials": "B"}, {"family": "Rinne", "given": "Sara S", "initials": "SS", "orcid": "0000-0003-2141-3982", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/3aea3edd98b441c98bb527b1e0c911f5.json"}}, {"family": "Dam", "given": "Johan H", "initials": "JH", "orcid": "0000-0001-6577-7011", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/8495e80a9bd54345a3d18eaf987f9dd5.json"}}, {"family": "Olsen", "given": "Birgitte B", "initials": "BB", "orcid": "0000-0002-6130-0387", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/883bae2a831c459ea60c589df0eb2d4d.json"}}, {"family": "Tolmachev", "given": "Vladimir", "initials": "V", "orcid": "0000-0002-6122-1734", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/896ae9fae8b74251afe11b4354c62794.json"}}, {"family": "Orlova", "given": "Anna", "initials": "A", "orcid": "0000-0001-6120-2683", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/1c374f429702489494c05f84f298b4b7.json"}}, {"family": "Thisgaard", "given": "Helge", "initials": "H", "orcid": "0000-0001-9492-448X", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/43de528e1e1d415bbd9fc1dc5a4285e6.json"}}], "type": "comparative study", "published": "2020-12-18", "journal": {"title": "Molecules", "issn": "1420-3049", "volume": "25", "issue": "24", "issn-l": "1420-3049"}, "abstract": "Gastrin-releasing peptide receptor (GRPR) is overexpressed in the majority of prostate cancers. This study aimed to investigate the potential of 64Cu (radionuclide for late time-point PET-imaging) for imaging of GRPR expression using NOTA-PEG2-RM26 and NODAGA-PEG2-RM26. Methods: NOTA/NODAGA-PEG2-RM26 were labeled with 64Cu and evaluated in GRPR-expressing PC-3 cells. Biodistribution of [64Cu]Cu-NOTA/NODAGA-PEG2-RM26 was studied in PC-3 xenografted mice and compared to the biodistribution of [57Co]Co-NOTA/NODAGA-PEG2-RM26 at 3 and 24 h p.i. Preclinical PET/CT imaging was performed in tumor-bearing mice. NOTA/NODAGA-PEG2-RM26 were stably labeled with 64Cu with quantitative yields. In vitro, binding of [64Cu]Cu-NOTA/NODAGA-PEG2-RM26 was rapid and GRPR-specific with slow internalization. In vivo, [64Cu]Cu-NOTA/NODAGA-PEG2-RM26 bound specifically to GRPR-expressing tumors with fast clearance from blood and normal organs and displayed generally comparable biodistribution profiles to [57Co]Co-NOTA/NODAGA-PEG2-RM26; tumor uptake exceeded normal tissue uptake 3 h p.i.. Tumor-to-organ ratios did not increase significantly with time. [64Cu]Cu-NOTA-PEG2-RM26 had a significantly higher liver and pancreas uptake compared to other agents. 57Co-labeled radioconjugates showed overall higher tumor-to-non-tumor ratios, compared to the 64Cu-labeled counterparts. [64Cu]Cu-NOTA/NODAGA-PEG2-RM26 was able to visualize GRPR-expression in a murine PC model using PET. However, [55/57Co]Co-NOTA/NODAGA-PEG2-RM26 provided better in vivo stability and overall higher tumor-to-non-tumor ratios compared with the 64Cu-labeled conjugates.", "doi": "10.3390/molecules25245993", "pmid": "33352838", "labels": [], "xrefs": [{"db": "pmc", "key": "PMC7766840"}, {"db": "pii", "key": "molecules25245993"}], "notes": [], "created": "2026-08-21T13:04:26.638Z", "modified": "2026-08-21T13:04:26.801Z"}, {"entity": "publication", "iuid": "14b8414b3f7f49fa83b23efa0275f562", "links": {"self": {"href": "https://publications-affiliated.scilifelab.se/publication/14b8414b3f7f49fa83b23efa0275f562.json"}, "display": {"href": "https://publications-affiliated.scilifelab.se/publication/14b8414b3f7f49fa83b23efa0275f562"}}, "title": "Preclinical Evaluation of the GRPR-Targeting Antagonist RM26 Conjugated to the Albumin-Binding Domain for GRPR-Targeting Therapy of Cancer.", "authors": [{"family": "Abouzayed", "given": "Ayman", "initials": "A"}, {"family": "Tano", "given": "Hanna", "initials": "H"}, {"family": "Nagy", "given": "\u00c1bel", "initials": "\u00c1", "orcid": "0000-0001-7755-2661", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/e3f654b84865408094467dd3b4aeeafc.json"}}, {"family": "Rinne", "given": "Sara S", "initials": "SS", "orcid": "0000-0003-2141-3982", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/3aea3edd98b441c98bb527b1e0c911f5.json"}}, {"family": "Wadeea", "given": "Fadya", "initials": "F", "orcid": "0000-0002-3539-0593", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/0f68792679bf4c0a8cf442afb702f625.json"}}, {"family": "Kumar", "given": "Sharmishtaa", "initials": "S"}, {"family": "Westerlund", "given": "Kristina", "initials": "K"}, {"family": "Tolmachev", "given": "Vladimir", "initials": "V", "orcid": "0000-0002-6122-1734", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/896ae9fae8b74251afe11b4354c62794.json"}}, {"family": "Eriksson Karlstr\u00f6m", "given": "Amelie", "initials": "A", "orcid": "0000-0002-0695-5188", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/084ac56a883542f0b79ac6f63a9d6b1d.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": "2020-10-16", "journal": {"title": "Pharmaceutics", "issn": "1999-4923", "volume": "12", "issue": "10", "issn-l": null}, "abstract": "The targeting of gastrin-releasing peptide receptors (GRPR) was recently proposed for targeted therapy, e.g., radiotherapy. Multiple and frequent injections of peptide-based therapeutic agents would be required due to rapid blood clearance. By conjugation of the GRPR antagonist RM26 (D-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH2) to an ABD (albumin-binding domain), we aimed to extend the blood circulation of peptides. The synthesized conjugate DOTA-ABD-RM26 was labelled with indium-111 and evaluated in vitro and in vivo. The labelled conjugate was stable in PBS and retained specificity and its antagonistic function against GRPR. The half-maximal inhibitory concentration (IC50) of natIn-DOTA-ABD-RM26 in the presence of human serum albumin was 49 \u00b1 5 nM. [111In]In-DOTA-ABD-RM26 had a significantly longer residence time in blood and in tumors (without a significant decrease of up to 144 h pi) than the parental RM26 peptide. We conclude that the ABD-RM26 conjugate can be used for GRPR-targeted therapy and delivery of cytotoxic drugs. However, the undesirable elevated activity uptake in kidneys abolishes its use for radionuclide therapy. This proof-of-principle study justified further optimization of the molecular design of the ABD-RM26 conjugate.", "doi": "10.3390/pharmaceutics12100977", "pmid": "33081166", "labels": [], "xrefs": [{"db": "pmc", "key": "PMC7594083"}, {"db": "pii", "key": "pharmaceutics12100977"}], "notes": [], "created": "2026-08-21T13:04:44.934Z", "modified": "2026-08-21T13:04:45.108Z"}]}