Ask about this productRelated genes to: SSTR2 antibody
- Gene:
- SSTR2 NIH gene
- Name:
- somatostatin receptor 2
- Previous symbol:
- -
- Synonyms:
- -
- Chromosome:
- 17q25.1
- Locus Type:
- gene with protein product
- Date approved:
- 1992-08-25
- Date modifiied:
- 2016-10-25
Related products to: SSTR2 antibody
Related articles to: SSTR2 antibody
- The advancement of precision medicine depends critically on well-defined molecular targets. Pathologically activated fibroblasts drive disease progression in cancer, fibrosis and chronic inflammation through sustained inflammation, extracellular matrix remodeling and pathological microenvironment formation. Among available markers, fibroblast activation protein (FAP) stands out due to its selective overexpression in diseased tissues versus minimal expression in healthy organs. This unique profile makes FAP a promising target for molecular imaging and targeted therapy, enabling precision theranostics across both oncological and nononcological diseases. FAP-targeted theranostics originated from the lead compound PT-100, which established the core pharmacophore. Subsequent key advance was the replacement of the boronic acid warhead with a cyano group, along with the introduction of fluorine and quinoline moieties, yielding the UAMC-1110 scaffold. This scaffold exhibits improved bioactivity and favorable pharmacokinetics. Systematic modification of the quinoline side chain and conjugation with chelators have allowed efficient radiolabeling, positioning radiolabeled FAP inhibitors as promising tools for precision theranostics. However, continued optimization of UAMC-1110-derived probes to enhance their stability, affinity, tumor retention, and cellular uptake, together with integration into advanced strategies such as nanomedicine, remains essential not only for refining FAP-targeted precision medicine but also for expanding its applications beyond oncology to nononcological diseases. Unlike previous reviews, this Account organizes the field around a unified chemical design language, following a "rational design-pharmacokinetics-translational validation" paradigm. After delineating the core biological functions of FAP-expressing fibroblasts in disease pathogenesis, we systematically examine the rapid advancement of radionuclide-labeled FAPIs, including optimization of linkers, chelators, and albumin-binding moieties, along with multimerization strategies, which significantly enhanced the pharmacokinetic profiles. Key innovations in the field include three strategic approaches. First, the albumin-binding therapeutic agent [177Lu]Lu-EB-FAPI achieves prolonged tumor retention and promising efficacy. Second, multimerization strategies have yielded bivalent and tetrameric FAPI constructs, which exhibit superior tumor accumulation. Third, heterodimeric probes such as [68Ga]Ga-FAPI-RGD and [68Ga]Ga-FAPI-LM3 enable dual targeting of FAP along with integrin αvβ3 or somatostatin receptor SSTR2, thereby addressing tumor heterogeneity and enhancing lesion detectability. Subsequently, the application scope of FAPI-based imaging has been expanded from oncology to nononcological diseases. The value of this technique in visualizing dynamic remodeling processes across key pathologic conditions has been established, offering quantitative assessment beyond the reach of standard modalities. Furthermore, we review recent advances in diverse FAP-targeted therapeutic strategies, including nanomaterials, CAR-T cells, and vaccines, and offer a forward-looking perspective on both the potential and the ongoing challenges of FAP as a cross-disease precision theranostic platform. - Source: PubMed
Liu JieZhao XinzhiLiu PeifeiYu JinmingChen XiaoyuanZhang Jingjing - Peptide receptor radionuclide therapy (PRRT) is an emerging and promising targeted treatment for aggressive pituitary neuroendocrine tumours (PitNETs) and pituitary carcinomas refractory to conventional therapies. Its use is supported by the frequent expression of somatostatin receptors (SSTR), predominantly SSTR2, in pituitary tumour cells, enabling selective delivery of β-emitting radionuclides such as 177Lu-DOTATATE and 90Y-DOTATOC, resulting in targeted antitumour and antisecretory effect. This narrative review summarizes current scanty evidence on PRRT efficacy and safety in aggressive pituitary tumours. Successful outcomes were reported in some cases, in terms of tumour growth and/or hormonal reduction, or relief of mass-effect-related symptoms. PRRT related adverse events are mostly mild and transient, predominantly hematologic, with clinically significant renal toxicity uncommon when amino-acid nephroprotection is used. Preserved pituitary function and no clinically significant PRRT-induced hypopituitarism have been reported. Overall, PRRT represents a biologically rational and potentially effective option for selected patients with SSTR-positive aggressive PitNETs after failure of previous therapies. - Source: PubMed
Publication date: 2026/08/11
Ferraù FrancescoBlanca Elena SofiaCosta Carla PaolaCannavò Salvatore - A significant proportion of meningiomas are resistant to current treatments. Somatostatin receptor 2 (SSTR2) is highly and consistently expressed in most meningiomas, providing a promising target for localized chimeric antigen receptor (CAR)-T cell therapy. Short-lived small-molecule CAR adapters can potentially prevent CAR-T cell exhaustion in solid tumors by alternating between active and resting states. - Source: PubMed
Publication date: 2026/07/21
Chen JiaweiPellegrino ChristianMastall MaximilianSzulzewsky FrankBijnen MitchellVan Hove Hannah JFavalli NicholasBassi GabrieleMoisoiu VladVasella FlavioPadevit LuisNeidert Marian CShelbourn AllisonCimino Patrick JReimann ReginaRoth PatrickManz Markus GGreter MelanieHolland Eric CNeri DarioWeller MichaelWirsching Hans-Georg - The incidental thyroid uptake of radiolabeled ligands used in positron emission tomography/computed tomography (PET/CT) targeting cell-surface proteins is observed in up to 6% of all scans. While diffuse thyroid uptake of ligands targeting somatostatin receptor type 2 (SSTR2), prostate-specific membrane antigen (PSMA), fibroblast activation protein (FAPI), or choline, is observed in normal thyroid or usually signifies a benign thyroid abnormality, a heterogenous or focal uptake is associated with malignant lesions in up to 19.7% of patients. The PET/CTs utilizing these ligands are characterized by decreased diagnostic sensitivity for detection of thyroid cancer metastases than cross-sectional imaging or 18-fluorodeoxyglucose (18FDG)-PET/CT but are highly specific for detection of a subset of thyroid cancers characterized by a high target protein expression. Increased uptake of radiolabeled ligands targeting SSTR2, PSMA, FAPI, integrin αvβ3 and minigastrin can be used for patients' selection for peptide receptor radionuclide therapy (PRRT). PRRT can be applied in clinical trials and/or off label for patients with advanced radioactive iodine-refractory thyroid cancer who have limited treatment options or for medullary thyroid carcinoma of neuroendocrine origin. The PRRT-induced disease control rate approaches 60% and PRRT is well tolerated with limited side effects. Efficacy could be improved with careful patients' selection based on the expression of molecular targets and their function, quantified by standard uptake values (SUVmax) in diagnostic PET/CT imaging. Adopting an individualized dosimetry-based approach and synthesizing ligands with better tumor retention and residence time may help optimize treatment response. - Source: PubMed
Publication date: 2026/07/31
Sridhar ArchanaBehairy NohaKlubo-Gwiezdzinska Joanna - Neuroblastoma is an aggressive paediatric malignancy with poor outcomes in high-risk patients despite multimodal therapy. [Lu]Lu-DOTATATE, targeting somatostatin receptor 2 (SSTR2), is under clinical investigation for neuroblastoma. Terbium-161 (Tb) shares chemical characteristics and a similar half-life with lutetium-177 (Lu) but offers advantages through its higher emission of Auger and conversion electrons, which may enhance therapeutic efficacy especially for micrometastases and recurrent disease. This study investigates [Tb]Tb-DOTATATE as a potential complement for treatment of SSTR2-expressing neuroblastoma. - Source: PubMed
Publication date: 2026/07/28
Chopra SaloniXu TianqiBerglund HannaGustafsson AmandaNestor Marika