BAY86-7548   Click here for help

GtoPdb Ligand ID: 11260

Synonyms: [68Ga]D-Phe6, Stat13, Leu14 Bn(6-14) | [68Ga]RM2 | Ga-RM2
 Ligand is labelled  Ligand is radioactive
Compound class: Peptide
Comment: This is a modified analogue of bombesin[6-14] that acts as a BB2 receptor antagonist [2]. It contains the DOTA (tetraxetan) chelator to facilitate addition of a radiolabel to generate a PET/CT imaging tool.
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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species
References
1. Kurth J, Potratz M, Heuschkel M, Krause BJ, Schwarzenböck SM. (2022)
GRPr Theranostics: Current Status of Imaging and Therapy using GRPr Targeting Radiopharmaceuticals.
Nuklearmedizin, 61 (3): 247-261. [PMID:35668669]
2. Kähkönen E, Jambor I, Kemppainen J, Lehtiö K, Grönroos TJ, Kuisma A, Luoto P, Sipilä HJ, Tolvanen T, Alanen K et al.. (2013)
In vivo imaging of prostate cancer using [68Ga]-labeled bombesin analog BAY86-7548.
Clin Cancer Res, 19 (19): 5434-43. [PMID:23935037]
3. Mansi R, Nock BA, Dalm SU, Busstra MB, van Weerden WM, Maina T. (2021)
Radiolabeled Bombesin Analogs.
Cancers (Basel), 13 (22). [PMID:34830920]
4. Mansi R, Wang X, Forrer F, Waser B, Cescato R, Graham K, Borkowski S, Reubi JC, Maecke HR. (2011)
Development of a potent DOTA-conjugated bombesin antagonist for targeting GRPr-positive tumours.
Eur J Nucl Med Mol Imaging, 38 (1): 97-107. [PMID:20717822]
5. Uehara H, González N, Sancho V, Mantey SA, Nuche-Berenguer B, Pradhan T, Coy DH, Jensen RT. (2011)
Pharmacology and selectivity of various natural and synthetic bombesin related peptide agonists for human and rat bombesin receptors differs.
Peptides, 32 (8): 1685-99. [PMID:21729729]