Development, synthesis and evaluation of novel fluorescent Endothelin-B receptor probes

Delahaye J, Stölting M, Geyer C, Vogl T, Eisenblätter M, Helfen A, Höltke C (2023)
European Journal of Medicinal Chemistry 258: 115568.

Zeitschriftenaufsatz | Veröffentlicht | Englisch
 
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Autor*in
Delahaye, Juliette; Stölting, Miriam; Geyer, Christiane; Vogl, Thomas; Eisenblätter, MichelUniBi; Helfen, Anne; Höltke, Carsten
Abstract / Bemerkung
The endothelin (ET) signaling system is comprised of three endothelin peptides (ET-1, -2 and -3) and two corresponding endothelin-A and -B receptors (ETAR and ETBR), which belong to the G-protein coupled receptor (GPCR) superfamily. The endothelin axis, as this system is also referred to, contributes to the maintenance of vascular tone, functions as regulator of inflammation and proliferation and helps in balancing water homeostasis. In pathological settings, the ET axis is known to contribute to endothelial activation in cardiovascular diseases, to cell proliferation, chemoresistance and metastasis in cancer and to inflammation and fibrosis in renal disease. Antagonists of ETAR and ETBR, either subtype-specific compounds or substances with high affinity to both receptors, have been developed for more than 30 years. In the preclinical context, in vivo imaging of endothelin receptor expression has been utilized to assess ET-axis contribution to e.g. cancer or myocardial infarction. In this work, we present the development and synthesis of two novel ETBR-specific fluorescent probes, based on the available antagonists BQ788 and IRL2500 and their preliminary evaluation in a breast cancer context. Copyright © 2023 Elsevier Masson SAS. All rights reserved.
Erscheinungsjahr
2023
Zeitschriftentitel
European Journal of Medicinal Chemistry
Band
258
Art.-Nr.
115568
eISSN
1768-3254
Page URI
https://pub.uni-bielefeld.de/record/2980724

Zitieren

Delahaye J, Stölting M, Geyer C, et al. Development, synthesis and evaluation of novel fluorescent Endothelin-B receptor probes. European Journal of Medicinal Chemistry. 2023;258: 115568.
Delahaye, J., Stölting, M., Geyer, C., Vogl, T., Eisenblätter, M., Helfen, A., & Höltke, C. (2023). Development, synthesis and evaluation of novel fluorescent Endothelin-B receptor probes. European Journal of Medicinal Chemistry, 258, 115568. https://doi.org/10.1016/j.ejmech.2023.115568
Delahaye, Juliette, Stölting, Miriam, Geyer, Christiane, Vogl, Thomas, Eisenblätter, Michel, Helfen, Anne, and Höltke, Carsten. 2023. “Development, synthesis and evaluation of novel fluorescent Endothelin-B receptor probes”. European Journal of Medicinal Chemistry 258: 115568.
Delahaye, J., Stölting, M., Geyer, C., Vogl, T., Eisenblätter, M., Helfen, A., and Höltke, C. (2023). Development, synthesis and evaluation of novel fluorescent Endothelin-B receptor probes. European Journal of Medicinal Chemistry 258:115568.
Delahaye, J., et al., 2023. Development, synthesis and evaluation of novel fluorescent Endothelin-B receptor probes. European Journal of Medicinal Chemistry, 258: 115568.
J. Delahaye, et al., “Development, synthesis and evaluation of novel fluorescent Endothelin-B receptor probes”, European Journal of Medicinal Chemistry, vol. 258, 2023, : 115568.
Delahaye, J., Stölting, M., Geyer, C., Vogl, T., Eisenblätter, M., Helfen, A., Höltke, C.: Development, synthesis and evaluation of novel fluorescent Endothelin-B receptor probes. European Journal of Medicinal Chemistry. 258, : 115568 (2023).
Delahaye, Juliette, Stölting, Miriam, Geyer, Christiane, Vogl, Thomas, Eisenblätter, Michel, Helfen, Anne, and Höltke, Carsten. “Development, synthesis and evaluation of novel fluorescent Endothelin-B receptor probes”. European Journal of Medicinal Chemistry 258 (2023): 115568.

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