We report the NMR characterization of the molecular interaction between Gastrin Releasing Peptide Receptor (GRP-R) and its natural ligand bombesin (BN). GRP-R is a transmembrane G-protein coupled receptor promoting the stimulation of cancer cell proliferation; in addition, being overexpressed on the surface of different human cancer cell lines, it is ideal for the development of new strategies for the selective targeted delivery of anticancer drugs and diagnostic devices to tumor cells. However, the design of new GRPR binders requires structural information on receptor interaction with its natural ligands. The experimental protocol presented herein, based on on-cell STD NMR techniques, is a powerful tool for the screening and the epitope mapping of GRP-R ligands aimed at the development of new anticancer and diagnostic tools. Notably, the study can be carried out in a physiological environment, at the surface of tumoral cells overespressing GRP-R. Moreover, to the best of our knowledge, this is the first example of an NMR experiment able to detect and investigate the structural determinants of BN/GRP-R interaction.

Palmioli, A., Ceresa, C., Tripodi, F., La Ferla, B., Nicolini, G., Airoldi, C. (2020). On-cell Saturation Transfer Difference NMR study of Bombesin binding to GRP receptor. BIOORGANIC CHEMISTRY, 99 [10.1016/j.bioorg.2020.103861].

On-cell Saturation Transfer Difference NMR study of Bombesin binding to GRP receptor

Palmioli, Alessandro
Primo
;
Ceresa, Cecilia
Secondo
;
Tripodi, Farida;La Ferla, Barbara;Nicolini, Gabriella;Airoldi, Cristina
Ultimo
2020

Abstract

We report the NMR characterization of the molecular interaction between Gastrin Releasing Peptide Receptor (GRP-R) and its natural ligand bombesin (BN). GRP-R is a transmembrane G-protein coupled receptor promoting the stimulation of cancer cell proliferation; in addition, being overexpressed on the surface of different human cancer cell lines, it is ideal for the development of new strategies for the selective targeted delivery of anticancer drugs and diagnostic devices to tumor cells. However, the design of new GRPR binders requires structural information on receptor interaction with its natural ligands. The experimental protocol presented herein, based on on-cell STD NMR techniques, is a powerful tool for the screening and the epitope mapping of GRP-R ligands aimed at the development of new anticancer and diagnostic tools. Notably, the study can be carried out in a physiological environment, at the surface of tumoral cells overespressing GRP-R. Moreover, to the best of our knowledge, this is the first example of an NMR experiment able to detect and investigate the structural determinants of BN/GRP-R interaction.
Articolo in rivista - Articolo scientifico
BombesinGastrin Releasing Peptide Receptor (GRP-R)ligand-receptor interaction studieson-cell STD NMRtumor targeting
English
18-apr-2020
2020
99
103861
none
Palmioli, A., Ceresa, C., Tripodi, F., La Ferla, B., Nicolini, G., Airoldi, C. (2020). On-cell Saturation Transfer Difference NMR study of Bombesin binding to GRP receptor. BIOORGANIC CHEMISTRY, 99 [10.1016/j.bioorg.2020.103861].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10281/271577
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