Impact of polyphenols on receptor-ligand interactions by NMR the case of neurotensin (NT)-neurotensin receptor fragment (NTS1) complex - INRAE - Institut national de recherche pour l’agriculture, l’alimentation et l’environnement Accéder directement au contenu
Article Dans Une Revue Journal of Biomolecular Structure and Dynamics Année : 2020

Impact of polyphenols on receptor-ligand interactions by NMR the case of neurotensin (NT)-neurotensin receptor fragment (NTS1) complex

Résumé

Ligand-receptor interactions can be implicated in many pathological events such as chronic neurodegenerative diseases. Thus, the discovery of molecules disrupting this type of interactions could be an interesting therapeutic approach. Polyphenols are well known for their affinity for proteins and several studies have characterized these direct interactions. But studying the direct influence of multi-therapeutic drugs on a ligand-receptor complex relevant to a neurodegenerative disorder is a challenging issue. Solution NMR, molecular modeling and iterative calculations were used to obtain information about the interaction between a phenolic compound, α-glucogallin (α-2) and a ligand/fragment receptor complex neurotensin (NT) and its receptor NTS1. The α-2 was shown to bind to NT and a peptidic fragment of its NTS1 receptor, independently. Although the formation of the corresponding ligand-receptor complex did not seem to be affected, this experimental modeling protocol will enable the evaluation of other anti-amyloidogenic compounds such as blockers of NT-NTS1 binding. These types of studies help in understanding the specificity and influence in binding and can provide information to develop new molecules with a putative pharmacological interest.

Domaines

Chimie
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Dates et versions

hal-02150440 , version 1 (06-07-2023)

Identifiants

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Tristan Richard, Eva Petit, Laurent Pouységu, Jean-Pierre Monti, Arnaud Bondon, et al.. Impact of polyphenols on receptor-ligand interactions by NMR the case of neurotensin (NT)-neurotensin receptor fragment (NTS1) complex. Journal of Biomolecular Structure and Dynamics, 2020, online first (5), pp.1-12. ⟨10.1080/07391102.2019.1608863⟩. ⟨hal-02150440⟩
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