Estimation of the dissociation rate of unlabelled ligand-receptor complexes by a 'two-step' competition binding approach.

Last updated on 23-3-2023 by Elena Debock

Public Access

Published

Peer reviewed scientific article

English

SCIENSANO

Abstract:

BACKGROUND AND PURPOSE: Because the in vivo effectiveness of ligands may also be determined by the rate by which they dissociate from their target receptors, drug candidates are being increasingly screened for this kinetic property. The dissociation rate of unlabelled ligand-receptor complexes can be estimated indirectly from their ability to slow the association of subsequently added radioligand molecules. EXPERIMENTAL APPROACH: We used the ‘two-step competition’ binding approach consisting of pre-incubating the receptor preparation with a wide range of ligand concentrations, washing of…

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