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Cell membrane receptors : tools for rational drug design
Nicole Moguilevsky, PhD
The laboratory pursued cloning and expression experiments on G-protein-coupled receptors. These recombinant receptors do not constitute therapeutical products but provide tools for the screening, the design and the evaluation of new drugs. Our interest has been directed towards the human adrenergic receptors, the H1-histaminic receptor, which is involved in various allergic diseases, and towards other G-protein-coupled receptors, like the secretin and vasointestinal peptide (VIP) receptors, which belong to the family of gut/brain peptides receptors.
Site-directed mutants and hybrid receptor molecules have been constructed and studied in terms of ligand affinity and specificity, in combination with computer-aided modelisation.
These studies aim at the precise definition of drug binding sites and at the conception of new drugs devoid of unwanted side effects.
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