Design of GPCR ligands

Design of GPCR ligands

Our research is focused on the conception, design and synthesis of ligands that target peptidic hormone GPCRs. More precisely we work on tufstin, cholecystokinin, bradykinin, bombesin, gastrin releasing peptide, neurotensin, ghrelin, gastrin… Our aim is to find very specific molecules that target one physiological biological activity of a given receptor and that can be developed in pre-clinical studies. These compounds can be peptides, pseudo-peptides or non-peptide moieties. They can exhibit agonist, antagonist or inverse agonist properties toward the desired receptor, depending on the expected biological activity. We also routinely synthesize biological tools useful for our biologist partners (purification of receptors, high throughput screening, radiopharmaceutical or fluorescent ligands for imaging, photoactivable probes for receptor identification, labeled N15 peptides for NMR interactions with the receptor…).

The important work in the field has allowed the identification of compound JMV 1843 that was recently commercialized (Macrilen™) as drug for the diagnosis of the growth hormone deficiency.

CONTACT

JEAN-ALAIN FEHRENTZ
JEAN-ALAIN FEHRENTZ
Jean Martinez
Jean Martinez
Séverine Denoyelle
Séverine Denoyelle
Luc Brunel
Luc Brunel
Pascal Verdier
Pascal Verdier

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