USE OF TRYPTOPHAN HYDROXYLASE 1 (TPH1) INHIBITORS FOR THE TREATMENT OF ATHEROSCLEROSIS

Tryptophan (Trp) is one of the nine essential amino acids supplied by the diet, whose metabolism appears as a key metabolic gatekeeper of intestinal homeostasis, although its systemic effects, particularly on atherosclerosis, remain unknown. The inventors show that the high-fat diet (HFD) but not the high-cholesterol diet (HCD) increases intestinal indoleamine 2, 3-dioxygenase 1 (IDO) activity, the main enzyme involved in Trp catabolism in the gut, which shifts intestinal Trp metabolism from microbiota-produced indole metabolites and serotonin or 5-hydroxytryptamine (5-HT) production towards Kynurenine production. Most importantly the inventors showed that inhibition of tryptophan hydroxylase 1 (TpH1), markedly reduces intestinal 5-HT production and alleviates atherosclerosis as well as plaque inflammation. Accordingly, the present invention relates to the use of tryptophan hydroxylase 1 (TpH1) inhibitors for the treatment of atherosclerosis.

Keywords: Atherosclerosis, new target, inflammation, cardiovascular diseases
Inventors:
TALEB Soraya,CHAJADINE Mouna
Publications:
Chajadine M, Laurans L, Radecke T, Mouttoulingam N, Al-Rifai R, Bacquer E, Delaroque C, Rytter H, Bredon M, Knosp C, Vilar J, Fontaine C, Suffee N, Vandestienne M, Esposito B, Dairou J, Launay JM, Callebert J, Tedgui A, Ait-Oufella H, Sokol H, Chassaing B, Taleb S. Harnessing intestinal tryptophan catabolism to relieve atherosclerosis in mice. Nat Commun. 2024 Jul 29;15(1):6390. doi: 10.1038/s41467-024-50807-x. PMID: 39080345; PMCID: PMC11289133.

Reference:

BIO22137-T1

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