Targeting Relevant HDACs to Support the Survival of Cone Photoreceptors in Inherited Retinal Diseases: Identification of a Potent Pharmacological Tool with In Vitro and In Vivo Efficacy.
Carullo G, Orsini N, Piano I, Pozzetti L, Papa A, Fontana A, Napoli D, Corsi F, Marco BD, Galante A, Marotta L, Panzeca G, O'Brien J, Sanchez AG, Doherty H, Mahon N, Clarke L, Contri C, Pasquini S, Gorelli B, Saponara S, Valoti M, Vincenzi F, Varani K, Ramunno A, Brogi S, Butini S, Gemma S, Kennedy BN, Gargini C, Strettoi E, Campiani G.
Carullo G, et al.
J Med Chem. 2024 Sep 12;67(17):14946-14973. doi: 10.1021/acs.jmedchem.4c00477. Epub 2024 Jul 4.
J Med Chem. 2024.
PMID: 38961727
We developed new HDAC inhibitors (5a-p), typified by a tetrahydro-gamma-carboline scaffold, characterized by high HDAC6 inhibition potency with balanced physicochemical properties for in vivo studies. Compound 5d (repistat, IC(50) HDAC6 = 6.32 nM) increased the levels of a …
We developed new HDAC inhibitors (5a-p), typified by a tetrahydro-gamma-carboline scaffold, characterized by high HDAC6 inhibition potency w …