Lipoyl-Homotaurine Derivative (ADM_12) Reverts Oxaliplatin-Induced Neuropathy and Reduces Cancer Cells Malignancy by Inhibiting Carbonic Anhydrase IX (CAIX).
Marco FragaiGiuseppina ComitoLorenzo Di Cesare MannelliRoberta GualdaniVito CalderoneAlexandra LoukaBarbara RichichiOscar FrancesconiAndrea AngeliAlessio NocentiniPaola GratteriPaola ChiarugiCarla GhelardiniFrancesco Tadini-BuoninsegniClaudiu T SupuranCristina NativiPublished in: Journal of medicinal chemistry (2017)
Oxaliplatin (OXA) is a valuable and largely used cancer drug which induces a serious and intractable neuropathy. The lipoyl-homotaurine derivative (ADM_12) reverts in vivo OXA-induced neuropathy, and it is an effective antagonist of the nociceptive sensor channel TRPA1. Unprecedentedly, this safe analgesic showed a synergy with OXA in vitro and proved to inhibit CA IX, a relevant therapeutic target, clearly interfering with pancreatic cancer cells' aggressiveness.