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. 2017 Nov 9;60(21):9003-9011.
doi: 10.1021/acs.jmedchem.7b01237. Epub 2017 Oct 27.

Lipoyl-Homotaurine Derivative (ADM_12) Reverts Oxaliplatin-Induced Neuropathy and Reduces Cancer Cells Malignancy by Inhibiting Carbonic Anhydrase IX (CAIX)

Marco Fragai  1   2 , Giuseppina Comito  3 , Lorenzo Di Cesare Mannelli  4 , Roberta Gualdani  1 , Vito Calderone  1   2 , Alexandra Louka  2 , Barbara Richichi  1 , Oscar Francesconi  1 , Andrea Angeli  4 , Alessio Nocentini  4 , Paola Gratteri  4 , Paola Chiarugi  3 , Carla Ghelardini, Francesco Tadini-Buoninsegni  1 , Claudiu T Supuran  4 , Cristina Nativi  1   5
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Lipoyl-Homotaurine Derivative (ADM_12) Reverts Oxaliplatin-Induced Neuropathy and Reduces Cancer Cells Malignancy by Inhibiting Carbonic Anhydrase IX (CAIX)

Marco Fragai et al. J Med Chem. .

Abstract

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.

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