Lipoyl-Homotaurine Derivative (ADM_12) Reverts Oxaliplatin-Induced Neuropathy and Reduces Cancer Cells Malignancy by Inhibiting Carbonic Anhydrase IX (CAIX)
(2017) Journal of Medicinal Chemistry — Vol. 60, n° 21, p. 9003-9011 (2017)
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- Authors
Fragai, Marco 
Nativi, Cristina
- 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.
- Affiliations
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Fragai, M., Comito, G., Di Cesare Mannelli, L., Gualdani, R., Calderone, V., Louka, A., Richichi, B., Francesconi, O., Angeli, A., Nocentini, A., Gratteri, P., Chiarugi, P., Ghelardini, C., Tadini-Buoninsegni, F., Supuran, C. T., & Nativi, C. (2017). Lipoyl-Homotaurine Derivative (ADM_12) Reverts Oxaliplatin-Induced Neuropathy and Reduces Cancer Cells Malignancy by Inhibiting Carbonic Anhydrase IX (CAIX). Journal of Medicinal Chemistry, 60(21), 9003-9011. https://doi.org/10.1021/acs.jmedchem.7b01237 (Original work published 2017)