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

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 an...

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Published inJournal of medicinal chemistry Vol. 60; no. 21; pp. 9003 - 9011
Main Authors Fragai, Marco, Comito, Giuseppina, Di Cesare Mannelli, Lorenzo, Gualdani, Roberta, Calderone, Vito, Louka, Alexandra, Richichi, Barbara, Francesconi, Oscar, Angeli, Andrea, Nocentini, Alessio, Gratteri, Paola, Chiarugi, Paola, Ghelardini, Carla, Tadini-Buoninsegni, Francesco, Supuran, Claudiu T, Nativi, Cristina
Format Journal Article
LanguageEnglish
Published WASHINGTON American Chemical Society 09.11.2017
Amer Chemical Soc
Subjects
Antineoplastic Agents - pharmacology
Antineoplastic Agents - toxicity
Carbonic Anhydrase Inhibitors - pharmacology
Carbonic Anhydrase IX - antagonists & inhibitors
Cell Line, Tumor
Chemistry, Medicinal
Drug Synergism
Humans
Life Sciences & Biomedicine
Neoplasms - complications
Neoplasms - drug therapy
Neoplasms - pathology
Organoplatinum Compounds - therapeutic use
Organoplatinum Compounds - toxicity
Oxaliplatin
Pancreatic Neoplasms - drug therapy
Pancreatic Neoplasms - pathology
Peripheral Nervous System Diseases - chemically induced
Peripheral Nervous System Diseases - drug therapy
Pharmacology & Pharmacy
Science & Technology
Taurine - analogs & derivatives
Taurine - chemistry
Taurine - pharmacology
TRPA1 Cation Channel - antagonists & inhibitors
PH REGULATION
TUMORS
PAIN
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Summary: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.
Bibliography:ObjectType-Article-1
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content type line 23
ISSN:0022-2623
1520-4804
DOI:10.1021/acs.jmedchem.7b01237