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J Med Chem. 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).

Author information

1
Department of Chemistry, University of Florence , via della Lastruccia 3-13, 50019 Sesto Fiorentino, Italy.
2
CERM, University of Florence , via L. Sacconi 6, 50019 Sesto Fiorentino, Italy.
3
Department of Experimental and Clinical Biomedical Sciences, University of Florence , V.le Morgagni 50, 50134 Firenze, Italy.
4
Department NEUROFARBA, University of Florence , V.le Pieraccini 6, 50134 Firenze, Italy.
5
FioGen , via L. Sacconi 6, 50019 Sesto Fiorentino, Italy.

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.

PMID:
29048889
DOI:
10.1021/acs.jmedchem.7b01237
[Indexed for MEDLINE]

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