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脂酰基牛磺酸衍生物（ADM_12）通过抑制碳酸酐酶 IX（CAIX）逆转奥沙利铂诱导的神经病变并降低癌细胞的恶性程度。

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

机构信息

Department of Chemistry, University of Florence , via della Lastruccia 3-13, 50019 Sesto Fiorentino, Italy.

CERM, University of Florence , via L. Sacconi 6, 50019 Sesto Fiorentino, Italy.

出版信息

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

DOI:10.1021/acs.jmedchem.7b01237
PMID:29048889
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.

摘要

奥沙利铂（OXA）是一种有价值且广泛应用的抗癌药物，可引起严重且难以治疗的周围神经病。脂酰高丝氨酸衍生物（ADM_12）可逆转体内奥沙利铂诱导的周围神经病，并且是伤害感受传感器通道 TRPA1 的有效拮抗剂。史无前例的是，这种安全的镇痛药在体外与奥沙利铂表现出协同作用，并被证明可抑制相关治疗靶点 CAIX，明显干扰胰腺癌细胞的侵袭性。

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