线粒体Kv1.3通道作为多发性骨髓瘤的治疗靶点

Mitochondrial Kv1.3 Channels as Target for Treatment of Multiple Myeloma.

作者信息

Kadow Stephanie, Schumacher Fabian, Kramer Melanie, Hessler Gabriele, Scholtysik René, Oubari Sara, Johansson Patricia, Hüttmann Andreas, Reinhardt Hans Christian, Kleuser Burkhard, Zoratti Mario, Mattarei Andrea, Szabò Ildiko, Gulbins Erich, Carpinteiro Alexander

机构信息

Institute of Molecular Biology, University Hospital Essen, University of Duisburg-Essen, 45147 Essen, Germany.

Institute of Pharmacy, Freie University Berlin, 14195 Berlin, Germany.

出版信息

Cancers (Basel). 2022 Apr 13;14(8):1955. doi: 10.3390/cancers14081955.

Abstract

Despite several new developments in the treatment of multiple myeloma, all available therapies are only palliative without curative potential and all patients ultimately relapse. Thus, novel therapeutic options are urgently required to prolong survival of or to even cure myeloma. Here, we show that multiple myeloma cells express the potassium channel Kv1.3 in their mitochondria. The mitochondrial Kv1.3 inhibitors PAPTP and PCARBTP are efficient against two tested human multiple myeloma cell lines (L-363 and RPMI-8226) and against ex vivo cultured, patient-derived myeloma cells, while healthy bone marrow cells are spared from toxicity. Cell death after treatment with PAPTP and PCARBTP occurs via the mitochondrial apoptotic pathway. In addition, we identify up-regulation of the multidrug resistance pump MDR-1 as the main potential resistance mechanism. Combination with ABT-199 (venetoclax), an inhibitor of Bcl2, has a synergistic effect, suggesting that mitochondrial Kv1.3 inhibitors could potentially be used as combination partner to venetoclax, even in the treatment of t(11;14) negative multiple myeloma, which represent the major part of cases and are rather resistant to venetoclax alone. We thus identify mitochondrial Kv1.3 channels as druggable targets against multiple myeloma.

摘要

尽管多发性骨髓瘤的治疗有了一些新进展,但所有可用疗法都只是姑息性的,没有治愈潜力,所有患者最终都会复发。因此,迫切需要新的治疗选择来延长骨髓瘤患者的生存期甚至治愈该病。在此,我们表明多发性骨髓瘤细胞在线粒体中表达钾通道Kv1.3。线粒体Kv1.3抑制剂PAPTP和PCARBTP对两种测试的人多发性骨髓瘤细胞系(L-363和RPMI-8226)以及体外培养的患者来源的骨髓瘤细胞有效,而健康骨髓细胞则不受毒性影响。用PAPTP和PCARBTP处理后的细胞死亡通过线粒体凋亡途径发生。此外,我们确定多药耐药泵MDR-1的上调是主要的潜在耐药机制。与Bcl2抑制剂ABT-199(维奈克拉)联合使用具有协同作用,这表明线粒体Kv1.3抑制剂甚至有可能作为维奈克拉的联合用药伙伴,用于治疗t(11;14)阴性多发性骨髓瘤,这类病例占大多数且对单独使用维奈克拉相当耐药。因此,我们确定线粒体Kv1.3通道是针对多发性骨髓瘤的可药物化靶点。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7229/9032553/50f14aec60b2/cancers-14-01955-g001.jpg

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