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碳酸酐酶 IX 抑制剂 SLC-0111 作为一种新兴药物,可抑制间充质干细胞衍生的促生存作用对黑色素瘤细胞的影响。

The Carbonic Anhydrase IX inhibitor SLC-0111 as emerging agent against the mesenchymal stem cell-derived pro-survival effects on melanoma cells.

机构信息

Department of Clinical and Experimental Biomedical Sciences "Mario Serio", Section of Experimental Pathology and Oncology, University of Florence, Florence, Italy.

Department of NEUROFARBA, University of Florence, Florence, Italy.

出版信息

J Enzyme Inhib Med Chem. 2020 Dec;35(1):1185-1193. doi: 10.1080/14756366.2020.1764549.

Abstract

Mesenchymal stem cells (MSC) take part to solid tumour-associated stroma and critically influence progression of malignancy. Our study represents a striking example of melanoma progression to a more malignant and resistant phenotype promoted by MSC and the possibility to contrast this diabolic liaison using CAIX inhibitors. In particular, we demonstrated that melanoma cells exposed to a MSC-conditioned medium switch to a more malignant phenotype, characterised by resistance to programmed cell death and endowed with an epithelial-to-mesenchymal transition and stem cell characteristics. These effects were reversed abrogating MSC CAIX activity using SLC-0111, a CAIX inhibitor. Moreover, the acquisition by melanoma cells of a Vemurafenib-resistant phenotype upon MSC-conditioned medium exposure was removed when MSC were treated with SLC-0111. Therefore, MSC may profoundly reprogramme melanoma cells towards a wide resistant phenotype through CAIX involvement, as the use of SLC-0111 is able to contrast the development of this highly risky adaptation for disease progression.

摘要

间充质干细胞 (MSC) 参与实体瘤相关基质,并对恶性肿瘤的进展起关键作用。我们的研究代表了一个显著的例子,即 MSC 促进黑色素瘤向更恶性和更具耐药性的表型进展,以及使用 CAIX 抑制剂来对抗这种恶性循环的可能性。具体而言,我们证明了暴露于 MSC 条件培养基中的黑色素瘤细胞会转变为更恶性的表型,其特征是对程序性细胞死亡的抵抗,并具有上皮间质转化和干细胞特征。使用 CAIX 抑制剂 SLC-0111 阻断 MSC 的 CAIX 活性可以逆转这些作用。此外,当用 SLC-0111 处理 MSC 时,暴露于 MSC 条件培养基的黑色素瘤细胞获得的威罗非尼耐药表型也被消除。因此,MSC 可能通过 CAIX 的参与,将黑色素瘤细胞深刻地重新编程为广泛的耐药表型,因为 SLC-0111 的使用能够对抗这种对疾病进展具有高度风险的适应性发展。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/adfb/7269050/50820ce587d8/IENZ_A_1764549_F0001_C.jpg

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