1,2,3,4-二噻二唑衍生物3-（4-硝基苯基）-5-苯基- 3h -1,2,3,4-二噻二唑-2-氧化物影响STIM1-和STIM1-依赖性储存操作钙通道。

IF 0.6 4区医学 Q4 MEDICINE, RESEARCH & EXPERIMENTAL

Bulletin of Experimental Biology and Medicine Pub Date : 2025-07-01 Epub Date: 2025-09-24 DOI:10.1007/s10517-025-06475-y

D A Grekhnev, Iu V Novikova, V N Yuskovets, N M Chernov, I P Yakovlev, A Yu Skopin, E V Kaznacheyeva, V A Vigont

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引用次数: 0

摘要

钙信号的紊乱，特别是储存操作的钙进入与多种疾病有关，包括神经退行性疾病、肿瘤和自身免疫性疾病。存储操作的钙进入抑制剂具有神经保护作用和抑制转移，这使得存储操作通道成为药物设计的一个有吸引力的靶点。在此之前，我们发现1,2,3,4-二噻二唑衍生物是通常由STIM1和STIM2蛋白激活的储存操作钙通道的负调节剂。在这里，我们研究了这类化合物中最有效的化合物之一3-（4-硝基苯基）-5-苯基- 3h -1,2,3,4-二噻二唑-2-氧化物对STIM1和STIM2介导的储存操作钙进入的特异性作用，并得出结论，它通过STIM1和STIM2激活的储存操作通道阻断钙进入。

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1,2,3,4-Dithiadiazole Derivative 3-(4-Nitrophenyl)-5-Phenyl-3H-1,2,3,4-Dithiadiazole-2-Oxide Affects Both STIM1- and STIM2-Dependent Store-Operated Calcium Channels.

Disturbances in calcium signaling and, in particular, store-operated calcium entry are associated with a wide range of diseases, including neurodegenerative, oncological, and autoimmune pathologies. Inhibitors of store-operated calcium entry have a neuroprotective effect and suppress metastasis, which makes store-operated channels an attractive target for drug design. Previously, we showed that 1,2,3,4-dithiadiazole derivatives are negative modulators of store-operated calcium channels that are normally activated by STIM1 and STIM2 proteins. Here, we studied the specificity of action of one of the most effective compounds of this class, 3-(4-nitrophenyl)-5-phenyl-3H-1,2,3,4-dithiadiazole-2-oxide, on STIM1- and STIM2-mediated store-operated calcium entry and concluded that it blocks calcium entry through store-operated channels activated by both STIM1 and STIM2.

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来源期刊

Bulletin of Experimental Biology and Medicine 医学-医学：研究与实验

CiteScore

1.50

自引率

14.30%

发文量

265

审稿时长

2 months

期刊介绍： Bulletin of Experimental Biology and Medicine presents original peer reviewed research papers and brief reports on priority new research results in physiology, biochemistry, biophysics, pharmacology, immunology, microbiology, genetics, oncology, etc. Novel trends in science are covered in new sections of the journal - Biogerontology and Human Ecology - that first appeared in 2005. World scientific interest in stem cells prompted inclusion into Bulletin of Experimental Biology and Medicine a quarterly scientific journal Cell Technologies in Biology and Medicine (a new Russian Academy of Medical Sciences publication since 2005). It publishes only original papers from the leading research institutions on molecular biology of stem and progenitor cells, stem cell as the basis of gene therapy, molecular language of cell-to-cell communication, cytokines, chemokines, growth and other factors, pilot projects on clinical use of stem and progenitor cells. The Russian Volume Year is published in English from April.