提问
盖德化工网  >  盖德问答  >  TRAM-34是一种...

TRAM-34是一种有效的、选择性的钾通道抑制剂? 1

0评论 +关注
共1个回答

TRAM-34是一种有效的、选择性的中电导Ca2+-activated K+channel(IKCa1,KCa3.1)抑制剂,具有高选择性和不抑制细胞色素P450的特点。与其他离子通道相比,TRAM-34的选择性高200到1500倍。在体外研究中,TRAM-34选择性抑制IKCa1而不会阻断细胞色素P450酶(CYP3A4)。TRAM-34还能有效抑制IKCa1转染的细胞中的IKCa1通道,以及人类T淋巴细胞和T84细胞中的IKCad电流。TRAM-34还能抑制人类T淋巴细胞的激活,对白血病细胞株的细胞学研究也具有潜力。此外,TRAM-34还能改善TGF-β1诱导的系膜细胞阻滞,减少细胞的早衰、表型转化和纤维样增生。

TRAM-34的应用领域

TRAM-34可用于白血病细胞株的细胞学研究。在对白血病细胞株HL-60的实验中,TRAM-34能够抑制细胞的增殖和侵袭能力,并诱导细胞凋亡和G0/G1期阻滞。此外,TRAM-34还能改善TGF-β1诱导的系膜细胞阻滞,减少细胞的早衰、表型转化和纤维样增生。研究结果表明,TRAM-34对于白血病细胞株的治疗具有潜在的临床应用价值。

参考文献

[1] Bradykinin-Induced Chemotaxis of Human Gliomas Requires the Activation of KCa3.1 and ClC-3.Cuddapah Vishnu Anand,Turner Kathryn L,Seifert Stefanie,Sontheimer Harald.The Journal of neuroscience:the official journal of the Society for Neuroscience.2013

[2] The inhibition of KCa3.1 channels activity reduces cell motility in glioblastoma derived cancer stem cells.Ruggieri Paola,Mangino Giorgio,Fioretti Bernard,Catacuzzeno Luigi,Puca Rosa,Ponti Donatella,Miscusi Massimo,Franciolini Fabio,Ragona Giuseppe,Calogero Antonella.PloS one.2012

[3] The Blockage of KCa 3.1 Channel inhibited proliferation,migration and promoted apoptosis of human hepatocellular carcinoma cells.Liu Y,Zhao L,Ma W,et al.Journal du Cancer.2015

[4] High expression of KCa3.1 in patients with clear cell renal carcinoma predicts high metastatic risk and poor survival.Rabjerg M,Olivan-Viguera A,Hansen LK,et al.Plo S One.2015

[5] The inhibition by oxaliplatin,a platinum-based anti-neoplastic agent,of the activity of intermediate-conductance Ca-(2+)-activated K-+channels in human glioma cells.Huang MH,Huang YM,Wu SN.Cellular Physiology and Biochemistry.2015

[6] Activation of K-+channel by 1-EBIO rescues the head and neck squamous cell carcinoma cells from Ca-(2+)ionophore-induced cell death.Yin MZ,Park SW,Kang TW,et al.Korean J Physiol Pharmacol.2016

[7] Targeting proliferation of chronic lymphocytic leukemia(CLL)cells through KCa3.1 blockade.Grossinger EM,Weiss L,Zierler S,et al.Leukemia.2014

[8] 姜天华,黄志刚.TRAM-34对白血病细胞株HL-60细胞增殖及侵袭的影响[J].中国实验血液学杂志,2017,25(01):104-109.

国内供应商(27家)
您可能感兴趣的问答
 
请填写举报原因
选择举报原因
 
增加悬赏
剩余能量值
能量值