相关实验视频

Updated: Jul 28, 2025

An Orthotopic Bladder Cancer Model for Gene Delivery Studies

An Orthotopic Bladder Cancer Model for Gene Delivery Studies

Published on: December 1, 2013

激素LaSOM 335对膀癌细胞具有活性,干扰Let-60 (hRas) 并降低CD73的表达/活性

Luciano Porto Kagami¹, Itamar Luís Gonçalves^1,2, Álisson Coldebella da Silva³

¹Laboratório de Síntese Orgânica Medicinal - LaSOM®, Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Porto Alegre, Brazil.

Chemical biology & drug design

|June 5, 2023

概括

一种新型化合物,LaSOM 335,通过抑制Ras信号和CD73表达,对膀癌细胞表现出强烈的活性. 这种双二胺是安全的,也是膀癌治疗开发的有前途的候选人.

科学领域:

在瘤学瘤学.
分子生物学分子生物学
药物发现药物发现药物发现

背景情况:

膀癌是一种显著的恶性瘤,通常是由RAS瘤基因的突变驱动的.
准异常Ras蛋白功能是癌症治疗开发中的关键策略.
CD73在癌细胞生存,进展和迁移中起着至关重要的作用.

研究的目的:

为了研究新型双二胺的抗癌潜力,LaSOM 335.
评估该化合物对膀癌细胞的活性及其作用机制.
在临床前模型中评估LaSOM 335的安全性和有效性.

主要方法:

在体外细胞毒性测定中使用T24膀癌细胞和非癌细胞系.
在体内研究中,Cayenorhabditis elegans具有突变的let-60基因 (Ras homolog).
对CD73的酶活性和表达分析,以及对Ras-Raf-ERK通路的研究.

主要成果:

拉索姆335在T24膀癌细胞 (IC50 = 10.73 ± 0.53μM) 上表现出高活性,具有选择性.
该化合物抑制了C. elegans中的let-60基因活性,并在体内显示出安全性.
拉索姆335抑制了CD73的酶活性,并降低了它的表达,可能是通过EGFR/Ras-Raf-ERK通路.

结论:

拉索姆335具有显著的抗膀癌活性.
该化合物针对Ras信号和CD73两者,突出显示了一种双重的作用机制.
拉索姆335是进一步开发作为膀癌治疗药物的有希望的候选者.

关键词:

凯诺哈比迪斯的优雅的植物.CD73 CD73 CD73 CD73 CD73 CD73 CD73 CD73 CD73 CD73 CD73 拉索姆 335 5个字母 T24 膀癌细胞一个二二胺基子.ecto-5′-核酸酶的使用情况.

更多相关视频

Induction of Invasive Transitional Cell Bladder Carcinoma in Immune Intact Human MUC1 Transgenic Mice: A Model for Immunotherapy Development

Induction of Invasive Transitional Cell Bladder Carcinoma in Immune Intact Human MUC1 Transgenic Mice: A Model for Immunotherapy Development

Published on: October 30, 2013

Portal Vein Injection of Colorectal Cancer Organoids to Study the Liver Metastasis Stroma

Portal Vein Injection of Colorectal Cancer Organoids to Study the Liver Metastasis Stroma

Published on: September 3, 2021

相关概念视频

lncRNA - Long Non-coding RNAs

lncRNA - Long Non-coding RNAs

In humans, more than 80% of the genome gets transcribed. However, only around 2% of the genome codes for proteins. The remaining part produces non-coding RNAs which includes ribosomal RNAs, transfer RNAs, telomerase RNAs, and regulatory RNAs, among other types. A large number of regulatory non-coding RNAs have been classified into two groups depending upon their length – small non-coding RNAs, such as microRNA, which are less than 200 nucleotides in length, and long non-coding RNA...

Non-LTR Retrotransposons

Non-LTR Retrotransposons

As the name suggests, non-LTR retrotransposons lack the long terminal repeats characteristic of the LTR retrotransposons. Additionally, both LTR and non-LTR retrotransposons use distinct mechanisms of mobilization. Non-LTR retrotransposons are further divided into two classes - Long interspersed nuclear elements (LINEs) and short interspersed nuclear elements (SINEs), both of which occur abundantly in most mammals, including humans. Some of the active non-LTR retrotransposons in humans are L1...