相关实验视频

Updated: Jul 9, 2025

Author Spotlight: Photodynamic Therapy as a Novel Approach to Induce Petite Colonies in Drug-Resistant Candida for Antifungal Research

Author Spotlight: Photodynamic Therapy as a Novel Approach to Induce Petite Colonies in Drug-Resistant Candida for Antifungal Research

Published on: March 29, 2024

3-基-3-甲基氨酸辅酶A降解酶的抑制剂降低了Candida glabrata和Candida albicans中的生长,欧戈斯特醇合成和小突变的产生

Dulce Andrade-Pavón¹, Eugenia Sánchez-Sandoval², Joaquín Tamariz³

¹Laboratorio de Biología Molecular de Bacterias y Levaduras, Departamento de Microbiología, Escuela Nacional de Ciencias Biológicas, Instituto Politécnico Nacional, Prolongación de Carpio y Plan de Ayala S/N, Col. Santo Tomás, Alc. Miguel Hidalgo, Ciudad de México 11340, Mexico.

International journal of molecular sciences

|December 9, 2023

概括

新的抗真菌化合物针对Candida物种中的HMGR显示出有希望. 这些抑制剂减少了酵母生长和厄戈斯特醇合成,同时产生了较少的抗药性小突变物,为阿佐醇提供了潜在的替代品.

科学领域:

药用化学医学化学
菌类学菌类学是指菌类学.
生物化学生化学

背景情况:

在Candida glabrata和Candida albicans中耐醇耐药性需要新的抗真菌策略.
抑制3 - 基-3 - 甲基氨酸共酶A减少酶 (HMGR) 的他类药物减少了酵母生长和厄戈斯特醇,但可以诱导DNA损伤和耐药性.
欧戈斯特醇对酵母细胞膜的完整性至关重要.

研究的目的:

为Candida物种合成新的HMGR抑制剂.
评估它们对酵母生长,厄戈斯特醇合成和小突变物生成的影响.
评估这些化合物作为未来抗真菌剂的潜力.

主要方法:

合成七个系列的HMGR抑制剂化合物.
对Candida glabrata和Candida albicans生长和厄戈斯特醇水平的复合作用的评估.
在酵母中评估小突变基因的产生.
在Pichia pastoris中重组CgHMGR的异构表达.
在体外酶抑制试验和结合能量的计算.

主要成果:

几个合成的HMGR抑制剂显示,与可纳和西姆瓦斯塔丁相比,降低了酵母生长和厄戈斯特醇合成.
新型抑制剂产生的微型突变物比参考药物少得多.
化合物1a,1b,6g和7a有效抑制了复合CgHMGR活性.
与α-asarone和simvastatin相比,这些化合物表现出更高的结合能.

结论:

新型HMGR抑制剂为开发新的抗真菌疗法提供了一个有前途的途径,用于对抗Candida物种.
这些化合物通过规避抗性机制,为醇提供了潜在的替代品.
化合物1a,1b,6g和7a是作为抗真菌药物的进一步临床前开发的强有力的候选者.

关键词:

在C. albicans中,它是最常见的.C. 格拉布拉塔 (C. glabrata) 是一种的动物.这就是HMGR.抗真菌剂是一种抗真菌剂.埃尔戈斯特醇合成纤维化物是一种纤维化物.小小的突变动物.酵母菌的生长酵母菌的生长这是一种α-asarone类似物.

更多相关视频

An Ex vivo Assay to Study Candida albicans Hyphal Morphogenesis in the Gastrointestinal Tract

An Ex vivo Assay to Study Candida albicans Hyphal Morphogenesis in the Gastrointestinal Tract

Published on: July 1, 2020

Small-Scale Plasma Membrane Preparation for the Analysis of Candida albicans Cdr1-mGFPHis

Small-Scale Plasma Membrane Preparation for the Analysis of Candida albicans Cdr1-mGFPHis

Published on: June 13, 2021

相关概念视频

Inhibition of Cdk Activity

Inhibition of Cdk Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...

Oral Hypoglycemic Agents: α-Glucosidase Inhibitors

Oral Hypoglycemic Agents: α-Glucosidase Inhibitors

α-glucosidase inhibitors, including acarbose (Precose), miglitol (Glyset), and voglibose (Voglib) (primarily available in Asia), are drugs that control blood sugar levels by delaying the digestion of starch and disaccharides. They achieve this by inhibiting α-glucosidase enzymes in the intestine, which slow the absorption of carbohydrates in the intestine, which in turn leads to a prolonged release of the glucoregulatory hormone GLP-1 from intestinal L-cells.
Acarbose and miglitol are...

Eukaryotic Transcription Inhibitors

Eukaryotic Transcription Inhibitors

Certain biochemical processes, such as embryonic development and cell growth regulation, depend on the repression of specific genes. DNA binding proteins known as eukaryotic transcription inhibitors regulate the repression of gene expression in eukaryotes. The presence of these inhibitors at the required location and time in the cell is triggered by the presence of hormones and additional signals from other cells.
Eukaryotic transcription inhibitors usually contain two distinct domains, a...