相关实验视频
Updated: Jul 11, 2025

08:36
Scaled-Up Preparation of an Intermediate of Upatinib, ACT051-3
Published on: April 7, 2023
1.1K
JAKinibs的选择性,有效性和安全性:为一个仍在发展的故事提供新的证据
Michael Bonelli1, Andreas Kerschbaumer2, Kastriot Kastrati2
1Division of Rheumatology, Department of Internal Medicine III, Medical University of Vienna, Vienna, Austria michael.bonelli@meduniwien.ac.at.
Annals of the rheumatic diseases
|November 3, 2023
概括
细胞因子向疗法彻底改变了炎症疾病的治疗方法. 简氏酶抑制剂 (JAKinibs) 通过向共享信号通路,提供了一个新的范式,新的选择性JAKinibs旨在提高疗效和安全性.
科学领域:
- 免疫学 免疫学 免疫学
- 药理学 药理学是指药理学的学科.
- 类风湿病学 类风湿病学
背景情况:
- 细胞因子是类风湿性关节炎和牛皮等炎症性疾病的关键驱动因素.
- 了解细胞因子的作用导致了向治疗,改善了患者的治疗结果.
- 复杂的细胞因子相互作用需要更广泛的治疗策略,而不仅仅是单一目标阻塞.
研究的目的:
- 审查比较泛JAK抑制剂 (JAKinibs) 与选择性JAKinibs的证据.
- 总结最近关于JAKinibs新副作用和扩大指示的发现.
- 讨论JAKinibs在治疗包括COVID-19在内的炎症性疾病中的作用.
主要方法:
- 对JAK抑制剂的当前证据的文献综述.
- 分析临床试验数据和关于JAKinib疗效和安全性的已发表研究.
- 综合关于泛对选择性JAKinib机制和应用的信息.
主要成果:
- 由JAKinibs抑制的JAK-STAT通路代表了治疗炎症疾病的范式转变.
- 已批准多种JAKinib药物,并正在研究新的适用性.
- 第二代选择性JAKinibs正在开发中,以提高选择性并可能减少副作用.
结论:
- 雅基尼布已经改变了对炎症状况的治疗方法.
- 选择性JAKinibs的开发为改善治疗概况提供了希望.
- 目前正在进行的研究继续扩大对JAKinibs在各种疾病中的理解和应用.
更多相关视频
相关概念视频
The JAK-STAT Signaling Pathway
8.9K
Several cytokine receptors have tightly bound Janus kinase or JAK proteins attached at their cytosolic tail. Small signaling molecules such as cytokines, growth hormones, or prolactins bind to the cytokine receptors and initiate their dimerization. The dimerization brings the cytosolic JAKs together that trans-phosphorylate and activates each other. The activated JAKs now phosphorylate cytosolic tails of the cytokine receptors, which serve as binding sites for adaptor proteins such as SH2...
8.9K
Dose-Response Relationship: Selectivity and Specificity
6.8K
Drugs exert their therapeutic effects by interacting with receptors, enzymes, or ion channels that are present throughout the human body. The strength and duration of the interaction between a drug and its target receptor are characterized by the selectivity and specificity of the drug. Selectivity refers to a drug's strong preference for its intended target over other targets. For instance, isoprenaline, a non-selective β-adrenergic agonist, interacts with both β1- and...
6.8K
Dipeptidyl Peptidase 4 Inhibitors
191
Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a...
191
Dose-Response Relationship: Potency and Efficacy
4.5K
The potency of a drug is the measure of its ability to produce a biological response and can be compared by looking at the half-maximum effective concentration or EC50 values of different drugs. A lower EC50 value indicates higher potency of the drug. In the dose–response curve of two antihypertensive drugs, candesartan and irbesartan, a significant difference is observed in their EC50 values. A lower EC50 value for candesartan indicates that it is more potent than irbesartan, as it...
4.5K
Targeted Cancer Therapies
7.7K
The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
There are several types of targeted therapies against...
7.7K
Transducer Mechanism: Enzyme-Linked Receptors
2.5K
Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
Major types that are helpful drug targets include:
2.5K

