一二三四区视频,亚洲少妇熟女色,日本久热无码视频网,欧美国产日韩大尺度,亚洲a视频,久久少妇一区二区,日韩999无码视频,刺激久久久久久久,啊啊啊啊不要啊在线

ChemicalBook >> journal list >> Cell Reports Medicine >>article
Cell Reports Medicine

Cell Reports Medicine

IF: 11.7
Download PDF

Entrectinib inhibits NLRP3 inflammasome and inflammatory diseases by directly targeting NEK7.

Published:19 December 2023 DOI: 10.1016/j.xcrm.2023.101310
Xiangyu Jin, Didi Liu, Xinru Zhou, Xianyu Luo, Qian Huang, Yi Huang

Abstract

Excessive inflammation caused by abnormal activation of the NLRP3 inflammasome contributes to the pathogenesis of multiple human diseases, but clinical drugs targeting the NLRP3 inflammasome are still not available. In this study, we identify entrectinib (ENB), a US Food and Drug Administration (FDA)-approved anti-cancer agent, as a target inhibitor of the NLRP3 inflammasome to treat related diseases. ENB specifically blocks NLRP3 without affecting activation of other inflammasomes. Furthermore, we demonstrate that ENB directly binds to arginine 121 (R121) of NEK7 and blocks the interaction between NEK7 and NLRP3, thereby inhibiting inflammasome assembly and activation. In?vivo studies show that ENB has a significant ameliorative effect on mouse models of NLRP3 inflammasome-related diseases, including lipopolysaccharide (LPS)-induced systemic inflammation, monosodium urate (MSU)-induced peritonitis, and high-fat diet (HFD)-induced type 2 diabetes (T2D). These data show that ENB is a targeted inhibitor of NEK7 with strong anti-NLRP3 inflammasome activity, making it a potential candidate drug for the treatment of inflammasome-related diseases.

Substances (36)

Materials Related products
Procduct Name CAS Molecular Formula Supplier Price
LOXO-101 1223403-58-4 C21H22F2N6O2 242 suppliers $19.00-$2841.00
LOXO-101 1223403-58-4 C21H22F2N6O2 242 suppliers $19.00-$2841.00
LOXO-101 1223403-58-4 C21H22F2N6O2 242 suppliers $19.00-$2841.00
LOXO-101 1223403-58-4 C21H22F2N6O2 242 suppliers $19.00-$2841.00
Entrectinib 1108743-60-7 C31H34F2N6O2 222 suppliers $10.00-$1397.00
Entrectinib 1108743-60-7 C31H34F2N6O2 222 suppliers $10.00-$1397.00
Entrectinib 1108743-60-7 C31H34F2N6O2 222 suppliers $10.00-$1397.00
Entrectinib 1108743-60-7 C31H34F2N6O2 222 suppliers $10.00-$1397.00
Repotrectinib 1802220-02-5 C18H18FN5O2 192 suppliers $8.00-$1600.00
Repotrectinib 1802220-02-5 C18H18FN5O2 192 suppliers $8.00-$1600.00

Similar articles

IF:2.9

TLR4 Inhibitor TAK‐242 Protected Henoch–Schonlein Purpura Nephritis in Rats by Regulating Inflammatory Response and Immune Competence via NF‐ κB/NLRP3 Signalling

Clinical and Experimental Pharmacology and Physiology Yirong Liu, Qiong Wu,etc Published: 20 November 2024
IF:5.4

Protective effects and mechanism of puerarin targeting PI3K/Akt signal pathway on neurological diseases.

ACS Applied Energy Materials Qian Wang, Zi-Nuo Shen,etc Published: 24 October 2022
IF:4.3

The Pharmacological Effect of Hemin in Inflammatory-Related Diseases: A Systematic Review

ACS Applied Electronic Materials Jo?o Estarreja, Gon?alo Caldeira,etc Published: 18 April 2024
鹤山市| 临邑县| 湖北省| 调兵山市| 湘潭市| 沅江市| 沂源县| 禄劝| 万山特区| 德格县| 延吉市| 互助| 文登市| 五常市| 红河县| 烟台市| 舟曲县| 贺州市| 彩票| 鹤壁市| 临沧市| 墨江| 枞阳县| 安乡县| 班戈县| 酉阳| 天津市| 伽师县| 曲沃县| 普洱| 海原县| 盐池县| 溆浦县| 灵川县| 龙泉市| 浑源县| 三江| 盐山县| 阳谷县| 东乌珠穆沁旗| 慈利县|