Design and evaluation of highly selective histone deacetylase 6 inhibitors derived from the natural product tryptoline [0.03%]
基于天然产物四氢异吡喃并咔吨衍生物的高效高选择性HDAC6抑制剂的设计与评价研究
Khan Hashim Ali,Chiranjeev Sharma,Yong Jin Oh et al.
Khan Hashim Ali et al.
The development of isoform-selective histone deacetylase (HDAC) inhibitors offers a promising approach to minimize the adverse effects of nonselective HDAC inhibitors. HDAC6, due to its unique structural and functional properties, regulates...
Molecular determinants of 2-aminoethoxydiphenyl borate sensitivity of transient receptor potential vanilloid 2-unexpected differences between 2 rodent orthologs [0.03%]
瞬时受体电位香草素2对2-氨基乙氧基二苯基硼酸敏感性的分子决定因素-两个正交同源物之间的意外差异
Tabea C Fricke,Anna Rämisch,Ruth A Pumroy et al.
Tabea C Fricke et al.
Transient receptor potential vanilloid 2 (TRPV2) is relevant for diseases like cancer, cardiac dysfunction, and infection, warranting drug development targeting TRPV2. However, this has been complicated by the lack of good modulators target...
Corticosterone stimulates synthesis of 2-arachidonoylglycerol via putative membrane-bound glucocorticoid receptors and inhibits GABA release via CB1 cannabinoid receptors in the ventrolateral periaqueductal gray [0.03%]
皮质酮通过假定的膜结合糖皮质激素受体刺激黑质腹外侧2-花生四烯酸甘油合成并抑制GABA释放：CB1大麻素受体的作用
Basile Coutens,Courtney A Bouchet,Lorenzo C Patti et al.
Basile Coutens et al.
The ventrolateral periaqueductal gray (vlPAG) plays a critical role in pain modulation. GABAergic neurotransmission within the vlPAG regulates the descending pain pathway. This study investigates the mechanisms through which corticosterone ...
The thiazolidinedione drug troglitazone inhibits Gq signaling through direct binding to the Gq alpha subunit through inhibition of GDP release [0.03%]
噻唑烷二酮类药物曲格列酮通过直接与Gq α亚基结合抑制Gq信号转导并通过抑制GDP释放发挥作用
Naiem T Issa,Tingzhen Shen,Alexander Vizurraga et al.
Naiem T Issa et al.
The cycle of GTP binding and hydrolysis controls heterotrimeric G proteins, and mutations reducing GTPase activity result in constitutive G protein signaling. In Gαq (gene: GNAQ) such mutations cause uveal melanoma and Sturge-Weber syndrom...
Comparative evaluation of the biological characteristics of a novel retinoid X receptor agonist and bexarotene [0.03%]
新型视黄酸X受体激动剂与贝沙罗汀生物学特性的比较评价研究
Koji Tomita,Ken-Ichi Nakashima,Eiji Yamaguchi et al.
Koji Tomita et al.
The retinoid X receptor (RXR) belongs to the nuclear receptor superfamily, which regulates various physiological processes. RXR agonists, classified as rexinoids, exhibit selectivity for RXR over the retinoic acid receptor and have therapeu...
Progress toward new function and design of extracellular G protein-coupled receptor nanobodies [0.03%]
外源G蛋白偶联受体纳米抗体新功能和设计研究进展
Roman R Schlimgen,Brian F Volkman
Roman R Schlimgen
Antibodies have played a pivotal role in G protein-coupled receptor (GPCR) research and drug development. Nanobodies, or variable domain heavy chain-only antibodies, have emerged as a next-generation antibody with unique advantages in targe...
An overview of autophagy inhibition as a potential clinical strategy in cancer therapy [0.03%]
概述自噬抑制在癌症治疗中的潜在临床策略
Ahmed M Elshazly,Nayyerehalsadat Hosseini,Aya A Elzahed et al.
Ahmed M Elshazly et al.
Autophagy is a cellular process responsible for the recycling of misfolded proteins and damaged organelles, contributing to cellular homeostasis and energy production. Tumor cells often exploit this mechanism, particularly through the form ...
Investigation of the binding mode of clobenprobit at CXCR4 and development of novel anti-inflammatory compounds with enhanced activity and minimal antagonist effects [0.03%]
克洛苯丙比特与CXCR4的结合模式研究及新型抗炎活性增强和拮抗作用最小化化合物的研发
Birgit Caspar,Nassima Bekaddour,Séverine Grinberg et al.
Birgit Caspar et al.
IT1t and clobenprobit (CB) have been shown to act as anti-inflammatory compounds in dependence of the chemokine receptor C-X-C receptor type 4 (CXCR4) in model systems. Here, the direct interaction between CB and CXCR4 is demonstrated via i...
Chemokine receptors - Exemplifying functional divergence in G protein-coupled receptors [0.03%]
趋化因子受体-G蛋白偶联受体功能分化典范
Omolade Otun,Sébastien Granier,Thierry Durroux et al.
Omolade Otun et al.
G protein-coupled receptors are known for their ability to generate a wide range of functional responses through interaction with various intracellular partners. This versatility is particularly evident within the chemokine receptor family,...
Molecular and cellular effects of hydroxy-1,4 naphthoquinones used in dermatological and cosmetic applications on human protein tyrosine phosphatase PTP1B in human keratinocytes [0.03%]
羟基-1,4萘醌类化合物在皮肤病学和化妆品应用中对人角质形成细胞蛋白酪氨酸磷酸酶PTP1B的分子及细胞作用效应
Tessa Arnaud,Christina Michail,Joséphine Gudin de Vallerin et al.
Tessa Arnaud et al.
The hydroxy-1,4-naphthoquinones-lawsone, juglone, and plumbagin-widely used in dermatological and cosmetic applications, exhibit a broad spectrum of biological activities, including notable cytotoxic effects. Of the various cellular process...