Suramin Inhibits Osteoarthritic Cartilage Degradation by Increasing Extracellular Levels of Chondroprotective Tissue Inhibitor of Metalloproteinases 3 [0.03%]
硫酸长春新碱通过增加软骨保护性基质金属蛋白酶抑制剂3的细胞外水平来抑制骨关节炎软骨降解
Anastasios Chanalaris,Christine Doherty,Brian D Marsden et al.
Anastasios Chanalaris et al.
Osteoarthritis is a common degenerative joint disease for which no disease-modifying drugs are currently available. Attempts to treat the disease with small molecule inhibitors of the metalloproteinases that degrade the cartilage matrix hav...
The Actions of Drug Combinations on the GABAA Receptor Manifest as Curvilinear Isoboles of Additivity [0.03%]
药物复合物作用于GABAA受体表现为加和性的抛物线等效剂量线(isobole)
Daniel J Shin,Allison L Germann,Joe Henry Steinbach et al.
Daniel J Shin et al.
Drug interactions are often analyzed in terms of isobolograms. In the isobologram, the line connecting the axial points corresponding to the concentrations of two different drugs that produce an effect of the same magnitude is termed an iso...
Molecular Mechanism of Taurocholate Transport by the Bile Salt Export Pump, an ABC Transporter Associated with Intrahepatic Cholestasis [0.03%]
与肝内胆汁淤积相关的胆盐出口泵的ABC转运蛋白的牛磺胆酸运输分子机制
Muhammad Imran Sohail,Diethart Schmid,Katrin Wlcek et al.
Muhammad Imran Sohail et al.
The bile salt export pump (BSEP/ABCB11) transports bile salts from hepatocytes into bile canaliculi. Its malfunction is associated with severe liver disease. One reason for functional impairment of BSEP is systemic administration of drugs, ...
Human Missense Mutations in Regulator of G Protein Signaling 2 Affect the Protein Function Through Multiple Mechanisms [0.03%]
人类G蛋白信号调节因子2错义突变通过多种机制影响蛋白质功能
Hoa T N Phan,Benita Sjögren,Richard R Neubig
Hoa T N Phan
Regulator of G protein signaling 2 (RGS2) plays a significant role in alleviating vascular contraction and promoting vascular relaxation due to its GTPase accelerating protein activity toward Gαq. Mice lacking RGS2 display a hypertensive p...
Nitro-Oleic Acid Regulates Endothelin Signaling in Human Endothelial Cells [0.03%]
硝基油酸调节内皮素在人血管内皮细胞中的信号作用
Emilia Kansanen,Suvi M Kuosmanen,Anna-Kaisa Ruotsalainen et al.
Emilia Kansanen et al.
Nitro-fatty acids are reactive signaling mediators that are formed when unsaturated fatty acids react with nitric oxide or nitric oxide-derived species. Nitro-fatty acids can modify specific signaling pathways via post-translational modific...
Zijian Li
Zijian Li
A receptor is a protein molecule that receives chemical signals from outside a cell, which enables the cell to respond to the signal molecule. Receptors mediate numerous important physiologic effects upon binding extracellular agonists. How...
Structural Determinants for the Selectivity of the Positive KCa3.1 Gating Modulator 5-Methylnaphtho[2,1- d]oxazol-2-amine (SKA-121) [0.03%]
5-甲基萘并[2,1- d ]恶唑-2-胺（SKA-121）作为KCa3.1通道正向门控调节剂的选择性结构决定因素
Brandon M Brown,Heesung Shim,Miao Zhang et al.
Brandon M Brown et al.
Intermediate-conductance (KCa3.1) and small-conductance (KCa2) calcium-activated K+ channels are gated by calcium binding to calmodulin (CaM) molecules associated with the calmodulin-binding domain (CaM-BD) of these channels. The existing K...
A Novel Selective Inverse Agonist of the CB2 Receptor as a Radiolabeled Tool Compound for Kinetic Binding Studies [0.03%]
一种新型的选择性CB2受体放射性配体结合研究工具化合物-inverse激动剂
Andrea Martella,Huub Sijben,Arne C Rufer et al.
Andrea Martella et al.
The endocannabinoid system, and in particular the cannabinoid type 2 receptor (CB2R), raised the interest of many medicinal chemistry programs for its therapeutic relevance in several (patho)physiologic processes. However, the physico-chemi...
Altenusin, a Nonsteroidal Microbial Metabolite, Attenuates Nonalcoholic Fatty Liver Disease by Activating the Farnesoid X Receptor [0.03%]
非甾体微生物代谢产物阿尔特奴辛通过激活法尼醇X受体抑制非酒精性脂肪肝病
Zhihui Zheng,Zanmei Zhao,Shuqiang Li et al.
Zhihui Zheng et al.
Nonalcoholic fatty liver disease (NAFLD) is a prevalent chronic liver disease. The incidence of NAFLD has increased steadily due to its close association with the global epidemic of obesity and type 2 diabetes. However, there is no effectiv...
Splice Variants of pH-Sensitive Chloride Channel Identify a Key Determinant of Ivermectin Sensitivity in the Larvae of the Silkworm Bombyx mori [0.03%]
pH敏感性氯通道的拼接变异体确定了家蚕Bo-mori幼虫中伊维菌素敏感性的关键决定因素
Daiki Okuhara,Shogo Furutani,Katsuhiko Ito et al.
Daiki Okuhara et al.
The pH-sensitive chloride channels (pHCls) are broadly expressed in insects, but little is known about their physiologic role, diversity, and sensitivity to insecticides acting on relevant chloride channels. Here we have sequenced 50 transc...