Identification of regions of the sigma-1 receptor ligand binding site using a novel photoprobe [0.03%]
一种新型光探针鉴定σ-1受体配体结合位点的区域
Arindam Pal,Abdol R Hajipour,Dominique Fontanilla et al.
Arindam Pal et al.
sigma Receptors, once considered a class of opioid receptors, are now regarded as a unique class of receptors that contain binding sites for a wide range of ligands, including the drug 1-N(2',6'-dimethylmorpholino)3-(4-t-butylpropylamine) (...
Separating transrepression and transactivation: a distressing divorce for the glucocorticoid receptor? [0.03%]
糖皮质激素受体的抑制作用与激活作用分离：一场令人痛苦的离婚？
Robert Newton,Neil S Holden
Robert Newton
Glucocorticoids (corticosteroids) are highly effective in combating inflammation in the context of a variety of diseases. However, clinical utility can be compromised by the development of side effects, many of which are attributed to the a...
Identification of a Bis-guanylhydrazone [4,4'-Diacetyldiphenylurea-bis(guanylhydrazone); NSC 109555] as a novel chemotype for inhibition of Chk2 kinase [0.03%]
一种双胍基腙[乙酰二苯甲脲双胍基腙;NSC 109555] USA)作为抑制Chk2激酶的新化学类型的确证研究
Andrew G Jobson,John H Cardellina nd,Dominic Scudiero et al.
Andrew G Jobson et al.
Chk2 is a protein kinase involved in the ATM-dependent checkpoint pathway (http://discover.nci.nih.gov/mim). This pathway is activated by genomic instability and DNA damage and results in either cell cycle arrest, to allow DNA repair to occ...
Induction of glutathione transferase in insulin-like growth factor type I receptor-overexpressed hepatoma cells [0.03%]
胰岛素样生长因子-I受体在肝癌细胞过表达中的作用及机制研究诱导GST的表达
Jeong Yong Lee,Chang Yeob Han,Jin Won Yang et al.
Jeong Yong Lee et al.
Insulin-like growth factor type I receptor (IGF-IR) is frequently overexpressed in human hepatocellular carcinoma cells (HCC), and this overexpression has been correlated with increased tumor growth. The protective response of HCC to reacti...
Application of beta-lactamase enzyme complementation to the high-throughput screening of toll-like receptor signaling inhibitors [0.03%]
β内酰胺酶补体技术在 toll 样受体信号通路抑制剂高通量筛选中的应用研究
Hyun-Ku Lee,Steven J Brown,Hugh Rosen et al.
Hyun-Ku Lee et al.
We describe a successful application of beta-lactamase fragment complementation to high-throughput screening (HTS) for Toll-like receptor 4 (TLR4) signaling inhibitors. We developed a stable cell line, HeLa/CL3-4, expressing MyD88/Bla(a) an...
Disruption of oligomerization induces nucleocytoplasmic shuttling of leukemia-associated rho Guanine-nucleotide exchange factor [0.03%]
寡聚化障碍诱导白血病相关Rho鸟苷酸交换因子核质穿梭现象发生
Elda Grabocka,Philip B Wedegaertner
Elda Grabocka
The rgsRhoGEFs comprise a subfamily of three guanine nucleotide exchange factors, which function in linking heterotrimeric G-proteins to the monomeric RhoGTPase. Here, we reveal the novel finding that oligomerization of leukemia-associated ...
Structural determinates for apolipoprotein E-derived peptide interaction with the alpha7 nicotinic acetylcholine receptor [0.03%]
与α7烟碱型乙酰胆碱受体结合的载脂蛋白E衍生肽的结构决定簇
Elaine A Gay,Rachelle J Bienstock,Patricia W Lamb et al.
Elaine A Gay et al.
Neuronal nicotinic acetylcholine receptor (nAChR) signaling has been implicated in a variety of normal central nervous system (CNS) functions as well as an array of neuropathologies. Previous studies have demonstrated both neurotoxic and ne...
Insulin facilitates the hepatic clearance of plasma amyloid beta-peptide (1 40) by intracellular translocation of low-density lipoprotein receptor-related protein 1 (LRP-1) to the plasma membrane in hepatocytes [0.03%]
胰岛素通过向肝细胞质膜转运低密度脂蛋白受体相关蛋白1促进肝脏对血浆淀粉样β肽的清除作用
Chihiro Tamaki,Sumio Ohtsuki,Tetsuya Terasaki
Chihiro Tamaki
The hepatic clearance of amyloid beta-peptide (1-40) [Abeta(1-40)] from plasma, which is largely mediated by low-density lipoprotein receptor-related protein (LRP-1), is suggested to play a role in preventing Abeta(1-40) accumulation in the...
Antithrombotic effect of a protein-type I class snake venom metalloproteinase, kistomin, is mediated by affecting glycoprotein Ib-von Willebrand factor interaction [0.03%]
一种蛋白质I类蛇毒金属蛋白酶Kistomin的抗血栓作用通过影响糖蛋白I-血管性假血友病因子之间的相互作用实现
Chun-Chieh Hsu,Wen-Bin Wu,Ya-Hui Chang et al.
Chun-Chieh Hsu et al.
Binding of von Willebrand factor (vWF) to platelet glycoprotein (GP) Ib-IX-V mediates platelet activation in the early stage of thrombus formation. Kistomin, a snake venom metalloproteinase (SVMP) purified from venom of Calloselasma rhodost...
Activation of the adenosine A1 receptor inhibits HIV-1 tat-induced apoptosis by reducing nuclear factor-kappaB activation and inducible nitric-oxide synthase [0.03%]
腺苷A1受体活化通过减少核转录因子κB的活化和诱导型一氧化氮合酶的表达抑制HIV-1-TAT引发的细胞凋亡
Sandeep C Pingle,Sarvesh Jajoo,Debashree Mukherjea et al.
Sandeep C Pingle et al.
Human immunodeficiency virus dementia (HIV-D) is a nonfocal central nervous system manifestation characterized by cognitive, behavioral, and motor abnormalities. The pathophysiology of neuronal damage in HIV-D includes a direct toxic effect...