The human UDP-glucuronosyltransferase: identification of key residues within the nucleotide-sugar binding site [0.03%]
人类UDPG结合型葡萄糖醛酸转移酶中核苷酸糖结合部位关键残基的鉴定
Anne-Sisko Patana,Mika Kurkela,Adrian Goldman et al.
Anne-Sisko Patana et al.
UDP-glucuronosyltransferases (UGTs) play important roles in the metabolism, detoxification,and clearance of many different xenobiotics, including drugs and endogenous compounds. Structural information about these membrane-bound enzymes of t...
Comparative Study
Molecular pharmacology. 2007 Sep;72(3):604-11. DOI:10.1124/mol.107.036871 2007
Low-dose BBR3610 toxicity in colon cancer cells is p53-independent and enhanced by inhibition of epidermal growth factor receptor (ERBB1)-phosphatidyl inositol 3 kinase signaling [0.03%]
小剂量BBR3610对结肠癌细胞的毒性作用不受P53的影响且该毒性作用可通过抑制表皮生长因子受体（ERBB1）-磷脂酰肌醇3激酶信号通路得到增强
Clint Mitchell,Peyman Kabolizadeh,John Ryan et al.
Clint Mitchell et al.
We have examined the mechanisms by which the multinuclear platinum chemotherapeutic BBR3610 kills human colon cancer cells. BBR3610 more efficiently killed HCT116, DLD1, SW480, and HT29 cells than BBR3464, cisplatin, or oxaliplatin. The amo...
Perturbation of dopamine metabolism by 3-amino-2-(4'-halophenyl)propenes leads to increased oxidative stress and apoptotic SH-SY5Y cell death [0.03%]
3-氨基-2-(4'-卤代苯基)丙烯对多巴胺代谢的干扰导致氧化应激加剧和SH-SY5Y细胞凋亡死亡
Warren C Samms,Rohan P Perera,D S Wimalasena et al.
Warren C Samms et al.
We have recently characterized a series of 3-amino-2-phenyl-propene (APP) derivatives as reversible inhibitors for the bovine adrenal chromaffin granule vesicular monoamine transporter (VMAT) that have been previously characterized as poten...
Phosphorylation of Galphas influences its association with the micro-opioid receptor and is modulated by long-term morphine exposure [0.03%]
Galphas磷酸化影响其与μ-阿片受体的结合并可受到长期阿片暴露的影响
Sumita Chakrabarti,Alan R Gintzler
Sumita Chakrabarti
The recent biochemical demonstration of the association of the mu-opioid receptor (MOR) with Galpha(s) that increases after long-term morphine treatment (Mol Brain Res 135:217-224, 2005) provides a new imperative for studying MOR-Galpha(s) ...
Nicotine glucuronidation and the human UDP-glucuronosyltransferase UGT2B10 [0.03%]
尼古丁葡萄糖醛酸结合反应及人类UDP-葡萄糖醛酸转移酶UGT2B10
Sanna Kaivosaari,Päivi Toivonen,Leah M Hesse et al.
Sanna Kaivosaari et al.
Nicotine biotransformation affects the smoking habits of addicted individuals and therefore their health risk. Using an improved analytical method, we have discovered that the human UDP-glucuronosyltransferase (UGT) 2B10, a liver enzyme pre...
Comparative Study
Molecular pharmacology. 2007 Sep;72(3):761-8. DOI:10.1124/mol.107.037093 2007
Human pregnane X receptor antagonists and agonists define molecular requirements for different binding sites [0.03%]
人类孕烷X受体拮抗剂和激动剂定义了不同结合位点的分子需求
Sean Ekins,Cheng Chang,Sridhar Mani et al.
Sean Ekins et al.
The pregnane X receptor (PXR) is an important transcriptional regulator of the expression of xenobiotic metabolism and transporter genes. The receptor is promiscuous, binding many structural classes of molecules that act as agonists at the ...
Discovery of a highly active ligand of human pregnane x receptor: a case study from pharmacophore modeling and virtual screening to "in vivo" biological activity [0.03%]
人孕烷x受体高效配体的发现——从药效团建模和虚拟筛选到“体内”生物学活性的一个案例研究
Géraldine Lemaire,Cindy Benod,Virginie Nahoum et al.
Géraldine Lemaire et al.
The human pregnane X receptor (hPXR) is a nuclear receptor that regulates the expression of phase I and II drug-metabolizing enzymes as well as that of drug transporters. In addition, this receptor plays a critical role in cholesterol homeo...
Comparative Study
Molecular pharmacology. 2007 Sep;72(3):572-81. DOI:10.1124/mol.106.033415 2007
Substrate specificities of g protein-coupled receptor kinase-2 and -3 at cardiac myocyte receptors provide basis for distinct roles in regulation of myocardial function [0.03%]
心肌细胞受体的G蛋白偶联受体激酶-2和-3的底物特异性为其在心肌功能调节中的不同作用提供了理论依据
Leif Erik Vinge,Kjetil W Andressen,Toril Attramadal et al.
Leif Erik Vinge et al.
The closely related G protein-coupled receptor kinases GRK2 and GRK3 are both expressed in cardiac myocytes. Although GRK2 has been extensively investigated in terms of regulation of cardiac beta-adrenergic receptors, the substrate specific...
Thiazolidinediones modulate the expression of beta-catenin and other cell-cycle regulatory proteins by targeting the F-box proteins of Skp1-Cul1-F-box protein E3 ubiquitin ligase independently of peroxisome proliferator-activated receptor gamma [0.03%]
噻唑烷二酮通过独立于过氧化物酶体增殖激活受体γ作用靶向Skp1-Cul1-F-box蛋白E3泛素连接酶的F-box蛋白来调节β-连环蛋白和其他细胞周期调节蛋白的表达
Shuo Wei,Li-Fang Lin,Chih-Cheng Yang et al.
Shuo Wei et al.
Considering the role of aberrant beta-catenin signaling in tumorigenesis, we investigated the mechanism by which the peroxisome proliferator-activated receptor gamma (PPARgamma) agonist troglitazone facilitated beta-catenin down-regulation....
Functional characterization of the promoter of human carbonyl reductase 1 (CBR1). Role of XRE elements in mediating the induction of CBR1 by ligands of the aryl hydrocarbon receptor [0.03%]
人型醛酮还原酶1(CBR1)启动子的功能表征。XRE元件在CBR1的诱导物介导CBR1诱导中的作用
Sukhwinder S Lakhman,Xiaomin Chen,Vanessa Gonzalez-Covarrubias et al.
Sukhwinder S Lakhman et al.
Human carbonyl reductase 1 (CBR1) metabolizes a variety of substrates, including the anticancer doxorubicin and the antipsychotic haloperidol. The transcriptional regulation of CBR1 has been largely unexplored. Therefore, we first investiga...