Polymorphic variants of CYP2C9: mechanisms involved in reduced catalytic activity [0.03%]
CYP2C9多态性变异：催化活性降低的机制参与因素分析
Lian Wei,Charles W Locuson,Timothy S Tracy
Lian Wei
CYP2C9 catalyzes the demethylation of the biphasic kinetics substrate (S)-naproxen, and the CYP2C9*2 (R144C) and CYP2C9*3 (I359L) variants are associated with lower rates of (S)-naproxen demethylation. To assess the reasons for these reduct...
Capacitative calcium entry contributes to the differential transactivation of the epidermal growth factor receptor in response to thiazolidinediones [0.03%]
硫氮杂卓类化合物不同活化表皮生长因子受体的反应中电容性钙流入起到了重要作用
Brian J Dewar,Olivia S Gardner,Ching-Shih Chen et al.
Brian J Dewar et al.
Thiazolidinediones (TZDs) are synthetic ligands for the peroxisome proliferator-activated receptor gamma (PPARgamma) but also elicit PPARgamma-independent effects, most notably activation of mitogen-activated protein kinases (MAPKs). Ciglit...
CCAAT/enhancer binding protein homologous protein-dependent death receptor 5 induction and ubiquitin/proteasome-mediated cellular FLICE-inhibitory protein down-regulation contribute to enhancement of tumor necrosis factor-related apoptosis-inducing ligand-induced apoptosis by dimethyl-celecoxib in human non small-cell lung cancer cells [0.03%]
二甲基塞来昔布通过诱导死亡受体5并下调细胞FLICE抑制蛋白增强肿瘤坏死因子相关凋亡诱导配体在人非小细胞肺癌中的促凋亡作用的CCAAT/增强子结合蛋白同源蛋白依赖机制
Shuzhen Chen,Xiangguo Liu,Ping Yue et al.
Shuzhen Chen et al.
2,5-Dimethyl-celecoxib (DMC) is a derivative of celecoxib, a cyclooxygenase-2 (COX-2) inhibitor with anticancer activity in both preclinical studies and clinical practice, and lacks COX-2-inhibitory activity. Several preclinical studies hav...
Comparative Study
Molecular pharmacology. 2007 Nov;72(5):1269-79. DOI:10.1124/mol.107.037465 2007
Purinergic 2X1 receptors mediate endothelial dependent vasodilation to ATP [0.03%]
腺苷三磷酸介导的内皮依赖性血管舒张涉及嘌呤能2X1受体
L S Harrington,R J Evans,J Wray et al.
L S Harrington et al.
ATP is an important endogenous mediator in the cardiovascular system. It induces endothelium dependent vasodilation, but the precise receptor pathway activated in this response is currently under debate. We have used traditional bioassay te...
8-benzyl-4-oxo-8-azabicyclo[3.2.1]oct-2-ene-6,7-dicarboxylic acid (SD-1008), a novel janus kinase 2 inhibitor, increases chemotherapy sensitivity in human ovarian cancer cells [0.03%]
8-苯甲基-4-氧代-8-aza-bicyclo[3.2.1]辛-2-烯-6,7-二羧酸（SD-1008），一种新型Janus激酶2抑制剂，可以增强人卵巢癌细胞的化疗敏感性
Zhenfeng Duan,James Bradner,Edward Greenberg et al.
Zhenfeng Duan et al.
Interleukin 6 and the signal transducer and activator of transcription (STAT) 3 proteins have important roles in cancer cell survival and proliferation. Recent studies demonstrate that abnormal STAT3 activation promotes tumor growth and sup...
Pharmacological characterization and molecular determinants of the activation of transient receptor potential V2 channel orthologs by 2-aminoethoxydiphenyl borate [0.03%]
2-氨基乙氧基二苯基硼酸激活瞬时受体电位V2通道同工酶的药理学特征和分子决定因素
Véronique Juvin,Aubin Penna,Jean Chemin et al.
Véronique Juvin et al.
Despite its expression in different cell types, transient receptor potential V2 (TRPV2) is still the most cryptic members of the TRPV channel family. 2-Aminoethoxydiphenyl borate (2APB) has been shown to be a common activator of TRPV1, TRPV...
2-amino-N-{4-[5-(2-phenanthrenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]-phenyl} acetamide (OSU-03012), a celecoxib derivative, directly targets p21-activated kinase [0.03%]
2-氨基-N-{4-[5-(2-菲苯并)-3-(三氟甲基)-1H-吡唑-1-基]苯基}乙酰胺(OSU-03012)，一种塞来昔布衍生物，可直接靶向p21激活的激酶
Leonardo M Porchia,Marcy Guerra,Yu-Chieh Wang et al.
Leonardo M Porchia et al.
p21-Activated kinases (PAKs) are regulators of cell motility and proliferation. PAK activity is regulated in part by phosphoinositide-dependent kinase 1 (PDK1). We hypothesized that reduced PAK activity was involved in the effects of 2-amin...
Inhibition of trail gene expression by cyclopentenonic prostaglandin 15-deoxy-delta12,14-prostaglandin J2 in T lymphocytes [0.03%]
环戊内前列腺素15-脱氧精氨前列腺素J2抑制T淋巴细胞中TRAIL基因的表达
Cinzia Fionda,Filomena Nappi,Mario Piccoli et al.
Cinzia Fionda et al.
15-Deoxy-Delta(12,14)-prostaglandin J(2) (15d-PGJ(2)) is a cyclopentenonic prostaglandin endowed with powerful anti-inflammatory activities, as shown in animal models of inflammatory/autoimmune diseases, where pharmacological administration...
Peroxisomal proliferator-activated receptor-alpha protects renal tubular cells from doxorubicin-induced apoptosis [0.03%]
过氧化物酶体增殖激活受体-α保护肾小管细胞免于阿霉素诱导的凋亡
Heng Lin,Chun-Cheng Hou,Ching-Feng Cheng et al.
Heng Lin et al.
Peroxisome proliferator-activated receptor-alpha (PPAR-alpha) is a transcription factor and has been reported to inhibit cisplatin-mediated proximal tubule cell death. In addition, doxorubicin (Adriamycin)-induced nephrosis in rats is a com...
Identification of two new synthetic histone deacetylase inhibitors that modulate globin gene expression in erythroid cells from healthy donors and patients with thalassemia [0.03%]
两种新的组蛋白去乙酰化酶抑制剂的鉴定及其调节健康供体和地中海贫血患者红细胞系中珠蛋白基因表达的作用机制研究
Antonello Mai,Katija Jelicic,Dante Rotili et al.
Antonello Mai et al.
We have identified two new histone deacetylase (HDAC) inhibitors (9 and 24) capable of inducing the expression of gamma-globin and/or beta-globin promoter-driven reporter genes in a synthetic model of Hb switch. Both compounds also increase...