- ABT-869, a Multitargeted Receptor Tyrosine Kinase Inhibitor, Reduces Tumor Microvascularity and Improves Vascular Wall Integrity in Preclinical Tumor Models
[作者:Jiang, F; Albert, DH; Luo, YP; Tapang, P; Zhang, K; Davidsen, SK; Fox, GB; Lesniewski, R; McKeegan, EM,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:134-142 , 文章类型: Article,,卷期:2011年338-1]
- N-[4-(3-amino-1H-indazol-4-yl)phenyl]-N1-(2-fluoro-5-methyl phenyl)-urea (ABT-869) is a novel multitargeted receptor tyrosine kinase inhibitor that demonstrates single-agent activity in preclinical studies and has underg...
- Retinol-Binding Protein 4 and Peroxisome Proliferator-Activated Receptor-gamma in Steatotic Liver Transplantation
[作者:Casillas-Ramirez, A; Alfany-Fernandez, I; Massip-Salcedo, M; Juan, ME; Planas, JM; Serafin, A; Pallas, M; Rimola, A; Rodes, J; Peralta, C,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:143-153 , 文章类型: Article,,卷期:2011年338-1]
- Numerous steatotic livers are discarded for transplantation because of their poor tolerance of ischemia-reperfusion (I/R). The injurious effects of retinol-binding protein 4 (RBP4) in various pathologies are well documen...
- Antiarthritis Effect of a Novel Bruton's Tyrosine Kinase (BTK) Inhibitor in Rat Collagen-Induced Arthritis and Mechanism-Based Pharmacokinetic/Pharmacodynamic Modeling: Relationships between Inhibition of BTK Phosphorylation and Efficacy
[作者:Liu, LC; Di Paolo, J; Barbosa, J; Rong, H; Reif, K; Wong, H,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:154-163 , 文章类型: Article,,卷期:2011年338-1]
- Bruton's tyrosine kinase (BTK) plays a critical role in the development, differentiation, and proliferation of B-lineage cells, making it an attractive target for the treatment of rheumatoid arthritis. The objective of t...
- Synergistic Suppression of Prostatic Cancer Cells by Coexpression of Both Murine Double Minute 2 Small Interfering RNA and Wild-Type p53 Gene In Vitro and In Vivo
[作者:Ji, K; Wang, B; Shao, YT; Zhang, L; Liu, YN; Shao, C; Li, XJ; Li, X; Hu, JD; Zhao, XJ; Xu, DQ; Li, Y; Cai, L,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:173-183 , 文章类型: Article,,卷期:2011年338-1]
- Our objective was to evaluate cell growth and death effects by inhibiting Murine Double Minute 2 (MDM2) expression in human prostate cancer cells overexpressing the wild-type (WT) p53 gene. Prostate PC-3 tumor cells were...
- Comparative Analysis of the Effects of Antimuscarinic Agents on Bladder Functions in Both Nonhuman Primates and Rodents
[作者:Nagabukuro, H; Villa, KL; Wickham, LA; Kulick, AA; Gichuru, L; Donnelly, MJ; Voronin, GO; Pereira, T; Tong, XC; Nichols, A; Alves, SE; O'Neill, GP; Johnson, CV; Hickey, EJ,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:220-227 , 文章类型: Article,,卷期:2011年338-1]
- Both the physiological role of muscarinic receptors for bladder function and the therapeutic efficacy of antimuscarinic agents for overactive bladder syndrome are well documented. We investigated the effect of antimuscar...
- Identification and Characterization of INCB9471, an Allosteric Noncompetitive Small-Molecule Antagonist of C-C Chemokine Receptor 5 with Potent Inhibitory Activity against Monocyte Migration and HIV-1 Infection
[作者:Shin, N; Solomon, K; Zhou, N; Wang, KH; Garlapati, V; Thomas, B; Li, YL; Covington, M; Baribaud, F; Erickson-Viitanen, S; Czerniak, P; Contel, N; Liu, P; Burn, T; Hollis, G; Yeleswaram, S; Vaddi, K; Xue, CB; Metcalf, B; Friedman, S; Scherle, P; Newton, R,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:228-239 , 文章类型: Article,,卷期:2011年338-1]
- C-C chemokine receptor 5 (CCR5) is a clinically proven target for inhibition of HIV-1 infection and a potential target for various inflammatory diseases. In this article, we describe 5-[(4-{(3S)-4-[(1R,2R)-2-ethoxy-5-(tr...
- Amperometric Measurement of Glutamate Release Modulation by Gabapentin and Pregabalin in Rat Neocortical Slices: Role of Voltage-Sensitive Ca(2+) alpha(2)delta-1 Subunit
[作者:Quintero, JE; Dooley, DJ; Pomerleau, F; Huettl, P; Gerhardt, GA,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:240-245 , 文章类型: Article,,卷期:2011年338-1]
- Gabapentin (GBP; Neurontin) and pregabalin (PGB; Lyrica, S-(+)-3-isobutylgaba) are used clinically to treat several disorders associated with excessive or inappropriate excitability, including epilepsy; pain from diabeti...
- Tamoxifen Regulation of Bone Growth and Endocrine Function in the Ovariectomized Rat: Discrimination of Responses Involving Estrogen Receptor alpha/Estrogen Receptor beta, G Protein-Coupled Estrogen Receptor, or Estrogen-Related Receptor gamma Using Fulvestrant (ICI 182780)
[作者:Fitts, JM; Klein, RM; Powers, CA,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:246-254 , 文章类型: Article,,卷期:2011年338-1]
- Tamoxifen is a selective estrogen receptor (ER) modulator, but it is also a deactivating ligand for estrogen-related receptor-gamma (ERR gamma) and a full agonist for the G protein-coupled estrogen receptor (GPER). Fulve...
- Up-Regulation of Extracellular Signal-Regulated Kinase 1/2-Dependent Thymidylate Synthase and Thymidine Phosphorylase Contributes to Cisplatin Resistance in Human Non-Small-Cell Lung Cancer Cells
[作者:Ko, JC; Tsai, MS; Chiu, YF; Weng, SH; Kuo, YH; Lin, YW,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:184-194 , 文章类型: Article,,卷期:2011年338-1]
- Chemotherapy for advanced human non-small-cell lung cancer (NSCLC) includes platinum-containing compound such as cisplatin in combination with a second- or third-generation cytotoxic agent. 5-Fluorouracil (5-FU) belongs ...
- Preclinical Pharmacology of AZD2327: A Highly Selective Agonist of the delta-Opioid Receptor
[作者:Hudzik, TJ; Maciag, C; Smith, MA; Caccese, R; Pietras, MR; Bui, KH; Coupal, M; Adam, L; Payza, K; Griffin, A; Smagin, G; Song, D; Swedberg, MDB; Brown, W,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:195-204 , 文章类型: Article,,卷期:2011年338-1]
- In the present article, we summarize the preclinical pharmacology of 4-{(R)-(3-aminophenyl)[4-(4-fluorobenzyl)-piperazin-1-yl]methyl}-N, N-diethylbenzamide (AZD2327), a highly potent and selective agonist of the delta-op...
- Celecoxib and 2,5-Dimethyl-Celecoxib Prevent Cardiac Remodeling Inhibiting Akt-Mediated Signal Transduction in an Inherited Dilated Cardiomyopathy Mouse Model
[作者:Fan, XL; Takahashi-Yanaga, F; Morimoto, S; Zhan, DY; Igawa, K; Tomooka, K; Sasaguri, T,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:2-11 , 文章类型: Article,,卷期:2011年338-1]
- Celecoxib, a cyclooxygenase-2 (COX-2)-selective nonsteroidal anti-inflammatory drug, has been shown to inhibit Akt and prevent cardiac remodeling in aortic banding-induced failing heart in mice. However, it may be diffic...
- Cinnamyl-3,4-Dihydroxy-alpha-Cyanocinnamate Is a Potent Inhibitor of 5-Lipoxygenase
[作者:Pergola, C; Jazzar, B; Rossi, A; Buehring, U; Luderer, S; Dehm, F; Northoff, H; Sautebin, L; Werz, O,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:205-213 , 文章类型: Article,,卷期:2011年338-1]
- Lipoxygenases (LOs) are iron-containing enzymes that catalyze the conversion of arachidonic acid into hydroperoxyeicosatetraenoic acids (HPETEs) and other bioactive lipid mediators. In mammals, 5-LO, 15-LO, and 12-LO enz...
- Selective GABA Transporter Inhibitors Tiagabine and EF1502 Exhibit Mechanistic Differences in Their Ability to Modulate the Ataxia and Anticonvulsant Action of the Extrasynaptic GABA(A) Receptor Agonist Gaboxadol
[作者:Madsen, KK; Ebert, B; Clausen, RP; Krogsgaard-Larsen, P; Schousboe, A; White, HS,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:214-219 , 文章类型: Article,,卷期:2011年338-1]
- Modulation of the extracellular levels of GABA via inhibition of the synaptic GABA transporter GAT1 by the clinically effective and selective GAT1 inhibitor tiagabine [(R)-N-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]nipecot...
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