- Tipifarnib-Induced Apoptosis in Acute Myeloid Leukemia and Multiple Myeloma Cells Depends on Ca2+ Influx through Plasma Membrane Ca2+ Channels
[作者:Yanamandra, N; Buzzeo, RW; Gabriel, M; Hazlehurst, LA; Mari, Y; Beaupre, DM; Cuevas, J,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:636-643 , 文章类型: Article,,卷期:2011年337-3]
- A major contributing factor to the high mortality rate associated with acute myeloid leukemia and multiple myeloma is the development of resistance to chemotherapy. We have shown that the combination of tipifarnib, a non...
- Efficacy of Ganitumab (AMG 479), Alone and in Combination with Rapamycin, in Ewing's and Osteogenic Sarcoma Models
[作者:Beltran, PJ; Chung, YA; Moody, G; Mitchell, P; Cajulis, E; Vonderfecht, S; Kendall, R; Radinsky, R; Calzone, FJ,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:644-654 , 文章类型: Article,,卷期:2011年337-3]
- Ewing's and osteogenic sarcoma are two of the leading causes of cancer deaths in children and adolescents. Recent data suggest that sarcomas may depend on the insulin-like growth factor type 1 (IGF-1) receptor (IGF1R) an...
- Agonist-Induced Internalization of CC Chemokine Receptor 5 as a Mechanism to Inhibit HIV Replication
[作者:Ferain, T; Hoveyda, H; Ooms, F; Schols, D; Bernard, J; Fraser, G,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:655-662 , 文章类型: Article,,卷期:2011年337-3]
- The chemokine G protein-coupled receptor CC chemokine receptor 5 (CCR5) is used as an entry gate by CCR5-tropic and dual- or CCR5/CXC chemokine receptor 4-tropic strains of HIV to enter the human host cells. Thus, CCR5 a...
- Treatment with Z-Ligustilide, a Component of Angelica sinensis, Reduces Brain Injury after a Subarachnoid Hemorrhage in Rats
[作者:Chen, D; Tang, JP; Khatibi, NH; Zhu, M; Li, YB; Wang, CY; Jiang, R; Tu, L; Wang, SL,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:663-672 , 文章类型: Article,,卷期:2011年337-3]
- Subarachnoid hemorrhage (SAH) is a devastating stroke subtype accounting for approximately 3 to 7% of cases each year. Despite its rarity among the various stroke types, SAH is still responsible for approximately 25% of ...
- Characterization of Vabicaserin (SCA-136), a Selective 5-Hydroxytryptamine 2C Receptor Agonist
[作者:Dunlop, J; Watts, SW; Barrett, JE; Coupet, J; Harrison, B; Mazandarani, H; Nawoschik, S; Pangalos, MN; Ramamoorthy, S; Schechter, L; Smith, D; Stack, G; Zhang, J; Zhang, GM; Rosenzweig-Lipson, S,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:673-680 , 文章类型: Article,,卷期:2011年337-3]
- The 5-hydroxytryptamine 2C (5-HT2C) receptor subtype has received considerable attention as a target for drug discovery, having been implicated in a wide variety of disorders. Here, we describe the in vitro pharmacologic...
- Discovery of a Calcimimetic with Differential Effects on Parathyroid Hormone and Calcitonin Secretion
[作者:Henley, C; Yang, YH; Davis, J; Lu, JYL; Morony, S; Fan, W; Florio, M; Sun, BH; Shatzen, E; Pretorius, JK; Richards, WG; St Jean, DJ; Fotsch, C; Reagan, JD,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:681-691 , 文章类型: Article,,卷期:2011年337-3]
- Calcimimetics are positive allosteric modulators to the calcium-sensing receptor (CaSR). Activation of the CaSR inhibits the secretion of parathyroid hormone (PTH), stimulates the secretion of calcitonin, and decreases s...
- Glucuronidation of Anticancer Prodrug PR-104A: Species Differences, Identification of Human UDP-Glucuronosyltransferases, and Implications for Therapy
[作者:Gu, YC; Tingle, MD; Wilson, WR,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:692-702 , 文章类型: Article,,卷期:2011年337-3]
- PR-104, the phosphate ester of a dinitrobenzamide mustard [PR-104A; 2-((2-bromoethyl)-2-{[(2-hydroxyethyl) amino] carbonyl}- 4,6-dinitroanilino)ethyl methanesulfonate], is currently in clinical trial as a hypoxia-and ald...
- Design of Novel Melatonin Analogs for the Reduction of Intraocular Pressure in Normotensive Rabbits
[作者:Alarma-Estrany, P; Guzman-Aranguez, A; Huete, F; Peral, A; Plourde, R; Pelaez, T; Yerxa, B; Pintor, J,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:703-709 , 文章类型: Article,,卷期:2011年337-3]
- Melatonin, the MT2 melatonin receptor agonist IIK7 [N-butanoyl-2-(2-methoxy-6H-isoindolo[2,1-a]indol-11-yl)ethanamine], and the putative MT3 melatonin receptor agonist 5-MCA-NAT [5-methoxycarbonylamino-N-acetyltryptamine...
- P-Glycoprotein (ABCB1) Transports the Primary Active Tamoxifen Metabolites Endoxifen and 4-Hydroxytamoxifen and Restricts Their Brain Penetration
[作者:Iusuf, D; Teunissen, SF; Wagenaar, E; Rosing, H; Beijnen, JH; Schinkel, AH,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:710-717 , 文章类型: Article,,卷期:2011年337-3]
- P-glycoprotein (P-gp, ABCB1) is a highly efficient drug efflux pump expressed in brain, liver, and small intestine, but also in tumor cells, that affects pharmacokinetics and confers therapy resistance for many anticance...
- Protein Kinase C beta(II)-Mediated Phosphorylation of Endothelial Nitric Oxide Synthase Threonine 495 Mediates the Endothelial Dysfunction Induced by FK506 (Tacrolimus)
[作者:Chiasson, VL; Quinn, MA; Young, KJ; Mitchell, BM,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:718-723 , 文章类型: Article,,卷期:2011年337-3]
- FK506 [tacrolimus; hexadecahydro-5,19-dihydroxy-3-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylethenyl]-14, 16-dimethoxy-4,10,12,18-tetramethyl-8-(2-propenyl)-15,19-epoxy-3H-pyrido[2,1-c][1,4]oxa-azacyclotricosine-1,7,20,2...
- Previous Exposure to Delta(9)-Tetrahydrocannibinol Enhances Locomotor Responding to but Not Self-Administration of Amphetamine
[作者:Cortright, JJ; Lorrain, DS; Beeler, JA; Tang, WJ; Vezina, P,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:724-733 , 文章类型: Article,,卷期:2011年337-3]
- Previous exposure to amphetamine leads to enhanced locomotor and nucleus accumbens (NAcc) dopamine (DA) responding to the drug as well as enhanced amphetamine self-administration. Here, we investigated the effects of exp...
- Mechanistic Modeling of the Effects of Glucocorticoids and Circadian Rhythms on Adipokine Expression
[作者:Sukumaran, S; Jusko, WJ; DuBois, DC; Almon, RR,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:734-746 , 文章类型: Article,,卷期:2011年337-3]
- A mechanism-based model was developed to describe the effects of methylprednisolone (MPL), circadian rhythms, and the glucose/free fatty acid (FFA)/insulin system on leptin and adiponectin expression in white adipose tis...
- Kaempferol Attenuates 4-Hydroxynonenal-Induced Apoptosis in PC12 Cells by Directly Inhibiting NADPH Oxidase
[作者:Jang, YJ; Kim, J; Shim, J; Kim, J; Byun, S; Oak, MH; Lee, KW; Lee, HJ,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:747-754 , 文章类型: Article,,卷期:2011年337-3]
- Kaempferol, a natural flavonoid isolated from various plant sources, has been identified as a potential neuroprotectant. In this study, we investigated the protective effect of kaempferol against 4-hydroxynonenal (HNE)-i...
- Behavioral and Cellular Modulation of L-DOPA-Induced Dyskinesia by beta-Adrenoceptor Blockade in the 6-Hydroxydopamine-Lesioned Rat
[作者:Lindenbach, D; Ostock, CY; Jaunarajs, KLE; Dupre, KB; Barnum, CJ; Bhide, N; Bishop, C,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:755-765 , 文章类型: Article,,卷期:2011年337-3]
- Chronic dopamine replacement therapy in Parkinson's disease (PD) leads to deleterious motor sequelae known as L-DOPA-induced dyskinesia (LID). No known therapeutic can eliminate LID, but preliminary evidence suggests tha...
- Inhibitory Effects of Antivascular Endothelial Growth Factor Strategies in Experimental Dopamine-Resistant Prolactinomas
[作者:Luque, GM; Perez-Millan, MI; Ornstein, AM; Cristina, C; Becu-Villalobos, D,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:766-774 , 文章类型: Article,,卷期:2011年337-3]
- Prolactin-secreting adenomas are the most frequent type among pituitary tumors, and pharmacological therapy with dopamine agonists remains the mainstay of treatment. But some adenomas are resistant, and a decrease in the...
- A Small-Molecule Inhibitor of Enterocytic Microsomal Triglyceride Transfer Protein, SLx-4090: Biochemical, Pharmacodynamic, Pharmacokinetic, and Safety Profile
[作者:Kim, E; Campbell, S; Schueller, O; Wong, E; Cole, B; Kuo, J; Ellis, J; Ferkany, J; Sweetnam, P,期刊:Journal of Pharmacology and Experimental Therapeutics, 页码:775-785 , 文章类型: Article,,卷期:2011年337-3]
- First-generation microsomal triglyceride transfer protein (MTP) inhibitors were designed to inhibit hepatic MTP and provide a novel treatment of dyslipidemia. Effective at lowering low-density lipoprotein-cholesterol (LD...
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