Alternative splicing as a biomarker and potential target for drug discovery.

abstract：AIM:Pim-2 is a short-lived serine/threonine kinase, which plays a key role in metastasis of breast cancer through persistent activation of STAT3. Although the crystal structure of Pim-2 has been reported, but thus far no specific Pim-2-targeted compounds have been reported. In this study, we identified a novel Pim-2 in...

journal_title：Acta pharmacologica Sinica

authors： Zhao YQ,Yin YQ,Liu J,Wang GH,Huang J,Zhu LJ,Wang JH

更新日期：2016-09-01 00:00:00

abstract：AIM:To investigate the role of CYP2E1 in isoniazid (INH)-induced hepatotoxicity and the influence of rifampicin (RFP) on INH-induced liver injury. METHODS:Rats were treated with INH alone (100 mg/kg, ip) or co-administered with RFP (100 mg/kg, ig) for 10 d and 21 d. Hepatotoxicity was assayed by plasma enzymes (sALT, ...

journal_title：Acta pharmacologica Sinica

authors： Yue J,Peng RX,Yang J,Kong R,Liu J

更新日期：2004-05-01 00:00:00

abstract：AIM:Matrine is an alkaloid from Sophora alopecuroides L, which has shown a variety of pharmacological activities and potential therapeutic value in cardiovascular diseases. In this study we examined the protective effects of matrine against diabetic cardiomyopathy (DCM) in rats. METHODS:Male SD rats were injected with...

journal_title：Acta pharmacologica Sinica

authors： Liu ZW,Wang JK,Qiu C,Guan GC,Liu XH,Li SJ,Deng ZR

更新日期：2015-03-01 00:00:00

abstract：AIM:Tolsultazolamide, a novel carbonic anhydrase inhibitor, is designed for the prophylaxis and treatment of acute mountain sickness. The aim of this study was to investigate the pharmacokinetics, tissue distribution, and excretion characteristics of tolsultazolamide and the sex difference in pharmacokinetics in rats. ...

journal_title：Acta pharmacologica Sinica

authors： Wang JD,Shi YP,Yin J,Pan ZY,Cui WY,Zhang YF,Wang H

更新日期：2014-02-01 00:00:00

abstract：AIM:To construct a recombinant adenovirus that can express human spermidine/ spermine N1-acetyltransferase (SSAT) and detect its inhibitory effect on colorectal cancer cell growth in vitro. METHODS:A 516 bp cDNA of SSAT was amplified and cloned into a pGL3-hTERT plasmid. The pGL3-hTERT-SSAT recombinant was digested, a...

journal_title：Acta pharmacologica Sinica

authors： Sun H,Liu B,Yang YP,Xu CX,Yan YF,Wang W,Liu XX

更新日期：2008-05-01 00:00:00

abstract：AIM:To model the three-dimensional structure and investigate the interaction mechanism of the proprotein convertase furin/kexin and their inhibitors (eglin c mutants). METHODS:The three-dimensional complex structures of furin/kexin with its inhibitors, eglin c mutants, were generated by modeller program using the newl...

journal_title：Acta pharmacologica Sinica

authors： Cai XH,Zhang Q,Ding DF

更新日期：2004-12-01 00:00:00

abstract：AIM:To investigate the expression of advanced glycation end products (AGEs) and their receptor RAGE in the livers and blood vessels of rats with non-alcoholic steatohepatitis (NASH) and the effect of pentoxifylline (PTX) on liver and artery function in rats with NASH. METHODS:Sprague-Dawley rats were fed a high-fat di...

journal_title：Acta pharmacologica Sinica

authors： Wu J,Zhao MY,Zheng H,Zhang H,Jiang Y

更新日期：2010-10-01 00:00:00

abstract：AIM:To evaluate the pharmacokinetic characteristics of L-valyl-ara-C, a peptidomimetic prodrug of ara-C. METHODS:After the synthesis of L-valyl-ara-C, the in vitro stability of L-valyl-ara-C was examined in various biological media. Plasma pharmacokinetic profiles of ara-C and L-valyl-ara-C were also evaluated in rats...

journal_title：Acta pharmacologica Sinica

authors： Cheon EP,Han HK

更新日期：2007-02-01 00:00:00

abstract：AIM:To investigate the effect of the Tob1 gene, a member of the Transducing Molecule of ErbB2/B-cell Translocation Ggene (TOB/BTG) family, by using the adenovirus-mediated expression of Tob1 on radiosensitivity in a human breast cancer cell line MDA-MB-231. METHODS:Cell survival was determined by clonogenic assay. Apo...

journal_title：Acta pharmacologica Sinica

authors： Jiao Y,Ge CM,Meng QH,Cao JP,Tong J,Fan SJ

更新日期：2007-10-01 00:00:00

abstract：:Esophageal cancer is one of the most common types of cancer in the world, and it demonstrates a distinct geographical distribution pattern in China. In the last decade, inducing apoptosis with traditional Chinese medicine (TCM) has become an active area in both fundamental and clinical research on cancer therapy. In t...

journal_title：Acta pharmacologica Sinica

authors： Zhang YS,Shen Q,Li J

更新日期：2016-03-01 00:00:00

abstract：:Terpene lactones are a class of bioactive constituents of standardized preparations of Ginkgo biloba leaf extract, extensively used as add-on therapies in patients with ischemic cardiovascular and cerebrovascular diseases. This investigation evaluated human pharmacokinetics of ginkgo terpene lactones and impact of the...

journal_title：Acta pharmacologica Sinica

authors： Liu XW,Yang JL,Niu W,Jia WW,Olaleye OE,Wen Q,Duan XN,Huang YH,Wang FQ,Du FF,Zhong CC,Li YF,Xu F,Gao Q,Li L,Li C

更新日期：2018-12-01 00:00:00

abstract：AIM:To investigate the effects of the cardiotonic steroid, ouabain, on cardiac differentiation of murine embyronic stem cells (mESCs). METHODS:Cardiac differentiation of murine ESCs was enhanced by standard hanging drop method in the presence of ouabain (20 μmol/L) for 7 d. The dissociated ES derived cardiomyocytes we...

journal_title：Acta pharmacologica Sinica

authors： Lee YK,Ng KM,Lai WH,Man C,Lieu DK,Lau CP,Tse HF,Siu CW

更新日期：2011-01-01 00:00:00

abstract：:Herbal and dietary supplements (HDS)-induced liver injury has been a great concern all over the world. Polygonum multiflorum Thunb., a well-known Chinese herbal medicine, is recently drawn increasing attention because of its hepatotoxicity. According to the clinical and experimental studies, P. multiflorum-induced liv...

journal_title：Acta pharmacologica Sinica

authors： Rao T,Liu YT,Zeng XC,Li CP,Ou-Yang DS

更新日期：2021-01-01 00:00:00

abstract：AIM:To investigate the metabolic characteristics of cytochrome P-450 C YP2A6 in human liver microsomes. METHODS:Cytochrome P-450 enzyme activities were measured by biochemical assays. Xenobiotics were employed to observe their effects on CYP2A6 in vitro. The kinetics of coumarin 7-hydroxylase was determined, and the c...

journal_title：Acta pharmacologica Sinica

authors： Xia XY,Peng RX,Yu JP,Wang H,Wang J

更新日期：2002-05-01 00:00:00

abstract：AIM:Toxicity of retinol (vitamin A) has been previously associated with apoptosis and/or cell malignant transformation. Thus, we investigated the pathways involved in the induction of proliferation, deformation and proliferative focus formation by retinol in cultured Sertoli cells of rats. METHODS:Sertoli cells were i...

journal_title：Acta pharmacologica Sinica

authors： Gelain DP,Pasquali MA,Caregnato FF,Castro MA,Moreira JC

更新日期：2012-04-01 00:00:00

abstract：:The signal transducer and activator of transcription 3 (STAT3) plays a critical role in platelet functions. This study sought to understand the effects of the STAT3 inhibitor SC99 on platelet activation and aggregation. Immunoblotting assays were applied to measure the effects of SC99 on the STAT3 signaling pathway. A...

journal_title：Acta pharmacologica Sinica

authors： Xu Z,Xu YJ,Hao YN,Ren LJ,Zhang ZB,Xu X,Cao BY,Dai KS,Zhu L,Fang Q,Kong Y,Mao XL

更新日期：2017-05-01 00:00:00

abstract：AIM:To study the regulation of monoamine oxidase-B (MAO-B) activity and imidazoline receptors (I-R) during long term treatment of morphine. METHODS:MAO-B activity was detected by high performance liquid chromatography; I-R was detected by [3H]idazoxan binding test. RESULTS:Idazoxan and morphine inhibited whole brain ...

journal_title：Acta pharmacologica Sinica

authors： Su RB,Li J,Li X,Qin BY

更新日期：2001-07-01 00:00:00

abstract：:Brain and eye tissues are subject to a reduced version of immune surveillance, which has evolved to protect the particularly sensitive tissues from accidental bystander damage created by regular inflammatory responses. Yet, there are autoimmune diseases in both organs. This review discusses the nature of immune reacti...

journal_title：Acta pharmacologica Sinica

authors： Wekerle H,Sun DM

更新日期：2010-09-01 00:00:00

abstract：:Anlotinib is a new oral tyrosine kinase inhibitor; this study was designed to characterize its pharmacokinetics and disposition. Anlotinib was evaluated in rats, tumor-bearing mice, and dogs and also assessed in vitro to characterize its pharmacokinetics and disposition and drug interaction potential. Samples were ana...

journal_title：Acta pharmacologica Sinica

authors： Zhong CC,Chen F,Yang JL,Jia WW,Li L,Cheng C,Du FF,Zhang SP,Xie CY,Zhang NT,Olaleye OE,Wang FQ,Xu F,Lou LG,Chen DY,Niu W,Li C

更新日期：2018-06-01 00:00:00

abstract：AIM:To evaluate the nasal absorption enhancement of insulin by sodium deoxycholate (SDC) in combination with cyclodextrins (CD). METHODS:The concentration of glucose in blood was measured. Scanning electron microscopy technique was used to investigate the effect of enhancers on the nasal mucocilia. The effect of SDC i...

journal_title：Acta pharmacologica Sinica

authors： Zhang Y,Jiang XG,Yao J

更新日期：2001-11-01 00:00:00

abstract：:AIDS is presently treatable, and patients can have a good prognosis due to the success of highly active antiretroviral therapy (HAART), but it is still not curable or preventable. High toxicity of HAART, and the emergence of drug resistance add to the imperative to continue research into new strategies and interventio...

journal_title：Acta pharmacologica Sinica

authors： Krambovitis E,Porichis F,Spandidos DA

更新日期：2005-10-01 00:00:00

abstract：AIM:To Study the interaction of macrophage colony-stimulating factor (M-CSF) and interleukin-10 (IL-10) in productions of IL-12 and IL-18 and expressions of CD14, CD23, and CD64 by human monocytes. METHODS:Purified adherent human monocytes were cultured with M-CSF or IL-10 alone, or with M-CSF+IL-10 and 2-3d later, th...

journal_title：Acta pharmacologica Sinica

authors： Ji XH,Yao T,Qin JC,Wang SK,Wang HJ,Yao K

更新日期：2004-10-01 00:00:00

abstract：AIM:To investigate the effects of trans-cinnamaldehyde (TCA) on the human leukemia K562 cell line and the cytotoxicity of cytokine-induced killer (CIK) cells against K562 cells. METHODS:Apoptosis, Fas expression, and mitochondrial transmembrane potential in K652 cells were analyzed using flow cytometry. K562 cells wer...

journal_title：Acta pharmacologica Sinica

authors： Zhang JH,Liu LQ,He YL,Kong WJ,Huang SA

更新日期：2010-07-01 00:00:00

abstract：:Aflibercept, as a soluble decoy vascular endothelial growth factor receptor, Which has been used as a first-line monotherapy for cancers. Aflibercept often causes cardiovascular toxicities including hypertension, but the mechanisms underlying aflibercept-induced hypertension remain unknown. In this study we investigat...

journal_title：Acta pharmacologica Sinica

authors： Dong ZC,Wu MM,Zhang YL,Wang QS,Liang C,Yan X,Zou LX,Chen C,Han X,Zhang B,Zhang ZR

更新日期：2020-12-10 00:00:00

abstract：AIM:To examine the effects of β3-adrenoceptor (β3-AR) activation on atherosclerotic plaque development in ApoE(-/-) mice. METHODS:Thirty six week-old male ApoE(-/-) mice on a high-fat diet were treated with atorvastatin (10 mg·kg(-1)·d(-1), po), BRL37344 (β3-AR agonist, 1.65 or 3.30 μg/kg, ip, twice a week) or SR52390...

journal_title：Acta pharmacologica Sinica

authors： Wang ZH,Li YF,Guo YQ

更新日期：2013-09-01 00:00:00

abstract：:Recent evidence shows that high glucose levels recruit carbohydrate response element-binding protein, which binds the promoter of thioredoxin-interacting protein (txnip), thereby regulating its expression in β-cells. Overexpression of txnip not only induces β-cell apoptosis but also reduces insulin production. Thus, t...

journal_title：Acta pharmacologica Sinica

authors： Li T,Lin GY,Zhong L,Zhou Y,Wang J,Zhu Y,Feng Y,Cai XQ,Liu Q,Nosjean O,Boutin JA,Renard P,Yang DH,Wang MW

更新日期：2017-07-01 00:00:00

abstract：:The combination of technological advances, genomic sequences and market success is catalyzing rapid development of antibody-based therapeutics. Cell surface receptors and ion channel proteins are well known drug targets, but the latter has seen less success. The availability of crystal structures, better understanding...

journal_title：Acta pharmacologica Sinica

authors： Sun H,Li M

更新日期：2013-02-01 00:00:00

abstract：AIM:To develop a novel, in situ gel system for nasal delivery of scopolamine hydrobromide (SCOP) and study its efficacy on motion sickness. METHODS:SCOP in situ gels at 0.2%, 0.5%, and 1.0% gellan gum concentration (w/v) were prepared, respectively, and characterized in terms of viscosity, in vitro release, and nasal ...

journal_title：Acta pharmacologica Sinica

authors： Cao SL,Zhang QZ,Jiang XG

更新日期：2007-04-01 00:00:00

abstract：AIM:To study the synaptic mechanisms involved in the 5-hydroxytryptamine1A/7 (5-HT1A/7) receptor-mediated reflex control of cardiac vagal preganglionic neurons (CVPN). METHODS:CVPN were retrogradely labeled and identified in brain stem slices of newborn rats, and their synaptic activity was examined using whole-cell p...

journal_title：Acta pharmacologica Sinica

authors： Chen YH,Hou LL,Wang JJ

更新日期：2008-05-01 00:00:00

abstract：AIM:To study the effects of the caspase-1 inhibitor Ac-YVAD-CHO on quinolinic acid (QA)-induced apoptosis. METHODS:Rats were pre-treated with intrastriatal infusion of Ac-YVAD-CHO (2-8 microg) before intrastriatal injection of QA (60 nmol). Striatal total proteins, genomic DNA, and nuclear proteins were isolated. The ...

journal_title：Acta pharmacologica Sinica

authors： Cao Y,Gu ZL,Lin F,Han R,Qin ZH

更新日期：2005-02-01 00:00:00