Activation of human ether-a-go-go related gene (hERG) potassium channels by small molecules.

Abstract:

:Human ether-a-go-go related gene (hERG) potassium (K(+)) channels play a critical role in cardiac action potential repolarization. Mutations that reduce hERG conductance or surface expression may cause congenital long QT syndrome (LQTS). However, the channels can be inhibited by structurally diverse small molecules, resulting in an acquired form of LQTS. Consequently, small molecules that increase the hERG current may be of value for treatment for LQTS. So far, nine hERG activators have been reported. The aim of this review is to discuss recent advances concerning the identification and action mechanism of hERG activators.

journal_name

Acta Pharmacol Sin

authors

Zhou PZ,Babcock J,Liu LQ,Li M,Gao ZB

doi

10.1038/aps.2011.70

subject

Has Abstract

pub_date

2011-06-01 00:00:00

pages

781-8

issue

6

eissn

1671-4083

issn

1745-7254

pii

aps201170

journal_volume

32

pub_type

杂志文章,评审
  • Functions and the related signaling pathways of the neurotrophic factor neuritin.

    abstract::Neuritin is a member of the neurotrophic factor family, which is activated by neural activity and neurotrophins, and promotes neurite growth and branching. It has shown to play an important role in neuronal plasticity and regeneration. It is also involved in other biological processes such as angiogenesis, tumorigenes...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章,评审

    doi:10.1038/aps.2017.197

    authors: Yao JJ,Zhao QR,Lu JM,Mei YA

    更新日期:2018-09-01 00:00:00

  • Oncogenesis of RON receptor tyrosine kinase: a molecular target for malignant epithelial cancers.

    abstract::Recepteur d'origine nantais (RON) belongs to a subfamily of receptor tyrosine kinases (RTK) with unique expression patterns and biological activities. RON is activated by a serum-derived growth factor macrophage stimulating protein (MSP). The RON gene transcription is essential for embryonic development and critical i...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章,评审

    doi:10.1111/j.1745-7254.2006.00361.x

    authors: Wang MH,Yao HP,Zhou YQ

    更新日期:2006-06-01 00:00:00

  • Function and mechanism of pyronaridine: a new inhibitor of P-glycoprotein-mediated multidrug resistance.

    abstract:AIM:To study the effect and mechanism of pyronaridine (PND) on the reversal of multidrug resistance (MDR) in K562/A02 and MCF7/ADR cell lines with mdr1+. METHODS:MTT assay was used to determine the cells growth inhibition after incubation for 72 h in the presence of doxorubicin (DOX) with or without PND. Intracellular...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:

    authors: Qi J,Yang CZ,Wang CY,Wang SB,Yang M,Wang JH

    更新日期:2002-06-01 00:00:00

  • Curcumin enhances vascular contractility via induction of myocardin in mouse smooth muscle cells.

    abstract::A variety of cardiovascular diseases is accompanied by the loss of vascular contractility. This study sought to investigate the effects of curcumin, a natural polyphenolic compound present in turmeric, on mouse vascular contractility and the underlying mechanisms. After mice were administered curcumin (100 mg·kg-1·d-1...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1038/aps.2017.18

    authors: Sun SW,Tong WJ,Guo ZF,Tuo QH,Lei XY,Zhang CP,Liao DF,Chen JX

    更新日期:2017-10-01 00:00:00

  • Computational insights into the subtype selectivity and "message-address-efficacy" mechanisms of opioid receptors through JDTic binding and unbinding.

    abstract::In drug design and discovery, binding affinity and selectivity are two basic properties of a drug candidate. Opioid receptors (ORs) are the main targets of strong analgesics. Like some other class A members of G-protein-coupled receptors (GPCRs), ORs exhibit complex selectivity on their ligands. The diversity of bindi...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1038/aps.2017.132

    authors: Cheng JX,Cheng T,Li WH,Liu GX,Zhu WL,Tang Y

    更新日期:2018-03-01 00:00:00

  • Cellular mechanism for spontaneous calcium oscillations in astrocytes.

    abstract:AIM:To determine the Ca2+ source and cellular mechanisms of spontaneous Ca2+ oscillations in hippocampal astrocytes. METHODS:The cultured cells were loaded with Fluo-4 AM, the indicator of intracellular Ca2+, and the dynamic Ca2+ transients were visualized with confocal laser-scanning microscopy. RESULTS:The spontane...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1111/j.1745-7254.2006.00397.x

    authors: Wang TF,Zhou C,Tang AH,Wang SQ,Chai Z

    更新日期:2006-07-01 00:00:00

  • Intranasal co-delivery of IL-6 gene enhances the immunogenicity of anti-caries DNA vaccine.

    abstract:AIM:To investigate the effects of co-delivering IL-6 expressing plasmid pCI-IL-6 on the immunogenicity of the anti-caries DNA vaccine pCIA-P, which encodes the surface protein antigen PAc of Streptococcus mutans. METHODS:Plasmid pCI-IL-6 was constructed by inserting the murine IL-6 gene into the pCI vector. Expression...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1038/aps.2013.184

    authors: Su LK,Yu F,Li ZF,Zeng C,Xu QA,Fan MW

    更新日期:2014-05-01 00:00:00

  • CJZ3, a lomerizine derivative, modulates P-glycoprotein function in rat brain microvessel endothelial cells.

    abstract:AIM:To investigate the modulatory effect of CJZ3, a lomerizine derivative, on P-glycoprotein (P-gp) function in rat brain microvessel endothelial cells (RBMEC). METHODS:RBMEC were isolated and cultured in Dulbecco modified Eagle medium/F12 (1:1) medium, and the amount of intracellular rhodamine 123 (Rh123) was determi...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1111/j.1745-7254.2006.00294.x

    authors: Ji BS,He L,Li XQ,Liu GQ

    更新日期:2006-04-01 00:00:00

  • Effects of tripcholorolide on inflammatory reaction of mouse alveolar macrophages in vitro.

    abstract:AIM:To observe the effects of tripcholorolide (T4) on inflammatory reaction of mouse alveolar macrophages. METHODS:RT-PCR was used to investigate tumor necrosis factor alpha (TNF alpha), interleukin-1 beta (IL-1 beta), IL-6, IL-10, and inducible nitric-oxide synthase (iNOS) mRNA expression in alveolar macrophages afte...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:

    authors: Qiu HB,Yang Y,Zhou SX

    更新日期:2000-12-01 00:00:00

  • Stereoselective metabolism of propafenone by human liver CYP3A4 expressed in transgenic Chinese hamster CHL cells lines.

    abstract:AIM:To investigate the stereoselective metabolism of propafenone (PPF) by human liver CYP3A4. METHODS:A chiral and an achiral HPLC were combined to determine the enantiomer of PPF in S9 incubates prepared from transgenic Chinese hamster CHL cells lines expressing CYP3A4. The time-dependent study was performed using in...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:

    authors: Zhou Q,Yao TW,Yu YN,Zeng S

    更新日期:2001-10-01 00:00:00

  • Effects of gamichunggantang on hyperlipidemia.

    abstract:AIM:To evaluate the therapeutic effects of gamichunggantang (GCT) on hyperlipidemia through high cholesterol diet model. GCT is an Oriental herbal medication, which has been used for the treatment of fatty liver, hyperlipidemia or alcoholic liver disease in Daejeon University Oriental Hospital, Korea since 1999. METHO...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:

    authors: Son CG,Choi WJ,Shin JW,Han SH,Cho JH,Song KC,Cho CK

    更新日期:2003-02-01 00:00:00

  • High prevalence of the B2+C2 subgenotype mixture in patients with chronic hepatitis B in Eastern China.

    abstract:AIM:To investigate the prevalence of hepatitis B virus (HBV) genotype mixtures among patients with chronic hepatitis B (CHB) in Eastern China. METHODS:A total of 4908 chronic HBV patients from Eastern China were enrolled. HBV genotypes and subgenotypes were determined using a multiplex PCR technique. Serum viral loads...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1038/aps.2012.78

    authors: Zhong J,Gao YQ,Sun XH,Zhu XJ,Li M

    更新日期:2012-10-01 00:00:00

  • Effect of tachykinins on ascending and descending reflex pathway in rat small intestine.

    abstract:AIM:To examine the effect of tachykinins on the ascending reflex pathway in rat small intestine, we used different selective neurokinin (NK) receptor antagonists (RA): a) NK1-RA: GR-82334 and CP-96.345, b) NK2-RA: MEN-10.376 and L-659.877. The aim was further to investigate the effect of substance P (SP) on the ascendi...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:

    authors: Hahn A,Storr M,Allescher HD

    更新日期:2002-04-01 00:00:00

  • Monocarbonyl curcumin analog A2 potently inhibits angiogenesis by inducing ROS-dependent endothelial cell death.

    abstract::Excessive and abnormal vessel growth plays a critical role in the pathogenesis of many diseases, such as cancer. Angiogenesis is one of the hallmarks of cancer growth, invasion, and metastasis. Discovery of novel antiangiogenic agents would provide new insights into the mechanisms of angiogenesis, as well as potential...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1038/s41401-019-0224-x

    authors: Liu B,Cui LS,Zhou B,Zhang LL,Liu ZH,Zhang L

    更新日期:2019-11-01 00:00:00

  • Mycophenolate mofetil as a treatment for refractory idiopathic thrombocytopenic purpura.

    abstract:AIM:To determine whether mycophenolate mofetil (MMF) has beneficial effects on refractory idiopathic thrombocytopenic purpura (ITP) and the corresponding cellular mechanism. METHODS:Twenty refractory ITP patients resistant to corticosteroid and/or splenectomy and chemical therapy were given MMF 1.5-2.0 g/d orally for ...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1111/j.1745-7254.2005.00088.x

    authors: Zhang WG,Ji L,Cao XM,Chen YX,He AL,Liu J,Zhao WH,Zou SP

    更新日期:2005-05-01 00:00:00

  • Blood pressure, baroreflex sensitivity, and end organ damage in hybrid offspring of spontaneously hypertensive rats and Sprague-Dawley rats.

    abstract:AIM:To investigate the blood pressure (BP), baroreflex sensitivity (BRS), and organ damage in hybrids of spontaneously hypertensive rats and Sprague-Dawley rats. METHODS:Spontaneously hypertensive rats and Sprague-Dawley rats were crossbred, and the F1 hybrids were inbred randomly to produce an F2 generation. At the a...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1111/j.1745-7254.2005.00162.x

    authors: Xie HH,Shen FM,Miao CY,Su DF

    更新日期:2005-09-01 00:00:00

  • Induction of collateral artery growth and improvement of post-infarct heart function by hepatocyte growth factor gene transfer.

    abstract:AIM:To study the effect of adenovirus5-mediated human hepatocyte growth factor (Ad(5)-HGF) transfer on post-infarct heart failure in a swine model. METHODS:Twelve young Suzhong swine were randomly divided into 2 groups: the Ad(5)-HGF group (n=6) and the null-Ad(5) group (n=6). Four weeks after left anterior descending...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1111/j.1745-7254.2006.00306.x

    authors: Wang W,Yang ZJ,Ma DC,Wang LS,Xu SL,Zhang YR,Cao KJ,Zhang FM,Ma WZ

    更新日期:2006-05-01 00:00:00

  • Pharmacokinetics and tissue distribution of a novel PDE5 inhibitor, SK-3530, in rats.

    abstract:AIM:To investigate the pharmacokinetic profile and tissue distribution of a novel phosphodiesterase type 5 inhibitor, 5-ethyl-2-{5-[4-(2-hydroxy-ethyl)-piperazine-1-sulfonyl]-2-propoxy-phenyl}-7-propyl-3,5-dihydro-pyrrolo(3,2-d)pyrimidin-4-one (SK-3530), in rats after administration of the (14)C-labeled compound. METH...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1111/j.1745-7254.2007.00611.x

    authors: Yoo HH,Kim NS,Im GJ,Kim DH

    更新日期:2007-08-01 00:00:00

  • Proteomics reveals potential non-neuronal cholinergic receptor-effectors in endothelial cells.

    abstract:AIM:The non-neuronal acetylcholine system (NNAS) in endothelial cells participates in modulating endothelial function, vascular tone, angiogenesis and inflammation, thus plays a critical role in cardiovascular diseases. In this study, we used a proteomic approach to study potential downstream receptor-effectors of NNAS...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1038/aps.2014.38

    authors: Zhang YY,Shen W,Zhang LC,Pan ZY,Long CL,Cui WY,Zhang YF,Wang H

    更新日期:2014-09-01 00:00:00

  • Protective effects of prostaglandin E1 on human umbilical vein endothelial cell injury induced by hydrogen peroxide.

    abstract:AIM:To investigate the protective effects of prostaglandin E(1) (PGE(1)) against H(2)O(2)-induced oxidative damage on human umbilical vein endothelial cells (HUVECs). METHODS:HUVECs were pretreated with PGE(1) (0.25, 0.50, and 1.00 micromol/L) for 24 h and exposed to H(2)O(2) (200 micromol/L) for 12 h, and cell viabil...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1038/aps.2010.23

    authors: Fang WT,Li HJ,Zhou LS

    更新日期:2010-04-01 00:00:00

  • Association of apolipoprotein E 4 polymorphism with cerebral infarction in Chinese Han population.

    abstract:AIM:To study the association between APOE polymorphisms and cerebral infarction through a case-control study among the Chinese Han population. METHODS:First-ever cerebral infarction patients (n=226) whose ages ranged from 40 to 60 years old were recruited from Department of Neurology, Zhongshan Hospital, Shanghai, and...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:

    authors: Jin ZQ,Fan YS,Ding J,Chen M,Fan W,Zhang GJ,Zhang BH,Yu SJ,Zhang YS,Ji WF,Zhang JG

    更新日期:2004-03-01 00:00:00

  • Chip-based digital PCR as a novel detection method for quantifying microRNAs in acute myocardial infarction patients.

    abstract::miRNAs have shown promise as potential biomarkers for acute myocardial infarction (AMI). However, the current used quantitative real-time PCR (qRT-PCR) allows solely for relative expression of nucleic acids and it is susceptible to day-to-day variability, which has limited the validity of using the miRNAs as biomarker...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1038/aps.2017.136

    authors: Robinson S,Follo M,Haenel D,Mauler M,Stallmann D,Heger LA,Helbing T,Duerschmied D,Peter K,Bode C,Ahrens I,Hortmann M

    更新日期:2018-07-01 00:00:00

  • Nitric oxide: a newly discovered function on wound healing.

    abstract::Wound healing impairment represents a particularly challenging clinical problem to which no efficacious treatment regimens currently exist. The factors ensuring appropriate intercellular communication during wound repair are not completely understood. Although protein-type mediators are well-established players in thi...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章,评审

    doi:10.1111/j.1745-7254.2005.00058.x

    authors: Luo JD,Chen AF

    更新日期:2005-03-01 00:00:00

  • Fragile privileges: autoimmunity in brain and eye.

    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

    pub_type: 杂志文章,评审

    doi:10.1038/aps.2010.149

    authors: Wekerle H,Sun DM

    更新日期:2010-09-01 00:00:00

  • Human T-cell lymphotropic virus type 1 and its oncogenesis.

    abstract::Human T-cell lymphotropic virus type 1 (HTLV-1) is the etiologic agent of adult T-cell leukemia/lymphoma (ATL), a rapidly progressing clonal malignancy of CD4+ T lymphocytes. Exploring the host-HTLV-1 interactions and the molecular mechanisms underlying HTLV-1-mediated tumorigenesis is critical for developing efficien...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章,评审

    doi:10.1038/aps.2017.17

    authors: Zhang LL,Wei JY,Wang L,Huang SL,Chen JL

    更新日期:2017-08-01 00:00:00

  • Preparation of ion-activated in situ gel systems of scopolamine hydrobromide and evaluation of its antimotion sickness efficacy.

    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

    pub_type: 杂志文章

    doi:10.1111/j.1745-7254.2007.00540.x

    authors: Cao SL,Zhang QZ,Jiang XG

    更新日期:2007-04-01 00:00:00

  • TSPO ligands prevent the proliferation of vascular smooth muscle cells and attenuate neointima formation through AMPK activation.

    abstract::Abnormal growth of the intimal layer of blood vessels (neointima formation) contributes to the progression of atherosclerosis and in-stent restenosis. Recent evidence shows that the 18-kDa translocator protein (TSPO), a mitochondrial membrane protein, is involved in diverse cardiovascular diseases. In this study we in...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1038/s41401-019-0293-x

    authors: Wu LP,Gong ZF,Wang H,Zhou ZS,Zhang MM,Liu C,Ren HM,Yang J,Han Y,Zeng CY

    更新日期:2020-01-01 00:00:00

  • Combinatorial strategies for cancer eradication by silibinin and cytotoxic agents: efficacy and mechanisms.

    abstract::In an effort to develop effective alternative strategies that increase the therapeutic efficacy and minimize the systemic toxicity of chemotherapeutic agents, more efforts are being directed towards the investigation of dietary supplements and other phytotherapeutic agents for their synergistic efficacy in combination...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章,评审

    doi:10.1111/j.1745-7254.2007.00691.x

    authors: Raina K,Agarwal R

    更新日期:2007-09-01 00:00:00

  • Transition from traditional to innovative teaching in and beyond pharmacology at Ziauddin Medical University.

    abstract::Innovative teaching methodologies in different parts of the world are being practiced since last 3 decades. The aim of this review is to report the transition from traditional to innovative self learning process in Ziauddin Medical University, a new medical institute of Pakistan. Various problems encountered have been...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:

    authors: Barakzai Q

    更新日期:2004-09-01 00:00:00

  • Inhibitory effect of picroside II on hepatocyte apoptosis.

    abstract:AIM:To investigate the influence of picroside II on hepatocyte apoptosis and its mechanism. METHODS:Morphological changes and quantification of apoptotic cells were determined under transmission electron microscopy and flow cytometry respectively. DNA fragmentation was visualized by agarose gel electrophoresis. Semi-q...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1111/j.1745-7254.2005.00729.x

    authors: Gao H,Zhou YW

    更新日期:2005-06-01 00:00:00