English
norskBlar i forfatter "Ravna, Aina Westrheim"
Viser treff 1-12 av 12
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Comparative molecular dynamics simulations of mitogen-activated protein kinase-activated protein kinase 5
(Journal article; Tidsskriftartikkel; Peer reviewed, 2014) -
Drug design på data'n
(Journal article; Tidsskriftartikkel, 2013)Hva skjer i hjernen når vi føler oss glade og optimistiske? Hvorfor virker penicillin mot bakterieinfeksjoner, mens paracet virker mot hodepine? Og hvordan i all verden kan antidepressiva påvirke humøret og dermed virke mot depresjon? Svaret er molekyler. -
Homology modeling and ligand docking of Mitogen-activated protein kinase-activated protein kinase 5 (MK5)
(Journal article; Tidsskriftartikkel; Peer reviewed, 2013)Background: Mitogen-activated protein kinase-activated protein kinase 5 (MK5) is involved in one of the major signaling pathways in cells, the mitogen-activated protein kinase pathway. MK5 was discovered in 1998 by the groups of Houng Ni and Ligou New, and was found to be highly conserved throughout the vertebrates. Studies, both in vivo and in vitro, have shown that it is implicated in tumor ... -
Identification and experimental confirmation of novel cGMP efflux inhibitors by virtual ligand screening of vardenafil-analogues
(Journal article; Tidsskriftartikkel; Peer reviewed, 2020-03-28)<i>Background</i> - Clinical studies have reported overexpression of PDE5 and elevation of intracellular cyclic GMP in various types of cancer cells. ABCC5 transports cGMP out of the cells with high affinity. PDE5 inhibitors prevent both cellular metabolism and cGMP efflux by inhibiting ABCC5 as well as PDE5. Increasing intracellular cGMP is hypothesized to promote apoptosis and growth restriction ... -
Identification of novel serotonin transporter compounds by virtual Screening
(Journal article; Tidsskriftartikkel; Peer reviewed, 2014-02-12)The serotonin (5-hydroxytryptamine, 5-HT) transporter (SERT) plays an essential role in the termination of serotonergic neurotransmission by removing 5-HT from the synaptic cleft into the presynaptic neuron. It is also of pharmacological importance being targeted by antidepressants and psychostimulant drugs. Here, five commercial databases containing approximately 3.24 million drug-like compounds ... -
Inhibition of ABCC5-mediated cGMP transport by progesterone, testosterone and their analogues
(Journal article; Tidsskriftartikkel; Peer reviewed, 2021-07-13)The biodynamics and biokinetics of sex hormones are complex. In addition to the classical steroid receptors (nuclear receptors), these hormones act through several non-genomic mechanisms. Modulation of ABC-transporters by progesterone represents a non-genomic mechanism. In the present study, we employed inside out vesicles from human erythrocytes to characterize high affinity cGMP transport by ABCC5 ... -
Inhibition of PDE5A1 guanosine cyclic monophosphate (cGMP) hydrolysing activity by sildenafil analogues that inhibit cellular cGMP efflux
(Journal article; Tidsskriftartikkel; Peer reviewed, 2017-02-17)<p><i>Objectives</i>: To determine the ability of 11 sildenafil analogues to discriminate between cyclic nucleotide phosphodiesterases (cnPDEs) and to characterise their inhibitory potencies (<kursiv>K</kursiv><sub>i</sub> values) of PDE5A1‐dependent guanosine cyclic monophosphate (cGMP) hydrolysis.</p> <p><i>Methods</i>: Sildenafil analogues were identified by virtual ligand screening (VLS) ... -
Modulation of high affinity ATP-dependent cyclic nucleotide transporters by specific and non-specific cyclic nucleotide phosphodiesterase inhibitors
(Journal article; Tidsskriftartikkel; Peer reviewed, 2014-11-07)Intracellular cyclic nucleotides are eliminated by phosphodiesterases (PDEs) and by ATP Binding cassette transporters such as ABCC4 and ABCC5. PDE5 and ABCC5 have similar affinity for cGMP whereas ABCC5 has much higher affinity for cGMP compared with cAMP. Since the substrate (cGMP) is identical for these two eliminatory processes it is conceivable that various PDE inhibitors also modulate ... -
Molecular modeling study of the testosterone metabolizing enzyme UDP-glucuronosyltransferase 2B17
(Journal article; Tidsskriftartikkel; Peer reviewed, 2021-02-20)The dominant sex hormone testosterone is mainly metabolized by liver enzymes belonging to the uridine-diphospho (UDP) glucuronosyltransferase (UGT) family. These enzymes are the main phase II enzymes, and they have an important role in the detoxification of endogenous and exogenous compounds in humans. The aim of the present study was to improve the understanding of the binding properties of UGT2B17. ... -
Synthesis, biological evaluation and molecular modeling studies of the PPARβ/δ antagonist CC618
(Journal article; Tidsskriftartikkel; Peer reviewed, 2015-03-05)Abstract: Herein, we describe the synthesis, biological evaluation and molecular docking of the selective PPARb/ d antagonist (4-methyl-2-(4-(trifluoromethyl)phenyl)-N-(2-(5-(trifluoromethyl)-pyridin-2-ylsulfonyl) ethyl)thiazole-5-carboxamide)), CC618. Results from in vitro luciferase reporter gene assays against the three known human PPAR subtypes revealed that CC618 selectively antagonizes ... -
Treatment of Cardiovascular Dysfunction with PDE3-Inhibitors in Moderate and Severe Hypothermia—Effects on Cellular Elimination of Cyclic Adenosine Monophosphate and Cyclic Guanosine Monophosphate
(Journal article; Tidsskriftartikkel; Peer reviewed, 2022-07-13)<p><b>Introduction:</b> Rewarming from accidental hypothermia is often complicated by hypothermia-induced cardiovascular dysfunction, which could lead to shock. Current guidelines do not recommend any pharmacological treatment at core temperatures below 30°C, due to lack of knowledge. However, previous in vivo studies have shown promising results when using phosphodiesterase 3 (PDE3) inhibitors, ... -
Treatment of cardiovascular dysfunction with PDE5-inhibitors - temperature dependent effects on transport and metabolism of cAMP and cGMP
(Journal article; Tidsskriftartikkel; Peer reviewed, 2021-07-30)<i>Introduction</i>: Cardiovascular dysfunction is a potentially lethal complication of hypothermia. Due to a knowledge gap, pharmacological interventions are not recommended at core temperatures below 30°C. Yet, further cooling is induced in surgical procedures and survival of accidental hypothermia is reported after rewarming from below 15°C, advocating a need for evidence-based treatment guidelines. ...
