English
norskBlar i forfatter Det helsevitenskapelige fakultet "Lyså, Roy Andre"
Viser treff 1-5 av 5
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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 ... -
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 ... -
Sodium nitroprusside inhibits HEK293 cell growth by cGMP-dependent and independent mechanisms
(Journal article; Tidsskriftartikkel, 2014) -
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. ...
