Results 121 to 130 of about 77,168 (243)

New pharmacological prospectives in erectile function [PDF]

open access: yes, 2009
Erectile dysfunction (ED), defined as the consistent or recurrent inability of a man to attain and/or maintain a penile erection sufficient for sexual activity ), can be caused by a number of different pathophysiological process.
Mitidieri, Emma
core   +1 more source

Critical time window for NO-cGMP-dependent long-term memory formation after one-trial appetitive conditioning

open access: yes, 2002
The nitric oxide (NO)-cGMP signaling pathway is implicated in an increasing number of experimental models of plasticity. Here, in a behavioral analysis using one-trial appetitive associative conditioning, we show that there is an obligatory requirement ...
Ildiko Kemenes (4460722)   +4 more
core  

New biosensors and transgenic mice for multiplex cGMP imaging

open access: yesBritish Journal of Pharmacology, EarlyView.
Background and Purpose Cyclic guanosine monophosphate (cGMP) is a versatile second messenger that is important for human (patho‐)physiology and pharmacotherapy. Live‐cell imaging of cGMP with biosensors allows to elucidate its spatiotemporal dynamics in real time under close‐to‐native conditions. However, to monitor two separate cGMP pools or cGMP/cAMP
Markus Wolters   +6 more
wiley   +1 more source

PDE4D and PDE3B orchestrate distinct cAMP microdomains in 3T3‐L1 adipocytes

open access: yesBritish Journal of Pharmacology, EarlyView.
Basal conditions: •Ins/PDE3B lowers cytoplasmic cAMP (cyt‐cAMP) without affecting plasma membrane cAMP (pm‐cAMP). •Insulin decreases lipid droplet cAMP (LD‐cAMP) independent of PDE3B. •FGF1/PDE4D modestly reduces both cyt‐ and pm‐cAMP, while PDE4D alone can modulate LD‐cAMP. ISO stimulation: •Ins/PDE3B has minimal impact on cyt‐cAMP.
Johannes Krier   +9 more
wiley   +1 more source

Structure-Guided Optimization of PDE9A Inhibitors Tackling Neuroinflammation: A Combined Computational and In Vitro Study. [PDF]

open access: yesChemMedChem
Computational studies allowed the identification of a PDE9A inhibitor. A novel HPLC‐based assay was developed and optimized to measure enzyme function to assess PDE9A inhibition. Furthermore, in vitro tests supported the activity of the compound against neuroinflammation. Oxidative stress and inflammation are key players in central nervous system (CNS)
Ribaudo G   +10 more
europepmc   +2 more sources

An intracellular recombinant single‐chain variable antibody fragment as a new class of phosphodiesterase type 5 inhibitors

open access: yesBritish Journal of Pharmacology, EarlyView.
Background and Purpose Cyclic guanosine monophosphate (cGMP) is a ubiquitous second messenger involved in human (patho‐)physiology. Phosphodiesterase 5 (PDE5) is a major cGMP hydrolyzing enzyme in many cell types including vascular smooth muscle cells (VSMCs). Several highly selective PDE5 inhibitors are in clinical use. However, there are currently no
Kürsat Kirkgöz   +8 more
wiley   +1 more source

Transgenic Mice for Real Time Visualization of cGMP in Intact Adult Cardiomyocytes.

open access: yes, 2014
cGMP is an important second messenger which regulates cardiac contractility and protects the heart from hypertrophy. However, due to the lack of real time imaging techniques, specific subcellular mechanisms and spatio-temporal dynamics of cGMP in adult ...
Götz, Konrad R.   +14 more
core   +1 more source

Differential segment‐specific signalling pathways for guanylate cyclase C‐activated anion secretion in murine ileocolon

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Guanylate cyclase‐C (GC‐C) is the receptor for endogenous (uro)guanylin peptides, bacterial toxins and pharmacological analogues. Receptor activation leads to intestinal fluid loss, but also activates an antiproliferative pathway and is a promising target in colorectal cancer therapy.
Renjie Xiu   +4 more
wiley   +1 more source

The GAF Domain of the cGMP-Binding, cGMP-Specific Phosphodiesterase (PDE5) Is a Sensor and a Sink for cGMP

open access: yes, 2008
We describe here a novel sensor for cGMP based on the GAF domain of the cGMP-binding, cGMP-specific phosphodiesterase 5 (PDE5) using bioluminescence resonance energy transfer (BRET).
Biswas, Kabir Hassan   +3 more
core   +1 more source

Targeting hexokinase 2 to induce breast cancer cell senescence

open access: yesBritish Journal of Pharmacology, EarlyView.
Background and Purpose Hexokinase 2 (HK2) is a key enzyme linked to high tumour cell proliferation. Its inhibitors such as 3‐bromopyruvic acid (3‐BP) induce cancer cell death, highlighting HK2 modulation as potential anti‐cancer treatment. However, standard chemotherapies often cause the emergence of senescent cancer cells, which goes along with cell ...
Helmut Bischof   +8 more
wiley   +1 more source

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