Results 131 to 140 of about 17,744 (296)

Non‐canonical PKG1 regulation in cardiovascular health and disease

British Journal of Pharmacology, EarlyView.
It is well established that the cyclic GMP‐dependent protein kinase I (PKG1) is canonically activated by cyclic guanosine monophosphate (cGMP), enabling its regulation of vascular tone, cardiac function and smooth muscle homeostasis. However, diverse non‐canonical stimuli of PKG1 have also been identified.
Jie Su, Joseph Robert Burgoyne
wiley   +1 more source

New biosensors and transgenic mice for multiplex cGMP imaging

British 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, Martin Thunemann, Barbara Birk, Susanne Feil, Viacheslav O. Nikolaev, Moritz Lehners, Robert Feil   +6 more
wiley   +1 more source

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

British 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, David Spähn, David Arturo Juarez Lopez, Judith L. Nono, Judith Seigner, Lisa Jacob, Siegfried Ussar, Robert Lukowski, Andreas L. Birkenfeld, Gencer Sancar   +9 more
wiley   +1 more source

An equal terms comparison of the proficiency of artificial phosphodiesterases by using simple models of RNA or DNA as benchmarks–the takeaway to design next generation supramolecular catalysts [PDF]

This comprehensive review aims at identifying the structural features and general rules governing the design of enzyme mimics and supramolecular catalysts having the ability to hydrolytically cleave the phosphodiester bonds. Rate and binding constants of
Salvio, Riccardo, Casnati, Alessandro, Casnati A., Salvio R.   +3 more
core   +1 more source

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

British 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, Sophie Sprenger, Olga Schweigert, Sanika Mohagaonkar, Matti Walsdorff, Tanja Zeller, Filip Berisha, Viacheslav O. Nikolaev, Sergei D. Rybalkin   +8 more
wiley   +1 more source

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

British 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, Johannes Reiner, Franz Hofmann, Azam Salari, Ursula Seidler   +4 more
wiley   +1 more source

Polarized effects of adenosine on blood–brain barrier integrity: Tightening from the luminal and opening from the abluminal side

British Journal of Pharmacology, EarlyView.
Background and Purpose Adenosine as a signalling molecule modifies blood–brain barrier (BBB) tightness in pathological conditions. Our aim was to investigate the direct and polarized effects of adenosine on the BBB using co‐culture and in vivo models. Experimental Approach The expression of adenosine receptors was measured by qRT‐PCR.
András Harazin, Gabriela Hurtado‐Alvarado, Lilla Barna, Arturo Contis‐Montes de Oca, Rocío Ruíz‐Manzano, Krisztián Laczi, András Kincses, Gergő Porkoláb, Gang Chen, Beatriz Gómez‐González, Mária A. Deli   +10 more
wiley   +1 more source

Dual pharmacological targeting of coactivator‐associated arginine methyltransferase 1 (CARM1) and salt inducible kinase (SIK) drives ketogenesis in both hepatocytes and mice

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Ketone bodies are liver‐derived circulating energy metabolites that positively impact most hallmarks of ageing. Ketone bodies increase during calorie restriction and fasting, two of the more widely perceived methods to increase health span.
Tábata Bergonci, Troels Kjær Rosenbæk, Samuel J. Windross, Ulrik B. Keiding, Estéfano Pinilla, Katrine P. Stuckert, Jakob Hansen, Camilla B. Nielsen, Jemila Peter Gomes, Lucy R. Davies, Johan Palmfeldt, Volker Loeschcke, Charlotte U. Andersen, Ulf Simonsen, Thomas B. Poulsen, Mogens Johannsen   +15 more
wiley   +1 more source

PKA phosphorylation and compartmentalisation of cAMP-phosphodiesterases [PDF]

, 2004
cAMP is a ubiquitous second messenger which conveys its cellular effects mainly through the activation of protein kinase A (PKA). Within a cell, activated PKA serves to phosphoiylate, and alter the conformational change of a wide variety of proteins ...
McSorley, Theresa
core  

Dimerisation induced formation of the active site and the identification of three metal sites in EAL-phosphodiesterases

, 2017
The bacterial second messenger cyclic di-3′,5′-guanosine monophosphate (c-di-GMP) is a key regulator of bacterial motility and virulence. As high levels of c-di-GMP are associated with the biofilm lifestyle, c-di-GMP hydrolysing phosphodiesterases (PDEs)
Horrell, Sam, Ivo Tews, Tews, Ivo, Hutchin, Andrew, Wagner, Armin, Webb, Jeremy S, Cai, Yuming, Martin A. Walsh, Walsh, Martin A, Curtis W. Phippen, Yuming Cai, Armin Wagner, Sam Horrell, Strange, Richard W, Dom Bellini, Jeremy S. Webb, Bellini, Dom, Phippen, Curtis W, Andrew Hutchin, Richard W. Strange   +19 more
core   +1 more source