Results 61 to 70 of about 7,241 (191)

The potential for biased signalling in the P2Y receptor family of GPCRs

British Journal of Pharmacology, EarlyView.
The purinergic receptor family is primarily activated by nucleotides, and contains members of both the G protein coupled‐receptor (GPCR) superfamily (P1 and P2Y) and ligand‐gated ion channels (P2X). The P2Y receptors are widely expressed in the human body, and given the ubiquitous nature of nucleotides, purinergic signalling is involved with a plethora
Claudia M. Sisk, Simon Pitchford, Graham Ladds   +2 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 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

Bicarbonate Stimulated Adenylyl Cyclases [PDF]

IUBMB Life, 2004
AbstractBicarbonate ion is fundamental to the biology of all living organisms. HCO3‐ is vital to such diverse physiological processes as carbon fixation, cellular homeostasis, sperm maturation, and nucleotide synthesis. A defined subset of adenylyl cyclases identified in eukaryotes and prokaryotes are directly activated by HCO3‐.
openaire   +2 more sources

Cannabigerol reverses mechanical allodynia through α2A‐adrenergic modulation of thalamocortical signaling in chemotherapy‐induced neuropathy

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Chemotherapy‐induced peripheral neuropathy (CIPN) is a prevalent and treatment‐resistant side effect of platinum‐based chemotherapy, characterised by mechanical allodynia. Cannabigerol (CBG), a non‐psychoactive cannabinoid, has shown antinociceptive potential, but its site and mechanism of action remain unclear.
Quinn W. Wade, Nathan Morris, Diana E. Sepulveda, Alonso Cortez‐Resendiz, Christopher Brandl, Jennifer E. Lausch, Mariya Starostina, Nicholas M. Graziane   +7 more
wiley   +1 more source

Atrial natriuretic peptide counteracts aldosterone secretion by preventing acute angiotensin II‐induced cAMP signalling

British Journal of Pharmacology, EarlyView.
Background and Purpose Aldosterone plays a key role in blood pressure and volume regulation. Enhanced aldosterone secretion contributes to cardiovascular and renal diseases. Therefore, inhibitors of aldosterone receptors and synthase are essential drugs for the treatment of hypertension and heart failure.
Sanika Mohagaonkar, Egor B. Skryabin, Bettina M. Buchholz, Michaela Kuhn, Celso E. Gomez‐Sanchez, Stepan Gambaryan, Viacheslav O. Nikolaev   +6 more
wiley   +1 more source

Dualsteric and dual‐acting modulation of muscarinic receptors by antagonist KH‐5

British Journal of Pharmacology, EarlyView.
Abstract Background and purpose Muscarinic acetylcholine receptors are key therapeutic targets, and ligands engaging both orthosteric and allosteric sites may offer improved selectivity and efficacy. Here, we investigated whether the muscarinic antagonist KH‐5 acts as a dualsteric antagonist and defined its mode of interaction with muscarinic receptors.
Alena Janoušková‐Randáková, Eva Dolejší, Nikolai Chetverikov, Jan Jakubík   +3 more
wiley   +1 more source

Ligand binding represses bacterial histidine kinase activity by inhibiting its dimerization

The FEBS Journal, EarlyView.
PdtaS is a kinase in the pathogen Mycobacterium tuberculosis that senses copper and nitric oxide and controls virulence gene expression, but how the kinase senses these compounds was unclear. We show that PdtaS is active as a dimer with each monomer phosphorylating the other in trans.
Gaurav D. Sankhe, Jiawei Xing, Xiansha Xiao, John A. Buglino, Huilin Li, Igor B. Zhulin, Michael S. Glickman   +6 more
wiley   +1 more source

Soluble adenylyl cyclase in the eye

Biochimica et Biophysica Acta (BBA) - Molecular Basis of Disease, 2014
Adenylyl cyclases (ACs) are a family of enzymes which convert ATP to cAMP, an essential intermediate in many signal transduction pathways. Of the 10 AC genes in man, 9 fall into the category of transmembrane ACs (tmACs), which associate with G-protein coupled receptors (GPCRs) and are activated by forskolin.
Lee, Yong S., Marmorstein, Lihua Y., Marmorstein, Alan D.   +2 more
openaire   +2 more sources

Malaria mosquito antimicrobial defence requires immunity and detoxification gene regulation by Lola

Insect Molecular Biology, EarlyView.
Malaria mosquito antimicrobial defence requires upregulation of lola. Attenuation of lola in the midgut of Anopheles albimanus mosquitoes inhibits the upregulation of immunity genes induced by challenge. Putative target genes of the Lola transcription factor were revealed by lola attenuation, including Cecropin‐C, Draper, PPAF2, Clip‐domain serine ...
Heidi Espadas‐Álvarez, Verónica Valverde‐Garduño   +1 more
wiley   +1 more source