Results 141 to 150 of about 623,776 (234)

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

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

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

Re‐thinking peripheral dysfunctions in obesity: The emerging role of sulphaceutics and sulphanutraceutics

British Journal of Pharmacology, EarlyView.
Obesity is a chronic, relapsing, multisystem disease in which cardiometabolic risk arises from excess adiposity and progressive dysfunction of peripheral organs, ultimately disrupting endocrine and metabolic crosstalk among tissues. Within this network, sulphur‐based biology, centred on hydrogen sulphide and related reactive sulphur species, has ...
Martina Smimmo, Veronica Casale, Roberta d'Emmanuele di Villa Bianca, Valentina Vellecco, Mariarosaria Bucci   +4 more
wiley   +1 more source

Phosphodiesterase inhibitors as adjunctive therapies for tuberculosis

EBioMedicine, 2016
Bintou Ahmadou Ahidjo, William R. Bishai
doaj   +1 more source

The discovery and development of ensifentrine: A novel inhaled dual PDE3/4 inhibitor having ‘bifunctional’ bronchodilator and anti‐inflammatory activity

British Journal of Pharmacology, EarlyView.
Abstract Ensifentrine (formerly called RPL 554) is a novel, first in class, inhaled bifunctional dual PDE3/4 inhibitor for the treatment of chronic respiratory diseases. Ensifentrine exhibits both bronchodilation via PDE3 inhibition and anti‐inflammatory activity via PDE4 inhibition.
Clive Page
wiley   +1 more source

The ongoing oleoylethanolamide story: Therapeutic implications in the control of obesity and its comorbidities

British Journal of Pharmacology, EarlyView.
The global burden of obesity continues to rise, demanding effective pharmacological strategies for individuals in whom prevention alone is insufficient. Recent incretin‐based and multi‐agonist therapies have delivered unprecedented weight loss, demonstrating that the simultaneous modulation of multiple metabolic pathways can optimize body weight ...
Marzia Friuli, Alessia Campagna, Barbara Eramo, Christian Sepe, Annarita Zuena, Silvana Gaetani, Adele Romano   +6 more
wiley   +1 more source

Treatment‐Free Remission in Chronic Myeloid Leukemia: Toward Precision and Personalized Approaches to Functional Cure

Cancer Science, EarlyView.
Immune surveillance of residual leukemic stem cells after tyrosine kinase inhibitor discontinuation involves coordinated NK‐cell, CTL, Treg, pDC, and neutrophil activity that predicts treatment‐free remission, while exhausted CTLs and Treg expansion predict relapse in chronic myeloid leukemia.
Hiroshi Ureshino, Shinya Kimura
wiley   +1 more source

Phosphodiesterase Inhibitor [PDF]

, 2020
openaire   +1 more source