Results 91 to 100 of about 41,822 (243)

Cardiotoxicity of BRAF/MEK inhibitors

British Journal of Pharmacology, EarlyView.
Abstract Rapidly accelerated fibrosarcoma type B/B‐Raf proto‐oncogene, serine/threonine kinase (BRAF) and mitogen‐activated protein kinase (MEK) inhibitors have transformed outcomes in cancer therapy, particularly in melanoma. However, cardiovascular toxicities are increasingly recognized in real‐world clinical practice.
Katharina Seuthe, Valerie Lohner, Kevin Terre, Thomas Riffelmacher, Roman Pfister   +4 more
wiley   +1 more source

Agonist‐specific conformational dynamics at the β2‐adrenoceptor dictate allosteric modulation of Gαs signalling and bronchodilation

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose β2‐adrenoceptor (β2AR) agonists are the cornerstone of asthma therapy and promote bronchodilation through Gαs signalling in airway smooth muscle (ASM), but their efficacy is limited by β‐arrestin‐mediated β2AR desensitization.
Sushrut D. Shah, Joshua Richard, Suvankar Ghosh, Jillian Jerwick, Joice T. Gavali, Raymond B. Penn, Alexander D. MacKerell Jr, Deepak A. Deshpande   +7 more
wiley   +1 more source

Pharmacological activation of NO‐cGMP signalling attenuates metabolic dysfunction‐associated steatohepatitis

British Journal of Pharmacology, EarlyView.
Background and Purpose Metabolic dysfunction‐associated steatohepatitis (MASH) is linked to activation of hepatic stellate cells (HSCs) to α‐smooth muscle actin–positive myofibroblasts that produce collagen and proinflammatory cytokines. Quiescent HSCs express the NO‐cGMP signalling axis.
Krithika Rajeeth, Malte Roessing, Moritz Lehners, Lisa Dietz, Anja Schmitt, Stephan Hailfinger, Andreas Peter, Leticia Quintanilla‐Martinez, Irene Gonzalez‐Menendez, Ingmar Mederacke, German Ott, Peter Sandner, Matthias Schwab, Robert Feil, Susanne Feil   +14 more
wiley   +1 more source

Targeting KRAS for cancer therapy

British Journal of Pharmacology, EarlyView.
In recent years, therapeutics targeted against KRAS proto‐oncogene GTPase (KRAS)‐mutant cancers have seen significant progress. Herein we outline the biology and epidemiology of KRAS alterations at the lineage and allele levels, reviewing the clinical evidence for KRASG12C inhibition from the discovery of the recessive switch pocket to sotorasib ...
Jianlong Jia, Ruonan Liu, Tonia A. Adamide, Isis E. Fernandez, Georgios T. Stathopoulos   +4 more
wiley   +1 more source

The chemokine receptor‐like fourth extracellular loop of the apelin receptor differentially regulates apelin and elabela binding and signalling

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Apelin and Elabela are endogenous ligands of the apelin receptor (apelin receptor/APJ), a GPCR involved in cardiovascular regulation and body fluid homeostasis. The human receptor contains a conserved disulfide bridge linking the N‐terminal domain to extracellular loop 3 (ECL3) via Cys19 and Cys281, forming a structural ...
Chloé Bonef, Hela Bouhsine, Carine Huynh, Marion Chaigneau, Steven Dubois, Mikel Garcia‐Marcos, Catherine Llorens‐Cortes, Denis Servent, Philippe Robin, Hervé Nozach, Isabel Alves, Xavier Iturrioz   +11 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

Emerging roles of pterins as signaling molecules in bacteria. [PDF]

Biochem Soc Trans
Rucker P, Augusta L, Fuqua C, Allen KD.
europepmc   +1 more source

RASD2 Drives Renal Clear Cell Carcinoma Progression via RAF1 (Ser338) Phosphorylation

Cancer Science, EarlyView.
RASD2 drives clear cell renal cell carcinoma (ccRCC) progression by physically interacting with RAF1 to induce its Ser338 phosphorylation, which subsequently activates the P38/ERK–MAPK signaling pathway to promote malignant tumor phenotypes and poor prognosis.
Jingxuan Yu, Gang Yu, Yuan Liu, Yu Zhou, Wei Liu, Lin Wang, Lide Liu, Yan Liu, Tiejun Pan, Zhenyu Liu, Lei Gao   +10 more
wiley   +1 more source

Septins in the Middle-Makers and Breakers of Membrane Contact Sites. [PDF]

J Neurochem
Holt TJ, Spiliotis ET.
europepmc   +1 more source

MiR‐375 in CAFs‐Derived EVs Promotes HCC Progression via Regulating RASA1 and May Potentially Serve as a Biomarker for HCC

Cancer Science, EarlyView.
CAFs could transfer EVs miR‐375 into endothelial cells with a low level of RASA1 and further promote EC angiogenesis. Plasma EVs miR‐375 have the potential values as a novel diagnostic and prognostic biomarker for HCC. ABSTRACT Cancer‐associated fibroblasts (CAFs) in the tumor microenvironment play an important role in cancer initiation and progression
Wei Qin, Li Wang, Beiyuan Hu, Cuicui Xiao, XiaoYing Wu, Huan Tian, Songlin Peng   +6 more
wiley   +1 more source