Results 171 to 180 of about 187,197 (244)

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

open access: yesBritish 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   +14 more
wiley   +1 more source

Targeting KRAS for cancer therapy

open access: yesBritish 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   +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

open access: yesBritish 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   +11 more
wiley   +1 more source

Pan-RAS Inhibitors: Expanding Therapeutic Potential and Evading Resistance. [PDF]

open access: yesCancers (Basel)
Ramesh S   +14 more
europepmc   +1 more source

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

open access: yesBritish 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   +3 more
wiley   +1 more source

RANBP3 and RAN orchestrate CRM1-mediated nuclear export of hepatitis B virus RNAs. [PDF]

open access: yesJ Virol
Wang M   +14 more
europepmc   +1 more source

Serotonin engages divergent 5‐HT receptor pathways for cell type‐resolved modulation of prefrontal layer 5 microcircuits

open access: yesBritish Journal of Pharmacology, EarlyView.
Serotonin differentially modulates layer 5 mPFC microcircuits through cell type‐specific pre‐ and postsynaptic receptor pathways. Presynaptic 5‐HT1BRs suppress glutamate and GABA release, whereas presynaptic and postsynaptic 5‐HT3ARs enhance fast‐spiking interneuron activity, whilst distinct pyramidal neuron subtypes exhibit divergent 5‐HT1AR‐ and 5 ...
Ramya Rama   +4 more
wiley   +1 more source

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