Results 281 to 290 of about 130,849 (328)

Allosteric regulation of Keap1 by 8β-hydroxy-α-cyclocostunolide for the treatment of acute lung injury. [PDF]

open access: yesActa Pharm Sin B
Zhang J   +7 more
europepmc   +1 more source

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

open access: yesBritish 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   +2 more
wiley   +1 more source

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

open access: yesBritish 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   +8 more
wiley   +1 more source

A helical fulcrum in eIF2B coordinates allosteric regulation of stress signaling. [PDF]

open access: yesNat Chem Biol
Lawrence RE   +7 more
europepmc   +1 more source

Novel approaches for drug development against chronic primary pain: A systematic review

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Chronic primary pain (CPP) persisting for more than 3 months, associated with significant emotional distress without any known underlying cause, is an unmet medical need. Traditional or adjuvant analgesics do not provide satisfactory pain relief for a great proportion of these patients.
Valéria Tékus   +5 more
wiley   +1 more source

Allosteric regulation of nitrate transporter NRT via the signaling protein PII. [PDF]

open access: yesProc Natl Acad Sci U S A
Li B   +8 more
europepmc   +1 more source

Sodium butyrate ameliorates renal tubular lipid accumulation through a protein phosphatase 2A/transcription factor EB axis in diabetic nephropathy

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Extensive evidence indicates that lipid accumulation causes renal tubular injury, which further contributes to diabetic nephropathy (DN) progression. Short‐chain fatty acids (SCFAs) play an important role in the maintenance of cellular metabolic health.
Jiayin Tao   +12 more
wiley   +1 more source

Molecular basis for a pore block of Tentonin 3 expressed in HEK293 cells by a conopeptide, NMB‐1

open access: yesBritish Journal of Pharmacology, EarlyView.
Background and Purpose Tentonin 3 (TTN3/TMEM150C) is a mechanosensitive ion channel that plays critical roles in mechanotransduction processes. TTN3 forms a tetramer with a predicted rectangular shape and a central pore. A conotoxin ρ‐TIA and its synthetic analog, noxious mechanosensation blocker 1 (NMB‐1), were initially developed to inhibit slowly ...
Sujin Lim   +10 more
wiley   +1 more source

Dynamic inter-domain transformations mediate the allosteric regulation of human 5, 10-methylenetetrahydrofolate reductase. [PDF]

open access: yesNat Commun
Blomgren LKM   +7 more
europepmc   +1 more source

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