Results 141 to 150 of about 36,245 (244)

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

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

Direct and efficient synthesis of nucleosides through the ortho-(tert-butylethynyl)phenyl thioglycosides (BEPTs) protocol. [PDF]

open access: yesNat Commun
Liu H   +12 more
europepmc   +1 more source

Novel drugs approved by the EMA, the FDA and the MHRA in 2025: A year in review

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract In the 2025 novel drug mini‐review, one can take a full measure of the ingenuity that underlies current drug design and development, despite the year's smaller harvest (46 novel drugs) compared to 2024 (53) and 2023 (70). 54% of the novel drugs are first‐in‐class (FIC).
Andreas Papapetropoulos   +16 more
wiley   +1 more source

The Role of SAMHD1 in Viral Resistance and Transduction Efficiency Challenges in Pediatric Hematological Malignancies: Mechanistic Insights and Clinical Perspectives

open access: yesEuropean Journal of Haematology, EarlyView.
SAMHD1 regulates intracellular dNTP pools, influencing lentiviral transduction, gene therapy efficiency, and disease progression in pediatric hematological malignancies. Integrated bioinformatics and targeted strategies, including CRISPR and pharmacological inhibition, highlight its therapeutic potential.
Waseem Alzamzami
wiley   +1 more source

Enzymatic synthesis of bioactive quinolones and (thio)coumarins by fungal type III polyketide synthases

open access: yesThe FEBS Journal, EarlyView.
Quinolones are valuable scaffolds for drug discovery but are rare in nature. Here, we show that two fungal enzymes, AthePKS and FerePKS, can generate 2‐quinolones and two additional heteroaromatic scaffolds. Using AthePKS, we designed an artificial enzymatic cascade towards an antimicrobial quinolone from a simple precursor and implemented it in E ...
Nika Sokolova   +5 more
wiley   +1 more source

NS5-targeting nucleoside analogs inhibit dengue virus and other flaviviruses. [PDF]

open access: yesPLoS Pathog
Bhakt P   +15 more
europepmc   +1 more source

Energetic stress in combination with impaired fatty acid oxidation induces sequestration of CoA and adaptation of CoA metabolism

open access: yesThe FEBS Journal, EarlyView.
Computational modelling and in vitro liver cell experiments indicate that medium‐chain acyl‐CoA dehydrogenase (MCAD) deficiency causes an accumulation of (especially medium‐chain) acyl‐CoAs at the cost of free CoA (CoASH). A substantial decrease in CoASH impairs flux through many pathways essential for energy homeostasis.
Ligia Akemi Kiyuna   +17 more
wiley   +1 more source

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