Results 151 to 160 of about 41,396 (291)

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

MYC Addiction as a Targetable Vulnerability in Nelarabine‐Resistant T‐Cell Acute Lymphoblastic Leukemia

open access: yesCancer Science, EarlyView.
MYC drives nelarabine resistance in T‐ALL via a hyperactive transcriptional program. Pharmacological degradation of BET proteins dismantles this addiction, restoring drug sensitivity and extending survival in vivo. ABSTRACT Acquired resistance represents a fundamental obstacle limiting the long‐term efficacy of cancer chemotherapy.
Jingjing Gao   +9 more
wiley   +1 more source

Discovery of a Novel γ‐Glutamylcyclotransferase Inhibitor Plumbagin by Luminescence‐Based High‐Throughput Screening

open access: yesCancer Science, EarlyView.
A cell‐based high‐throughput screening system utilizing the luminescent probe LISA‐103 was developed to monitor γ‐glutamylcyclotransferase (GGCT) activity in cancer cells. Through this assay, plumbagin was identified as a novel GGCT inhibitor that induces cell cycle arrest and suppresses cancer cell growth. ABSTRACT γ‐Glutamylcyclotransferase (GGCT) is
Keiko Taniguchi   +10 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

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

Contrasting effects of different molecular crowding environments on base‐pair opening/closing dynamics of DNA triplex structures

open access: yesThe FEBS Journal, EarlyView.
Base‐pair opening and closing regulate nucleic‐acid structure, stability, and function, but how these motions behave under intracellular molecular crowding remains unclear. Using NMR, we quantified these dynamics in a DNA triplex under two crowder‐reconstituted environments that mimic cellular crowding.
Tomoki Sakamoto   +3 more
wiley   +1 more source

Suppression of Indoleamine 2,3‐Dioxygenase Enhances Immune Responses to the Therapeutic Vaccine for Chronic Hepatitis B

open access: yesHepatology Research, EarlyView.
Indoleamine 2,3‐dioxygenase (IDO) activity modulates immune responses to the therapeutic HBV vaccine NASVAC. Genetic or pharmacological suppression of IDO enhanced vaccine efficacy in mice, and lower serum kynurenine levels predicted favorable responses in humans, suggesting IDO as both a therapeutic target and a biomarker.
Yohei Shirakami   +15 more
wiley   +1 more source

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