Viral kinetics in adults with Covid-19 treated with nirmatrelvir-ritonavir or molnupiravir: a population-based, observational cohort study. [PDF]
Prager M +16 more
europepmc +1 more source
We narrated the identification of benzotriazole‐based cereblon ligands for their potential use either in PROTAC or CELMoD chemical space, through systematic design and SAR studies, synthesis, biological, and docking experiments resulting in a non‐cytotoxic, potent, drug‐like compound 13, offering scope for optimization to yield an in vivo efficacious ...
Pramit Ganguly +12 more
wiley +1 more source
<i>In vitro</i> susceptibility and provisional epidemiological cutoff values for eight antifungal agents against <i>Trichophyton mentagrophytes</i> and <i>Trichophyton interdigitale</i>: a multicenter study from China. [PDF]
Zheng H +18 more
europepmc +1 more source
Targeting PIKfyve: Chemical Biology and Drug Discovery Insights
PIKfyve inhibitors have progressed from niche chemical probes to powerful tools for interrogating endolysosomal biology, enabled by rapid and robust cellular phenotypes. Compounds such as apilimod establish PIKfyve as a druggable lipid kinase, while agents like vacuolin‐1 underscore the importance of distinguishing true target engagement from ...
Athavan Alias Anand Selvam +1 more
wiley +1 more source
Roles of Ceramide Glucosyltransferase in Controlling Cerebral Microvascular Endothelial Integrity and Angiogenesis Post-Ischemia/Reperfusion. [PDF]
Mohamud Yusuf A +9 more
europepmc +1 more source
Novel benzothiazole‐triazole derivatives were designed and synthesized as potential anticancer agents targeting the PI3K/Akt pathway. Compound 5h exhibited potent Akt1 inhibition, induced apoptosis and mitochondrial dysfunction in MCF‐7 cells, and demonstrated stable binding in molecular docking and dynamics studies, highlighting its promise for breast
Bilge Çiftçi +3 more
wiley +1 more source
The Therapeutic Potential of Purmorphamine Across Disease Models
ABSTRACT Purmorphamine (PUR) is a trisubstituted purine compound that selectively activates Smoothened receptor, thereby initiating Sonic Hedgehog (Shh) signalling—a pathway critical for embryonic patterning, neuronal specification and tissue regeneration across multiple organ systems. Dysregulation of Shh signalling has been implicated in degenerative
Ashis Dhar +4 more
wiley +1 more source
Netupitant versus aprepitant: model-predicted neurokinin-1 receptor occupancy and implications for long-delayed nausea and vomiting prevention. [PDF]
Iihara H +12 more
europepmc +1 more source
From Fragments to Function: Novel Hydrazone Derivatives as Monoamine Oxidase Inhibitors
Twelve N‐acylhydrazone derivatives (5a–f, 6a–f) were synthesized and characterized. Compounds displayed potent submicromolar inhibition against both MAO‐A and MAO‐B. Compound 6e exhibited the strongest activity (IC50 = 0.073 μM for MAO‐A; 0.064 μM for MAO‐B). Kinetic and docking analyses confirmed reversible, competitive inhibition via FAD interaction.
Hasan Erdinç Sellitepe +5 more
wiley +1 more source
Genetic Background Modulates Zoliflodacin and Gepotidacin Cross-Resistance and Fitness in Neisseria gonorrhoeae. [PDF]
Mukherjee A +5 more
europepmc +1 more source

