Results 121 to 130 of about 5,995 (180)
ChemMedChem, Volume 21, Issue 20, 28 October 2026.Riluzole metabolism guided the design of benzo[d]thiazole inhibitors of casein kinase 1 delta (CK1δ), a kinase linked to amyotrophic lateral sclerosis (ALS). Docking supported ATP site recognition by the hydroxylamine metabolite and hydrazine analogues, leading to compounds showing improved potency and retained predicted blood brain barrier ...
Simone Adorinni +18 more
wiley +1 more source
ChemMedChem, Volume 21, Issue 19, 14 October 2026.A series of diethylene glycol‐linked cyclic derivatives with diversity in the heterocyclic motif have been synthesized and screened for antitumor activity. Two bis‐thiazolo[3,2‐a]pyrimidinone derivatives displayed moderate cytotoxicity, high selectivity against hepatocellular carcinoma cells, promising VEGFR2, and remarkable FGFR2 inhibitory activities
Sami A. Al‐Hussain +6 more
wiley +1 more source
Searching for Novel COVID19 Treatments: Towards Covalent TMPRSS2 Inhibitors
ChemMedChem, Volume 21, Issue 19, 14 October 2026.We designed, synthesised, and evaluated new guanidine derivatives as potential covalent inhibitors of TMPRSS2, a key protease for SARS‐CoV‐2 entry. Computational studies showed that some compounds have improved binding over nafamostat. However, experimentally none effectively blocked viral entry in cell assays, indicating further optimisation is needed.
Marco Minneci +6 more
wiley +1 more source
Caffeine intake and CYP1A2 variants associated with high caffeine intake protect non-smokers from hypertension [PDF]
, 2017 The 15q24.1 locus, including CYP1A2, is associated with blood pressure (BP). The CYP1A2 rs762551 C allele is associated with lower CYP1A2 enzyme activity. CYP1A2 metabolizes caffeine and is induced by smoking. The association of caffeine consumption with
Cappuccio, Franco +19 more
core
, 2005 Clozapine, an atypical antipsychotic, depends mainly on cytochrome P4501A2 (CYP1A2) for its metabolic clearance. CYP1A2 is inducible by smoking, and lower plasma concentrations of clozapine are measured in smokers than in nonsmokers.
Bondolfi, G. +11 more
core +1 more source
AhR is required for skatole-mediated CYP1A1 and CYP1A2 up-regulation.
, 2016 (A) RT-qPCR analysis of AhR, CYP1A1 and CYP1A2 mRNA expression in PHHs (Donor #391) after siRNA-mediated AhR down-regulation. (B) RT-qPCR analysis of CYP1A1 (B) and CYP1A2(C) mRNA expression in PHHs after siRNA-mediated AhR down-regulation and incubation
Sabine Gerbal-Chaloin (2637070) +4 more
core +1 more source
, 2019 We report the first genome-wide association study of habitual caffeine intake. We included 47,341 individuals of European descent based on five population-based studies within the United States.
Subar, Amy +32 more
core +1 more source
, 2020 ABBREVIATIONS: CYP1A2, cytochrome P450 isoform CYP1A2; QSAR, quantitative structure-activity relationship; 1 ,7-DMX, 1 ,7 ...
Uwe Fuhr +10 more
core