Results 61 to 70 of about 20,284 (182)

Impact of CYP2C19 Genotype Variants on PCSK9 Inhibitor Efficacy in Lipid‐Lowering Among Patients With Symptomatic Intracranial Atherosclerotic Stenosis

Lipids, EarlyView.
ABSTRACT Ischemic stroke is frequently associated with symptomatic intracranial atherosclerotic stenosis (sICAS), is a leading cause of global disability and mortality. Current guidelines recommend dual antiplatelet and intensive statin therapies. Proprotein convertase subtilisin 9/kexin type 9 (PCSK9) inhibitors have emerged as a potent lipid‐lowering
Chao Zhao, Nuan Wang, Di Shi, Hao Zhou, Dan Chen, Guofang Chen   +5 more
wiley   +1 more source

Design, Synthesis, Cytotoxicity Assessment, and Molecular Docking of Novel Triazolopyrimidines as Potent Cyclin‐Dependent Kinase 4 Inhibitors

ChemistryOpen, EarlyView.
A novel series of 1,5‐dihydro‐[1,2,4]triazolo[4,3‐a]pyrimidines (5a–g) is synthesized and evaluated as potential CDK4 inhibitors. Compounds 5c and 5d exhibit strong cytotoxicity toward HepG2 and MCF‐7 cells with IC50 ≈ 1–2 µM, comparable to doxorubicin.
Tariq Z. Abolibda, Sami A. Al‐Hussain, Basant Farag, Mohamed El‐Naggar, Magdi E. A. Zaki, Emad S. A. Alhazmi, Adel S. M. Almohammadi, Sobhi M. Gomha   +7 more
wiley   +1 more source

Abietic Acid Enhances the Sedative Activity of Diazepam: In vivo Approach along with Receptor Binding Affinity and Molecular Interaction with the GABAergic System

ChemistryOpen, EarlyView.
Abietic acid (AA) reveals potent sedative potential by expressing fast sleeping onset and increased sleeping duration compare to the control group in thiopental sodium induced sleeping mice. The compound also exhibited notable binding affinity (–7.9 kcal/mol) toward GABAA receptors.
Meher Afroz, Rubel Hasan, Mst Muslima Khatun, Mokammel Hossain Tito, Md Shadin, Ranjit Chakma, Mohammed Asiri, Faisal H. Altemani, Abdullah H. Altemani, Md Shimul Bhuia, Muhammad Torequl Islam   +10 more
wiley   +1 more source

Computational Study on Potentially Active Antibacterial Compounds in Secondary Metabolites of Extremophilic Microorganisms

ChemistryOpen, EarlyView.
This study employed density functional theory (DFT) and conceptual DFT (CDFT) to calculate the structures and properties of potential antibacterial compounds derived from 16‐membered lactone ring‐containing secondary metabolites of extremophiles, as well as midecamycin.
Dilong Li, Yanni Wang, Yinhuan Huang, Hui Zhou, Xiaoyun Xia, Wei Huang, Chaojie Wang   +6 more
wiley   +1 more source

Computational Evaluation of Statin Analogs Targeting HMG‐CoA Reductase for Coronary Artery Disease Treatment

ChemistryOpen, EarlyView.
Molecular dynamics analysis of novel statin analogs shows that binding induces superior stabilization of HMG‐CoA reductase. As shown by the solvent‐accessible surface area profile, ligand‐induced rigidity offers a new, effective strategy for drug design. Cardiovascular diseases remain a leading cause of global mortality.
Yoshua B. Mtulo, Geradius Deogratias, James E. Mgaya, Andrew S. Paluch, Lucas Paul   +4 more
wiley   +1 more source

Transforming Treatment: The Impact of Bariatric Surgery on Oral Drug Absorption

Obesity Reviews, EarlyView.
ABSTRACT Obesity represents a significant threat to global public health, with an estimated 16% of adults worldwide (2022) being classified as people with obesity, with a body mass index of 30 or more. Bariatric surgery is regarded as the most effective treatment option for people with obesity, with the three main types of bariatric surgery being ...
Danielle Wigg, Andrea Edginton, Matthew D. Jones, Nikoletta Fotaki   +3 more
wiley   +1 more source

Antiplasmodial Activity and Pharmacokinetic Profiling of Cryptolepine and 2,7‐Dibromocryptolepine With a View to Informing the Design of Novel Antimalarial Cryptolepine Analogues

Drug Development Research, Volume 87, Issue 2, April 2026.
ABSTRACT The roots of the climbing shrub Cryptolepis sanguinolenta are traditionally used in West Africa for the treatment of malaria. The principal constituent, cryptolepine (1), has been shown to have antimalarial activity but there are concerns regarding its toxicity on account of its DNA‐intercalating property.
Elodie Chenu, James Duffy, Arnold Donkor Forkuo, Stephen Y. Gbedema, Seham Abdelall, Muhammad Wahajuddin, Huw S. Jones, Colin W. Wright   +7 more
wiley   +1 more source

METTL3-mediated methylation of CYP2C19 mRNA may aggravate clopidogrel resistance in ischemic stroke patients

Open Medicine
N6-methyladenosine (m6A) is the most frequently occurring interior modification in eukaryotic messenger RNA (mRNA), and abnormal mRNA modifications can affect many biological processes.
Tan Quandan, Yang Le, Yuan Shanshan, Zheng Danni, Lin Yapeng, Chen Kejie, He Ying, Chen Shuntian, Hao Junli, Dai Jin, He Song, Mao Fengkai, Leng Xinyi, Jiang Haisong, Yang Jie   +14 more
doaj   +1 more source

Both CYP2C19 and PON1 Q192R Genotypes Influence Platelet Response to Clopidogrel by Thrombelastography in Patients with Acute Coronary Syndrome

Cardiovascular Therapeutics, 2019
Objective. The objective of this study is to explore the relationships of the effects of CYP2C19 and PON1 Q192R polymorphism on the activity of clopidogrel and the risk of high platelet responsiveness (HPR) by thrombelastography in patients with acute ...
Wenxing Peng, Xiujin Shi, Xiaoyu Xu, Yang Lin   +3 more
doaj   +1 more source

Pregnane X Receptor Regulates Human Endocrine System by Inducing Sex Hormone–Binding Globulin Expression

Basic &Clinical Pharmacology &Toxicology, Volume 138, Issue 4, April 2026.
ABSTRACT Sex hormone–binding globulin (SHBG) is a sex hormone carrier. We aimed to characterize the role of pregnane X receptor (PXR), a major regulator of drug metabolism, in SHBG regulation. Serum SHBG was measured in four clinical trials (n = 61) and expression in in vitro experiments in human 3D hepatocyte spheroids and HepG2 cells.
Maria H. Ahonen, Anja Konzack, Tomas Smutny, Petr Pavek, Jukka Hakkola, Janne Hukkanen   +5 more
wiley   +1 more source