Results 181 to 190 of about 2,738,308 (324)

Improving Proteolysis‐Targeting Chimera Delivery by Targeting Key Biomarkers in Tumor Endocytosis Pathways

MedComm – Biomaterials and Applications, Volume 5, Issue 3, September 2026.
The image illustrates how PROTACs utilize endocytosis, mediated by cell surface proteins, to overcome bioavailability limitations and enable efficient intracellular delivery. ABSTRACT Proteolysis‐targeting chimeras (PROTACs) are promising therapeutic agents for targeted protein degradation via the ubiquitin‐proteasome system; however, their clinical ...
Huahua Chen, Jiayan Jiao, Huiling Yang, Tao He   +3 more
wiley   +1 more source

In vitro formation kinetics of two 2,5-dimethylfuran phase-I metabolites: cis-3-hexene-2,5-dione and 5-methylfurfuryl alcohol. [PDF]

Arch Toxicol
Appel J, Kulosa C, Becker N, Stegmüller S, Sadzik S, Richling E.   +5 more
europepmc   +1 more source

Comprehensive Investigation of Benzimidazolium Derivatives Through Synthesis, Characterization, Cytotoxicity Activity, Immunocytochemistry, and ADME and Toxicity Analyses

ChemistryOpen, Volume 15, Issue 9, September 2026.
Three benzimidazolium derivatives bearing fluoro, chloro, and methoxy substituents are synthesized and evaluated for anticancer activity. Compound 2b shows the highest antiproliferative activity and induces apoptosis through caspase‐3 activation and PARP1 cleavage. In this study, three novel benzimidazolium derivatives (2a–c) bearing 4‐fluoro, 3‐chloro,
Gulay Dilek, Senem Akkoc
wiley   +1 more source

Stereoselective Biotransformation: Transfer of Learning to Advance Drug Metabolism and Biocatalysis. [PDF]

Angew Chem Int Ed Engl
Okunlola GA, Aleku GA.
europepmc   +1 more source

Codeine and Metabolite Concentrations in the Breastfed Neonate

Pediatric Anesthesia, Volume 36, Issue 9, Page 1016-1022, September 2026.
ABSTRACT Analgesic effect from codeine is from its metabolite, morphine. Morphine is formed by the O‐demethylation of codeine and that enzyme is controlled by the cytochrome P450 2D6. More than 60 alleles in the CYP2D6 gene have been identified. This spectrum of polymorphism can be categorized into four groups: poor (PM), intermediate (IM), normal (NM),
Brian J. Anderson, Jacqueline A. Hannam
wiley   +1 more source

Cross-Species Hepatic Metabolism of the Antileishmanial Chalcone NAT22 Generates Metabolites with Predicted Enhanced Affinity for the Parasite Target cTXNPx. [PDF]

Pharmaceutics
Barreto ARR, Valente APC, Schaeffer E, de Almeida VM, Muzitano MF, Barth T, de Souza AMT, de A A Vieira B, da Silva AM, Santos-Filho OA, Steel PG, Rossi-Bergmann B.   +11 more
europepmc   +1 more source

Application of Physiologically Based Pharmacokinetic Modeling to Optimize Assessment of Age‐Related Fluoxetine Accumulation in the Elderly

CPT: Pharmacometrics &Systems Pharmacology, Volume 15, Issue 9, September 2026.
ABSTRACT This study quantified age‐related differences in fluoxetine pharmacokinetics and evaluated the influence of CYP2D6 phenotype using physiologically based pharmacokinetic (PBPK) modeling integrated with clinical therapeutic drug monitoring data.
Yoo Jin Jang, Dong‐Gyu Heo, Eunjin Hong   +2 more
wiley   +1 more source

Discovery of Novel Bicyclic Pyrazole Amides as Potent Neuronal K_V7 Potassium Channel Openers with Strong Preclinical Antiseizure Activity. [PDF]

ACS Med Chem Lett
Sun S, Jia Q, Bankar G, Burford KN, Christabel J, Clement HA, de Boer G, Feng Z, Hambira CM, Jackson SK, Khakh K, Kwan R, Lee S, Li J, Lindgren A, Mezeyova J, Sabbatini J, Urrutia A, Charifson P, Clark MP, Wesolowski SS, Johnson JP, Empfield JR, Dehnhardt CM, Dean R.   +24 more
europepmc   +1 more source

Introduction to Single‐Cell Physiologically‐Based Pharmacokinetic (scPBPK) Models

CPT: Pharmacometrics &Systems Pharmacology, Volume 15, Issue 9, September 2026.
ABSTRACT The current investigation introduces single‐cell physiologically based pharmacokinetic (scPBPK) models to gain insight into drug disposition at the cellular scale. The transition from standard PBPK (sPBPK) models to scPBPK models required depiction of expression‐dependent (ED) processes, such as drug metabolism or membrane transport.
Anshul Saini, James M. Gallo
wiley   +1 more source

Pharmacokinetics and Brain Distribution of a Purine-Derived Neuroprotective Agent after Intranasal Administration in Neonatal Rats with Hypoxic-Ischemic Brain Injury. [PDF]

Pharm Res
Maïza A, Disdier C, Tsintzou A, Nguyen AL, Pruvost A, Théodoro F, Zang Z, Wang B, Oumata N, Galons H, Stonestreet BS, Mabondzo A, Chen XF.   +12 more
europepmc   +1 more source