Results 91 to 100 of about 20,922 (255)

CAQ Corner: Basic concepts of transplant immunology

open access: yes, 2022
Liver Transplantation, EarlyView.
Amanda Cheung, Josh Levitsky
wiley   +1 more source

Stafib‐2‐CR: an Improved Nanomolar and Selective Inhibitor of the Transcription Factor STAT5b Developed by Conformational Restriction of Stafib‐2

open access: yesChemistry – A European Journal, EarlyView.
Conformational restriction strategies to increase the activity and selectivity of the STAT5b inhibitor Stafib‐2 are presented. The best conformationally restricted inhibitor Stafib‐2‐CR has threefold higher activity against STAT5b than Stafib‐2. A cell‐permeable prodrug of Stafib‐2‐CR inhibits phosphorylation of STAT5b in cultured human leukemia cells ...
Theresa Münzel   +5 more
wiley   +1 more source

Chemotherapeutic Potential of Fluorouracil‐Platinum (IV) Prodrugs Against Cisplatin‐Resistant Colorectal Cancer Cells

open access: yesChemistry – A European Journal, EarlyView.
ABSTRACT Fluorouracil‐platinum(IV) prodrugs represent a novel class of multimechanistic chemotherapeutics with enhanced anticancer potential. The prodrugs PtIVP‐5FUMeOBut and PtIV56‐5FUMeOBut were actualized by derivatising the clinical drug 5‐fluorouracil (5FU) and coordinating it to platinum(IV) complexes, leveraging the established cytotoxicity of ...
Maria George Elias   +9 more
wiley   +1 more source

Living Microbial Drugs

open access: yesChemistry – A European Journal, EarlyView.
The introduction outlines the review scope. Microbial cell factories as living drugs cover host–gut microbiota, bacteria, yeast, and other microbial systems, with comparative host advantages. Engineering strategies include synthetic circuits, quorum sensing, and memory.
Cemile Elif Özçelik   +3 more
wiley   +1 more source

Protease-Activated Drug Development

open access: yesTheranostics, 2012
In this extensive review, we elucidate the importance of proteases and their role in drug development in various diseases with an emphasis on cancer. First, key proteases are introduced along with their function in disease progression.
Ki Young Choi, Magdalena Swierczewska, Seulki Lee, Xiaoyuan Chen
doaj  

Bioresponsive pseudoGlucosinolates (psGSLs) Release Isothiocyanates (ITCs) in the Presence of Nitroreductases

open access: yesChemistry – A European Journal, EarlyView.
This work introduces the concept of pseudoglucosinolates (psGSLs) and reports the synthesis and evaluation of nitroreductase‐responsive psGSLs. These compounds represent a complementary prodrug strategy to natural glucosinolates (GSLs) for the controlled release of isothiocyanates (ITCs), enabling bio‐responsive protein labeling, as demonstrated in ...
Claire C. Jimidar   +13 more
wiley   +1 more source

In pursuit of feedback activation: New insights into redox-responsive hydropersulfide prodrug combating oxidative stress

open access: yesRedox Biology
Redox-responsive hydropersulfide prodrugs are designed to enable a more controllable and efficient hydropersulfide (RSSH) supply and to thoroughly explore their biological and therapeutic applications in oxidative damage.
Bi-Xin Xu   +10 more
doaj   +1 more source

Membrane‐Permeable Nucleoside T‐1106 Diphosphate and Triphosphate Analogues as Antiviral Pronucleotides

open access: yesChemistry – A European Journal, EarlyView.
Favipiravir (T‐705) and the non‐fluorinated counterpart (T‐1106) are antiviral agents that inhibit the RNA‐dependent RNA polymerase (RdRp) of various RNA viruses. The antiviral efficacy of nucleoside analogues is strongly dependent on their intracellular activation by cellular kinases to produce their corresponding triphosphate metabolites (T‐705‐RTP ...
Chris Meier   +7 more
wiley   +1 more source

Organelle‐Resolved Tetrazine‐trans‐Cyclooctene Click Chemistry for Cargo Delivery and Release

open access: yesChemistry – A European Journal, EarlyView.
Bioorthogonal click chemistry tools provide a means for specific intracellular conjugation of molecules. In this study, we used reactive tetrazine (Tz) and TCO moieties for labeling of organelles and organelle‐specific delivery and activation of doxorubicin prodrugs.
Oleh Durydivka   +6 more
wiley   +1 more source

Clinical Model‐Informed Precision Dosing Consult Service for Accelerating Personalized Medication in Pediatric Patients

open access: yesClinical Pharmacology &Therapeutics, EarlyView.
Traditional dosing strategies often rely on a “one‐size‐fits‐all” paradigm, assuming an “average” patient with typical demographic and pharmacological characteristics. In reality, this often overlooks existing between‐patient variability and can lead to suboptimal drug exposure or toxicity. This issue is especially pronounced in pediatric patients, who
Zachary L. Taylor   +12 more
wiley   +1 more source

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