Results 41 to 50 of about 65,300 (300)

Coarse-Grained Model-Assisted Design of Optimized Polymer Prodrug Nanoparticles: A Combined Theoretical and Experimental Study

, 2023
To achieve efficient drug release from polymer prodrug nanoparticles, the drug-polymer linker must be accessible for cleavage to release the drug, which can occur under certain physiological conditions (e.g., presence of specific enzymes). Supramolecular
Tâp, Ha-Duong, Ping, Gao, Julien, Nicolas   +2 more
core   +1 more source

Identifying transcription factors controlling the basal expression of human MRP4 highlights a substantial role for Sp1

FEBS Open Bio, EarlyView.
The MRP4 transporter exports several drugs and signaling molecules. Here, we identified key promoter elements regulating basal MRP4 expression. Using reporter assays, we defined a conserved region with essential Sp1 and contributory Ets sites, which controlled basal MRP4 expression.
Debora Singer, Angelique Kragl, Katrin Ziems, Juliane Glaubitz, Sophie Grammbauer, Susanne Hildebrandt, Mladen V. Tzvetkov, Gabriele Jedlitschky   +7 more
wiley   +1 more source

PLA₂-Triggered Activation of Cyclosporine-Phospholipid Prodrug as a Drug Targeting Approach in Inflammatory Bowel Disease Therapy

Pharmaceutics, 2022
Oral medication with activity specifically at the inflamed sites throughout the gastrointestinal tract and limited systemic exposure would be a major advance in our therapeutic approach to inflammatory bowel disease (IBD).
Milica Markovic, Shimon Ben-Shabat, Jagadeesh Nagendra Manda, Karina Abramov-Harpaz, Clil Regev, Yifat Miller, Aaron Aponick, Ellen M. Zimmermann, Arik Dahan   +8 more
doaj   +1 more source

Electrodrugs: An electrochemical prodrug activation strategy

, 2018
Dataset corresponding to manuscript entitled "Electrodrugs: an electrochemical prodrug activation strategy"
Murray, Alan, Bradley, Mark, Tucker, Lulu, González-Fernández, Eva, Norman, D, Staderini, Matteo, Clavadetscher, Jessica, Mount, Andrew R   +7 more
core   +1 more source

UiO‐66 metal–organic frameworks in biomedicine: From structural tunability to bioimaging, photodiagnostics, and photodynamic cancer therapy

FEBS Open Bio, EarlyView.
UiO‐66(Zr) metal–organic frameworks are chemically stable, biocompatible, and highly tunable nanomaterials. Their modular structure enables controlled drug delivery, multimodal bioimaging, and light‐activated photodynamic therapy, supporting integrated diagnostic and therapeutic (theranostic) applications in cancer and biomedical research.
Veronika Huntošová, Grigorii Rakhalskii, Miroslav Almáši   +2 more
wiley   +1 more source

Lipophilic nanocrystal prodrug-release defines the extended pharmacokinetic profiles of a year-long cabotegravir

Nature Communications, 2021
Here, the authors provide a mechanism for an improved version of a nanoformulated myristoylated prodrug of cabotegravir (CAB), named NM2CAB, and its bioavailability, stability and pharmacokinetics in mice and rats performed in independent academic and a ...
Nagsen Gautam, JoEllyn M. McMillan, Devendra Kumar, Aditya N. Bade, Qiaoyu Pan, Tanmay A. Kulkarni, Wenkuan Li, Brady Sillman, Nathan A. Smith, Bhagya L. Dyavar Shetty, Adam Szlachetka, Benson J. Edagwa, Howard E. Gendelman, Yazen Alnouti   +13 more
doaj   +1 more source

Intrinsic Photoactive Star ZnPc–Poly(glutamate) Nanoplatforms for Multimodal Glioblastoma Therapy and Brain‐Targeted Delivery

Advanced Functional Materials, EarlyView.
An intrinsic photoactive star‐shaped zinc phtalocyanine‐poly(L‐glutamic acid) (ZnPc‐PGA) nanoplatform for multimodal glioblastoma (GBM) therapy and brain‐targeted elivery. A ZnPc‐PGA‐based multifunctional theranostic nanocarrier platform enables image‐guided, multimodal GBM therapy. ZnPc‐PGA nanocarriers support the integration of fluorescence imaging,
Amina Benaicha‐Fernández, Teodora Ranđelović, Ana Armiñán, Víctor Sebastián, Manuel Fuentes, Cristián Huck‐Iriart, Esther Masiá, Paula Carrascosa‐Marco, Pablo Juanes‐Velasco, Snežana Đorđević, Clara Bayona, Ignacio Ochoa, Maria Medel, Inmaculada Conejos‐Sánchez, María J. Vicent   +14 more
wiley   +1 more source

Structure-guided microbial targeting of antistaphylococcal prodrugs

eLife, 2021
Carboxy ester prodrugs are widely employed to increase oral absorption and potency of phosphonate antibiotics. Prodrugging can mask problematic chemical features that prevent cellular uptake and may enable tissue-specific compound delivery. However, many
Justin J Miller, Ishaan T Shah, Jayda Hatten, Yasaman Barekatain, Elizabeth A Mueller, Ahmed M Moustafa, Rachel L Edwards, Cynthia S Dowd, Geoffrey C Hoops, R Jeremy Johnson, Paul J Planet, Florian L Muller, Joseph M Jez, Audrey R Odom John   +13 more
doaj   +1 more source

Engineering Pendant Group Chemistry to Control Hydrophilicity and Oxidative Degradation of Thioketal‐Based Biomaterials

Advanced Functional Materials, EarlyView.
Thioketal (TK) polymers are promising biomaterials due to their selective biodegradation by reactive oxygen species (ROS), but they respond slowly to physiologic doses of ROS. Here, the TK bond's pendant groups are modified to enhance the degradation of TK‐based implants both in vitro and in vivo.
Karina A. Bruce, Dylan W. Marques, Alan J. Fullenkamp, Emma‐Louise Lowell, Rais B. Fataki, Jake D. Ryan, John R. Martin   +6 more
wiley   +1 more source

Enzyme-mediated hydrolytic activation of prodrugs

Acta Pharmaceutica Sinica B, 2011
Prodrug design is an important part of drug discovery. Prodrugs can offer many advantages over parent drugs such as increased solubility, enhanced stability, improved bioavailability, reduced side effects, and better selectivity.
Yan-hui Yang, Herve Aloysius, Daigo Inoyama, Yu Chen, Long-qin Hu   +4 more
doaj   +1 more source