Nanofibre forming peptide amphiphiles were conjugated to naproxen through an esterase-sensitive linker. The amount of naproxen released, in the presence of enzymes, was influenced by the linker conjugating the drug to the supramolecular assembly. In vitro studies showed the anti-inflammatory activity of the released drug was maintained.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4201510 | PMC |
| http://dx.doi.org/10.1039/c4cc06340f | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Mitochondria Localized Anticancer Iridium(III) Prodrugs for Targeted Delivery of Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors and Cytotoxic Iridium(III) Complex.
Inorg Chem
December 2024
Department of Chemistry, Indian Institute of Technology Roorkee, Roorkee, Uttarakhand 247667, India.
Myeloid cell leukemia-1 (Mcl-1) is an antiapoptotic oncoprotein overexpressed in several malignancies and acts as one of the promising therapeutic targets for cancer. Even though there are several small molecule based Mcl-1 inhibitors reported, the delivery of Mcl-1 inhibitor at the target site is quite challenging. In this regard, we developed a series of mitochondria targeting luminescent cyclometalated iridium(III) prodrugs bearing Mcl-1 inhibitors via ester linkage due to the presence of Mcl-1 protein in the outer mitochondrial membrane.
View Article and Find Full Text PDFEsterase-Activated Hydrogen Sulfide Donors with Self-Reporting Fluorescence Properties and Highly Tunable Rates of Delivery.
ACS Chem Biol
September 2024
Department of Chemistry, Wake Forest University, Winston-Salem, North Carolina 27101, United States.
Hydrogen sulfide (HS) has emerged as a significant biomolecule with diverse activities, akin to other gaseous signaling molecules such as nitric oxide (NO) and carbon monoxide (CO). In the present study, we report on the development of esterase-activated donors that track their direct cellular donation of HS by enlisting a cyclization reaction onto a thioamide that forms a fluorogenic byproduct. This simple donor design provides a noninvasive method for monitoring the biological delivery and activity of HS, along with access to a library of compounds with highly variable rates of HS delivery.
View Article and Find Full Text PDFA Tween-80 modified hypoxia/esterase dual stimulus-activated nanomicelle as a delivery platform for carmustine - Design, synthesis, and biological evaluation.
Int J Biol Macromol
August 2024
Beijing Key Laboratory of Environmental & Viral Oncology, College of Chemistry and Life Science, Beijing University of Technology, Beijing 100124, China.
As a clinical anti-glioma agent, the therapeutic effect of carmustine (BCNU) was largely decreased because of the drug resistance mediated by O-alkylguanine-DNA alkyltransferase (AGT) and the blood-brain barrier (BBB). To overcome these obstacles, we synthesized a BCNU-loaded hypoxia/esterase dual stimulus-activated nanomicelle, abbreviated as T80-HACB/BCNU NPs. In this nano-system, Tween 80 acts as the functional coating on the surface of the micelle to facilitate transport across the BBB.
View Article and Find Full Text PDFA modular scaffold for triggerable and tunable nitroxyl (HNO) generation with a fluorescence reporter.
Chem Commun (Camb)
March 2023
Department of Chemistry, Indian Institute of Science Education and Research Pune, Pune 411 008, Maharashtra, India.
Nitroxyl (HNO) is a short-lived mediator of cell signalling and can enhance the sulfane sulfur pool, a cellular antioxidant reservoir, by reacting with hydrogen sulfide (HS). Here, we report esterase-activated HNO-generators that are suitable for tunable HNO release and the design of these donors allows for real-time monitoring of HNO release. These tools will help gain a better understanding of the cross-talk among short-lived gaseous signalling molecules that have emerged as major players in health and disease.
View Article and Find Full Text PDFEsterase-Activated, pH-Responsive, and Genetically Targetable Nano-Prodrug for Cancer Cell Photo-Ablation.
Small
May 2023
Key Laboratory of Flexible Electronics (KLOFE) & Institute of Advanced Materials (IAM), Nanjing Tech University (NanjingTech), Nanjing, 211816, China.
Activatable prodrugs have drawn considerable attention for cancer cell ablation owing to their high specificity in drug delivery systems. However, phototheranostic prodrugs with dual organelle-targeting and synergistic effects are still rare due to low intelligence of their structures. Besides, the cell membrane, exocytosis, and diffusional hindrance by the extracellular matrix reduce drug uptake.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!