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Improving iPSC Differentiation Using a Nanodot Platform.
ACS Appl Mater Interfaces
July 2024
Center for Regenerative Medicine and Cellular Therapy, National Yang Ming Chiao Tung University, Hsinchu, 300, Taiwan, ROC.
Differentiation of induced pluripotent stem cells (iPSCs) is an extremely complex process that has proven difficult to study. In this research, we utilized nanotopography to elucidate details regarding iPSC differentiation by developing a nanodot platform consisting of nanodot arrays of increasing diameter. Subjecting iPSCs cultured on the nanodot platform to a cardiomyocyte (CM) differentiation protocol revealed several significant gene expression profiles that were associated with poor differentiation.
View Article and Find Full Text PDFIntegrated anti-vascular and immune-chemotherapy for colorectal carcinoma using a pH-responsive polymeric delivery system.
J Control Release
June 2024
State Key Laboratory of Vaccines for Infectious Diseases, Center for Molecular Imaging and Translational Medicine, Xiang An Biomedicine Laboratory, School of Public Health, Xiamen University, Xiamen 361102, China; State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, National Innovation Platform for Industry-Education Integration in Vaccine Research, Xiamen University, Xiamen 361102, China. Electronic address:
Colorectal carcinoma (CRC) has become one of the most prevalent malignant tumors and exploring a potential therapeutic strategy with diminished drug-associated adverse effects to combat CRC is urgent. Herein, we designed a pH-responsive polymer to efficiently encapsulate a stimulator of interferon genes (STING) agonist (5,6- dimethylxanthenone-4-acetic acid, termed ASA404) and a common clinically used chemotherapeutic agent (1-hexylcarbamoyl-5-fluorouracil, termed HCFU). Investigations in vitro demonstrated that polymer encapsulation endowed the system with a pH-dependent disassembly behavior (pH 6.
View Article and Find Full Text PDFComparison of the antifungal activity of the pyrimidine analogs flucytosine and carmofur against human-pathogenic dematiaceous fungi.
Med Mycol
March 2024
Mycology Laboratory, National Institute of Infectious Diseases Evandro Chagas, INI/Fiocruz, Rio de Janeiro, Brazil.
Article Synopsis
- Chromoblastomycosis (CBM) and pheohyphomycosis (PHM) are fungal infections caused by dematiaceous fungi, with flucytosine (5-FC) historically used for treatment but often leading to resistance.
- This study evaluated carmofur, a related drug, showing it has higher selectivity and potential synergistic effects when used with other antifungals against certain fungal strains.
- While carmofur demonstrated some advantages in combating resistance, it also faced its own challenges, indicating the need for careful consideration in its clinical use alongside other treatments.
Cyclodextrin Metal-Organic Frameworks as a Drug Delivery System for Selected Active Pharmaceutical Ingredients.
ACS Omega
February 2024
Department of Medical Chemistry, Medical University of Lublin, Chodzki 4A, Lublin 20-093, Poland.
The cyclodextrin-based metal-organic frameworks (CD MOFs) are a suitable molecular platform for drug delivery systems of various active pharmaceutical ingredients (APIs). The low toxicity and cost-efficient synthesis make CD MOFs an attractive host for the encapsulation of APIs. In this study, we created a model system based on γCD-K MOFs with widely used drugs carmofur (HCFU), 5-fluorouracil (5-FU), and salicylic acid (HBA) to study host-guest encapsulation methods using different crystallization protocols.
View Article and Find Full Text PDFDiscovery of antiviral SARS-CoV-2 main protease inhibitors by structure-guided hit-to-lead optimization of carmofur.
Eur J Med Chem
November 2023
School of Life Sciences, Gwangju Institute of Science and Technology, 123 Cheomdangwagi-ro, Buk-gu, Gwangju, 61005, Republic of Korea. Electronic address:
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (M) has been targeted for the development of anti-SARS-CoV-2 agents against COVID-19 infection because M processes essential viral polyproteins and plays a key role in SARS-CoV-2 replication. In this study, we report the development of novel SARS-CoV-2 M inhibitors derived from carmofur, a previously identified compound that has shown moderate potency as a covalent inhibitor of SARS-CoV-2 M. To employ a structure-guided drug design strategy, a putative intact binding mode of carmofur at catalytic active site of M was initially predicted by docking simulation.
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