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Discovery of Potent Dengue Virus NS2B-NS3 Protease Inhibitors Among Glycyrrhizic Acid Conjugates with Amino Acids and Dipeptides Esters.
Viruses
December 2024
Department of Medical Laboratory Science and Biotechnology, Asia University, Taichung 41354, Taiwan.
This study investigated a library of known and novel glycyrrhizic acid (GL) conjugates with amino acids and dipeptide esters, as inhibitors of the DENV NS2B-NS3 protease. We utilized docking algorithms to evaluate the interactions of these GL derivatives with key residues (His51, Asp75, Ser135, and Gly153) within 10 Å of the DENV-2 NS2B-NS3 protease binding pocket (PDB ID: 2FOM). It was found that compounds and exhibited unique binding patterns, forming hydrogen bonds with Asp75, Tyr150, and Gly153.
View Article and Find Full Text PDFEvaluation of Integrated Child Health Days as a Catch-Up Strategy for Immunization in Three Districts in Uganda.
Vaccines (Basel)
November 2024
U.S. Centers for Disease Control and Prevention, Global Immunization Division, Global Health Center, Atlanta, GA 30329, USA.
Uganda's Integrated Child Health Day (ICHD) initiative aims to improve children's access to vaccinations. Although widely used as a catch-up vaccination strategy, the effectiveness of the ICHD program in increasing immunization coverage, especially among vulnerable populations, has not been recently evaluated. This study assessed the reach and uptake of ICHD for immunizations in Uganda.
View Article and Find Full Text PDFRecent Advances in Porphyrin-Based Covalent Organic Frameworks for Synergistic Photodynamic and Photothermal Therapy.
Pharmaceutics
December 2024
School of Pharmacy, Nantong University, Nantong 226001, China.
Porphyrin's excellent biocompatibility and modifiability make it a widely studied photoactive material. However, its large π-bond conjugated structure leads to aggregation and precipitation in physiological solutions, limiting the biomedical applications of porphyrin-based photoactive materials. It has been demonstrated through research that fabricating porphyrin molecules into nanoscale covalent organic frameworks (COFs) structures can circumvent issues such as poor dispersibility resulting from hydrophobicity, thereby significantly augmenting the photoactivity of porphyrin materials.
View Article and Find Full Text PDFNovel Cyclic Peptide-Drug Conjugate P6-SN38 Toward Targeted Treatment of EGFR Overexpressed Non-Small Cell Lung Cancer.
Pharmaceutics
December 2024
Department of Chemical Engineering, Biotechnology and Materials, Ariel University, Ariel 40700, Israel.
Here, we report on the synthesis and biological evaluation of a novel peptide-drug conjugate, P6-SN38, which consists of the EGFR-specific short cyclic peptide, P6, and the Topo I inhibitor SN38, which is a bioactive metabolite of the anticancer drug irinotecan. SN38 is attached to the peptide at position 20 of the E ring's tertiary hydroxyl group via a mono-succinate linker. The developed peptide-drug conjugate (PDC) exhibited sub-micromolar anticancer activity on EGFR-positive (EGFR+) cell lines but no effect on EGFR-negative (EGFR-) cells.
View Article and Find Full Text PDFColon-Targeted Poly(ADP-ribose) Polymerase Inhibitors Synergize Therapeutic Effects of Mesalazine Against Rat Colitis Induced by 2,4-Dinitrobenzenesulfonic Acid.
Pharmaceutics
December 2024
College of Pharmacy, Pusan National University, Busan 46241, Republic of Korea.
In addition to oncological applications, poly(ADP-ribose) polymerase (PARP) inhibitors have potential as anti-inflammatory agents. Colon-targeted delivery of PARP inhibitors has been evaluated as a pharmaceutical strategy to enhance their safety and therapeutic efficacy against gut inflammation. Colon-targeted PARP inhibitors 5-aminoisoquinoline (5-AIQ) and 3-aminobenzamide (3-AB) were designed and synthesized by azo coupling with salicylic acid (SA), yielding 5-AIQ azo-linked with SA (AQSA) and 3-AB azo-linked with SA (ABSA).
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