A series of sulfonamides (1) has been prepared as inhibitors of interleukin-1beta converting enzyme (ICE), also known as caspase 1. These compounds were designed to improve potency by rigidifying the enzyme bound molecule through an intramolecular hydrogen bond. An X-ray crystal structure of a representative member of this series bound to the active site of ICE, confirms the presence of the hydrogen bonding interaction.
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http://dx.doi.org/10.1016/j.bmcl.2003.10.065 | DOI Listing |
J Mater Chem B
January 2025
Department of Advanced Materials Science & Engineering, Hanseo University, Seosan, Chungnam 31962, Republic of Korea.
MXenes are a class of 2D transition metal carbides and nitrides (MXT) that have attracted significant interest owing to their remarkable potential in various fields. The unique combination of their excellent electromagnetic, optical, mechanical, and physical properties have extended their applications to the biological realm as well. In particular, their ultra-thin layered structure holds specific promise for diverse biomedical applications.
View Article and Find Full Text PDFJACS Au
January 2025
School of Chemistry and Chemical Engineering, Chemistry and Biomedicine Innovation Center (ChemBIC), State Key Laboratory of Coordination Chemistry, Najing University, Nanjing 210023, PR China.
Cancer cells often upregulate ribosome biogenesis to meet increased protein synthesis demands for rapid proliferation; therefore, targeting ribosome biogenesis has emerged as a promising cancer therapeutic strategy. Herein, we introduce two Pt complexes, ataluren monosubstituted platinum(IV) (SPA, formula: c,c,t,-[Pt(NH)Cl(OH)(CHFNO)], where CHFNO = ataluren) and ataluren bisubstituted platinum(IV) complex (DPA, formula: c,c,t,-[Pt(NH)Cl(CHFNO)], where CHFNO = ataluren), which effectively suppress ribosome biogenesis by inhibiting 47s pre-RNA expression. Furthermore, SPA and DPA induce nucleolar stress by dispersing nucleolar protein NPM1, ultimately inhibiting protein generation in tumor cells.
View Article and Find Full Text PDFJACS Au
January 2025
Key Lab for Ultrafine Materials of Ministry of Education, School of Materials Science and Engineering, East China University of Science and Technology, Shanghai 200237, China.
The creation of spatially coupled meso-/microenvironments with biomimetic compartmentalized functionalities is of great significance to achieve efficient signal transduction and amplification. Herein, using a soft-template strategy, UiO-67-type hierarchically mesoporous metal-organic frameworks (HMMOFs) were constructed to satisfy the requirements of such an artificial system. The key to the successful synthesis of HMUiO-67 is rooted in the utilization of the preformed cerium-oxo clusters as metal precursors, aligning the growth of MOF crystals with the mild conditions required for the self-assembly of the soft template.
View Article and Find Full Text PDFInt J Nanomedicine
January 2025
School of Pharmacy, Jiangxi Medical College, Nanchang University, Nanchang, 330006, People's Republic of China.
Purpose: To improve the oral absorption of relugolix (RLGL), which has low oral bioavailability due to its low solubility and being a substrate of P-glycoprotein (P-gp). A solid self-microemulsifying drug delivery system of relugolix (RLGL-S-SMEDDS) was prepared and evaluated in vitro and in vivo.
Methods: The composition of the solid self-microemulsifying drug delivery system (S-SMEDDS) was selected by solubility study and pseudo-ternary phase diagram, and further optimized by Design-Expert optimization design.
Recruitment and retention in cancer trials are long-standing issues, exacerbated by the COVID-19 pandemic. The UK National Institute of Health Research and leading clinicians have emphasised the urgency to achieve and surpass prepandemic levels of participation. Data from a recent UK trial demonstrated the impact of COVID-19 and highlighted factors that limited recruitment.
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