Dual action compounds (DACs) based on 4-substituted aza-bicyclo[5.3.0]decane Smac mimetic scaffolds (ABDs) linked to a Zn(2+)-chelating moiety (DPA, o-hydroxy, m-allyl, N-acyl (E)-phenylhydrazone) through their 10 position are reported and characterized. Their synthesis, their target affinity (XIAP BIR3, Zn(2+)) in cell-free assays, their pro-apoptotic effects and cytotoxicity in tumor cells with varying sensitivity to Smac mimetics are described. The results are interpreted to evaluate the influence of Zn(2+) chelators on cell-free potency and on cellular permeability of DACs, and to propose novel avenues towards more potent antitumoral DACs based on Smac mimetics and Zn(2+) chelation.
Center of Radiation Processing for Polymer Modification and Nanotechnology (CRPN), Department of Materials Science, Faculty of Science, Kasetsart University, 50 Ngam Wong Wan Rd., Ladyao, Chatuchak, Bangkok 10900, Thailand; Department of Materials Science, Faculty of Science, Kasetsart University, 50 Ngam Wong Wan Rd., Ladyao, Chatuchak, Bangkok 10900, Thailand. Electronic address:
Cyclic amine-multibranched poly(lactic acid) (mPLA) was prepared as a dual antioxidant and antimicrobial toward PLA active packaging for food shelf-life extension in a case study of bread. The mPLA was coupled with piperidine (PPR) containing a heterocyclic amine derivative, which is a nature-rich bioactive function. The functions of mPLA-PPR enhancing the PLA film performance were studied in comparison with PPR, mPLA and Tinuvin® 770.
Objective: Oral squamous cell carcinoma (OSCC) is a public health concern. The current study aimed to explore the role of circRNA Dedicator of Cytokinesis 1 (circ_DOCK1) and associated action mode in OSCC.
Methods: The expression of circ_DOCK1 and microRNA-1297 (miR-1297) was measured by quantitative real-time polymerase chain reaction (qRT-PCR).
Postsurgical adhesions are a common complication associated with surgical procedures; they not only impact the patient's well-being but also impose a financial burden due to medical expenses required for reoperative surgeries or adhesiolysis. Adhesions can range from a filmy, fibrinous, or fibrous vascular band to a cohesive attachment, and they can form in diverse anatomical locations such as the peritoneum, pericardium, endometrium, tendons, synovium, and epidural and pleural spaces. Numerous strategies have been explored to minimize the occurrence of postsurgical adhesions.
Mycobacterium tuberculosis causes human tuberculosis. As mycobacteria are protected by thick lipid cell wall, humans have developed immune responses against diverse mycobacterial lipids. Most of these immunostimulatory lipids are known as adjuvants acting through innate immune receptors, such as C-type lectin receptors.
The response to climate change and air pollution control demonstrates strong synergy across scientific mechanisms, targets, strategies, and governance systems. This report, based on a monitoring indicator system for coordinated governance of air pollution and climate change, employs an interdisciplinary approach combining natural and social sciences. It establishes 20 indicators across five key areas: air pollution and climate change, governance systems and practices, structural transformation and technologies, atmospheric components and emission reduction pathways, and health impacts and co-benefits.
