Hydrophobic dipeptide molecules can be used to create interfacial films covering bubbles and droplets made from a range of oils. At high pH, the dipeptide molecules form micelles which transform into a hydrogel of fibres in response to the addition of salt. We characterize the properties of the hydrogel for two different salt (MgSO) concentrations and then we use these gels to stabilize interfaces. Under high shear, the hydrogel is disrupted and will reform around bubbles or droplets. Here, we reveal that at low dipeptide concentration, the gel is too weak to prevent ripening of the bubbles; this then reduces the long-term stability of the foam. Under the same conditions, emulsions prepared from some oils are highly stable. We examine the wetting properties of the oil droplets at a hydrogel surface as a guide to the resulting emulsions.
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http://dx.doi.org/10.1039/c7ob01053b | DOI Listing |
Biomolecules
January 2025
Institute of Biostructures and Bioimaging, Italian National Council for Research (IBB-CNR), Area di Ricerca Site and Headquarters, Via Pietro Castellino 111, 80131 Naples, Italy.
In recent years, fungal infections have emerged as a significant health concern across veterinary species, especially in livestock such as cattle, where fungal diseases can result in considerable economic losses, as well as in humans. In particular, species, notably and , are opportunistic pathogens that pose a threat to both animals and humans. This study focuses on the synthesis and antifungal evaluation of novel 9-fluorenylmethoxycarbonyl (Fmoc)-protected 1,2,4-triazolyl-α-amino acids and their dipeptides, designed to combat fungal pathogens.
View Article and Find Full Text PDFBioconjug Chem
January 2025
Biotherapeutics Discovery Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Hydrophobic payloads incorporated into antibody-drug conjugates (ADCs) typically are superior to hydrophilic ones in tumor penetration and "bystander killing" upon release from ADCs. However, they are prone to aggregation and accelerated plasma clearance, which lead to reduced efficacies and increased toxicities of ADC molecules. Shielding the hydrophobicity of payloads by incorporating polyethylene glycol (PEG) elements or sugar groups into the ADC linkers has emerged as a viable alternative to directly adopting hydrophilic payloads.
View Article and Find Full Text PDFJ Med Chem
January 2025
Institute of Pharmacy, Pharmaceutical/Medicinal Chemistry and Tübingen Center for Academic Drug Discovery, Eberhard Karls University Tübingen, Auf der Morgenstelle 8, 72076 Tübingen, Germany.
The main protease (M) of SARS-CoV-2 is a key drug target for the development of antiviral therapeutics. Here, we designed and synthesized a series of small-molecule peptidomimetics with various cysteine-reactive electrophiles. Several compounds were identified as potent SARS-CoV-2 M inhibitors, including compounds (IC = 0.
View Article and Find Full Text PDFPhys Chem Chem Phys
January 2025
Institut für Ionenphysik und Angewandte Physik, Universität Innsbruck, A-6020 Innsbruck, Austria.
Peptide bond formation from the pure protonated glycine dimer, H(Gly), and from the mixed protonated glycine-diglycine dimer, HGly(Gly), was recently found experimentally to occur in gas-phase experiments in the absence of any catalyst and especially under anhydrous conditions [, 2023, , 775]. In this contribution we further examine the conditions of such unimolecular reactions by means of density-functional theory calculations at the DFT/M06 2X/6-311G++(2df,p) level, focusing in particular on the role played by the protonation site. Two pathways, stepwise and concerted, are identified for the pure protonated dimer, and six pathways are examined for the mixed dimer.
View Article and Find Full Text PDFTetrahedron
February 2025
Department of Chemistry and Biochemistry, Baylor University, One Bear Place, No. 97348, Waco, Texas 76798-7348, United States.
Antibody-drug conjugates (ADCs) have advanced as a mainstay among the most promising cancer therapeutics, offering enhanced antigen targeting and encompassing wide diversity in their linker and payload components. Small-molecule inhibitors of tubulin polymerization have found success as payloads in FDA approved ADCs and represent further promise in next-generation, pre-clinical and developmental ADCs. Unique dual-mechanism payloads (previously designed and synthesized in our laboratories) function as both potent antiproliferative agents and promising vascular disrupting agents capable of imparting selective and effective damage to tumor-associated microvessels.
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