The furyl group of (2-furyl)-L-alanine-containing peptides obtained from Fmoc solid-phase synthesis is partially degraded to several by-products during the final TFA-mediated deprotection in the presence of cation scavengers such as ethanedithiol and propanedithiol. The major by-product corresponds to a bis-dithioacetale formed after acidic hydrolysis of the furyl group. We examined several cleavage conditions and found that cleavage cocktails containing water and triisopropylsilane or 3,6-dioxa-1,8-octanedithiol (DODT) in trifluoroacetic acid are sufficient to minimize the side reaction.
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http://dx.doi.org/10.2174/0929866043406238 | DOI Listing |
HIV-1 assembly is initiated by the binding of Gag polyproteins to the inner leaflet of the plasma membrane, mediated by the myristylated matrix (MA) domain of Gag. Subsequent to membrane binding, Gag oligomerizes and buds as an immature, non-infectious virus particle, which, upon cleavage of the Gag precursor by the viral protease, transforms into a mature, infectious virion. During maturation, the MA lattice underlying the viral membrane undergoes a structural rearrangement and the newly released capsid (CA) protein forms a mature capsid that encloses the viral genome.
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January 2025
Department of Chemistry and Chemical Biology, Indian Institute of Technology (ISM), Dhanbad, Jharkhand 826004, India.
Aminophosphonates serve as extremely important moieties with respect to their activities in biological systems. However, incorporating a Nitrogen and Phosphorus moiety by conventional techniques in ionic mode is usually associated with extensive prefunctionalization of the substrates, employing harsh conditions and reagents that limit the viability of these methods. Introducing both of these components as radicals may be a viable option.
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January 2025
Department of Chemistry, Indian Institute of Technology Kharagpur, Kharagpur 721 302, India.
The "catalytic triad" present at the active site of ribonuclease A (RNase A) is responsible for the cleavage of the 5'-phosphodiester bond; amino acid residues His12, Lys41 and His119 constituting this triad provide a positively charged environment at the physiological pH. Based on docking studies, 1,4,5-trisubstituted-carboxylated 1,2,3-triazoles (1,4,5-TTs) were identified as a new class of RNase A inhibitors. Therefore, two different groups of 1,4,5-TTs, functionalized with carboxylic acid groups, were synthesized by reacting pre functionalized butyne-1,4-diol derivatives with several aryl/alkyl azides under solvent and catalyst free conditions.
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December 2024
State Key Laboratory of Supramolecular Structure and Materials, College of Chemistry, Jilin University Changchun Jilin 130012 China
The chemical recycling of polystyrene (PS) waste to value-added aromatic compounds is an attractive but formidable challenge due to the inertness of the C-C bonds in the polymer backbone. Here we develop a light-driven, copper-catalyzed protocol to achieve aerobic oxidation of various alkylarenes or real-life PS waste to benzoic acid and oxidized styrene oligomers. The resulting oligomers can be further transformed under heating conditions, thus achieving benzoic acid in up to 65% total yield through an integrated one-pot two-step procedure.
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December 2024
Digital Technologies Research Center, National Research Council Canada, Ottawa, ON, K1A 0R6, Canada.
Motivation: Clustered Regularly Interspaced Short Palindromic Repeats (CRISPR)-Cas9 system is a ground-breaking genome editing tool, which has revolutionized cell and gene therapies. One of the essential components involved in this system that ensures its success is the design of an optimal single-guide RNA (sgRNA) with high on-target cleavage efficiency and low off-target effects. This is challenging as many conditions need to be considered, and empirically testing every design is time-consuming and costly.
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