Acta Chimica Sinica, Journal Year: 2025, Volume and Issue: 83(4), P. 341 - 341
Published: Jan. 1, 2025
Language: Английский
Journal of the American Chemical Society, Journal Year: 2025, Volume and Issue: unknown
Published: Jan. 23, 2025
The technology of native chemical ligation and postligation desulfurization has greatly expanded the scope modern protein synthesis. Here, we report that ultrasonic energy can trigger robust clean desulfurization, developed an ultrasound-induced (USID) strategy is simple to use generally applicable peptides proteins. USID involves a cleaning bath easy-to-use easy-to-remove sonosensitizer, titanium dioxide. It features mild convenient reaction conditions excellent functional group compatibility, e.g., with thiazolidine (Thz) serotonin, which are sensitive other strategies. robust: without reoptimizing conditions, same procedure be used for broad range proteins one or more sulfhydryl groups, even in multi-hundred-milligram scale reactions. utility was demonstrated by one-pot synthesis bioactive cyclopeptides such as Cycloleonuripeptide E Segetalin F, well convergent functionally important histone H3.5 using Thz temporary protecting group. A mechanistic investigation indicated proceeds via radical-based mechanism promoted low-frequency low-intensity ultrasonication. Overall, our work introduces mechanically triggered approach potential become method general both academic industrial laboratories.
Language: Английский
Citations
2
Molecular Pharmaceutics, Journal Year: 2025, Volume and Issue: unknown
Published: Feb. 6, 2025
The first-in-class oncolytic peptide LTX-315 has exhibited positive anticancer responses in multiple phase I/II clinical trials. Nevertheless, the linear suffers from poor proteolytic stability and undesired toxicity, especially hemolysis, which may limit its widespread applications. Except for direct structural modifications, drug delivery systems (DDSs) are expected to protect degradation shield hemolytic properties. Therefore, zeolitic imidazolate framework (ZIF-8)-based nanoparticles (NPs) were constructed with a high encapsulation rate of 59.9%, utilizing biomineralized "one-pot method" an aqueous system. release LTX-315, vitro potency, serum stability, durability, antimigration activity, hemolysis effect, subcellular localization, membrane disruption/permeation effects LTX-315@ZIF-8 NPs investigated. potent cytotoxicity against cancer cells. experiment time-inhibition curve assay indicated that ZIF-8 could effectively improve prolong duration action, enhance cytostatic potency. Especially, not only attenuated toxicity but also achieved pH-responsive LTX-315. mechanism investigation possessed membranolytic activity reduced mitochondrial potential trigger cell death. Collectively, this paper established robust strategy reduce properties provided reliable reference future peptides.
Language: Английский
Citations
1
Bioorganic & Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 111, P. 117869 - 117869
Published: Aug. 3, 2024
Language: Английский
Citations
6
Published: Jan. 1, 2025
Natural cytotoxic peptides (NCPs) are emerging sources of novel anticancer chemotherapeutics. Especially, Melittin, which is the major component bee venom and first-in-class NCP, has been considered as a promising scaffold. Nevertheless, classical linear, cationic, amphipathic, membrane-lytic peptide, Melittin may be easily degraded by proteases, suffering from poor stability, moderate durability, severe hemolysis. In this study, applying terminal modification hybridization strategies, ten Melittin-based derivatives were designed, synthesized, investigated for their potential. The robust economic synthetic method, in vitro efficiency, time-kill kinetics, serum anti-migration activity, hemolysis effects, mechanism explored. As expected, exhibited highly potent cytotoxicity against all six tested cancer cell lines. particular, compared with natural derived LJ-5 containing both N-terminal acetylation C-terminal hydrazidation, LJ-6, methotrexate MTX-GFLG-Melittin conjugate significantly improved proteolytic more durable higher well reduced effects. Besides, it was further verified that LJ-6 could efficiently disrupt integrity membrane, localize to mitochondria rapidly reduce mitochondrial membrane potential cells. Collectively, method stability-guided optimization conducted on affording hydrolysis-resistant serve candidates useful references optimizations peptides.
Language: Английский
Citations
0
Journal of the American Chemical Society, Journal Year: 2025, Volume and Issue: unknown
Published: Jan. 30, 2025
Modular chemical postmodification of peptides is a promising strategy that supports the optimization and innovation hit peptide therapeutics by enabling rapid derivatization. However, current methods are primarily limited to traditional bio-orthogonal strategies ligation techniques, which require preintroduction non-natural amino acids impose fixed limit diversity. Here, we developed Tyrosine-1,2,3-Triazine Ligation (YTL) strategy, constructs novel linkages (pyridine pyrimidine) through "one-pot, two-step" process combining SNAr IEDDA reactions, promoting modular post modification Tyr-containing peptides. After optimizing YTL establishing standard procedures, successfully applied it solid-phase various biorelated peptides, such as synthesis dual-mode imaging probes long-acting GLP-1 analogs. As proof concept, library 384 amphipathic was constructed using based on 96-well microfiltration plates. modifications were then performed screened template tripeptide RYR, leading generation 20 derivatives. The antibacterial activity these derivatives systematically characterized, identifying Z8 potential candidate.
Language: Английский
Citations
0
Chemometrics and Intelligent Laboratory Systems, Journal Year: 2025, Volume and Issue: unknown, P. 105337 - 105337
Published: Feb. 1, 2025
Language: Английский
Citations
0
Journal of Molecular Graphics and Modelling, Journal Year: 2025, Volume and Issue: 137, P. 108981 - 108981
Published: Feb. 24, 2025
Language: Английский
Citations
0
Journal of Microencapsulation, Journal Year: 2025, Volume and Issue: unknown, P. 1 - 27
Published: Feb. 24, 2025
Gadolinium (Gd) nanoparticles hold significant promise in medical theranostics due to their unique properties. This review outlines the synthesis, characterisation, and applications of Gd nanostructures combating microbial threats advancing cancer theragnostic strategies. Synthesis methods such as co-precipitation, microemulsion, laser ablation are discussed, alongside TEM, SEM, magnetic characterisation. The antimicrobial efficacy nanostructures, potential combination therapy, promising anticancer mechanisms explored. Biocompatibility, toxicity, regulatory considerations also evaluated. Challenges, future perspectives, emerging trends nanostructure research highlighted, emphasising transformative applications.
Language: Английский
Citations
0
Spectrochimica Acta Part A Molecular and Biomolecular Spectroscopy, Journal Year: 2025, Volume and Issue: 334, P. 125956 - 125956
Published: Feb. 27, 2025
Language: Английский
Citations
0
Bioorganic Chemistry, Journal Year: 2025, Volume and Issue: unknown, P. 108331 - 108331
Published: March 1, 2025
Language: Английский
Citations
0