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ChemMatrix, a poly(ethylene glycol)-based support for the solid-phase synthesis of complex peptides.
TLDR
CM (ChemMatrix) resin is a new, totally poly(ethylene glycol) (PEG)-based resin, made exclusively from primary ether bonds and, therefore, highly chemically stable, and performs excellently for the preparation of hydrophobic, highly structured, and poly-Arg peptides, as compared to polystyrene (PS) resins.
Polymers and drug delivery systems.
TLDR
Polymeric systems of drug carriers are of high interest because they are an appropriate tool for time- and distribution-controlled drug delivery, and the mechanisms involved in controlled release require polymers with a variety of physicochemical properties.
The synergy of ChemMatrix resin and pseudoproline building blocks renders RANTES, a complex aggregated chemokine.
TLDR
An efficient stepwise solid-phase synthesis of RANTES (1-68) is reported on by combining the advantages of the totally PEG-based ChemMatrix resin and pseudoproline dipeptides.
ChemMatrix® for complex peptides and combinatorial chemistry
TLDR
The high loading of this resin permits the use of a tiny quarter of a bead as a microreactor for HPLC and MALDI‐TOF analysis, thus further extending its applications in the field of combinatorial chemistry.
Optimized Fmoc solid‐phase synthesis of the cysteine‐rich peptide linaclotide
TLDR
An optimized solid‐phase synthesis of linaclotide is described that should allow the production of this peptide in multigram amounts and select distinct protecting groups for the thiol function.
Rescuing biological activity from synthetic phakellistatin 19.
Phakellistatins is one of the families of Pro-rich cyclic peptides whose synthetic counterparts have revealed cytotoxicities that differ greatly from those displayed by their corresponding natural
Single-molecule kinetics and footprinting of DNA bis-intercalation: the paradigmatic case of Thiocoraline
TLDR
Experiments with the peptide Thiocoraline show, for the first time, that bis-intercalation is driven by a very slow off-rate that steeply decreases with applied force, and develop a novel single-molecule footprinting technique that provides direct access to the binding sites of small ligands to nucleic acids without the need of cleavage agents.
N,N,N',N'-tetramethylchloroformamidinium hexafluorophosphate (TCFH), a powerful coupling reagent for bioconjugation.
TLDR
The use of N,N,N',N'-tetramethylchloroformamidinium hexafluorophosphate (TCFH) resulted in good yields of ester prodrugs of thiocoraline and could be applicable to other drugs with similar limitations.
NMe amide as a synthetic surrogate for the thioester moiety in thiocoraline.
TLDR
Bridged N-methyl amides are used as isosteres for depsi and thiodepsi bonds in thiocoraline and displayed an increased stability in human serum as compared to the parent natural product.
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