1159531-18-6Relevant articles and documents
Compatibility between the cysteine-cyclopentenedione reaction and the copper(i)-catalyzed azide-alkyne cycloaddition
Agramunt, Jordi,Saltor, Laia,Pedroso, Enrique,Grandas, Anna
, p. 9185 - 9190 (2018)
The cysteine-cyclopentenedione reaction can be combined with the copper(i)-catalyzed azide-alkyne cycloaddition provided that the former is carried out first. If not, the azide and the cyclopentenedione undergo a 1,3-dipolar cycloaddition, which furnishes triazole-containing compounds and products resulting from nitrogen loss. Both of these products were fully characterized. Attempts to obtain either of them as the main compound or to drive the reaction nearly to completion were unsuccessful, which points to the azide-cyclopentenedione reaction as not being useful for bioconjugation.
Synthesis of peptide homo- and heterodimers as potential mimics of platelet-derived growth factor BB
Stubbing, Louise A.,Kaur, Harveen,Feng, Sheryl X.,Aalderink, Miranda,Dragunow, Michael,Brimble, Margaret A.
, (2020/07/28)
Pericyte loss is correlated with blood-brain barrier leakage in neurological disorders such as Alzheimer's disease. The platelet-derived growth factor receptor β (PDGFRβ)/platelet-derived growth factor BB (PDGF-BB) signalling pathway is key to the regulation of pericyte survival and proliferation. A series of peptide dimers mimicking the ligand PDGF-BB were prepared in the hope of stimulating PDGFRβ internalisation and activation of this pathway. Copper-catalysed azide-alkyne cycloaddition of peptide monomers with PEGylated linkers of varying length afforded the desired peptide dimers. Evaluation of the peptide dimers in human brain pericyte assays revealed no effect on PDGFRβ internalisation nor cell proliferation at concentrations 10 μM. The peptide dimers also did not act as antagonists at PDGFRβ at concentrations 10 μM.
OPTICAL PROBE FOR THROMBIN
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Page/Page column 37, (2016/10/11)
Optical probes are presented, the probes comprising a first probe element, and a second probe element connected to a core. The first probe element comprises a first fluorophore connected to a first quencher by a first cleavable linker. The second probe el