The
blood–brain tumor barrier (BTB) and blood–brain barrier
(BBB) have always been the major barriers in glioma therapy. In this
report, we proposed D-T7 peptide-modified nanoparticles actively targeted
glioma by overcoming the BBB and BTB to improve the antiglioma efficacy.
Glioma-targeting experiments showed that the penetration effect of
the D-T7 peptide-modified nanoparticles was 7.89-fold higher than
that of unmodified nanoparticles. Furthermore, cediranib (CD) and
paclitaxel (PTX) were used for the combination of the antiangiogenesis
and chemotherapy for glioma. PEGylated bilirubin nanoparticles (BRNPs)
were selected as a suitable drug delivery system (CD&PTX@TBRBPs)
owing to the antioxidant, anti-inflammatory, and reactive oxygen species-responsive
ability. 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide
(MTT) and apoptosis assays showed that CD&PTX@TBRBPs had the highest
cytotoxicity and the median survival time of the CD&PTX@TBRNP
group was 3.31-fold and 1.23-fold longer than that of the saline and
CD&PTX@BRNP groups, respectively. All the results showed that
we constructed a novel and accessible peptide-modified dual drug carrier
with an enhanced antiglioma effect.
Despite the growing application of tetrazine bioorthogonal chemistry, it is still challenging to access tetrazines conveniently from easily available materials. Described here is the de novo formation of tetrazine from nitriles and hydrazine hydrate using a broad array of thiol‐containing catalysts, including peptides. Using this facile methodology, the syntheses of 14 unsymmetric tetrazines, containing a range of reactive functional groups, on the gram scale were achieved with satisfactory yields. Using tetrazine methylphosphonate as a building block, a highly efficient Horner–Wadsworth–Emmons reaction was developed for further derivatization under mild reaction conditions. Tetrazine probes with diverse functions can be scalably produced in yields of 87–93 %. This methodology may facilitate the widespread application of tetrazine bioorthogonal chemistry.
Despite the growing application of tetrazine bioorthogonal chemistry,itisstill challenging to access tetrazines conveniently from easily available materials.Described here is the de novo formation of tetrazine from nitriles and hydrazine hydrate using ab road array of thiol-containing catalysts, including peptides.Using this facile methodology,the syntheses of 14 unsymmetric tetrazines,c ontaining ar ange of reactive functional groups,o nt he gram scale were achieved with satisfactory yields.U sing tetrazine methylphosphonate as ab uilding block, ah ighly efficient Horner-Wadsworth-Emmons reaction was developed for further derivatization under mild reaction conditions.T etrazine probes with diverse functions can be scalably produced in yields of 87-93 %. This methodology may facilitate the widespread application of tetrazine bioorthogonal chemistry.
Alzheimer's disease (AD) is a high mortality and high disability rates neurodegenerative disease characterized by irreversible progression and poses a significant social and economic burden throughout the world. However, currently approved AD therapeutic agents only alleviate symptoms and there is still a lack of practical therapeutic regimens to stop or slow the progression of this disease. Thus, there is urgently needed novel diagnosis tools and drugs for early diagnosis and treatment of AD. Among several AD pathological hallmarks, amyloid-β (Aβ) peptide deposition is considered a critical initiating factor in AD. In recent years, with the advantages of excellent sensitivity and high resolution, near-infrared fluorescence (NIRF) imaging has attracted the attention of many researchers to develop Aβ plaque probes. This review mainly focused on different NIRF probe design strategies for imaging Aβ species to pave the way for the future design of novel NIRF probes for early diagnosis AD.
Fluorophores with different emission wavelengths were efficiently quenched by tert-butyl terminated tetrazylmethyl group and activated by isonitrile-tetrazine click-to-release reaction. Nucleic acid templated chemistry significantly accelerated this bioorthogonal cleavage. Moreover, two...
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