2015
DOI: 10.1002/marc.201500243
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Rational Design of Cancer-Targeted Benzoselenadiazole by RGD Peptide Functionalization for Cancer Theranostics

Abstract: A cancer-targeted conjugate of the selenadiazole derivative BSeC (benzo[1,2,5] selenadiazole-5-carboxylic acid) with RGD peptide as targeting molecule and PEI (polyethylenimine) as a linker is rationally designed and synthesized in the present study. The results show that RGD-PEI-BSeC forms nanoparticles in aqueous solution with a core-shell nanostructure and high stability under physiological conditions. This rational design effectively enhances the selective cellular uptake and cellular retention of BSeC in … Show more

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Cited by 16 publications
(18 citation statements)
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“…First, CS‐RP was synthesized through an amidation reaction of CS, RC‐12, and PG‐6 peptide ,,. Briefly, solutions of RC‐12 and PG‐6 peptide (5 mg) were dissolved in DMSO (1 mL), and then EDC and NHS were added with stirring for 2 h at ambient temperature and pressure.…”
Section: Methodssupporting
confidence: 90%
“…First, CS‐RP was synthesized through an amidation reaction of CS, RC‐12, and PG‐6 peptide ,,. Briefly, solutions of RC‐12 and PG‐6 peptide (5 mg) were dissolved in DMSO (1 mL), and then EDC and NHS were added with stirring for 2 h at ambient temperature and pressure.…”
Section: Methodssupporting
confidence: 90%
“…This compound also enhanced the sensitivity of cancerous cells to X-ray induced apoptosis by inhibition of TrxR, with good results in vitro and in vivo . Related benzo­[ c ]­[1,2,5]­selenadiazole-5-carboxylic acid was conjugated into polyethylenimine (PEI) nanoparticles with RGD (Arg-Gly-Asp) peptide as integrin targeting molecule, achieving good selectivity in human glioma cells and provoking apoptosis by ROS-mediated p53 phosphorylation pathway . Conjugation in mesoporous silica nanoparticles (MSNs) improved blood–brain barrier (BBB) permeability and cellular uptake in glioma cells, achieving cell death .…”
Section: 25-selenadiazolesmentioning
confidence: 99%
“…In recent years, with the rapid development of oncology and nanomaterials, nanodrug delivery systems (NDDS) have shown remarkable therapeutic effects in tumor diagnosis and treatment, and a variety of nanodrug carriers have been applied to tumor treatment [ 10 , 11 , 12 , 13 ]. Compared with drug delivery methods, NDDS have the advantages of improving drug utilization, achieving stimulated release, and reducing drug toxicity and side effects [ 14 , 15 , 16 , 17 , 18 ].…”
Section: Introductionmentioning
confidence: 99%