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Table 2 The uPAR-targeted nanoplatforms carrying therapeutic agents

From: Urokinase-type plasminogen activator receptor (uPAR) as a therapeutic target in cancer

Nano platform

Target

Drug

Imaging

Effect

References, year

uPA-SP@CaP NPs

uPA peptide, amino acid sequence: VSNKYFSNIHWGC (uPAR)

BRCA1 siRNA, Pro-Pt

Fluorescence imaging (Dir)

Improve anticancer efficacy of the TNBC (pH-responsive sequential release ability, lysosomal escape property, dual tumour targeting, and irreversible DNA damage behavior)

[161], 2019

ATF-IO-Dox

ATF (uPAR)

Dox

MRI

A marked inhibition of tumour cell growth in 4T1 and MDA-MB-231 cells

[162], 2008

iWnt-ATF24-IONP-Dox

iWnt, amino acid sequence: NSNAIKNKKHHH (Wnt/LRP5/6), ATF24, amino acid sequence: CHHHCLNGGTCVSNKYFSNIHWCNCPKK (uPAR)

Dox

NIR-830 dye for optical imaging

Strong tumour growth inhibition in a human chemo-resistant cancer patient-derived xenograft model (inhibited Wnt/β-catenin signaling and cancer stem-like phenotype of tumour cells; marked reduction of Wnt ligand, CD44 and uPAR)

[163], 2018

ATF-IONP-Gem

ATF (uPAR)

Gem

MRI

Inhibit the growth of orthotopic human pancreatic cancer xenografts in nude mice (overcoming the tumour stromal barrier)

[164], 2013

ATF-PEG-IONP-Cis or ATF-PEG-IONP-Dox

ATF (uPAR)

Cis or Dox

NIR optical imaging and MRI

Inhibit the growth of pancreatic tumours (i.p.); decrease proliferating tumour cells and tumour vessels; reduce the amount of ascites production

[165], 2017

LHRH-AE105-IONPs-PTX

LHRH (LHRH-R), AE105 (uPAR)

PTX

MRI

10 times reduction in the concentration of PTX required to achieve similar cytotoxic effect produced by the free drug (LHRH-R- and uPAR-overexpressing PC-3 cells)

[166], 2017

DTX/AE Lipo

AE147 (uPAR)

DTX

Fluorescence imaging

DTX/AE-Lipo (IC50 4.61 µg/mL) achieves better anticancer activity than free DTX (IC50 7.18 µg/mL) or DTX/Lipo (IC50 8.59 µg/mL)

[167], 2021

PAI-2 N-AI liposomes

PAI-2 (uPAR)

N-alkylisatin

NA

An increased accumulation at the primary tumour site in an orthotopic MDA-MB-231 BALB/c-Fox1nu/Ausb xenograft mouse model

[168], 2020

U11 peptide targeted NPs

U11 peptide (uPAR)

Plasmid DNA

Fluorescence imaging (Rhodamine)

Transfection of uPAR positive DU145 cells is essentially tenfold higher compared to transfection achieved by NPs having a scrambled peptide sequence on their surface

[105], 2009

U11-Dox/Cur NPs

U11 peptide (uPAR)

Dox/Cur

Fluorescence imaging (Coumarin 6)

Inhibit the tumour growth to a level of 85%

[169], 2019

ATF24-PEG-Lipo-β-E

ATF24 (uPAR)

β-E

Fluorescence imaging (Did)

Combined with Cis, exert a synergistic effect on cellular apoptosis and cell arrest at the G2/M phase (dependent on the caspase-dependent pathway and Cdc25C/Cdc2/cyclin B1 pathways)

[170], 2020

uPA-Anti-miR-21-Anti-miR-10b-NPs

uPA peptide (VSNKYFSNIHWGC)

Antisense-miR-21, antisense-miR-10b

Optical bioluminescence imaging (MDA-MB-231-Fluc-eGFP cells)

40% reduction in tumour growth compared to scrambled peptide conjugated NPs treated mice (0.15 mg/kg)

[171], 2015

  1. siRNA small interfering RNA, TNBC triple-negative breast cancer, NIR near infrared, MRI magnetic resonance imaging, Gem gemcitabine, Cis Cisplatin, Dox doxorubicin, DTX docetaxel, Cur curcumin, PTX paclitaxel, β-E β-elemene, Cdc25C cell division cyclin 25C, Cdc2 cell division cycle protein 2, Dir 1,1′-dioctadecyl-3,3,3′,3′-tetramethylindotricarbocyanine iodide, Did 1,1′-dioctadecyl-3,3,3′,3′-tetramethylindodicarbocyanine perchlorate, NPs nanoparticles