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. 2021 Jun 3;8(16):2101090. doi: 10.1002/advs.202101090

Table 1.

Summary of the targets and strategies to restore BBB integrity

Therapeutic targets Targeting strategies Ref.
Paracellular permeability VE‐cadherin

miR‐27a/VE‐cadherin interaction:

e.g., BlockmiR CD5‐2

[ 92 ]

S1PR1 agonist or modulator:

e.g., SEW2871, FTY720

[96, 97, 98]
Claudin‐5

Chronic antidepressant treatment:

e.g., imipramine

[ 21 ]

microRNAs:

e.g., miR‐15a/16‐1

[ 100 ]

Regulation of transcription factor:

e.g., HADC inhibitor (MS‐275) for FOXO1;

SOX18

[ 17 ]
VE‐cadherin: e.g., BlockmiR CD5‐2 [ 92 ]
ZO‐1 miR‐501‐3p [ 101 ]
Occludins Short‐chain fatty acids (SCFAs) [ 102 ]
Transcellular permeability Caveolae‐mediated transcytosis

Small GTPase:

RhoA inhibitor: e.g., H‐1152

Rac‐1 activator: e.g., IFN‐α, IFN‐β

[ 103 ]
Msfd2a [ 15 ]
Efflux transporter P­gp Pregnane X receptor (PXR) agonist [ 104 ]
ABCC1 Thiethylperazine [ 105 ]
Pharmacological restoration of LRP1 or GLUT1 expression VEGF‐B inhibitor? [ 106 ]