Table 2 Summary of existing pharmacological modulators that act directly or indirectly on endothelial activation-mediated leukocytes recruitment

Phellopterin

C₁₇H₁₆O₅

Akt, PKC

Reduce TNF-α-induced VCAM-1 expression and inhibits the adhesion of monocytes to endothelium

¹⁴²

K-7174,K-7174 dihydrochloride

C₃₃H₄₈N₂O₆/C₃₃H₅₀Cl₂N₂O₆

GATA

Inhibit the expression of VCAM-1 induced by either IL-1β or TNF-α

^143,144,145

Natalizumab

Monoclonal antibody

α4β1 integrin

A recombinant, humanized monoclonal antibody, binds to α4β1-integrin and blocks its interaction with VCAM-1

¹⁴⁶

Gypenoside XLIX

C₅₂H₈₆O₂₁

PPAR-α

A selective peroxisome proliferator-activated receptor (PPAR)-αactivator and inhibits cytokine-induced VCAM-1 overexpression

¹⁴⁷

ICAM-1-IN-1

C₁₅H₁₁BrN₂O₂S

Integrin

A potent and selective inhibitor of ICAM-1

¹⁴⁸

A-205804

C₁₅H₁₂N₂OS₂

ICAM-1, E-selectin

A potent and selective lead inhibitor of ICAM-1 and E-selectin

¹⁴⁹

Lifitegrast (SAR 118)

C₂₉H₂₄Cl₂N₂O₇S

LFA-1

Inhibit T cell attachment to ICAM-1

^150,151

RWJ 50271

C₁₈H₁₇F₃N₄O₂S

LFA-1/ICAM-1

A selective inhibitor of LFA-1/ICAM-1

¹⁵²

BMS-688521

C₂₆H₁₉Cl₂N₅O₄

LFA-1/ICAM-1

Inhibitor of the LFA-1/ICAM interaction

¹⁵³

Bimosiamose (TBC-1269)

C₄₆H₅₄O₁₆

E-selectin/ P-selectin

A nonoligosaccharide pan-selectin antagonist

¹⁵⁴

Andrographolide

C₂₀H₃₀O₅

NF-κB

Suppress the activation of NF-κB in stimulated endothelial cells

¹⁵⁵

Sialyl-Lewis X

C₃₁H₅₂N₂O₂₃

E-selectin

A high-affinity ligand for selectins and inhibits E-selectin-mediated neutrophil recruitment

¹⁵⁶

PSI-697

C₂₁H₁₈ClNO₃

P-selectin

Inhibit the binding of a soluble human P-selectin to PSGL-1

¹⁵⁷

Parmodulin 2

C₁₇H₁₇BrN₂O₂

PAR1

An allosteric inhibitor of protease-activated receptor 1 (PAR1)

^158,159