Skip to main content
. 2021 Jan 29;11:617836. doi: 10.3389/fphar.2020.617836

TABLE 1.

Solid-phase, SPA binding and inhibition of cell adhesion of integrin antagonists MN27, DS-70 and SR714 to VCAM-1 or ICAM-1 (2 μg/mL) (Baiula et al., 2016; Dattoli et al., 2018).

Integrin antagonists Solid-phase binding/SPA a IC50 (nM) Cell adhesion b Jurkat, α4β1/VCAM-1 IC50 (nM) Cell adhesion b Jurkat, αLβ2/ICAM-1 IC50 (nM)
MN27 (αLβ2) 6.7 ± 2.5 (αLβ2) 574.0 ± 1.7 0.39 ± 0.02
DS-70 (α4β1) 8.3 ± 3.2 (α4β1) 5.04 ± 0.51 >5000
SR714 (α4β1) 1.1 ± 0.1 (α4β1) 1.39 ± 0.04 >5000
a

IC50 values of β-lactam compounds and DS-70 on leukocyte integrins determined by a competitive solid-phase binding assay to specific ligand (ICAM-1 for αLβ2) or by scintillation proximity assay (SPA, FN for α4β1). Six independent experiments were run in quadruplicate. Data are expressed as means ± SD (Baiula et al., 2016; Dattoli et al., 2018).

b

In a cell-based assay, the adhesion of a cell line preferentially expressing a specific integrin heterodimer to an immobilized adhesion molecule was measured. Six independent experiments were run in quadruplicate. Data are expressed as means ± SD (Baiula et al., 2016; Dattoli et al., 2018).