TABLE 1.
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 |
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).
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).