Integrin α2β1 Inhibitor

BTT 3033 (1) is a selective inhibitor of integrin α2β1 with EC₅₀ = 130 nM on the basis of binding for the integrin to collagen I.¹⁾ On the other hand, 1 does not inhibit other integrins like α3β1, α4β1, α5β1 and αvβ1, as shown in Table 1.
1 also has anti-inflammatory effects in a platelet-activating factor (PAF)-stimulated air pouch model and moderate anti-inflammatory effects in an arachidonic acid-induced ear edema model.²⁾

References

• 1) Novel α2β1 Integrin Inhibitors Reveal That Integrin Binding to Collagen under Shear Stress Conditions Does Not Require Receptor Preactivation
  • L. Nissinen, J. Koivunen, J. Käpylä, M. Salmela, J. Nieminen, J. Jokinen, K. Sipilä, M. Pihlavisto, O. T. Pentikäinen, A. Marjamäki, J. Heino, J. Biol. Chem. 2012, 287, 44694.
• 2) Sulfonamide inhibitors of α2β1 integrin reveal the essential role of collagen receptors in in vivo models of inflammation
  • L. Nissinen, M. Ojala, B. Langen, R. Dost, M. Pihlavisto, J. Käpylä, A. Marjamäki, J. Heino, Pharma. Res. Per. 2015, 3, e00146.

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