Journal article

Reversibility versus persistence of GPIIb/IIIa blocker-induced conformational change of GPIIb/IIIa (alpha(IIb)beta(3), CD41/CD61)

M Schwarz, Y Katagiri, M Kotani, N Bassler, C Loeffler, C Bode, K Peter

JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS | AMER SOC PHARMACOLOGY EXPERIMENTAL THERAPEUTICS | Published : 2004

Abstract

Clinically used GPIIb/IIIa blockers are ligand mimetics, and thereby their binding can induce conformational changes of the platelet integrin GPIIb/IIIa. Since the reversibility of these conformational changes may be an important determinant of potential adverse effects of GPIIb/IIIa blockers, we produced a new monoclonal antibody (anti-LIBS-mAb), and by using its binding properties, we investigated the conformational changes of GPIIb/IIIa during the binding and especially the dissociation of GPIIb/IIIa blockers. Production of monoclonal antibody (mAb) clones was performed using purified GPIIb/IIIa in a high affinity conformation and using activated platelets. Clone anti-LIBS-145-mAb was cho..

View full abstract