Novel BMP2 antagonist inhibitors for bone graft substitution

Recombinant bone morphogenetic protein 2 (BMP-2) is a known bone graft substitute used in the treatment of bone fractures and bone defects and is currently available on the market. BMP-2 must be applied in high concentrations to induce bone formation in clinical settings. Its limited therapeutic efficacy may be due to the presence of BMP antagonists that neutralize exogenous BMP-2. Inventors at the University of Würzburg (Germany) have identied a novel inactive BMP-2 mutein, named L51P, which acts as an inhibitor of BMP antagonists noggin, chordin and gremlin. In vitro and in vivo validation studies with a combination of BMP-2 and L51P led to a signi cant increase in BMP activity.

BMP-2 and other members of the TGF-b superfamily regulate the development, maintenance and regeneration of many tissues and organs. Dysregulation of BMP and TGF-b signalling is critical during several disorders including fibrosis, osteoporosis, cancer, arthritis and bone or cartilage repair.

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