Ruprecht-karls-universitat Heidelberg

Ruprecht-karls-universität

Peter P Nawroth

Thomas H Fleming

Walter Mier

Sebastian Brings

Angelika Bierhaus

The present invention relates to cyclic peptide compounds which inhibit or antagonize the binding of methylglyoxal (MG) and/or other reactive carbonyl species (RCS) to an arginine- or lysine-containing protein. Preferred scavenger compounds are said cyclic peptides comprising a specific amino acid motif and a hydrophobic modification, and pharmaceutical compositions thereof. The present invention furthermore relates to the use of the cyclic peptides as scavenger or antagonists of methylglyoxal and/or related reactive carbonyl species (RCS). The present invention furthermore relates to the use of the cyclic peptides for the prevention and/or treatment of a disease caused by or associated with methylglyoxal (MG) and/or reactive carbonyl species (RCS), in particular caused by or associated with elevated MG levels, such as diabetes and its associated complications, cardiovascular diseases and obesity.

Methylglyoxal-scavenging cyclic peptides and their use for the prevention and treatment of diseases associated with elevated methylglyoxal levels

The present invention relates to compounds which inhibit or antagonize the binding of methylglyoxal (MG) and/or other reactive carbonyl species (RCS) to an arginine- or lysine- containing protein, preferably an arginine- or lysine-containing cellular protein, such as a sodium ion channel, e.g. the sodium ion channel Na(v)1.8. Preferred scavenger compounds are peptides comprising several or multiple repeats of the amino acid sequence motif Gly-Glu-X-Pro (GEXP), wherein X is Arg or Lys, and pharmaceutical compositions thereof. The present invention furthermore relates to the use of the compounds as scavenger or antagonists of methylglyoxal and/or related reactive carbonyl species (RCS). The present invention furthermore relates to the use of the compounds for the prevention and/or treatment of pain, hyperalgesia and pain related diseases, in particular pain and/or hyperalgesia caused by or associated with methylglyoxal and/or reactive carbonyl species (RCS).

Growing community of inventors

Leimen, Germany

Peter P Nawroth