Bilipeptides and processes for their preparation

Details Bilipeptides and processes for their preparation Bilipeptides and processes for their preparation

C - Chemistry, Metallurgy

12

P

195/134, 530/7.0

C12P 21/02 (2006.01) C07K 4/12 (2006.01) C07K 7/04 (2006.01)

Patent

CA 2035809

- 1- ABSTRACT Novel bilipeptides are provided which retain the pigment binding site and its neighbouring amino acid sequences of natural delta-bilirubin in solution, but are of much smaller molecular size than delta-bilirubin. Under certain circmstances, they are useful as cytoprotectants and show enhanced activity over delta-bilirubin in such applications. In place of the albumin chain of delta-bilirubin, they have an amino acid sequence of up to 50 units including a sequence-Lys-Glx-Arg- with Lys covalently linked to a propionic acid group on the bilirubin nucleus. Processes for making such bilipeptides are also provided. One such process comprises activating unconjugated bilirubin with an appropriate site specific reagent under specific conditions of pH, and reacting the complex so formed with albumin or a peptide of the general formula R-Lys-Glx- Arg-R'. Another such process for making bilipeptides comprises subjecting delta-bilirubin to controlled enzymatic cleavage to reduce the chain length of the albumin protein attached to the bilirubin component.

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