Crystals of glucokinase regulatory protein (gkrp)
AssigneeBoehringer Ingelheim International GmbH
InventorsGisela SCHNAPP, Adina Berg, Stefan Kauschke, Martin Lenter, Alexander Pautsch, Wolfgang Rist
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Abstract
The present invention pertains to crystals of glucokinase regulatory protein (GKRP) and of GKRP variants, to the molecular biology of certain GKRP variants, to processes for the crystallization of GKRP and GKRP variants, to such crystals and corresponding structural information obtained by X-ray crystallography. Such crystals and crystallographic data can be used for the identification of compounds that bind to GKRP, especially of compounds that inhibit GKRP or interfere with the interaction of GKRP with its natural interacting partner Glucokinase (GK).
Claims20
A crystal of
- (a) a glucokinase regulatory protein (GKRP) comprising
- (i) at least 82% identity to SEQ ID NO:
- 2,
- (ii) at least 82% identity to SEQ ID NO:
- 4,
- (iii) at least 82% identity to SEQ ID NO:
- 6, or
- (iv) at least 82% identity to SEQ ID NOS:
- 2 and 4, to SEQ ID NOS:
- 4 and 6, or to SEQ ID NOS:
- 2 and 6;
- or
- (b) a deletion mutant (truncated form of GKRP) comprising
- (i) at least 82% identity to positions 6 to 606 of SEQ ID NO:
- 2,
- (ii) at least 82% identity to positions 6 to 606 of SEQ ID NO:
- 4,
- (iii) at least 82% identity to positions 6 to 606 of SEQ ID NO:
- 6, or
- (iv) at least 82% identity to positions 6 to 606 of SEQ ID NOS:
- 2 and 4, to positions 6 to 606 of SEQ ID NOS:
- 4 and 6, or to positions 6 to 606 of SEQ ID NOS:
- 2 and 6.
A process for the crystallization of a GKRP or GKRP variant comprising the steps of:
- (1) purification of the protein, and
- (2) crystallization of the purified protein,
- wherein step (2), the purified protein is complexed with a low molecular weight binding ligand in the active site.
Dependencies are inferred from the claim text.