Crystal structure

C - Chemistry – Metallurgy – 12 – N

Patent

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Details

C12N 15/54 (2006.01) A61K 38/45 (2006.01) C12N 9/12 (2006.01) C12N 15/11 (2006.01) C12N 15/52 (2006.01) C12N 15/66 (2006.01) C12Q 1/00 (2006.01)

Patent

CA 2378565

The present invention relates to crystals of pyruvate dehydrogenase kinase (PDHK) wherein the PDHK protein includes PDHK-2 amino acid sequence as shown in SEQ ID NO: 2 but starting at amino acid position 16, or a homologue, fragment, variant or derivative thereof.). The invention also relates to high resolution three dimensional structures of PDHK in the presence and absence of physiological and synthetic ligands obtained by X-ray diffraction and use of the structures to identify, design or select compounds that bind to PDHK. The invention further relates to compounds identified, designed or selected using high resolution structures of PDHK. Also provided are nucleotide sequences used to obtain crystallisable PDHK protein.

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