4PXS

Human GKRP bound to AMG-0265 (N-[(R)-(2-CHLOROPHENYL){7-[4-(2-HYDROXYPROPAN-2-YL) PYRIDIN-2-YL]-1-BENZOTHIOPHEN-2-YL}METHYL]CYCLOPROPANESULFONAMIDE) and Sorbitol-6-phosphate

Summary for 4PXS

• Entry DOI: 10.2210/pdb4pxs/pdb
• Descriptor: Glucokinase regulatory protein, N-[(R)-(2-chlorophenyl){7-[4-(2-hydroxypropan-2-yl)pyridin-2-yl]-1-benzothiophen-2-yl}methyl]cyclopropanesulfonamide, D-SORBITOL-6-PHOSPHATE, ... (7 entities in total)
• Functional Keywords: sis domain containing protein, gkrp binds to and inhibits glucokinase activity, glucokinase, liver, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (human)
• Cellular location: Cytoplasm : Q14397
• Total number of polymer chains: 2
• Total formula weight: 146316.27

Authors

Jordan, S.R.,Chmait, S. (deposition date: 2014-03-24, release date: 2015-03-18, Last modification date: 2023-09-20)

• Primary citation: Pennington, L.D.,Bartberger, M.D.,Croghan, M.D.,Andrews, K.L.,Ashton, K.S.,Bourbeau, M.P.,Chen, J.,Chmait, S.,Cupples, R.,Fotsch, C.; Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disruptors of GK-GKRP Binding.; To be Published,

Experimental method

X-RAY DIFFRACTION (2.6 Å)