Brand  (β version)

PDB ID: 2XCH

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Ligands
Code Name Style Show Link
CKG 8-(cyclohexa-2,5-dien-1-ylideneamino)-1-(piperidin-4-ylmethyl)-4,5-dihydro-1h-pyrazolo[4,3-H]quinazoline-3-carboxamide PoSSuM
GOL Glycerol PoSSuM
SO4 Sulfate ion PoSSuM
Non-standard Residues
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SEP Phosphoserine
Glycosylation
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Modification
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Structure summary

Code : 2XCH   PDBj   RCSB PDB   PDBe
Header : TRANSFERASE
Title : Crystal structure of PDK1 in complex with a pyrazoloquinazoline inhibitor
Release Data : 2010-07-28
Compound :
mol_id molecule chains synonym
1 3-PHOSPHOINOSITIDE DEPENDENT PROTEIN KINASE 1 A HPDK1
ec: 2.7.11.1
fragment: KINASE CATALYTIC DOMAIN, RESIDUES 1-309
Source :
mol_id organism_scientific organism_common expression_system
1 HOMO SAPIENS  (taxid:9606) HUMAN SPODOPTERA FRUGIPERDA  (taxid:7108)
expression_system_common: FALL ARMYWORM
expression_system_vector_type: BACULOVIRUS
Authors : Angiolini, M., Banfi, P., Casale, E., Casuscelli, F., Fiorelli, C., Saccardo, M.B., Silvagni, M., Zuccotto, F.
Keywords : PI3-KINASE SIGNALLING, TRANSFERASE, SERINE/THREONINE-PROTEIN KINASE, ATP-BINDING
Exp. method : X-RAY DIFFRACTION ( 2.00 Å )
Citation :

Structure-Based Optimization of Potent Pdk1 Inhibitors.

Angiolini, M.,Banfi, P.,Casale, E.  et al.
(2010)  Bioorg.Med.Chem.Lett.  20 : 4095

PubMed: 20621725
DOI: 10.1016/J.BMCL.2010.05.070

Reaction

Chain : A
UniProt : O15530 (PDPK1_HUMAN)
Reaction: EC: Evidence:
Physiological Direction:
ATP + L-seryl-[protein] = ADP + H(+) + O-phospho-L-seryl- [protein] 2.7.11.1 -
-
ATP + L-threonyl-[protein] = ADP + H(+) + O-phospho-L- threonyl-[protein] 2.7.11.1 -
-