Structure of PDB 5zxb Chain B

Receptor sequence
>5zxbB (length=241) Species: 9606 (Homo sapiens) [Search protein sequence]
LTCLIGEKDLRLLEKLGDVVRRGEWDAPSGKTVSVAVKCLQPEAMDDFIR
EVNAMHSLDHRNLIRLYGVVLTPPMKMVTELAPLGSLLDRLRKHQGHFLG
TLSRYAVQVAEGMGYLESKRFIHRDLAARNLLLATRDLVKIGDFPFAWCA
PESLKTRTFSHASDTWMFGVTLWEMFTYGQEPWIGLNGSQILHKIDKEGE
RLPRPEDCPQDIYNVMVQCWAHKPEDRPTFVALRDFLLEAQ
3D structure
PDB5zxb First SAR Study for Overriding NRAS Mutant Driven Acute Myeloid Leukemia.
ChainB
Resolution2.198 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D252 R256 N257 D270
Catalytic site (residue number reindexed from 1) D125 R129 N130 D143
Enzyme Commision number 2.7.10.2: non-specific protein-tyrosine kinase.
2.7.11.1: non-specific serine/threonine protein kinase.
Interaction with ligand
Site
#
Ligand Ligand
chain
Binding residues on receptor
(original residue number in PDB)
Binding residues on receptor
(residue number reindexed from 1)
Binding affinity
BS01 9KO B L132 V140 A156 K158 E177 M181 T205 L207 A208 G211 H250 L259 G269 D270 F271 L16 V20 A36 K38 E51 M55 T79 L81 A82 G85 H123 L132 G142 D143 F144 MOAD: ic50=8nM
BindingDB: IC50=8.0nM
Gene Ontology
Molecular Function
GO:0004672 protein kinase activity
GO:0004713 protein tyrosine kinase activity
GO:0005524 ATP binding
Biological Process
GO:0006468 protein phosphorylation

View graph for
Molecular Function

View graph for
Biological Process
External links
PDB RCSB:5zxb, PDBe:5zxb, PDBj:5zxb
PDBsum5zxb
PubMed30153003
UniProtQ07912|ACK1_HUMAN Activated CDC42 kinase 1 (Gene Name=TNK2)

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