Structure of PDB 4cxw Chain A

Receptor sequence
>4cxwA (length=431) Species: 9606 (Homo sapiens) [Search protein sequence]
RGSHMTPKDDEFYQQWQLKYPKLILREASSVSEELHKEVQEAFLTLHKHG
CLFRDLVRIQGKDLLTPVSRILIGNPGCTYKYLNTRLFTVPWPVKGTEAE
IAAACETFLKLNDYLQIETIQALEELAAKEKDEVDIKSRAAYNVTLLNFM
DPQKLKEEPYFGMGKMAVSWHHDENLVDRSAVAVYSYSCELEGRDPDIWH
VGFKISWDIETPGLAIPLHQGDCYFMLDDLNATHQHCVLAGSQPRFSSTH
RVAECSTGTLDYILQRCQLALQNVCDDVDNDDVSLKSFEPAVLKQGEEIH
NEVEFEWLRQFWFQGNRYRKCTDWWCQPMAQLEALWKKMEGVTNAVLHEV
KREGLPVEQRNEILTAILASLTARQNLRREWHARCQSRIARTLPADQKPE
CRPYWEKDDASMPLPFDLTDIVSELRGQLLE
3D structure
PDB4cxw A strategy based on nucleotide specificity leads to a subfamily-selective and cell-active inhibitor ofN6-methyladenosine demethylase FTO.
ChainA
Resolution3.1 Å
3D
structure
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Enzymatic activity
Enzyme Commision number 1.14.11.-
1.14.11.53: mRNA N(6)-methyladenine demethylase.
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 6MK A Y106 Y108 V228 H231 D233 E234 Y295 H307 R316 S318 R322 Y80 Y82 V168 H171 D173 E174 Y224 H236 R245 S247 R251 PDBbind-CN: -logKd/Ki=6.09,IC50=0.81uM
Gene Ontology
Molecular Function
GO:0008198 ferrous iron binding
GO:0016706 2-oxoglutarate-dependent dioxygenase activity
GO:0016740 transferase activity
GO:0035515 oxidative RNA demethylase activity
GO:0035516 broad specificity oxidative DNA demethylase activity
GO:0046872 metal ion binding
GO:0051213 dioxygenase activity
GO:1990931 mRNA N6-methyladenosine dioxygenase activity
GO:1990984 tRNA demethylase activity
Biological Process
GO:0001659 temperature homeostasis
GO:0006307 DNA alkylation repair
GO:0010883 regulation of lipid storage
GO:0016180 snRNA processing
GO:0040014 regulation of multicellular organism growth
GO:0042245 RNA repair
GO:0044065 regulation of respiratory system process
GO:0060612 adipose tissue development
GO:0061157 mRNA destabilization
GO:0070350 regulation of white fat cell proliferation
GO:0090335 regulation of brown fat cell differentiation
Cellular Component
GO:0005634 nucleus
GO:0005654 nucleoplasm
GO:0005737 cytoplasm
GO:0005829 cytosol
GO:0005886 plasma membrane
GO:0016607 nuclear speck
GO:0043231 intracellular membrane-bounded organelle

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Molecular Function
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Biological Process
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Cellular Component
External links
PDB RCSB:4cxw, PDBe:4cxw, PDBj:4cxw
PDBsum4cxw
PubMed28553460
UniProtQ9C0B1|FTO_HUMAN Alpha-ketoglutarate-dependent dioxygenase FTO (Gene Name=FTO)

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