Structure of PDB 5f3g Chain D

Receptor sequence
>5f3gD (length=339) Species: 9606 (Homo sapiens) [Search protein sequence]
SARIMTFYPTMEEFRNFSRYIAYIESQGAHRAGLAKVVPPKEWKPRASYD
DIDDLVIPAPIQQLVTGQSGLFTQYNIQKKAMTVREFRKIANSDKYCTPR
YSEFEELERKYWKNLTFNPPIYGADVNGTLYEKHVDEWNIGRLRTILDLV
EKESGITIVNTPYLYFGMWKTSFAWHTEDMDLYSINYLHFGEPKSWYSVP
PEHGKRLERLAKGFFPGSAQSCEAFLRHKMTLISPLMLKKYGIPFDKVTQ
EAGEFMITFPYGYHAGFNHGFNCAESTNFATRRWIEYGKQAVLCSCMVKI
SMDVFVRKFQPERYKLWKAGKDNTVIDHTLPTPEAAEFL
3D structure
PDB5f3g 8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors.
ChainD
Resolution2.5 Å
3D
structure
Catalytic site residues are labeled in the structure
[Spin on]
[Spin off]
[Reset orientation]

[High quality]
[Low quality]

[White background]
[Black background]

[Download]
[Download structure with residue number starting from 1]
Enzymatic activity
Catalytic site (original residue number in PDB) Y177 H188 E190 H276 S288
Catalytic site (residue number reindexed from 1) Y165 H176 E178 H264 S276
Enzyme Commision number 1.14.11.66: [histone H3]-trimethyl-L-lysine(9) demethylase.
1.14.11.69: [histone H3]-trimethyl-L-lysine(36) 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 ZN D H188 E190 H276 H176 E178 H264
BS02 ZN D C234 H240 C306 C308 C222 H228 C294 C296
BS03 5UL D Y132 Y177 F185 H188 K206 W208 K241 H276 Y122 Y165 F173 H176 K194 W196 K229 H264 MOAD: ic50=0.126uM
BindingDB: IC50=126nM
External links
PDB RCSB:5f3g, PDBe:5f3g, PDBj:5f3g
PDBsum5f3g
PubMed26741168
UniProtO75164|KDM4A_HUMAN Lysine-specific demethylase 4A (Gene Name=KDM4A)

[Back to BioLiP]