Structure of PDB 7lzb Chain A

Receptor sequence

>7lzbA (length=235) Species: 9606 (Homo sapiens) [Search protein sequence]

GPSCVMDDFRDPQRWKECAKQGKMPCYFDLIEENVYLTERMQCECTPLSK
DERAQGEIACGEDCLNRLLMIECSSRCPNGDYCSNRRFQRKQHADVEVIL
TEKKGWGLRAAKDLPSNTFVLEYCGEVLDHKEFKARVKEYARNKNIHYYF
MALKNDEIIDATQKGNCSRFMNHSCEPNCETQKWTVNGQLRVGFFTTKLV
PSGSELTFDYQFQRYGKEAQKCFCGSANCRGYLGG

3D structure

PDB

7lzb Discovery of a First-in-Class Inhibitor of the Histone Methyltransferase SETD2 Suitable for Preclinical Studies.

Chain

Resolution

2.28 Å

3D
structure

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Enzymatic activity

Enzyme Commision number

2.1.1.-
2.1.1.359: [histone H3]-lysine(36) N-trimethyltransferase.

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)
BS01	ZN	A	C1499 C1501 C1516 C1520	C43 C45 C60 C64
BS02	ZN	A	C1516 C1529 C1533 C1539	C60 C73 C77 C83
BS03	ZN	A	C1631 C1678 C1680 C1685	C175 C222 C224 C229
BS04	SAM	A	K1560 G1561 W1562 H1603 Y1604 Y1605 R1625 N1628 H1629 Q1676 C1678 F1679 L1689	K104 G105 W106 H147 Y148 Y149 R169 N172 H173 Q220 C222 F223 L233
BS05	YJ1	A	Y1579 Y1604 F1606 F1664 Y1666 Y1671	Y123 Y148 F150 F208 Y210 Y215

Gene Ontology

	Molecular Function
GO:0016279	protein-lysine N-methyltransferase activity
GO:0042054	histone methyltransferase activity
GO:0046975	histone H3K36 methyltransferase activity

	Cellular Component
GO:0005634	nucleus

View graph for
Molecular Function

View graph for
Cellular Component

External links

PDB	RCSB:7lzb, PDBe:7lzb, PDBj:7lzb
PDBsum	7lzb
PubMed	34671445
UniProt	Q9BYW2\|SETD2_HUMAN Histone-lysine N-methyltransferase SETD2 (Gene Name=SETD2)

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