Summary Structural details Experimental details Functional details Sequence Neighbor History Downloads

6E22

Displacement of WDR5 from chromatin by a pharmacological WIN site inhibitor with picomolar affinity

Functional Information from GO Data

Chain	GOid	namespace	contents
A	0000122	biological_process	negative regulation of transcription by RNA polymerase II
A	0000123	cellular_component	histone acetyltransferase complex
A	0001501	biological_process	skeletal system development
A	0005515	molecular_function	protein binding
A	0005634	cellular_component	nucleus
A	0005654	cellular_component	nucleoplasm
A	0005669	cellular_component	transcription factor TFIID complex
A	0006094	biological_process	gluconeogenesis
A	0006325	biological_process	chromatin organization
A	0006355	biological_process	regulation of DNA-templated transcription
A	0006357	biological_process	regulation of transcription by RNA polymerase II
A	0006367	biological_process	transcription initiation at RNA polymerase II promoter
A	0016251	molecular_function	RNA polymerase II general transcription initiation factor activity
A	0035064	molecular_function	methylated histone binding
A	0035097	cellular_component	histone methyltransferase complex
A	0042393	molecular_function	histone binding
A	0042800	molecular_function	histone H3K4 methyltransferase activity
A	0044545	cellular_component	NSL complex
A	0044665	cellular_component	MLL1/2 complex
A	0044666	cellular_component	MLL3/4 complex
A	0045722	biological_process	positive regulation of gluconeogenesis
A	0045815	biological_process	transcription initiation-coupled chromatin remodeling
A	0045893	biological_process	positive regulation of DNA-templated transcription
A	0045995	biological_process	regulation of embryonic development
A	0048188	cellular_component	Set1C/COMPASS complex
A	0051302	biological_process	regulation of cell division
A	0051726	biological_process	regulation of cell cycle
A	0071339	cellular_component	MLL1 complex
A	0072686	cellular_component	mitotic spindle
A	0090043	biological_process	regulation of tubulin deacetylation
A	0140672	cellular_component	ATAC complex
B	0000122	biological_process	negative regulation of transcription by RNA polymerase II
B	0000123	cellular_component	histone acetyltransferase complex
B	0001501	biological_process	skeletal system development
B	0005515	molecular_function	protein binding
B	0005634	cellular_component	nucleus
B	0005654	cellular_component	nucleoplasm
B	0005669	cellular_component	transcription factor TFIID complex
B	0006094	biological_process	gluconeogenesis
B	0006325	biological_process	chromatin organization
B	0006355	biological_process	regulation of DNA-templated transcription
B	0006357	biological_process	regulation of transcription by RNA polymerase II
B	0006367	biological_process	transcription initiation at RNA polymerase II promoter
B	0016251	molecular_function	RNA polymerase II general transcription initiation factor activity
B	0035064	molecular_function	methylated histone binding
B	0035097	cellular_component	histone methyltransferase complex
B	0042393	molecular_function	histone binding
B	0042800	molecular_function	histone H3K4 methyltransferase activity
B	0044545	cellular_component	NSL complex
B	0044665	cellular_component	MLL1/2 complex
B	0044666	cellular_component	MLL3/4 complex
B	0045722	biological_process	positive regulation of gluconeogenesis
B	0045815	biological_process	transcription initiation-coupled chromatin remodeling
B	0045893	biological_process	positive regulation of DNA-templated transcription
B	0045995	biological_process	regulation of embryonic development
B	0048188	cellular_component	Set1C/COMPASS complex
B	0051302	biological_process	regulation of cell division
B	0051726	biological_process	regulation of cell cycle
B	0071339	cellular_component	MLL1 complex
B	0072686	cellular_component	mitotic spindle
B	0090043	biological_process	regulation of tubulin deacetylation
B	0140672	cellular_component	ATAC complex

Functional Information from PDB Data

site_id	AC1
Number of Residues	12
Details	binding site for residue HLS A 401

Chain	Residue
A	SER28
A	PHE242
A	ILE284
A	HOH697
A	SER70
A	PHE112
A	PHE128
A	PRO152
A	SER154
A	TYR170
A	TYR239
A	CYS240

site_id	AC2
Number of Residues	9
Details	binding site for residue SO4 A 402

Chain	Residue
A	ARG160
A	ASN204
A	LYS206
A	HOH504
A	HOH622
A	HOH794
B	SER96
B	HOH634
B	HOH668

site_id	AC3
Number of Residues	13
Details	binding site for residue HLS B 401

Chain	Residue
B	SER28
B	SER70
B	PHE112
B	PHE128
B	PRO152
B	SER154
B	TYR170
B	TYR239
B	CYS240
B	PHE242
B	ILE284
B	HOH719
B	HOH756

site_id	AC4
Number of Residues	7
Details	binding site for residue SO4 B 402

Chain	Residue
A	SER96
B	ARG160
B	ASN204
B	LYS206
B	HOH518
B	HOH590
B	HOH632

Functional Information from PROSITE/UniProt

site_id	PS00678
Number of Residues	15
Details	WD_REPEATS_1 Trp-Asp (WD) repeats signature. LVSAsdDkTLKIWDV

Chain	Residue	Details
A	LEU81-VAL95
A	ILE123-VAL137
A	ILE165-THR179
A	ILE253-LEU267

Functional Information from SwissProt/UniProt

site_id	SWS_FT_FI1
Number of Residues	8
Details	SITE: Important for interaction with histone H3

Chain	Residue	Details
A	ASP86
A	PHE112
A	PHE242
A	GLU301
B	ASP86
B	PHE112
B	PHE242
B	GLU301

site_id	SWS_FT_FI2
Number of Residues	2
Details	MOD_RES: N6-acetyllysine => ECO:0007744\|PubMed:19608861

Chain	Residue	Details
A	LYS91
B	LYS91

site_id	SWS_FT_FI3
Number of Residues	6
Details	CROSSLNK: Glycyl lysine isopeptide (Lys-Gly) (interchain with G-Cter in SUMO2) => ECO:0007744\|PubMed:28112733

Chain	Residue	Details
A	LYS6
A	LYS25
B	LYS6
B	LYS25

		Sequence (fasta)
		PDBx/mmCIF
		PDBML format (no-atom)
		PDB format (full)
		Validation report (PDF)
		EDMap 2fo-fc (MTZ)