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 | 0005515 | molecular_function | protein binding |
| A | 0005634 | cellular_component | nucleus |
| A | 0005654 | cellular_component | nucleoplasm |
| A | 0006355 | biological_process | regulation of DNA-templated transcription |
| A | 0006357 | biological_process | regulation of transcription by RNA polymerase II |
| A | 0035097 | cellular_component | histone methyltransferase complex |
| A | 0042800 | molecular_function | histone H3K4 methyltransferase activity |
| A | 0044545 | cellular_component | NSL complex |
| A | 0044666 | cellular_component | MLL3/4 complex |
| 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 | 0140004 | molecular_function | histone H3Q5ser reader activity |
| A | 0140109 | molecular_function | histone H3K4me1 reader activity |
| A | 0140566 | molecular_function | histone reader activity |
| 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 | 0005515 | molecular_function | protein binding |
| B | 0005634 | cellular_component | nucleus |
| B | 0005654 | cellular_component | nucleoplasm |
| B | 0006355 | biological_process | regulation of DNA-templated transcription |
| B | 0006357 | biological_process | regulation of transcription by RNA polymerase II |
| B | 0035097 | cellular_component | histone methyltransferase complex |
| B | 0042800 | molecular_function | histone H3K4 methyltransferase activity |
| B | 0044545 | cellular_component | NSL complex |
| B | 0044666 | cellular_component | MLL3/4 complex |
| 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 | 0140004 | molecular_function | histone H3Q5ser reader activity |
| B | 0140109 | molecular_function | histone H3K4me1 reader activity |
| B | 0140566 | molecular_function | histone reader activity |
| 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 | 78 |
| Details | Repeat: {"description":"WD 1"} |
| Chain | Residue | Details |
| site_id | SWS_FT_FI2 |
| Number of Residues | 82 |
| Details | Repeat: {"description":"WD 2"} |
| Chain | Residue | Details |
| site_id | SWS_FT_FI3 |
| Number of Residues | 80 |
| Details | Repeat: {"description":"WD 3"} |
| Chain | Residue | Details |
| site_id | SWS_FT_FI4 |
| Number of Residues | 78 |
| Details | Repeat: {"description":"WD 4"} |
| Chain | Residue | Details |
| site_id | SWS_FT_FI5 |
| Number of Residues | 41 |
| Details | Repeat: {"description":"WD 5"} |
| Chain | Residue | Details |
| site_id | SWS_FT_FI6 |
| Number of Residues | 80 |
| Details | Repeat: {"description":"WD 6"} |
| Chain | Residue | Details |
| site_id | SWS_FT_FI7 |
| Number of Residues | 68 |
| Details | Repeat: {"description":"WD 7"} |
| Chain | Residue | Details |
| site_id | SWS_FT_FI8 |
| Number of Residues | 8 |
| Details | Site: {"description":"Important for interaction with histone H3"} |
| Chain | Residue | Details |
| site_id | SWS_FT_FI9 |
| Number of Residues | 2 |
| Details | Modified residue: {"description":"N6-acetyllysine","evidences":[{"source":"PubMed","id":"19608861","evidenceCode":"ECO:0007744"}]} |
| Chain | Residue | Details |
| site_id | SWS_FT_FI10 |
| Number of Residues | 4 |
| Details | Cross-link: {"description":"Glycyl lysine isopeptide (Lys-Gly) (interchain with G-Cter in SUMO2)","evidences":[{"source":"PubMed","id":"28112733","evidenceCode":"ECO:0007744"}]} |
| Chain | Residue | Details |
