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6U5M

Discovery and optimization of salicyclic acid-derived sulfonamide inhibitors of the WDR5:MYC protein-protein interaction

Functional Information from GO Data
ChainGOidnamespacecontents
A0000122biological_processnegative regulation of transcription by RNA polymerase II
A0000123cellular_componenthistone acetyltransferase complex
A0001501biological_processskeletal system development
A0005515molecular_functionprotein binding
A0005634cellular_componentnucleus
A0005654cellular_componentnucleoplasm
A0006094biological_processgluconeogenesis
A0006325biological_processchromatin organization
A0006355biological_processregulation of DNA-templated transcription
A0006357biological_processregulation of transcription by RNA polymerase II
A0035064molecular_functionmethylated histone binding
A0035097cellular_componenthistone methyltransferase complex
A0042393molecular_functionhistone binding
A0042800molecular_functionhistone H3K4 methyltransferase activity
A0044545cellular_componentNSL complex
A0044665cellular_componentMLL1/2 complex
A0044666cellular_componentMLL3/4 complex
A0045722biological_processpositive regulation of gluconeogenesis
A0045815biological_processtranscription initiation-coupled chromatin remodeling
A0045893biological_processpositive regulation of DNA-templated transcription
A0045995biological_processregulation of embryonic development
A0048188cellular_componentSet1C/COMPASS complex
A0051302biological_processregulation of cell division
A0051726biological_processregulation of cell cycle
A0071339cellular_componentMLL1 complex
A0072686cellular_componentmitotic spindle
A0090043biological_processregulation of tubulin deacetylation
A0140672cellular_componentATAC complex
B0000122biological_processnegative regulation of transcription by RNA polymerase II
B0000123cellular_componenthistone acetyltransferase complex
B0001501biological_processskeletal system development
B0005515molecular_functionprotein binding
B0005634cellular_componentnucleus
B0005654cellular_componentnucleoplasm
B0006094biological_processgluconeogenesis
B0006325biological_processchromatin organization
B0006355biological_processregulation of DNA-templated transcription
B0006357biological_processregulation of transcription by RNA polymerase II
B0035064molecular_functionmethylated histone binding
B0035097cellular_componenthistone methyltransferase complex
B0042393molecular_functionhistone binding
B0042800molecular_functionhistone H3K4 methyltransferase activity
B0044545cellular_componentNSL complex
B0044665cellular_componentMLL1/2 complex
B0044666cellular_componentMLL3/4 complex
B0045722biological_processpositive regulation of gluconeogenesis
B0045815biological_processtranscription initiation-coupled chromatin remodeling
B0045893biological_processpositive regulation of DNA-templated transcription
B0045995biological_processregulation of embryonic development
B0048188cellular_componentSet1C/COMPASS complex
B0051302biological_processregulation of cell division
B0051726biological_processregulation of cell cycle
B0071339cellular_componentMLL1 complex
B0072686cellular_componentmitotic spindle
B0090043biological_processregulation of tubulin deacetylation
B0140672cellular_componentATAC complex
Functional Information from PDB Data
site_idAC1
Number of Residues13
Detailsbinding site for residue Q0S A 401
ChainResidue
ASER223
ATRP273
ALEU288
AGLN289
AHOH643
APRO224
AASN225
ATYR228
ALEU240
ALYS250
APHE266
ASER267
ALYS272

site_idAC2
Number of Residues17
Detailsbinding site for residue Q0S B 401
ChainResidue
BSER223
BPRO224
BASN225
BTYR228
BLEU240
BLYS250
BPHE266
BSER267
BVAL268
BLYS272
BTRP273
BLEU288
BGLN289
BHOH621
BHOH632
BHOH752
BHOH754

Functional Information from PROSITE/UniProt
site_idPS00678
Number of Residues15
DetailsWD_REPEATS_1 Trp-Asp (WD) repeats signature. LVSAsdDkTLKIWDV
ChainResidueDetails
ALEU102-VAL116
AILE144-VAL158
AILE186-THR200
AILE274-LEU288

Functional Information from SwissProt/UniProt
site_idSWS_FT_FI1
Number of Residues8
DetailsSITE: Important for interaction with histone H3
ChainResidueDetails
AASP107
APHE133
APHE263
AGLU322
BASP107
BPHE133
BPHE263
BGLU322

site_idSWS_FT_FI2
Number of Residues2
DetailsMOD_RES: N6-acetyllysine => ECO:0007744|PubMed:19608861
ChainResidueDetails
ALYS112
BLYS112

site_idSWS_FT_FI3
Number of Residues4
DetailsCROSSLNK: Glycyl lysine isopeptide (Lys-Gly) (interchain with G-Cter in SUMO2) => ECO:0007744|PubMed:28112733
ChainResidueDetails
ALYS46
BLYS46

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PDB entries from 2024-11-06

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