6ZS2

Crystal Structure of the bromodomain of human transcription activator BRG1 (SMARCA4) in complex with 2-(6-amino-5-(piperazin-1-yl)pyridazin-3-yl)phenol

External Resource: Annotation

Domain Annotation: SCOP/SCOPe Classification
Domain Annotation: SCOP2 Classification
Domain Annotation: ECOD Classification
Protein Family Annotation
Gene Ontology: Gene Product Annotation
InterPro: Protein Family Classification
Pharos: Disease Associations

Domain Annotation: SCOP/SCOPe Classification SCOP-e Database Homepage

Chains	Domain Info	Class	Fold	Superfamily	Family	Domain	Species	Provenance Source (Version)
A	d6zs2a1	All alpha proteins	Bromodomain-like	Bromodomain	automated matches	automated matches	Human (Homo sapiens ) [TaxId: 9606 ],	SCOPe (2.08)
A	d6zs2a2	Artifacts	Tags	Tags	Tags	N-terminal Tags	Human (Homo sapiens ) [TaxId: 9606 ],	SCOPe (2.08)
B	d6zs2b1	All alpha proteins	Bromodomain-like	Bromodomain	automated matches	automated matches	Human (Homo sapiens ) [TaxId: 9606 ],	SCOPe (2.08)
B	d6zs2b2	Artifacts	Tags	Tags	Tags	N-terminal Tags	Human (Homo sapiens ) [TaxId: 9606 ],	SCOPe (2.08)

Domain Annotation: SCOP2 Classification SCOP2 Database Homepage

Chains	Type	Family Name	Domain Identifier	Family Identifier	Provenance Source (Version)
A	SCOP2B Superfamily	Bromodomain	8084301	3001843	SCOP2B (2022-06-29)
B	SCOP2B Superfamily	Bromodomain	8084301	3001843	SCOP2B (2022-06-29)

Domain Annotation: ECOD Classification ECOD Database Homepage

Chains	Family Name	Domain Identifier	Architecture	Possible Homology	Homology	Topology	Family	Provenance Source (Version)
A	Bromodomain	e6zs2A1	A: alpha bundles	X: Bromodomain-like	H: Bromodomain (From Topology)	T: Bromodomain	F: Bromodomain	ECOD (1.6)
B	Bromodomain	e6zs2B1	A: alpha bundles	X: Bromodomain-like	H: Bromodomain (From Topology)	T: Bromodomain	F: Bromodomain	ECOD (1.6)

Protein Family Annotation Pfam Database Homepage

Chains	Accession	Name	Description	Comments	Source
A, B	PF00439	Bromodomain (Bromodomain)	Bromodomain	Bromodomains are 110 amino acid long domains, that are found in many chromatin associated proteins. Bromodomains can interact specifically with acetylated lysine [3].	Domain

Gene Ontology: Gene Product Annotation Gene Ontology Database Homepage

Chains	Polymer	Molecular Function	Biological Process	Cellular Component
A, B	Transcription activator BRG1	protein binding binding histone binding hydrolase activity catalytic activity ATP-dependent activity, acting on DNA catalytic activity, acting on DNA catalytic activity, acting on a nucleic acid ATP-dependent activity transcription factor binding transcription coregulator binding adenyl ribonucleotide binding nucleotide binding purine ribonucleotide binding protein binding binding histone binding hydrolase activity catalytic activity ATP-dependent activity, acting on DNA catalytic activity, acting on DNA catalytic activity, acting on a nucleic acid ATP-dependent activity transcription factor binding transcription coregulator binding adenyl ribonucleotide binding nucleotide binding purine ribonucleotide binding purine ribonucleoside triphosphate binding nucleoside phosphate binding ion binding purine nucleotide binding organic cyclic compound binding anion binding adenyl nucleotide binding ATP binding heterocyclic compound binding carbohydrate derivative binding ribonucleotide binding small molecule binding DNA binding nucleic acid binding p53 binding helicase activity transcription coactivator activity transcription regulator activity transcription coregulator activity protein-macromolecule adaptor activity molecular adaptor activity RNA polymerase II-specific DNA-binding transcription factor binding DNA-binding transcription factor binding Tat protein binding RNA binding ATP-dependent chromatin remodeler activity nuclear receptor binding nuclear androgen receptor binding transcription corepressor activity DNA polymerase binding enzyme binding	regulation of chromosome segregation regulation of cell cycle phase transition regulation of cellular process regulation of metaphase/anaphase transition of cell cycle regulation of cellular component organization cell cycle phase transition regulation of mitotic metaphase/anaphase transition mitotic cell cycle cellular component organization regulation of mitotic cell cycle cell cycle cellular component organization or biogenesis regulation of cell cycle chromosome segregation regulation of chromosome segregation regulation of cell cycle phase transition regulation of cellular process regulation of metaphase/anaphase transition of cell cycle regulation of cellular component organization cell cycle phase transition regulation of mitotic metaphase/anaphase transition mitotic cell cycle cellular component organization regulation of mitotic cell cycle cell cycle cellular component organization or biogenesis regulation of cell cycle chromosome segregation cell cycle process regulation of biological process regulation of cell cycle process biological regulation chromosome organization sister chromatid segregation regulation of chromosome organization regulation of organelle organization regulation of mitotic cell cycle phase transition organelle organization mitotic cell cycle process regulation of sister chromatid segregation nuclear chromosome segregation metaphase/anaphase transition of mitotic cell cycle cellular process metaphase/anaphase transition of cell cycle mitotic cell cycle phase transition developmental process regulation of developmental process cellular developmental process positive regulation of biological process regulation of cell differentiation positive regulation of myoblast differentiation muscle structure development positive regulation of developmental process positive regulation of cell differentiation cell differentiation anatomical structure development regulation of myoblast differentiation myoblast differentiation positive regulation of cellular process RNA metabolic process positive regulation of macromolecule biosynthetic process positive regulation of gene expression, epigenetic RNA biosynthetic process nucleobase-containing compound metabolic process positive regulation of metabolic process DNA-templated transcription nucleic acid biosynthetic process transcription by RNA polymerase II positive regulation of biosynthetic process chromatin organization chromatin remodeling positive regulation of macromolecule metabolic process transcription initiation at RNA polymerase II promoter regulation of biosynthetic process epigenetic regulation of gene expression primary metabolic process regulation of macromolecule metabolic process gene expression nucleobase-containing compound biosynthetic process macromolecule biosynthetic process nucleic acid metabolic process DNA-templated transcription initiation regulation of gene expression biosynthetic process positive regulation of gene expression transcription initiation-coupled chromatin remodeling regulation of macromolecule biosynthetic process metabolic process macromolecule metabolic process regulation of metabolic process positive regulation of DNA-binding transcription factor activity regulation of primary metabolic process positive regulation of molecular function regulation of RNA metabolic process regulation of nucleobase-containing compound metabolic process regulation of RNA biosynthetic process regulation of molecular function regulation of DNA-binding transcription factor activity regulation of DNA-templated transcription regulation of growth negative regulation of biological process growth negative regulation of cell growth regulation of cell growth cell growth negative regulation of growth negative regulation of cellular process cellular component disassembly protein-containing complex organization protein-DNA complex disassembly protein-containing complex disassembly protein-DNA complex organization nucleosome disassembly nucleosome organization positive regulation of DNA-templated transcription positive regulation of miRNA transcription positive regulation of miRNA metabolic process miRNA transcription regulation of miRNA metabolic process miRNA metabolic process positive regulation of nucleobase-containing compound metabolic process positive regulation of RNA metabolic process positive regulation of RNA biosynthetic process regulation of miRNA transcription cellular response to stimulus positive regulation of cell communication positive regulation of signal transduction response to stimulus signaling regulation of signal transduction cell communication positive regulation of response to stimulus positive regulation of Wnt signaling pathway signal transduction Wnt signaling pathway regulation of signaling cell surface receptor signaling pathway regulation of Wnt signaling pathway regulation of response to stimulus regulation of cell communication positive regulation of signaling viral gene expression biological process involved in interspecies interaction between organisms modulation by host of symbiont process viral process biological process involved in interaction with symbiont viral transcription positive regulation by host of viral transcription biological process involved in symbiotic interaction multicellular organism development multicellular organismal process nervous system development system development negative regulation of developmental process negative regulation of cell differentiation negative regulation of RNA biosynthetic process negative regulation of nucleobase-containing compound metabolic process negative regulation of macromolecule metabolic process regulation of transcription by RNA polymerase II negative regulation of DNA-templated transcription negative regulation of transcription by RNA polymerase II negative regulation of metabolic process negative regulation of biosynthetic process negative regulation of macromolecule biosynthetic process negative regulation of RNA metabolic process sensory organ development eye development animal organ development retina development in camera-type eye visual system development neural retina development camera-type eye development sensory system development positive regulation of transcription by RNA polymerase II regulation of double-strand break repair regulation of cellular response to stress positive regulation of DNA repair cellular response to stress response to stress regulation of response to stress DNA repair double-strand break repair DNA metabolic process positive regulation of double-strand break repair regulation of DNA repair positive regulation of DNA metabolic process DNA damage response regulation of DNA metabolic process regulation of stem cell population maintenance stem cell population maintenance positive regulation of stem cell population maintenance positive regulation of multicellular organismal process regulation of multicellular organismal process maintenance of cell number hexose mediated signaling homeostatic process regulation of glucose mediated signaling pathway response to monosaccharide response to carbohydrate positive regulation of glucose mediated signaling pathway carbohydrate homeostasis cellular response to hexose stimulus intracellular chemical homeostasis cellular response to monosaccharide stimulus response to oxygen-containing compound cellular response to glucose stimulus intracellular glucose homeostasis cellular response to oxygen-containing compound response to hexose sugar mediated signaling pathway glucose mediated signaling pathway cellular response to carbohydrate stimulus cellular response to chemical stimulus cellular homeostasis chemical homeostasis response to glucose response to chemical glucose homeostasis carbohydrate mediated signaling cell population proliferation positive regulation of cell population proliferation regulation of cell population proliferation adaptive thermogenesis multicellular organismal-level homeostasis regulation of cold-induced thermogenesis cold-induced thermogenesis temperature homeostasis positive regulation of cold-induced thermogenesis nucleotide-excision repair regulation of nucleotide-excision repair regulation of G0 to G1 transition G0 to G1 transition transcription preinitiation complex assembly RNA polymerase I preinitiation complex assembly cellular component biogenesis transcription initiation at RNA polymerase I promoter cellular component assembly transcription by RNA polymerase I protein-containing complex assembly protein-DNA complex assembly intracellular receptor signaling pathway response to lipid negative regulation of signaling negative regulation of intracellular signal transduction hormone-mediated signaling pathway intracellular signal transduction negative regulation of cell communication negative regulation of intracellular steroid hormone receptor signaling pathway cellular response to endogenous stimulus response to hormone regulation of intracellular signal transduction response to steroid hormone regulation of intracellular steroid hormone receptor signaling pathway androgen receptor signaling pathway nuclear receptor-mediated steroid hormone signaling pathway cellular response to steroid hormone stimulus response to organic cyclic compound steroid hormone receptor signaling pathway cellular response to hormone stimulus negative regulation of response to stimulus response to endogenous stimulus cellular response to organic cyclic compound negative regulation of signal transduction regulation of androgen receptor signaling pathway cellular response to lipid negative regulation of androgen receptor signaling pathway nuclear receptor-mediated signaling pathway regulation of cell cycle G1/S phase transition cell cycle G1/S phase transition regulation of G1/S transition of mitotic cell cycle G1/S transition of mitotic cell cycle regulation of transcription of nucleolar large rRNA by RNA polymerase I rRNA transcription rRNA metabolic process positive regulation of transcription by RNA polymerase I regulation of transcription by RNA polymerase I nucleolar large rRNA transcription by RNA polymerase I positive regulation of transcription of nucleolar large rRNA by RNA polymerase I regulation of leukocyte differentiation regulation of leukocyte activation regulation of cell activation mononuclear cell differentiation lymphocyte differentiation positive regulation of T cell differentiation regulation of cell development positive regulation of cell activation T cell activation positive regulation of leukocyte activation T cell differentiation regulation of immune system process positive regulation of immune system process positive regulation of T cell activation positive regulation of cell development regulation of leukocyte cell-cell adhesion leukocyte differentiation cell development positive regulation of leukocyte cell-cell adhesion lymphocyte activation leukocyte cell-cell adhesion leukocyte activation positive regulation of cell-cell adhesion regulation of T cell differentiation positive regulation of lymphocyte activation cell adhesion cell-cell adhesion positive regulation of hemopoiesis regulation of cell-cell adhesion regulation of lymphocyte differentiation regulation of multicellular organismal development hemopoiesis positive regulation of cell adhesion regulation of cell adhesion cell activation regulation of T cell activation immune system process regulation of hemopoiesis positive regulation of leukocyte differentiation positive regulation of lymphocyte differentiation regulation of lymphocyte activation	cellular anatomical structure membrane membrane-bounded organelle ATPase complex protein-containing complex intracellular anatomical structure catalytic complex GBAF complex nucleus nuclear protein-containing complex intracellular membraneless organelle chromatin chromosome intracellular membrane-bounded organelle cellular anatomical structure membrane membrane-bounded organelle ATPase complex protein-containing complex intracellular anatomical structure catalytic complex GBAF complex nucleus nuclear protein-containing complex intracellular membraneless organelle chromatin chromosome intracellular membrane-bounded organelle intracellular organelle organelle membraneless organelle SWI/SNF superfamily-type complex SWI/SNF complex nBAF complex npBAF complex extracellular region extracellular space membrane-enclosed lumen intracellular organelle lumen organelle lumen nuclear periphery nuclear lumen nuclear matrix nucleolus RSC-type complex nucleoplasm bBAF complex chromosomal region kinetochore chromosome, centromeric region condensed chromosome, centromeric region supramolecular complex condensed chromosome fibrillar center

InterPro: Protein Family Classification InterPro Database Homepage

Chains	Accession	Name	Type
A, B	IPR030100	SWI/SNF complex subunit BRG1, ATP-binding	Domain
A, B	IPR018359	Bromodomain, conserved site	Conserved Site
A, B	IPR049730	SNF2/RAD5-like, C-terminal helicase domain	Domain
A, B	IPR014978	Glutamine-Leucine-Glutamine, QLQ	Domain
A, B	IPR006576	BRK domain	Domain
A, B	IPR027417	P-loop containing nucleoside triphosphate hydrolase	Homologous Superfamily
A, B	IPR037259	BRK domain superfamily	Homologous Superfamily
A, B	IPR001650	Helicase, C-terminal domain-like	Domain
A, B	IPR014001	Helicase superfamily 1/2, ATP-binding domain	Domain
A, B	IPR036427	Bromodomain-like superfamily	Homologous Superfamily
A, B	IPR029295	Snf2, ATP coupling domain	Domain
A, B	IPR000330	SNF2, N-terminal	Domain
A, B	IPR001487	Bromodomain	Domain
A, B	IPR038718	SNF2-like, N-terminal domain superfamily	Homologous Superfamily
A, B	IPR014012	Helicase/SANT-associated domain	Domain

Pharos: Disease Associations Pharos Homepage Annotation

Chains	Drug Target	Associated Disease
A, B	Pharos: P51532	Coffin-Siris syndrome rhabdoid tumor predisposition syndrome 2 small cell lung carcinoma Burkitt lymphoma intellectual disability, autosomal dominant 16 sarcoma spindle cell sarcoma atypical teratoid rhabdoid tumor cocaine dependence Sezary syndrome intellectual disability lung cancer ovarian cancer small cell carcinoma cocaine abuse Coffin-Siris syndrome rhabdoid tumor predisposition syndrome 2 small cell lung carcinoma Burkitt lymphoma intellectual disability, autosomal dominant 16 sarcoma spindle cell sarcoma atypical teratoid rhabdoid tumor cocaine dependence Sezary syndrome intellectual disability lung cancer ovarian cancer small cell carcinoma cocaine abuse Precursor T-Cell Lymphoblastic Leukemia-Lymphoma invasive ductal breast carcinoma lung adenocarcinoma lymphoplasmacytic lymphoma abdominal aortic aneurysm medulloblastoma neoplasm of thorax osteosarcoma ovarian neoplasm peripheral arterial disease congenital anomaly of kidney and urinary tract primitive neuroectodermal tumor ductal breast carcinoma in situ rhabdoid tumor juvenile dermatomyositis thoracic cancer malignant colon neoplasm myocardial infarction carotid artery disease ovarian small cell carcinoma plasma cell myeloma dermatomyositis progressive supranuclear palsy epithelioid sarcoma spina bifida large cell medulloblastoma myopathy astrocytic tumor non-small cell lung carcinoma cancer ovarian carcinoma pancreatic ductal adenocarcinoma diabetes mellitus psoriasis heart disease

RCSB PDB Core Operations are funded by the U.S. National Science Foundation (DBI-2321666), the US Department of Energy (DE-SC0019749), and the National Cancer Institute, National Institute of Allergy and Infectious Diseases, and National Institute of General Medical Sciences of the National Institutes of Health under grant R01GM157729.