5LSS

Structure of the Epigenetic Oncogene MMSET and inhibition by N-Alkyl Sinefungin Derivatives

External Resource: Annotation

Domain Annotation: SCOP/SCOPe 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	d5lssa_	Membrane and cell surface proteins and peptides	SNF-like	SNF-like	Amino acid antiporter-like	Protein lysine methyltransferase (PKMT) SET domain-containing protein 2 (SETD2)	Human (Homo sapiens ) [TaxId: 9606 ],	SCOPe (2.08)

Domain Annotation: ECOD Classification ECOD Database Homepage

Chains	Family Name	Domain Identifier	Architecture	Possible Homology	Homology	Topology	Family	Provenance Source (Version)
A	SET	e5lssA2	A: beta barrels	X: beta-clip	H: SET domain-like (From Topology)	T: SET domain-like	F: SET	ECOD (1.6)
A	AWS	e5lssA1	A: few secondary structure elements	X: Zn3Cys9 preSET domain-related (From Topology)	H: Zn3Cys9 preSET domain-related (From Topology)	T: Zn3Cys9 preSET domain-related	F: AWS	ECOD (1.6)

Protein Family Annotation Pfam Database Homepage

Chains	Accession	Name	Description	Comments	Source
A	PF00856	SET domain (SET)	SET domain	-	Family
A	PF17907	AWS domain (AWS)	AWS domain	This entry represents the AWS (associated with SET domain) domain [1]. This is a zinc binding domain. The full AWS domain contains 8 cysteines. This entry represents the N-terminal part of the domain, with the C-terminal part interwoven with the SET ...	This entry represents the AWS (associated with SET domain) domain [1]. This is a zinc binding domain. The full AWS domain contains 8 cysteines. This entry represents the N-terminal part of the domain, with the C-terminal part interwoven with the SET domain.	Domain

Gene Ontology: Gene Product Annotation Gene Ontology Database Homepage

Chains	Polymer	Molecular Function	Biological Process	Cellular Component
A	Histone-lysine N-methyltransferase SETD2	protein-lysine N-methyltransferase activity catalytic activity, acting on a protein transferase activity, transferring one-carbon groups lysine N-methyltransferase activity protein methyltransferase activity N-methyltransferase activity transferase activity methyltransferase activity catalytic activity S-adenosylmethionine-dependent methyltransferase activity histone H3 methyltransferase activity histone modifying activity histone methyltransferase activity cytoskeletal protein binding protein-lysine N-methyltransferase activity catalytic activity, acting on a protein transferase activity, transferring one-carbon groups lysine N-methyltransferase activity protein methyltransferase activity N-methyltransferase activity transferase activity methyltransferase activity catalytic activity S-adenosylmethionine-dependent methyltransferase activity histone H3 methyltransferase activity histone modifying activity histone methyltransferase activity cytoskeletal protein binding protein binding binding tubulin binding alpha-tubulin binding histone H3K36 methyltransferase activity histone H3K36 trimethyltransferase activity cation binding ion binding metal ion binding small molecule binding	cellular response to stimulus regulation of DNA recombination regulation of cellular process regulation of double-strand break repair response to stimulus regulation of cellular response to stress regulation of primary metabolic process nucleobase-containing compound metabolic process cellular response to stress response to stress regulation of response to stress recombinational repair regulation of nucleobase-containing compound metabolic process double-strand break repair via homologous recombination cellular response to stimulus regulation of DNA recombination regulation of cellular process regulation of double-strand break repair response to stimulus regulation of cellular response to stress regulation of primary metabolic process nucleobase-containing compound metabolic process cellular response to stress response to stress regulation of response to stress recombinational repair regulation of nucleobase-containing compound metabolic process double-strand break repair via homologous recombination DNA repair double-strand break repair regulation of biological process DNA recombination biological regulation primary metabolic process DNA metabolic process regulation of macromolecule metabolic process nucleic acid metabolic process regulation of DNA repair regulation of double-strand break repair via homologous recombination DNA damage response regulation of response to stimulus metabolic process cellular process macromolecule metabolic process regulation of metabolic process regulation of DNA metabolic process cell migration involved in vasculogenesis developmental process multicellular organismal process cellular developmental process blood vessel morphogenesis tube development vasculogenesis vasculature development circulatory system development multicellular organism development anatomical structure morphogenesis tube morphogenesis cell differentiation anatomical structure development cell migration cell motility blood vessel development system development mismatch repair regulation of biosynthetic process cellular biosynthetic process cellular metabolic process regulation of cellular metabolic process gene expression macromolecule biosynthetic process regulation of cellular biosynthetic process regulation of gene expression biosynthetic process regulation of macromolecule biosynthetic process peptidyl-lysine methylation protein methylation peptidyl-lysine modification peptidyl-lysine trimethylation macromolecule methylation protein alkylation methylation macromolecule modification peptidyl-amino acid modification protein metabolic process protein modification process embryonic epithelial tube formation chordate embryonic development tube formation embryo development epithelial tube formation primary neural tube formation embryo development ending in birth or egg hatching epithelial tube morphogenesis morphogenesis of embryonic epithelium epithelium development neural tube development embryonic morphogenesis morphogenesis of an epithelium nervous system development tissue development tissue morphogenesis neural tube closure neural tube formation anatomical structure formation involved in morphogenesis tube closure biological process involved in interspecies interaction between organisms immune response response to other organism defense response response to cytokine defense response to symbiont response to external stimulus response to biotic stimulus response to peptide response to chemical immune system process defense response to other organism innate immune response response to external biotic stimulus response to type I interferon regulation of cytokinesis regulation of cell cycle process cytokinesis regulation of cell division cell division cell cycle regulation of cell cycle cell cycle process RNA metabolic process RNA biosynthetic process nucleic acid biosynthetic process DNA-templated transcription regulation of RNA metabolic process regulation of RNA biosynthetic process nucleobase-containing compound biosynthetic process regulation of DNA-templated transcription transcription elongation by RNA polymerase II DNA-templated transcription elongation transcription by RNA polymerase II defense response to virus response to virus positive regulation of autophagy catabolic process autophagy positive regulation of biological process positive regulation of cellular metabolic process regulation of catabolic process regulation of autophagy cellular catabolic process positive regulation of catabolic process positive regulation of metabolic process regulation of cellular catabolic process positive regulation of cellular catabolic process process utilizing autophagic mechanism positive regulation of cellular process interferon-alpha production positive regulation of macromolecule biosynthetic process positive regulation of biosynthetic process cytokine production regulation of cytokine production regulation of multicellular organismal process positive regulation of macromolecule metabolic process regulation of interferon-alpha production positive regulation of type I interferon production type I interferon production positive regulation of interferon-alpha production positive regulation of gene expression positive regulation of multicellular organismal process positive regulation of cytokine production positive regulation of cellular biosynthetic process regulation of type I interferon production heart development animal organ development pericardium development angiogenesis regulation of localization cellular localization nitrogen compound transport nucleocytoplasmic transport transport regulation of mRNA export from nucleus nuclear transport mRNA transport localization mRNA export from nucleus establishment of localization in cell RNA localization nuclear export nucleobase-containing compound transport ribonucleoprotein complex localization regulation of intracellular transport regulation of ribonucleoprotein complex localization RNA transport regulation of transport regulation of RNA export from nucleus regulation of nucleobase-containing compound transport nucleic acid transport intracellular transport regulation of nucleocytoplasmic transport establishment of localization RNA export from nucleus establishment of RNA localization regulation of cellular localization macromolecule localization embryonic organ morphogenesis embryonic cranial skeleton morphogenesis skeletal system development cranial skeletal system development animal organ morphogenesis embryonic skeletal system development skeletal system morphogenesis embryonic organ development embryonic skeletal system morphogenesis formation of primary germ layer gastrulation endoderm development endoderm formation endodermal cell differentiation protein localization protein localization to chromatin regulation of protein localization protein localization to chromosome protein localization to organelle cellular macromolecule localization regulation of protein localization to chromatin response to metal ion coronary vasculature development coronary vasculature morphogenesis morphogenesis of a branching structure head development forebrain development brain development central nervous system development placenta development in utero embryonic development embryonic placenta morphogenesis embryonic placenta development ossification positive regulation of ossification regulation of ossification response to nitrogen compound response to alkaloid stem cell development stem cell differentiation cell development cellular component organization protein-DNA complex organization protein-containing complex organization chromatin organization chromatin remodeling cellular component organization or biogenesis nucleosome organization microtubule cytoskeleton organization mitotic cell cycle organelle organization mitotic cell cycle process microtubule-based process microtubule cytoskeleton organization involved in mitosis cytoskeleton organization response to organic cyclic compound mesoderm morphogenesis mesoderm development	intracellular anatomical structure cytoplasm cellular anatomical entity intracellular organelle organelle intracellular non-membrane-bounded organelle chromosome non-membrane-bounded organelle membrane-bounded organelle nucleus membrane-enclosed lumen intracellular membrane-bounded organelle intracellular organelle lumen nucleoplasm intracellular anatomical structure cytoplasm cellular anatomical entity intracellular organelle organelle intracellular non-membrane-bounded organelle chromosome non-membrane-bounded organelle membrane-bounded organelle nucleus membrane-enclosed lumen intracellular membrane-bounded organelle intracellular organelle lumen nucleoplasm organelle lumen nuclear lumen

InterPro: Protein Family Classification InterPro Database Homepage

Chains	Accession	Name	Type
A	IPR046341	SET domain superfamily	Homologous Superfamily
A	IPR001214	SET domain	Domain
A	IPR036020	WW domain superfamily	Homologous Superfamily
A	IPR003616	Post-SET domain	Domain
A	IPR035441	TFIIS/LEDGF domain superfamily	Homologous Superfamily
A	IPR044437	SETD2/Set2, SET domain	Domain
A	IPR042294	Histone-lysine N-methyltransferase SETD2, animal	Family
A	IPR013257	Set2 Rpb1 interacting domain	Domain
A	IPR006560	AWS domain	Domain
A	IPR038190	Set2 Rpb1 interacting domain superfamily	Homologous Superfamily
A	IPR001202	WW domain	Domain

Pharos: Disease Associations Pharos Homepage Annotation

Chains	Drug Target	Associated Disease
A	Pharos: Q9BYW2	renal cell carcinoma Luscan-Lumish syndrome Sotos syndrome malignant mesothelioma acute myeloid leukemia papillary renal cell carcinoma prostate cancer chromophobe renal cell carcinoma intellectual disability Microsatellite Instability adenoid cystic carcinoma breast carcinoma salivary gland adenoid cystic carcinoma leukemia leukemia, acute lymphocytic, susceptibility to, 1 renal cell carcinoma Luscan-Lumish syndrome Sotos syndrome malignant mesothelioma acute myeloid leukemia papillary renal cell carcinoma prostate cancer chromophobe renal cell carcinoma intellectual disability Microsatellite Instability adenoid cystic carcinoma breast carcinoma salivary gland adenoid cystic carcinoma leukemia leukemia, acute lymphocytic, susceptibility to, 1 benign breast phyllodes tumor cancer collecting duct carcinoma sarcomatoid renal cell carcinoma breast cancer renal carcinoma rheumatoid arthritis malignant breast phyllodes tumor osteosarcoma phyllodes tumor clear cell renal carcinoma dermatomyositis ovarian cancer psoriasis Gaucher 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.