4CSJ

The discovery of potent selective glucocorticoid receptor modulators, suitable for inhalation

External Resource: Annotation

Domain Annotation: SCOP/SCOPe Classification
Domain Annotation: SCOP2 Classification
Domain Annotation: ECOD Classification
Domain Annotation: CATH
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	d4csja_	All alpha proteins	Nuclear receptor ligand-binding domain	Nuclear receptor ligand-binding domain	Nuclear receptor ligand-binding domain	automated matches	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	Nuclear receptor ligand-binding domain	8033332	3001442	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	Hormone_recep	e4csjA1	A: alpha arrays	X: Nuclear receptor ligand-binding domain (From Topology)	H: Nuclear receptor ligand-binding domain (From Topology)	T: Nuclear receptor ligand-binding domain	F: Hormone_recep	ECOD (1.6)

Domain Annotation: CATH CATH Database Homepage

Chain	Domain	Class	Architecture	Topology	Homology	Provenance Source (Version)
A	1.10.565.10	Mainly Alpha	Orthogonal Bundle	Retinoid X Receptor	Retinoid X Receptor	CATH (4.3.0)

Protein Family Annotation Pfam Database Homepage

Chains	Accession	Name	Description	Comments	Source
A	PF00104	Ligand-binding domain of nuclear hormone receptor (Hormone_recep)	Ligand-binding domain of nuclear hormone receptor	This all helical domain is involved in binding the hormone in these receptors.	Domain

Gene Ontology: Gene Product Annotation Gene Ontology Database Homepage

Chains	Polymer	Molecular Function	Biological Process	Cellular Component
B	NUCLEAR RECEPTOR COACTIVATOR 2	protein binding binding protein domain specific binding DNA binding sequence-specific DNA binding double-stranded DNA binding nucleic acid binding RNA polymerase II transcription regulatory region sequence-specific DNA binding cis-regulatory region sequence-specific DNA binding sequence-specific double-stranded DNA binding transcription cis-regulatory region binding organic cyclic compound binding transcription regulatory region nucleic acid binding RNA polymerase II cis-regulatory region sequence-specific DNA binding protein binding binding protein domain specific binding DNA binding sequence-specific DNA binding double-stranded DNA binding nucleic acid binding RNA polymerase II transcription regulatory region sequence-specific DNA binding cis-regulatory region sequence-specific DNA binding sequence-specific double-stranded DNA binding transcription cis-regulatory region binding organic cyclic compound binding transcription regulatory region nucleic acid binding RNA polymerase II cis-regulatory region sequence-specific DNA binding chromatin binding transcription coactivator activity transcription regulator activity transcription coregulator activity protein-macromolecule adaptor activity molecular adaptor activity transcription factor binding RNA polymerase II-specific DNA-binding transcription factor binding nuclear receptor binding DNA-binding transcription factor binding RNA polymerase II intronic transcription regulatory region sequence-specific DNA binding intronic transcription regulatory region sequence-specific DNA binding nuclear receptor coactivator activity protein dimerization activity signaling receptor binding aryl hydrocarbon receptor binding	regulation of biological process regulation of cellular process regulation of lipid metabolic process biological regulation primary metabolic process metabolic process cellular process regulation of metabolic process lipid metabolic process regulation of primary metabolic process developmental process multicellular organismal process regulation of developmental process connective tissue development regulation of biological process regulation of cellular process regulation of lipid metabolic process biological regulation primary metabolic process metabolic process cellular process regulation of metabolic process lipid metabolic process regulation of primary metabolic process developmental process multicellular organismal process regulation of developmental process connective tissue development adipose tissue development positive regulation of adipose tissue development animal organ development positive regulation of biological process tissue development positive regulation of developmental process regulation of adipose tissue development anatomical structure development positive regulation of multicellular organismal process regulation of multicellular organismal process response to ketone response to lipid response to stimulus response to hormone response to steroid hormone response to chemical response to endogenous stimulus response to progesterone response to oxygen-containing compound response to organic cyclic compound cellular response to stimulus cellular response to endogenous stimulus cellular response to chemical stimulus cellular response to hormone stimulus regulation of biosynthetic process rhythmic process circadian regulation of gene expression circadian rhythm regulation of macromolecule metabolic process gene expression macromolecule biosynthetic process regulation of gene expression biosynthetic process regulation of macromolecule biosynthetic process macromolecule metabolic process RNA metabolic process nucleobase-containing compound metabolic process RNA biosynthetic process nucleic acid biosynthetic process DNA-templated transcription regulation of RNA metabolic process regulation of nucleobase-containing compound metabolic process regulation of RNA biosynthetic process nucleobase-containing compound biosynthetic process nucleic acid metabolic process regulation of DNA-templated transcription intracellular receptor signaling pathway signaling intracellular signal transduction cell communication peroxisome proliferator activated receptor signaling pathway signal transduction nuclear receptor-mediated signaling pathway mRNA transcription by RNA polymerase II mRNA transcription mRNA metabolic process transcription by RNA polymerase II behavior circadian behavior locomotory behavior rhythmic behavior locomotor rhythm response to Thyroglobulin triiodothyronine cellular response to Thyroglobulin triiodothyronine negative regulation of biological process negative regulation of RNA biosynthetic process negative regulation of cellular 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 cellular response to nitrogen compound response to peptide hormone cellular response to peptide hormone stimulus response to nitrogen compound regulation of cellular response to insulin stimulus cellular response to oxygen-containing compound regulation of response to stimulus response to insulin cellular response to insulin stimulus positive regulation of DNA-templated transcription positive regulation of macromolecule biosynthetic process positive regulation of metabolic process positive regulation of biosynthetic process positive regulation of macromolecule metabolic process positive regulation of cellular process positive regulation of nucleobase-containing compound metabolic process positive regulation of transcription by RNA polymerase II positive regulation of RNA metabolic process positive regulation of RNA biosynthetic process monosaccharide metabolic process carbohydrate metabolic process hexose metabolic process regulation of small molecule metabolic process small molecule metabolic process regulation of carbohydrate metabolic process regulation of glucose metabolic process glucose metabolic process	RNA polymerase II transcription regulator complex membrane-bounded organelle protein-containing complex intracellular anatomical structure nucleus nuclear protein-containing complex transcription regulator complex intracellular membrane-bounded organelle intracellular organelle cellular anatomical structure organelle cytoplasm membrane-enclosed lumen intracellular organelle lumen RNA polymerase II transcription regulator complex membrane-bounded organelle protein-containing complex intracellular anatomical structure nucleus nuclear protein-containing complex transcription regulator complex intracellular membrane-bounded organelle intracellular organelle cellular anatomical structure organelle cytoplasm membrane-enclosed lumen intracellular organelle lumen nucleoplasm organelle lumen nuclear lumen membraneless organelle intracellular membraneless organelle chromatin chromosome nuclear body
A	GLUCOCORTICOID RECEPTOR	DNA binding sequence-specific DNA binding sequence-specific double-stranded DNA binding transcription cis-regulatory region binding binding double-stranded DNA binding organic cyclic compound binding core promoter sequence-specific DNA binding nucleic acid binding transcription regulatory region nucleic acid binding steroid hormone binding steroid binding lipid binding hormone binding DNA binding sequence-specific DNA binding sequence-specific double-stranded DNA binding transcription cis-regulatory region binding binding double-stranded DNA binding organic cyclic compound binding core promoter sequence-specific DNA binding nucleic acid binding transcription regulatory region nucleic acid binding steroid hormone binding steroid binding lipid binding hormone binding DNA-binding transcription factor activity, RNA polymerase II-specific transcription regulator activity DNA-binding transcription factor activity RNA polymerase II transcription regulatory region sequence-specific DNA binding cis-regulatory region sequence-specific DNA binding estrogen response element binding RNA polymerase II cis-regulatory region sequence-specific DNA binding transcription factor binding protein binding TBP-class protein binding general transcription initiation factor binding nuclear receptor activity molecular transducer activity ligand-activated transcription factor activity signaling receptor activity nuclear steroid receptor activity nuclear glucocorticoid receptor activity DNA-binding transcription activator activity, RNA polymerase II-specific DNA-binding transcription activator activity identical protein binding DNA-binding transcription repressor activity, RNA polymerase II-specific DNA-binding transcription repressor activity Hsp90 protein binding heat shock protein binding RNA binding kinase binding enzyme binding protein kinase binding cation binding transition metal ion binding zinc ion binding ion binding metal ion binding small molecule binding	cellular process cell division cell cycle chromosome segregation cell cycle process apoptotic process cell death programmed cell death regulation of biological process neuron apoptotic process positive regulation of programmed cell death regulation of cellular process regulation of apoptotic process biological regulation cellular process cell division cell cycle chromosome segregation cell cycle process apoptotic process cell death programmed cell death regulation of biological process neuron apoptotic process positive regulation of programmed cell death regulation of cellular process regulation of apoptotic process biological regulation positive regulation of biological process regulation of programmed cell death positive regulation of apoptotic process positive regulation of neuron apoptotic process positive regulation of cellular process regulation of neuron apoptotic process cellular response to stimulus response to lipid response to stimulus response to endogenous stimulus cellular response to organic cyclic compound cellular response to endogenous stimulus cellular response to chemical stimulus response to hormone response to chemical response to steroid hormone cellular response to lipid cellular response to steroid hormone stimulus response to organic cyclic compound cellular response to hormone stimulus developmental process multicellular organismal process epithelium development tube development mammary gland morphogenesis mammary gland development gland development animal organ development morphogenesis of an epithelium tissue development mammary gland duct morphogenesis tissue morphogenesis anatomical structure morphogenesis multicellular organism development tube morphogenesis gland morphogenesis mammary gland epithelium development anatomical structure development animal organ morphogenesis epithelial tube morphogenesis response to ketone cellular response to ketone cellular response to dexamethasone stimulus response to glucocorticoid cellular response to glucocorticoid stimulus response to oxygen-containing compound cellular response to oxygen-containing compound cellular response to corticosteroid stimulus response to corticosteroid response to dexamethasone positive regulation of DNA-templated transcription RNA metabolic process positive regulation of miRNA transcription positive regulation of miRNA metabolic process positive regulation of macromolecule biosynthetic process regulation of primary metabolic process nucleobase-containing compound metabolic process RNA biosynthetic process DNA-templated transcription nucleic acid biosynthetic process positive regulation of metabolic process regulation of RNA metabolic process miRNA transcription positive regulation of biosynthetic process regulation of miRNA metabolic process positive regulation of macromolecule metabolic process regulation of nucleobase-containing compound metabolic process miRNA metabolic process regulation of RNA biosynthetic process regulation of biosynthetic process positive regulation of nucleobase-containing compound metabolic process primary metabolic process regulation of macromolecule metabolic process nucleobase-containing compound biosynthetic process gene expression macromolecule biosynthetic process nucleic acid metabolic process positive regulation of RNA metabolic process regulation of gene expression biosynthetic process positive regulation of RNA biosynthetic process metabolic process regulation of macromolecule biosynthetic process macromolecule metabolic process regulation of DNA-templated transcription regulation of metabolic process regulation of miRNA transcription negative regulation of biological process negative regulation of RNA biosynthetic process transcription by RNA polymerase II negative regulation of cellular 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 positive regulation of transcription by RNA polymerase II cellular component organization chromatin organization cellular component organization or biogenesis monosaccharide metabolic process gluconeogenesis regulation of small molecule metabolic process small molecule metabolic process regulation of carbohydrate metabolic process regulation of glucose metabolic process carbohydrate metabolic process small molecule biosynthetic process carbohydrate biosynthetic process hexose metabolic process monosaccharide biosynthetic process hexose biosynthetic process regulation of gluconeogenesis regulation of carbohydrate biosynthetic process glucose metabolic process glucocorticoid metabolic process steroid metabolic process lipid metabolic process cellular response to growth factor stimulus response to transforming growth factor beta cellular response to transforming growth factor beta stimulus response to growth factor defense response response to stress inflammatory response neuroinflammatory response maternal behavior behavior parental behavior reproductive process multicellular organismal reproductive process reproductive behavior intracellular receptor signaling pathway signaling hormone-mediated signaling pathway intracellular signal transduction cell communication signal transduction nuclear receptor-mediated steroid hormone signaling pathway steroid hormone receptor signaling pathway nuclear receptor-mediated signaling pathway myeloid leukocyte differentiation cellular developmental process hemopoiesis macrophage differentiation cell development mononuclear cell differentiation nervous system development neurogenesis central nervous system development gliogenesis glial cell differentiation myeloid cell differentiation cell differentiation microglia differentiation system development leukocyte differentiation astrocyte differentiation adrenal gland development endocrine system development motor behavior regulation of steroid biosynthetic process regulation of hormone biosynthetic process regulation of hormone metabolic process regulation of lipid metabolic process lipid biosynthetic process regulation of glucocorticoid metabolic process regulation of biological quality regulation of glucocorticoid biosynthetic process steroid biosynthetic process hormone biosynthetic process steroid hormone biosynthetic process regulation of steroid hormone biosynthetic process regulation of hormone levels regulation of steroid metabolic process hormone metabolic process glucocorticoid biosynthetic process regulation of lipid biosynthetic process trans-synaptic signaling synaptic transmission, glutamatergic cell-cell signaling chemical synaptic transmission synaptic signaling anterograde trans-synaptic signaling	cellular anatomical structure membrane membrane-bounded organelle intracellular anatomical structure nucleus membrane-enclosed lumen intracellular membrane-bounded organelle intracellular organelle lumen nuclear speck nuclear body intracellular organelle nucleoplasm organelle lumen organelle cellular anatomical structure membrane membrane-bounded organelle intracellular anatomical structure nucleus membrane-enclosed lumen intracellular membrane-bounded organelle intracellular organelle lumen nuclear speck nuclear body intracellular organelle nucleoplasm organelle lumen organelle nuclear lumen cytoplasm cytosol membraneless organelle intracellular membraneless organelle chromatin chromosome cytoskeleton spindle microtubule cytoskeleton centrosome microtubule organizing center protein-containing complex synapse cell junction mitochondrion mitochondrial matrix

InterPro: Protein Family Classification InterPro Database Homepage

Chains	Accession	Name	Type
B	IPR010011	Nuclear receptor coactivator, DUF1518	Domain
B	IPR009110	Nuclear receptor coactivator, interlocking	Homologous Superfamily
B	IPR037077	Nuclear receptor coactivator, Ncoa-type, interlocking domain superfamily	Homologous Superfamily
B	IPR017426	Nuclear receptor coactivator	Family
B	IPR014935	Nuclear receptor coactivator, receptor-binding domain	Domain
B	IPR013767	PAS fold	Domain
B	IPR000014	PAS domain	Domain
B	IPR011598	Myc-type, basic helix-loop-helix (bHLH) domain	Domain
B	IPR014920	Nuclear receptor coactivator, Ncoa-type, interlocking	Domain
B	IPR035965	PAS domain superfamily	Homologous Superfamily
B	IPR028822	Nuclear receptor coactivator 2, basic helix-loop-helix	Domain
B	IPR032565	Nuclear receptor coactivator 2/3, DUF4927	Domain
B	IPR036638	Helix-loop-helix DNA-binding domain superfamily	Homologous Superfamily
A	IPR001628	Zinc finger, nuclear hormone receptor-type	Domain
A	IPR050200	Nuclear hormone receptor family NR3 subfamily	Family
A	IPR013088	Zinc finger, NHR/GATA-type	Homologous Superfamily
A	IPR001409	Glucocorticoid receptor	Family
A	IPR001723	Nuclear hormone receptor	Family
A	IPR000536	Nuclear hormone receptor, ligand-binding domain	Domain
A	IPR035500	Nuclear hormone receptor-like domain superfamily	Homologous Superfamily

Pharos: Disease Associations Pharos Homepage Annotation

Chains	Drug Target	Associated Disease
B	Pharos: Q15596	breast carcinoma prostate cancer psoriasis ulcerative colitis adenoma endometriosis interstitial cystitis Mammary Neoplasms osteosarcoma testicular cancer atypical teratoid rhabdoid tumor Crohn disease Gaucher disease large cell medulloblastoma pancreatic intraductal papillary-mucinous neoplasm breast carcinoma prostate cancer psoriasis ulcerative colitis adenoma endometriosis interstitial cystitis Mammary Neoplasms osteosarcoma testicular cancer atypical teratoid rhabdoid tumor Crohn disease Gaucher disease large cell medulloblastoma pancreatic intraductal papillary-mucinous neoplasm testicular germ cell tumor breast cancer endogenous depression glioblastoma medulloblastoma plasma cell myeloma
A	Pharos: P04150	glucocorticoid resistance endometriosis potassium deficiency disease psoriasis ocular hypertension atrial fibrillation 46,XX disorder of sex development melancholia schizophrenia ulcerative colitis hypokalemia cocaine abuse plasma cell myeloma endogenous depression cocaine dependence glucocorticoid resistance endometriosis potassium deficiency disease psoriasis ocular hypertension atrial fibrillation 46,XX disorder of sex development melancholia schizophrenia ulcerative colitis hypokalemia cocaine abuse plasma cell myeloma endogenous depression cocaine dependence obstructive lung disease bipolar disorder schizoaffective disorder hypertensive disorder prostate cancer sympathetic ophthalmia keratitis otitis externa exanthem autoimmune hemolytic anemia pulmonary fibrosis Crohn disease temporal arteritis ovarian cancer eye disease bacterial conjunctivitis thyroiditis perennial allergic rhinitis granuloma annulare blepharoconjunctivitis rhinitis breast cancer scalp dermatosis dermatitis herpetiformis trichinosis acute lymphoblastic leukemia polymyalgia rheumatica Diamond-Blackfan anemia seasonal allergic rhinitis multiple sclerosis vasomotor rhinitis alopecia areata proctitis inherited aplastic anemia skin disease neurotic disorder anterior uveitis pseudohermaphroditism iridocyclitis epicondylitis aspiration pneumonitis atopic conjunctivitis psoriatic arthritis juvenile idiopathic arthritis congenital adrenal hyperplasia synovitis atypical teratoid rhabdoid tumor pulmonary emphysema large cell medulloblastoma autoimmune thrombocytopenic purpura punctate epithelial keratoconjunctivitis lung cancer tendinitis pancreatic intraductal papillary-mucinous carcinoma rheumatic heart disease dacryocystitis tinea corporis hemorrhoid rosacea medulloblastoma depressive disorder breast carcinoma dermatophytosis of groin and perianal area tuberculosis Addison disease hyperaldosteronism Burkitt lymphoma schizophreniform disorder mood disorder allergic asthma idiopathic acute eosinophilic pneumonia seborrheic dermatitis musculoskeletal system disease ductal breast carcinoma in situ allergic rhinitis primary cutaneous T-cell lymphoma inflammatory bowel disease choroiditis angioedema intrinsic asthma chronic obstructive pulmonary disease eosinophilic esophagitis anxiety disorder iritis erythema multiforme asthma atopic eczema contact dermatitis osteosarcoma autoimmune disease pulmonary eosinophilia lichen planus corneal ulcer systemic lupus erythematosus extrinsic allergic alveolitis B-cell chronic lymphocytic leukemia major depressive disorder tenosynovitis pemphigus rheumatoid arthritis tinea pedis gout sarcoidosis acquired thrombocytopenia pneumocystosis Hodgkins lymphoma bronchitis miliary tuberculosis adrenocortical insufficiency bursitis uveitis allergic bronchopulmonary aspergillosis mycosis fungoides primitive neuroectodermal tumor chronic beryllium disease Sjogren syndrome nephrotic syndrome ankylosing spondylitis invasive ductal breast carcinoma Stevens-Johnson syndrome eosinophilic pneumonia aphthous stomatitis