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SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 2

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Target not currently curated in GtoImmuPdb

Target id: 2739

Nomenclature: SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 2

Abbreviated Name: SMARCA2

Family: Non-enzymatic BRD containing proteins

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1590 9p24.3 SMARCA2 SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 2
Mouse - 1583 19 C1 Smarca2 SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 2
Rat - 1597 1q51 Smarca2 SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 2
Previous and Unofficial Names Click here for help
BAF190 | SNF2 | SNF2L2 | SNF2LA | SWI2 | SWI/SNF related
Database Links Click here for help
Alphafold P51531 (Hs)
CATH/Gene3D 1.20.920.10, 2.130.10.10
ChEMBL Target CHEMBL2362979 (Hs)
Ensembl Gene ENSG00000080503 (Hs), ENSMUSG00000024921 (Mm), ENSRNOG00000011931 (Rn)
Entrez Gene 6595 (Hs), 67155 (Mm), 361745 (Rn)
Human Protein Atlas ENSG00000080503 (Hs)
KEGG Gene hsa:6595 (Hs), mmu:67155 (Mm), rno:361745 (Rn)
OMIM 600014 (Hs)
Pharos P51531 (Hs)
RefSeq Nucleotide NM_003070 (Hs), NM_011416 (Mm), NM_001004446 (Rn)
RefSeq Protein NP_003061 (Hs), NP_035546 (Mm), NP_001004446 (Rn)
UniProtKB P51531 (Hs)
Wikipedia SMARCA2 (Hs)

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
GNE-235 Small molecule or natural product Click here for species-specific activity table Hs Binding 5.2 pKd 2
⤷ pKd 5.2 (Kd 6x10-6 M) [2]
Description: Binding affinity for hSMARCA2
GNE-064 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.8 pIC50 3
⤷ pIC50 7.8 (IC50 1.6x10-8 M) [3]
Description: Potency determined by BromoScan assay
Other Binding Ligands
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
SMD-3040 Small molecule or natural product Click here for species-specific activity table Hs Binding 8.0 pKd 4
⤷ pKd 8.0 (Kd 1x10-8 M) [4]
Description: Binding affinity of SMARCA2/4 ligand 3 moiety
A947 Small molecule or natural product Click here for species-specific activity table Hs Binding 7.0 pKd 1
⤷ pKd 7.0 (Kd 9.3x10-8 M) [1]
Description: Binding affinity for SMARCA2 bromodomain.
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Nicolaides-Baraitser syndrome
Synonyms: Intellectual disability - sparse hair - brachydactyly [Orphanet: ORPHA3051]
OMIM: 601358
Orphanet: ORPHA3051

References

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1. Cantley J, Ye X, Rousseau E, Januario T, Hamman BD, Rose CM, Cheung TK, Hinkle T, Soto L, Quinn C et al.. (2022) Selective PROTAC-mediated degradation of SMARCA2 is efficacious in SMARCA4 mutant cancers. Nat Commun, 13 (1): 6814. [PMID:36357397]

2. Cochran AG, Flynn M. (2023) GNE-235: A Lead Compound Selective for the Second Bromodomain of PBRM1. J Med Chem, 66 (18): 13116-13134. [PMID:37702400]

3. Taylor AM, Bailey C, Belmont LD, Campbell R, Cantone N, Côté A, Crawford TD, Cummings R, DeMent K, Duplessis M et al.. (2022) GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1. J Med Chem, 65 (16): 11177-11186. [PMID:35930799]

4. Yang L, Tu W, Huang L, Miao B, Kaneshige A, Jiang W, Leng L, Wang M, Wen B, Sun D et al.. (2023) Discovery of SMD-3040 as a Potent and Selective SMARCA2 PROTAC Degrader with Strong in vivo Antitumor Activity. J Med Chem, 66 (15): 10761-10781. [PMID:37523716]

How to cite this page

Non-enzymatic BRD containing proteins: SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 2. Last modified on 18/01/2024. Accessed on 20/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2739.