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Target not currently curated in GtoImmuPdb
Target id: 3128
Nomenclature: acyl-CoA synthetase short chain family member 2
Family: Acyl-CoA synthetases
Gene and Protein Information | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 701 | 20q11.22 | ACSS2 | acyl-CoA synthetase short chain family member 2 | |
Gene and Protein Information Comments | ||||||
Alternative splicing results in multiple transcript variants and isozymes. |
Database Links | |
Alphafold | Q9NR19 (Hs) |
ChEMBL Target | CHEMBL4523467 (Hs) |
Ensembl Gene | ENSG00000131069 (Hs) |
Entrez Gene | 55902 (Hs) |
Human Protein Atlas | ENSG00000131069 (Hs) |
KEGG Gene | hsa:55902 (Hs) |
OMIM | 605832 (Hs) |
Pharos | Q9NR19 (Hs) |
RefSeq Nucleotide | NM_018677 (Hs) |
RefSeq Protein | NP_061147 (Hs) |
UniProtKB | Q9NR19 (Hs) |
Wikipedia | ACSS2 (Hs) |
Download all structure-activity data for this target as a CSV file
Inhibitors | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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View species-specific inhibitor tables |
General Comments |
Acyl-CoA synthetase short chain family member 2 (ACSS2) is a monomeric cytosolic enzyme that catalyses the activation of acetate for use in lipid synthesis and energy generation. Cellular stress induced by oxygen or glucose deprivation increases intracellular acetate levels. Under these conditions ACSS2 translocates to the nucleus where it promotes acetylation of the stress-responsive hypoxia Inducible factor 2αα and increases histone H3K27 acetylation [1]. The acetate/ACSS2/histone acetylation influence on epithelial-mesenchymal transition (EMT) and cancer cell metastasis is being investigated [5], and ACSS2 inhibitor development is underway [2,4]. |
1. Chen R, Xu M, Nagati J, Garcia JA. (2017) Coordinate regulation of stress signaling and epigenetic events by Acss2 and HIF-2 in cancer cells. PLoS ONE, 12 (12): e0190241. [PMID:29281714]
2. Kargbo RB. (2019) Inhibition of ACSS2 for Treatment of Cancer and Neuropsychiatric Diseases. ACS Med Chem Lett, 10 (8): 1100-1101. [PMID:31413791]
3. Mews P, Berger Sl, Winkler JD, Glass A. (2019) Compositions and methods for inhibiting acss2. Patent number: WO2019067528A1. Assignee: The Trustees Of The University Of Pennsylvania. Priority date: 26/09/2017. Publication date: 04/04/2019.
4. Nakache P, Erez O, Botti S, Goutopoulos A, Labelle M. (2019) Acss2 inhibitors and methods of use thereof. Patent number: WO2019097515A1. Assignee: Metabomed Ltd. Priority date: 15/11/2017. Publication date: 23/05/2019.
5. Yao L, Jiang L, Zhang F, Li M, Yang B, Zhang F, Guo X. (2020) Acetate promotes SNAI1 expression by ACSS2-mediated histone acetylation under glucose limitation in renal cell carcinoma cell. Biosci Rep, 40 (6). DOI: 10.1042/BSR20200382 [PMID:32458971]
Acyl-CoA synthetases: acyl-CoA synthetase short chain family member 2. Last modified on 03/08/2023. Accessed on 07/11/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=3128.