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Acetyl-CoA carboxylase 1

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Target id: 1263

Nomenclature: Acetyl-CoA carboxylase 1

Abbreviated Name: ACC1

Family: Carboxylases

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 2346 17q12 ACACA acetyl-CoA carboxylase alpha
Mouse - 2345 11 C Acaca acetyl-Coenzyme A carboxylase alpha
Rat - 2345 10q26 Acaca acetyl-CoA carboxylase alpha
Previous and Unofficial Names Click here for help
ACACA | ACAC | ACC | acetyl-CoA carboxylase alpha | ACCα
Database Links Click here for help
Alphafold Q13085 (Hs), Q5SWU9 (Mm), P11497 (Rn)
BRENDA 6.4.1.2
CATH/Gene3D 3.30.1490.20
ChEMBL Target CHEMBL3351 (Hs), CHEMBL3086 (Mm), CHEMBL2397 (Rn)
Ensembl Gene ENSG00000278540 (Hs), ENSMUSG00000020532 (Mm), ENSRNOG00000034013 (Rn)
Entrez Gene 31 (Hs), 107476 (Mm), 60581 (Rn)
Human Protein Atlas ENSG00000278540 (Hs)
KEGG Enzyme 6.4.1.2
KEGG Gene hsa:31 (Hs), mmu:107476 (Mm), rno:60581 (Rn)
OMIM 200350 (Hs)
Pharos Q13085 (Hs)
UniProtKB Q13085 (Hs), Q5SWU9 (Mm), P11497 (Rn)
Wikipedia ACACA (Hs)
Enzyme Reaction Click here for help
EC Number: 6.4.1.2
Products Click here for help
Product Species Reference
Pi Human

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
compound 21 [PMID: 23981033] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.0 pIC50 3
⤷ pIC50 8.0 (IC50 1x10-8 M) [3]
clesacostat Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.9 pIC50 5
⤷ pIC50 7.9 (IC50 1.24x10-8 M) [5]
CP-640186 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Inhibition 7.3 pIC50 1
⤷ pIC50 7.3 (IC50 5.3x10-8 M) [1]
CP-640186 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.4 pIC50 2
⤷ pIC50 6.4 (IC50 4.1x10-7 M) [2]
TOFA Small molecule or natural product Click here for species-specific activity table Hs Inhibition 4.9 pIC50 6
⤷ pIC50 4.9 (IC50 1.23x10-5 M) [6]
View species-specific inhibitor tables
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
firsocostat Small molecule or natural product Click here for species-specific activity table Hs Negative 8.7 pIC50 4
⤷ pIC50 8.7 (IC50 2.1x10-9 M) [4]

References

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1. Chonan T, Oi T, Yamamoto D, Yashiro M, Wakasugi D, Tanaka H, Ohoka-Sugita A, Io F, Koretsune H, Hiratate A. (2009) (4-Piperidinyl)-piperazine: a new platform for acetyl-CoA carboxylase inhibitors. Bioorg Med Chem Lett, 19 (23): 6645-8. [PMID:19853443]

2. Clark RF, Zhang T, Xin Z, Liu G, Wang Y, Hansen TM, Wang X, Wang R, Zhang X, Frevert EU et al.. (2006) Structure-activity relationships for a novel series of thiazolyl phenyl ether derivatives exhibiting potent and selective acetyl-CoA carboxylase 2 inhibitory activity. Bioorg Med Chem Lett, 16 (23): 6078-81. [PMID:16973360]

3. Griffith DA, Dow RL, Huard K, Edmonds DJ, Bagley SW, Polivkova J, Zeng D, Garcia-Irizarry CN, Southers JA, Esler W et al.. (2013) Spirolactam-based acetyl-CoA carboxylase inhibitors: toward improved metabolic stability of a chromanone lead structure. J Med Chem, 56 (17): 7110-9. [PMID:23981033]

4. Harriman G, Greenwood J, Bhat S, Huang X, Wang R, Paul D, Tong L, Saha AK, Westlin WF, Kapeller R et al.. (2016) Acetyl-CoA carboxylase inhibition by ND-630 reduces hepatic steatosis, improves insulin sensitivity, and modulates dyslipidemia in rats. Proc Natl Acad Sci USA, 113 (13): E1796-805. [PMID:26976583]

5. Huard K, Smith AC, Cappon G, Dow RL, Edmonds DJ, El-Kattan A, Esler WP, Fernando DP, Griffith DA, Kalgutkar AS et al.. (2020) Optimizing the Benefit/Risk of Acetyl-CoA Carboxylase Inhibitors through Liver Targeting. J Med Chem, 63 (19): 10879-10896. [PMID:32809824]

6. Zhou W, Simpson PJ, McFadden JM, Townsend CA, Medghalchi SM, Vadlamudi A, Pinn ML, Ronnett GV, Kuhajda FP. (2003) Fatty acid synthase inhibition triggers apoptosis during S phase in human cancer cells. Cancer Res, 63 (21): 7330-7. [PMID:14612531]

How to cite this page

Carboxylases: Acetyl-CoA carboxylase 1. Last modified on 09/11/2022. Accessed on 11/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1263.