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Literature summary for 2.1.1.319 extracted from

  • Kaniskan, H.U.e.; Eram, M.S.; Liu, J.; Smil, D.; Martini, M.L.; Shen, Y.; Santhakumar, V.; Brown, P.J.; Arrowsmith, C.; Vedadi, M.; Jin, J.
    Design and synthesis of selective, small molecule inhibitors of coactivator-associated arginine methyltransferase 1 (CARM1) (2016), MedChemComm, 7, 1793-1796 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.1.1.319

Inhibitors

Inhibitors Comment Organism Structure
N-(3-bromobenzyl)-1-(2-(methylamino)ethyl)piperidin-4-amine potent and selective inhibitor of CARM1. It is around 20fold selective for CARM1 over PRMT6 and highly selective over PRMT1, PRMT3, PRMT8 as well as PRMT5 and PRMT7 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2 S-adenosyl-L-methionine + [CBP/p300]-L-arginine Homo sapiens
-
 2 S-adenosyl-L-homocysteine + [CBP/p300]-Nomega,Nomega-dimethyl-L-arginine
-
 ?
2 S-adenosyl-L-methionine + [histone H3R17]-L-arginine Homo sapiens
-
 2 S-adenosyl-L-homocysteine + [histone H3R17]-Nomega,Nomega-dimethyl-L-arginine
-
 ?
2 S-adenosyl-L-methionine + [histone H3R26]-L-arginine Homo sapiens
-
 2 S-adenosyl-L-homocysteine + [histone H3R26]-Nomega,Nomega-dimethyl-L-arginine
-
 ?
2 S-adenosyl-L-methionine + [NCOA2]-L-arginine Homo sapiens
-
 2 S-adenosyl-L-homocysteine + [NCOA2]-Nomega,Nomega-dimethyl-L-arginine
-
 ?
2 S-adenosyl-L-methionine + [PABP1]-L-arginine Homo sapiens
-
 2 S-adenosyl-L-homocysteine + [PABP1]-Nomega,Nomega-dimethyl-L-arginine
-
 ?
2 S-adenosyl-L-methionine + [SAP49]-L-arginine Homo sapiens
-
 2 S-adenosyl-L-homocysteine + [SAP49]-Nomega,Nomega-dimethyl-L-arginine
-
 ?
2 S-adenosyl-L-methionine + [SRC-3]-L-arginine Homo sapiens
-
 2 S-adenosyl-L-homocysteine + [SRC-3]-Nomega,Nomega-dimethyl-L-arginine
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q86X55
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2 S-adenosyl-L-methionine + [CBP/p300]-L-arginine
-
 Homo sapiens 2 S-adenosyl-L-homocysteine + [CBP/p300]-Nomega,Nomega-dimethyl-L-arginine
-
 ?
2 S-adenosyl-L-methionine + [histone H3R17]-L-arginine
-
 Homo sapiens 2 S-adenosyl-L-homocysteine + [histone H3R17]-Nomega,Nomega-dimethyl-L-arginine
-
 ?
2 S-adenosyl-L-methionine + [histone H3R26]-L-arginine
-
 Homo sapiens 2 S-adenosyl-L-homocysteine + [histone H3R26]-Nomega,Nomega-dimethyl-L-arginine
-
 ?
2 S-adenosyl-L-methionine + [NCOA2]-L-arginine
-
 Homo sapiens 2 S-adenosyl-L-homocysteine + [NCOA2]-Nomega,Nomega-dimethyl-L-arginine
-
 ?
2 S-adenosyl-L-methionine + [PABP1]-L-arginine
-
 Homo sapiens 2 S-adenosyl-L-homocysteine + [PABP1]-Nomega,Nomega-dimethyl-L-arginine
-
 ?
2 S-adenosyl-L-methionine + [peptide]-L-arginine
-
 Homo sapiens 2 S-adenosyl-L-homocysteine + [peptide]-Nomega,Nomega-dimethyl-L-arginine
-
 ?
2 S-adenosyl-L-methionine + [SAP49]-L-arginine
-
 Homo sapiens 2 S-adenosyl-L-homocysteine + [SAP49]-Nomega,Nomega-dimethyl-L-arginine
-
 ?
2 S-adenosyl-L-methionine + [SRC-3]-L-arginine
-
 Homo sapiens 2 S-adenosyl-L-homocysteine + [SRC-3]-Nomega,Nomega-dimethyl-L-arginine
-
 ?

Synonyms

Synonyms Comment Organism
CARM1
-
 Homo sapiens
coactivator-associated arginine methyltransferase 1
-
 Homo sapiens
PRMT4
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000094
-
 pH and temperature not specified in the publication Homo sapiens N-(3-bromobenzyl)-1-(2-(methylamino)ethyl)piperidin-4-amine

General Information

General Information Comment Organism
drug target the enzme is associated with several human cancers including breast, colon, prostate and lung cancers and thus, is a potential oncological target Homo sapiens
physiological function the enzyme (CARM1) functions as a coactivator for various proteins that have been linked to cancer such as p53, NF-kappabeta, beta-catenin, E2F1 and steroid hormone receptor ERalpha. CARM1 is involved in transcriptional activation, cellular differentiation, cell cycle progression, RNA splicing and DNA damage response Homo sapiens