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Literature summary for 2.1.1.244 extracted from

  • Chen, D.; Dong, G.; Noinaj, N.; Huang, R.
    Discovery of bisubstrate inhibitors for protein N-terminal methyltransferase 1 (2019), J. Med. Chem., 62, 3773-3779 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.1.1.244

Cloned(Commentary)

Cloned (Comment) Organism
recombinant expression of His-tagged enzyme in Escherichia coli strain BL21-CodonPlus(DE3)-RIL Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
purified recombinant His-tagged enzyme in complex with inhibitor NAM-C3-PKRIA-NH2 , hanging drop vapor diffusion method, mixing of 30 mg/ml protein and 2 mM ligand, with 1.5 M lithium sulfate and 0.1 M Na-HEPES, pH 7.5, 20°C, X-ray diffraction structure determination and analysis at 1.47 A resolution, molecular replacement using the structure PDB ID 6DTN as template, and modelling Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
5'-([3-[(2S)-2-acetylpyrrolidin-1-yl]propyl][(3S)-3-amino-3-carboxypropyl]amino)-5'-deoxyadenosine
-
 Homo sapiens
NAM-C3-GPRRRS
-
 Homo sapiens
NAM-C3-PKRIA-NH2 discovery of the potent NTMT1 bisubstrate inhibitor NAM-C3-PKRIA-NH2 that exhibits greater than 100fold selectivity against a panel of methyltransferases. Crystal structure analysis of NTMT1 in complex with the inhibitor reveals that NAM-C3-PKRIA-NH2 occupies substrate and cofactor binding sites of NTMT1 Homo sapiens
NAM-C3-PPKR-NH2
-
 Homo sapiens
NAM-C3-PRRRS-NH2
-
 Homo sapiens
NAM-TZ-SPKRIA
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3 S-adenosyl-L-methionine + GPKRIA Homo sapiens trimethylation by NTMT1 3 S-adenosyl-L-homocysteine + ?
-
 ?
additional information Homo sapiens protein N-terminal methyltransferase 1 (NTMT1/NRMT1) catalyzes the transfer of a methyl group from S-adenosyl-L-methionine (SAM) to protein alpha-N-terminal amines. It recognizes a specific motif X-P-K/R (X represents any amino acid other than D/E) ?
-
-

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9BV86
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant His-tagged enzyme from Escherichia coli strain BL21-CodonPlus(DE3)-RIL by nickel affinity chromatography Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3 S-adenosyl-L-methionine + GPKRIA trimethylation by NTMT1 Homo sapiens 3 S-adenosyl-L-homocysteine + ?
-
 ?
additional information protein N-terminal methyltransferase 1 (NTMT1/NRMT1) catalyzes the transfer of a methyl group from S-adenosyl-L-methionine (SAM) to protein alpha-N-terminal amines. It recognizes a specific motif X-P-K/R (X represents any amino acid other than D/E) Homo sapiens ?
-
-

Synonyms

Synonyms Comment Organism
NTMT1
-
 Homo sapiens
protein N-terminal methyltransferase 1
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000035
-
 recombinant His-tagged enzyme, pH 7.5, 37°C Homo sapiens NAM-C3-PKRIA-NH2

General Information

General Information Comment Organism
physiological function protein N-terminal methyltransferase 1 (NTMT1) plays an important role in regulating mitosis and DNA repair Homo sapiens