2.1.1.184: 23S rRNA (adenine2085-N6)-dimethyltransferase

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For detailed information about 23S rRNA (adenine2085-N6)-dimethyltransferase, go to the full flat file.

Word Map on EC 2.1.1.184

2.1.1.184

macrolide

macrolide-lincosamide-streptogramin

methyltransferases

lincosamide

unmethylated

mtases

streptogramine

medicine

Reaction

2 S-adenosyl-L-methionine +

= 2 S-adenosyl-L-homocysteine +

Synonyms

23S ribosomal RNA adenine N-6 methyltransferase, EC 2.1.1.48, ErmC, ermC 23 S rRNA methyltransferase, ErmC 23S rRNA methyltransferase, ermC methylase, ErmC methyltransferase, ErmC', ErmC' methyltransferase, ErmC' MTase, erythromycin resistance protein, rRNA methyltransferase ErmC', rRNA:m6A methyltransferase ErmC'

ECTree

2 Transferases

2.1 Transferring one-carbon groups

2.1.1 Methyltransferases

2.1.1.184 23S rRNA (adenine2085-N6)-dimethyltransferase

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Results	in table
322	AA Sequence
3	Application
5	Cloned(Commentary)
3	Crystallization (Commentary)
2	Expression
3	General Information
3	IC50 Value
8	Inhibitors
48	kcat/KM [mM/s]
6	Ki Value [mM]
58	KM Value [mM]
1	Localization
6	Natural Substrates/ Products (Substrates)
17	Organism
1	PDB ID
6	pH Optimum
1	pH Range
35	Protein Variants
4	Purification (Commentary)
5	Reaction
15	Reference
24	Substrates and Products (Substrate)
20	Synonyms
1	Systematic Name
6	Temperature Optimum [°C]
49	Turnover Number [1/s]

Inhibitors

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Inhibitors on EC 2.1.1.184 - 23S rRNA (adenine2085-N6)-dimethyltransferase

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2-([[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl][3-(1H-imidazol-1-yl)propyl]amino]methyl)-1H-isoindole-1,3(2H)-dione

Bacillus subtilis

P13956

i.e. PD00556

703219

4-methyl-2,6-di[(4-methylphenyl)thio]nicotinonitrile

Bacillus subtilis

P13956

i.e. RF00667

703219

N6-dimethyladenine2085 containing 23S rRNA

Bacillus subtilis

P13956

linear competitive inhibition kinetics with RNA as the variable substrate, mixed inhibition with S-adenosyl-L-methionine as the variable substrate

485438

nicotinaldehyde-N-[3-(2-chlorobenzyl)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-7-yl]hydrazone

Bacillus subtilis

P13956

i.e. HTS12610

703219

S-adenosyl-L-homocysteine

sinefungin

competitive

additional information

Bacillus subtilis

P13956

the crystal structure of ErmC methyltransferase is used as a target for structure-based virtual screening of a database composed of 58679 lead-like compounds. Among 77 compounds selected for experimental validation (63 predicted to bind to the catalytic pocket and 14 compounds predicted to bind to the putative RNA binding site), several novel inhibitors are found that decrease the minimal inhibitory concentration of a macrolide antibiotic erythromycin toward an Escherichia coli strain that constitutively expresses ErmC'. Analysis of docking models of the identified inhibitors suggests a novel strategy to develop potent and clinically useful inhibitors

703219