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Literature summary for 6.3.4.14 extracted from

  • Miller, J.R.; Dunham, S.; Mochalkin, I.; Banotai, C.; Bowman, M.; Buist, S.; Dunkle, B.; Hanna, D.; Harwood, H.J.; Huband, M.D.; Karnovsky, A.; Kuhn, M.; Limberakis, C.; Liu, J.Y.; Mehrens, S.; Mueller, W.T.; Narasimhan, L.; Ogden, A.; Ohren, J.; Prasad, J.V.; Shelly, J.A.; Skerlos, L.; Sulavik, M.; Thomas,
    A class of selective antibacterials derived from a protein kinase inhibitor pharmacophore (2009), Proc. Natl. Acad. Sci. USA, 106, 1737-1742.
    View publication on PubMedView publication on EuropePMC

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with inhibitors 6-(2,6-dibromophenyl)pyrido[2,3-d]pyrimidine-2,7-diamine and 6-(2,6-methoxyphenyl)pyrido[2,3-d]pyrimidine-2,7-diamine Escherichia coli

Protein Variants

Protein Variants Comment Organism
H438P decrease in sensitivity to inhibitors 6-(2,6-dibromophenyl)pyrido[2,3-d]pyrimidine-2,7-diamine and 6-(2,6-methoxyphenyl)pyrido[2,3-d]pyrimidine-2,7-diamine Escherichia coli
I437T decrease in sensitivity to inhibitors 6-(2,6-dibromophenyl)pyrido[2,3-d]pyrimidine-2,7-diamine and 6-(2,6-methoxyphenyl)pyrido[2,3-d]pyrimidine-2,7-diamine Escherichia coli

Inhibitors

Inhibitors Comment Organism Structure
6-(2,6-dibromophenyl)pyrido[2,3-d]pyrimidine-2,7-diamine targets the ATP-binding site of biotin carboxylase. Biophysics of binding, crystallization data. Effective in vivo and in vitro, selective for bacterial biotin carboxylase. Pharmacological studies in rat and mouse Escherichia coli
6-(2,6-dimethoxyphenyl)pyrido[2,3-d]pyrimidine-2,7-diamine targets the ATP-binding site of biotin carboxylase. Biophysics of binding, crystallization data. Effective in vivo and in vitro, selective for bacterial biotin carboxylase. Pharmacological studies in rat and mouse Escherichia coli

Organism

Organism UniProt Comment Textmining
Escherichia coli P24182
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000005
-
or below, wild-type Escherichia coli 6-(2,6-dibromophenyl)pyrido[2,3-d]pyrimidine-2,7-diamine
0.000028
-
wild-type Escherichia coli 6-(2,6-dimethoxyphenyl)pyrido[2,3-d]pyrimidine-2,7-diamine
0.00016
-
mutant H438P Escherichia coli 6-(2,6-dibromophenyl)pyrido[2,3-d]pyrimidine-2,7-diamine
0.00056
-
mutant I437T Escherichia coli 6-(2,6-dibromophenyl)pyrido[2,3-d]pyrimidine-2,7-diamine
0.0012
-
wild-type Escherichia coli 6-(2,6-dimethoxyphenyl)pyrido[2,3-d]pyrimidine-2,7-diamine
0.0073
-
wild-type Escherichia coli 6-(2,6-dimethoxyphenyl)pyrido[2,3-d]pyrimidine-2,7-diamine