Application | Comment | Organism |
---|---|---|
drug development | the enzyme is a possible target for treatment of cryptosporidiosis caused by the organism | Cryptosporidium hominis |
Cloned (Comment) | Organism |
---|---|
expression in Escherichia coli | Cryptosporidium hominis |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2,4-diamino-5-[(R)-3-(3-methoxy-5-phenylphenyl)but-1-ynyl]-6-methylpyrimidine | - |
Cryptosporidium hominis | |
2,4-diamino-5-[(S)-3-(3-methoxy-5-phenylphenyl)but-1-ynyl]-6-methylpyrimidine | - |
Cryptosporidium hominis | |
2,4-diamino-5-[3-(3-methoxy-4-(2,6-diisopropylphenyl)phenyl)-but-1-ynyl]-6-methylpyrimidine | - |
Cryptosporidium hominis | |
2,4-diamino-5-[3-(3-methoxy-4-(2,6-dimethylphenyl)phenyl)but-1-ynyl]-6-methylpyrimidine | - |
Cryptosporidium hominis | |
2,4-diamino-5-[3-(3-methoxy-4-(2-methylphenyl)phenyl)but-1-ynyl]-6-methylpyrimidine | - |
Cryptosporidium hominis | |
2,4-diamino-5-[3-(3-methoxy-4-phenylphenyl)but-1-ynyl]-6-methylpyrimidine | - |
Cryptosporidium hominis | |
2,4-diamino-5-[3-(3-methoxy-5-(2,6-diisopropylphenyl)phenyl)-but-1-ynyl]-6-methylpyrimidine | - |
Cryptosporidium hominis | |
2,4-diamino-5-[3-(3-methoxy-5-(2,6-dimethylphenyl)phenyl)but-1-ynyl]-6-methylpyrimidine | - |
Cryptosporidium hominis | |
2,4-diamino-5-[3-(3-methoxy-5-(2-methylphenyl)phenyl)but-1-ynyl]-6-methylpyrimidine | - |
Cryptosporidium hominis | |
2,4-diamino-5-[3-(3-methoxy-5-phenylphenyl)but-1-ynyl]-6-methylpyrimidine | - |
Cryptosporidium hominis | |
6-methyl-5-[3-(3,4,5-trimethoxyphenyl)but-1-yn-1-yl]pyrimidine-2,4-diamine | - |
Cryptosporidium hominis | |
additional information | inhibitor design and synthesis, computational modeling, analysis of the interactions of the biphenyl compounds with the enzyme, and drug selectivity in comparison to the human enzyme, overview | Cryptosporidium hominis |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | Cryptosporidium hominis | in Cryptosporidium, DHFR and thymidylate synthase are present as a bifunctional enzyme, DHFR-TS | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Cryptosporidium hominis | - |
- |
- |
Purification (Comment) | Organism |
---|---|
recombinant enzyme from Escherichia coli by methotrexate affinity chromatography | Cryptosporidium hominis |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | in Cryptosporidium, DHFR and thymidylate synthase are present as a bifunctional enzyme, DHFR-TS | Cryptosporidium hominis | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
DHFR | - |
Cryptosporidium hominis |
DHFR-TS | - |
Cryptosporidium hominis |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0000011 | - |
- |
Cryptosporidium hominis | 2,4-diamino-5-[(R)-3-(3-methoxy-5-phenylphenyl)but-1-ynyl]-6-methylpyrimidine | |
0.0000018 | - |
- |
Cryptosporidium hominis | 2,4-diamino-5-[3-(3-methoxy-5-phenylphenyl)but-1-ynyl]-6-methylpyrimidine | |
0.0000021 | - |
- |
Cryptosporidium hominis | 2,4-diamino-5-[3-(3-methoxy-5-(2-methylphenyl)phenyl)but-1-ynyl]-6-methylpyrimidine | |
0.0000021 | - |
- |
Cryptosporidium hominis | 2,4-diamino-5-[3-(3-methoxy-5-(2,6-dimethylphenyl)phenyl)but-1-ynyl]-6-methylpyrimidine | |
0.0000074 | - |
- |
Cryptosporidium hominis | 2,4-diamino-5-[3-(3-methoxy-4-(2,6-dimethylphenyl)phenyl)but-1-ynyl]-6-methylpyrimidine | |
0.00001 | - |
- |
Cryptosporidium hominis | 2,4-diamino-5-[3-(3-methoxy-5-(2,6-diisopropylphenyl)phenyl)-but-1-ynyl]-6-methylpyrimidine | |
0.000016 | - |
- |
Cryptosporidium hominis | 2,4-diamino-5-[3-(3-methoxy-4-(2,6-diisopropylphenyl)phenyl)-but-1-ynyl]-6-methylpyrimidine | |
0.000019 | - |
- |
Cryptosporidium hominis | 2,4-diamino-5-[3-(3-methoxy-4-phenylphenyl)but-1-ynyl]-6-methylpyrimidine | |
0.00003 | - |
- |
Cryptosporidium hominis | 2,4-diamino-5-[(S)-3-(3-methoxy-5-phenylphenyl)but-1-ynyl]-6-methylpyrimidine | |
0.000036 | - |
- |
Cryptosporidium hominis | 2,4-diamino-5-[3-(3-methoxy-4-(2-methylphenyl)phenyl)but-1-ynyl]-6-methylpyrimidine | |
0.000038 | - |
- |
Cryptosporidium hominis | 6-methyl-5-[3-(3,4,5-trimethoxyphenyl)but-1-yn-1-yl]pyrimidine-2,4-diamine |