Cloned (Comment) | Organism |
---|---|
- |
Homo sapiens |
Crystallization (Comment) | Organism |
---|---|
by hanging-drop method, HNMT bound to four different inhibitors at resolution limits of 1.9 A (diphenhydramine), 2.3 A (amodiaquine), 2.48 A (metoprine), and 2.97 A (tacrine) and in complex with S-adenosyl-L-homocysteine | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
amodiaquine | potent HNMT inhibitor, occupies the histamine-binding site, thus blocks access to the enzymes active site | Homo sapiens | |
diphenhydramine | potent HNMT inhibitor, occupies the histamine-binding site, thus blocks access to the enzymes active site | Homo sapiens | |
Metoprine | potent HNMT inhibitor, occupies the histamine-binding site, thus blocks access to the enzymes active site | Homo sapiens | |
additional information | near the N-terminus of HNMT, several aromatic residues (Phe9, Tyr15, and Phe19) adopt different rotamer conformations or become disordered in the enzyme-inhibitor complexes, accommodating the diverse, rigid hydrophobic groups of the inhibitors, maximized shape complementarity between the protein aromatic side-chains and aromatic rings of the inhibitors are responsible for the tight binding of the different inhibitors | Homo sapiens | |
tacrine | potent HNMT inhibitor, occupies the histamine-binding site, thus blocks access to the enzymes active site | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P50135 | - |
- |
Purification (Comment) | Organism |
---|---|
- |
Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
S-adenosyl-L-methionine + histamine | - |
Homo sapiens | S-adenosyl-L-homocysteine + Ntau-methylhistamine | - |
? |
Synonyms | Comment | Organism |
---|---|---|
HNMT | - |
Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0000186 | - |
amodiaquine | - |
Homo sapiens | |
0.0000382 | - |
tacrine | - |
Homo sapiens | |
0.000091 | - |
Metoprine | - |
Homo sapiens |