Literature summary for 2.1.1.8 extracted from

Horton, J.R.; Sawada, K.; Nishibori, M.; Cheng, X.
Structural basis for inhibition of histamine N-methyltransferase by diverse drugs (2005), J. Mol. Biol., 353, 334-344.

Search for more literature for 2.1.1.8

Cloned(Commentary)

Cloned (Comment)	Organism
-	Homo sapiens

Crystallization (Commentary)

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

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

Organism	UniProt	Comment	Textmining
Homo sapiens	P50135	-	-

Purification (Commentary)

Purification (Comment)	Organism
-	Homo sapiens

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
S-adenosyl-L-methionine + histamine	-	Homo sapiens	S-adenosyl-L-homocysteine + Ntau-methylhistamine	-	?

Synonyms

Synonyms	Comment	Organism
HNMT	-	Homo sapiens

Ki Value [mM]

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

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Release 2023.1 (January 2023)