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Literature summary for 2.5.1.46 extracted from

  • Hyvoenen, M.T.; Khomutov, M.; Petit, M.; Weisell, J.; Kochetkov, S.N.; Alhonen, L.; Vepsaelaeinen, J.; Khomutov, A.R.; Keinaenen, T.A.
    Enantiomers of 3-methylspermidine selectively modulate deoxyhypusine synthesis and reveal important determinants for spermidine transport (2015), ACS Chem. Biol., 10, 1417-1424.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(R)-3-methylspermidine competitive inhibition versus spermidine Homo sapiens
(S)-3-methylspermidine competitive inhibition versus spermidine Homo sapiens
additional information no growth inhibition by alpha-difluoromethylornithine, an inhibitor of polyamine biosynthesis, and (R)-3-methylspermidine, while the the combination of alpha-difluoromethylornithine with a racemate or (S)-3-methylspermidine causes cessation of cell growth. Cells treated with racemic 3-MeSpd accumulat intracellularly mainly (S)-3-methylspermidine, but not DHS substrate (R)-3-methylspermidine, explaining the inability of the racemate to support long-term growth Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
[eIF5A-precursor]-lysine + spermidine Homo sapiens
-
[eIF5A-precursor]-deoxyhypusine + propane-1,3-diamine
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens P49366 gene Dhps
-

Source Tissue

Source Tissue Comment Organism Textmining
DU-145 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information (R)-3-methylspermidine competes with spermidine for cellular uptake less efficiently than the (S)-3-methylspermidine Homo sapiens ?
-
?
[eIF5A-precursor]-lysine + (R)-3-methylspermidine enzyme DHS prefers the (R)- over the (S)-enantiomer as a substrate Homo sapiens ?
-
?
[eIF5A-precursor]-lysine + spermidine
-
Homo sapiens [eIF5A-precursor]-deoxyhypusine + propane-1,3-diamine
-
?
[eIF5A-precursor]-lysine + spermidine formation of [N(epsilon)-(4-amino-2-hydroxybutyl)lysine] Homo sapiens [eIF5A-precursor]-deoxyhypusine + propane-1,3-diamine
-
?

Synonyms

Synonyms Comment Organism
DHS
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.019
-
(S)-3-methylspermidine pH and temperature not specified in the publication Homo sapiens
0.141
-
(R)-3-methylspermidine pH and temperature not specified in the publication Homo sapiens

General Information

General Information Comment Organism
physiological function the eukaryotic translation initiation factor 5A (eIF5A) is essential for cell proliferation, becoming functionally active only after post-translational conversion of a specific Lys to hypusine catalyzed by deoxyhypusine synthase, the rate-limiting enzyme of this two-step process Homo sapiens