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Literature summary for 4.2.1.24 extracted from

  • Lawrence, S.H.; Ramirez, U.D.; Selwood, T.; Stith, L.; Jaffe, E.K.
    Allosteric inhibition of human porphobilinogen synthase (2009), J. Biol. Chem., 284, 35807-35817.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 4.2.1.24

Protein Variants

Protein Variants Comment Organism
A274K naturally occurring ALAD porphyria-associated human PBGS mutants are shown to have an increased susceptibility to inhibition by both N-(3-methoxyphenyl)-1-methyl-6-oxo-2-[(pyridin-2-ylmethyl)sulfanyl]-1,6-dihydropyrimidine-5-carboxamide and 7-(3-aminopentan-3-yl)-5-chloroquinolin-8-ol Homo sapiens
E89K naturally occurring ALAD porphyria-associated human PBGS mutants are shown to have an increased susceptibility to inhibition by both N-(3-methoxyphenyl)-1-methyl-6-oxo-2-[(pyridin-2-ylmethyl)sulfanyl]-1,6-dihydropyrimidine-5-carboxamide and 7-(3-aminopentan-3-yl)-5-chloroquinolin-8-ol Homo sapiens
F12L low activity mutant F12L shows a hexameric structure, mutant F12L is used for in silico screening of 111000 structures for hexamer-stabilizing inhibitors Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
7-(3-aminopentan-3-yl)-5-chloroquinolin-8-ol using in silico screening two hexamer-stabilizing inhibitors of PBGS are identified: N-(3-methoxyphenyl)-1-methyl-6-oxo-2-[(pyridin-2-ylmethyl)sulfanyl]-1,6-dihydropyrimidine-5-carboxamide and 7-(3-aminopentan-3-yl)-5-chloroquinolin-8-ol Homo sapiens
N-(3-methoxyphenyl)-1-methyl-6-oxo-2-[(pyridin-2-ylmethyl)sulfanyl]-1,6-dihydropyrimidine-5-carboxamide using in silico screening two hexamer-stabilizing inhibitors of PBGS are identified: N-(3-methoxyphenyl)-1-methyl-6-oxo-2-[(pyridin-2-ylmethyl)sulfanyl]-1,6-dihydropyrimidine-5-carboxamide and 7-(3-aminopentan-3-yl)-5-chloroquinolin-8-ol Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P13716
-
-

Subunits

Subunits Comment Organism
dimer
-
 Homo sapiens
hexamer hexameric structure of the enzyme only shows low activity. Using in silico screening two hexamer-stabilizing inhibitors of PBGS are identified: N-(3-methoxyphenyl)-1-methyl-6-oxo-2-[(pyridin-2-ylmethyl)sulfanyl]-1,6-dihydropyrimidine-5-carboxamide and 7-(3-aminopentan-3-yl)-5-chloroquinolin-8-ol Homo sapiens
octamer high activity octamer is the dominant assembly Homo sapiens

Synonyms

Synonyms Comment Organism
PBGS
-
 Homo sapiens
Porphobilinogen synthase
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
8
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.01
-
-
 Homo sapiens 7-(3-aminopentan-3-yl)-5-chloroquinolin-8-ol
0.058
-
-
 Homo sapiens N-(3-methoxyphenyl)-1-methyl-6-oxo-2-[(pyridin-2-ylmethyl)sulfanyl]-1,6-dihydropyrimidine-5-carboxamide