Literature summary for 4.3.2.10 extracted from

Myers, R.S.; Jensen, J.R.; Deras, I.L.; Smith, J.L.; Davisson, V.J.
Substrate-induced changes in the ammonia channel for imidazole glycerol phosphate synthase (2003), Biochemistry, 42, 7013-7022 .

Search for more literature for 4.3.2.10

Protein Variants

Protein Variants	Comment	Organism
K258A	about 2600fold decrease in kcat/Km for glutamine dependent cyclase reaction, basal and stimulated glutaminase functions are not altered. The stoichiometry of reaction glutamine: 5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide turnover is 43:1 compared to wild-type value 1:1	Saccharomyces cerevisiae
K258R	about 20fold decrease in kcat/Km for glutamine dependent cyclase reaction,basal and stimulated glutaminase functions are not altered. The stoichiometry of reaction glutamine: 5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide turnover is 43:1 compared to wild-type value 3:1	Saccharomyces cerevisiae
K360A	synthase activity is similar to wild type. The stoichiometry of the reaction is 3:1 indicating some degree of uncoupling due to loss of ammonia	Saccharomyces cerevisiae
K360R	synthase activity is similar to wild type. The mutant retains both structural and functional integrity of the enzyme in the case of glutaminase functions	Saccharomyces cerevisiae
R239A	a 1000fold reduction in kcat/Km is observed in the glutamine dependent synthase reaction. The stoichiometry of reaction glutamine: 5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide turnover is 43:1 compared to wild-type value 122:1	Saccharomyces cerevisiae
R239H	a 1000fold reduction in kcat/Km is observed in the glutamine dependent synthase reaction. The stoichiometry of reaction glutamine: 5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide turnover is 43:1 compared to wild-type value 154:1	Saccharomyces cerevisiae
R239K	a 1000fold reduction in kcat/Km is observed in the glutamine dependent synthase reaction. The stoichiometry of reaction glutamine: 5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide turnover is 43:1 compared to wild-type value 40:1	Saccharomyces cerevisiae

Inhibitors

Inhibitors	Comment	Organism	Structure
albizziin	mixed-type inhibitor versus 5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide, competitive versus glutamine	Saccharomyces cerevisiae
rPRFAR-1	competitive inhibitor versus 5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide inhibitor, mixed-type inhibitor versus glutamine	Saccharomyces cerevisiae
rPRFAR-2	competitive versus 5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	Saccharomyces cerevisiae

KM Value [mM]

KM Value [mM]	KM Value Maximum [mM]	Substrate	Comment	Organism	Structure
0.0016	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: L-glutamine, mutant enzyme R239K	Saccharomyces cerevisiae
0.0018	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: L-glutamine, mutant enzyme K360A	Saccharomyces cerevisiae
0.002	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: L-glutamine, mutant enzyme K258R	Saccharomyces cerevisiae
0.0023	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: L-glutamine, mutant enzyme K360R	Saccharomyces cerevisiae
0.003	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: L-glutamine, mutant enzyme R239A	Saccharomyces cerevisiae
0.005	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: L-glutamine, wild-type enzyme	Saccharomyces cerevisiae
0.0079	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: L-glutamine, mutant enzyme R239H	Saccharomyces cerevisiae
0.046	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: NH4+, mutant enzyme K258R	Saccharomyces cerevisiae
0.053	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: NH4+, mutant enzyme R239A	Saccharomyces cerevisiae
0.055	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: NH4+, wild-type enzyme	Saccharomyces cerevisiae
0.065	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: NH4+, mutant enzyme K360A	Saccharomyces cerevisiae
0.072	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: NH4+, mutant enzyme K360R	Saccharomyces cerevisiae
0.075	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: NH4+, mutant enzyme R239H	Saccharomyces cerevisiae
0.08	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: NH4+, mutant enzyme R239K	Saccharomyces cerevisiae
0.098	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: L-glutamine, mutant enzyme K258A	Saccharomyces cerevisiae
0.139	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: NH4+, mutant enzyme K258A	Saccharomyces cerevisiae

Organism

Organism	UniProt	Comment	Textmining
Saccharomyces cerevisiae	P33734	-	-
Saccharomyces cerevisiae ATCC 204508	P33734	-	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide + L-glutamine	4900fold upregulation of glutamine hydrolysis in the presence of an acceptor substrate. Transfer of ammonia from the glutaminase site occurs through the (beta/alpha)(8) core of the protein. The conserved K258 residue is key to productive binding and the overall stoichiometry of the reaction. The binding of the ribulosyl phosphate portion of the substrate appears to be transduced through reorientation of K258 resulting in a conformational switch at the base of the (beta/alpha)(8) core that enables the passage of ammonia through the core of the protein	Saccharomyces cerevisiae	5-amino-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide + D-erythro-1-(imidazol-4-yl)glycerol 3-phosphate + L-glutamate	-	?
5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide + L-glutamine	4900fold upregulation of glutamine hydrolysis in the presence of an acceptor substrate. Transfer of ammonia from the glutaminase site occurs through the (beta/alpha)(8) core of the protein. The conserved K258 residue is key to productive binding and the overall stoichiometry of the reaction. The binding of the ribulosyl phosphate portion of the substrate appears to be transduced through reorientation of K258 resulting in a conformational switch at the base of the (beta/alpha)(8) core that enables the passage of ammonia through the core of the protein	Saccharomyces cerevisiae ATCC 204508	5-amino-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide + D-erythro-1-(imidazol-4-yl)glycerol 3-phosphate + L-glutamate	-	?
5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide + NH4+	-	Saccharomyces cerevisiae	5-amino-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide + D-erythro-1-(imidazol-4-yl)glycerol 3-phosphate + H2O	-	?
5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide + NH4+	-	Saccharomyces cerevisiae ATCC 204508	5-amino-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide + D-erythro-1-(imidazol-4-yl)glycerol 3-phosphate + H2O	-	?

Synonyms

Synonyms	Comment	Organism
IGP synthase	-	Saccharomyces cerevisiae

Turnover Number [1/s]

Turnover Number Minimum [1/s]	Turnover Number Maximum [1/s]	Substrate	Comment	Organism	Structure
0.045	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: L-glutamine, mutant enzyme K258A	Saccharomyces cerevisiae
0.126	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: L-glutamine, mutant enzyme K258R	Saccharomyces cerevisiae
0.15	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: NH4+, mutant enzyme R239A	Saccharomyces cerevisiae
0.21	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: NH4+, mutant enzyme R239H	Saccharomyces cerevisiae
0.24	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: L-glutamine, mutant enzyme K360A	Saccharomyces cerevisiae
0.29	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: L-glutamine, mutant enzyme K360R	Saccharomyces cerevisiae
0.3	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: NH4+, mutant enzyme R239K	Saccharomyces cerevisiae
0.31	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: NH4+, mutant enzyme K360R	Saccharomyces cerevisiae
0.7	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: NH4+, mutant enzyme K360A	Saccharomyces cerevisiae
0.845	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: NH4+, wild-type enzyme	Saccharomyces cerevisiae
3.9	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: L-glutamine, mutant enzyme R239H	Saccharomyces cerevisiae
4.3	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: L-glutamine, mutant enzyme R239A	Saccharomyces cerevisiae
5	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: NH4+, mutant enzyme K258R	Saccharomyces cerevisiae
5.4	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: L-glutamine, wild-type enzyme	Saccharomyces cerevisiae
5.4	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: NH4+, mutant enzyme K258A	Saccharomyces cerevisiae
8.7	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: L-glutamine, mutant enzyme R239K	Saccharomyces cerevisiae

kcat/KM [mM/s]

kcat/KM Value [1/mMs^-1]	kcat/KM Value Maximum [1/mMs^-1]	Substrate	Comment	Organism	Structure
0.039	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: NH4+, mutant enzyme K258A	Saccharomyces cerevisiae
0.12	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: NH4+, mutant enzyme K258R	Saccharomyces cerevisiae
0.46	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: L-glutamine, mutant enzyme K258A	Saccharomyces cerevisiae
0.5	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: L-glutamine, mutant enzyme R239H	Saccharomyces cerevisiae
1.4	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: L-glutamine, mutant enzyme R239A	Saccharomyces cerevisiae
2.8	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: NH4+, mutant enzyme R239A	Saccharomyces cerevisiae
2.9	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: NH4+, mutant enzyme R239H	Saccharomyces cerevisiae
3.8	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: NH4+, mutant enzyme R239K	Saccharomyces cerevisiae
4.3	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: NH4+, mutant enzyme K360R	Saccharomyces cerevisiae
5.5	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: L-glutamine, mutant enzyme R239K	Saccharomyces cerevisiae
11	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: NH4+, mutant enzyme K360A	Saccharomyces cerevisiae
60	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: L-glutamine, mutant enzyme K258R	Saccharomyces cerevisiae
110	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: L-glutamine, mutant enzyme K360R	Saccharomyces cerevisiae
130	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: L-glutamine, mutant enzyme K360A	Saccharomyces cerevisiae
150	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: NH4+, wild-type enzyme	Saccharomyces cerevisiae
1200	-	5-[(5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino]-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide	30°C, pH 7.0, cosubstrate: L-glutamine, wild-type enzyme	Saccharomyces cerevisiae

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Release 2023.1 (January 2023)