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Literature summary for 1.14.13.39 extracted from

  • Igarashi, J.; Li, H.; Jamal, J.; Ji, H.; Fang, J.; Lawton, G.R.; Silverman, R.B.; Poulos, T.L.
    Crystal structures of constitutive nitric oxide synthases in complex with de novo designed inhibitors (2009), J. Med. Chem., 52, 2060-2066.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli BL21(DE3) cells Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
sitting drop vapor diffusion method Homo sapiens

Protein Variants

Protein Variants Comment Organism
D597N/M336V mutant of nNOS, the Ki values for the nNOS double mutant increase for all inhibitors but the mutant still binds these inhibitors better than eNOS Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(4S)-N-(4-amino-5-[aminoethyl]aminopentyl)-N''-nitroguanidine
-
Homo sapiens
3-[cis-4'-[(6''-aminopyridin-2''-yl)methyl]pyrrolidin-3'-ylamino]propan-1-ol
-
Homo sapiens
L-Nomega-nitroarginine-(4R)-amino-L-proline amide
-
Homo sapiens
L-Nomega-nitroarginine-2,4-L-diaminobutyramide
-
Homo sapiens
N1-[cis-4'-[(6''-amino-4''-methylpyridin-2''-yl)methyl]pyrrolidin-3'-yl]-N2-(4'-chlorobenzyl)ethane-1,2-diamine
-
Homo sapiens
N1-[cis-4'-[(6''-aminopyridin-2''-yl)methyl]pyrrolidin-3'-yl]ethane-1,2-diamine
-
Homo sapiens
N1-[trans-4'-[(6''-amino-4''-methylpyridin-2''-yl)methyl]pyrrolidin-3'-yl]-N2-(3'-chlorobenzyl)ethane-1,2-diamine
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0019
-
L-arginine mutant nNOS D597N/M336V Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P29474
-
-
Homo sapiens P29475
-
-

Purification (Commentary)

Purification (Comment) Organism
Ni Sepharose column chromatography, 2',5'-ADP Sepharose column chromatography, and Superdex 200 gel filtration Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2 L-arginine + 3 NADPH + 3 H+ + 4 O2
-
Homo sapiens 2 citrulline + 2 nitric oxide + 3 NADP+ + 4 H2O
-
?

Synonyms

Synonyms Comment Organism
endothelial nitric oxide synthase
-
Homo sapiens
eNOS
-
Homo sapiens
neuronal nitric oxide synthase
-
Homo sapiens
nNOS
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000085
-
N1-[cis-4'-[(6''-amino-4''-methylpyridin-2''-yl)methyl]pyrrolidin-3'-yl]-N2-(4'-chlorobenzyl)ethane-1,2-diamine wild type nNOS Homo sapiens
0.0001
-
L-Nomega-nitroarginine-(4R)-amino-L-proline amide wild type nNOS Homo sapiens
0.00015
-
(4S)-N-(4-amino-5-[aminoethyl]aminopentyl)-N''-nitroguanidine wild type nNOS Homo sapiens
0.00025
-
N1-[trans-4'-[(6''-amino-4''-methylpyridin-2''-yl)methyl]pyrrolidin-3'-yl]-N2-(3'-chlorobenzyl)ethane-1,2-diamine wild type nNOS Homo sapiens
0.0003
-
L-Nomega-nitroarginine-2,4-L-diaminobutyramide wild type nNOS Homo sapiens
0.000388
-
N1-[cis-4'-[(6''-aminopyridin-2''-yl)methyl]pyrrolidin-3'-yl]ethane-1,2-diamine wild type nNOS Homo sapiens
0.0012
-
N1-[cis-4'-[(6''-amino-4''-methylpyridin-2''-yl)methyl]pyrrolidin-3'-yl]-N2-(4'-chlorobenzyl)ethane-1,2-diamine mutant nNOS D597N/M336V Homo sapiens
0.0061
-
N1-[trans-4'-[(6''-amino-4''-methylpyridin-2''-yl)methyl]pyrrolidin-3'-yl]-N2-(3'-chlorobenzyl)ethane-1,2-diamine mutant nNOS D597N/M336V Homo sapiens
0.0094
-
3-[cis-4'-[(6''-aminopyridin-2''-yl)methyl]pyrrolidin-3'-ylamino]propan-1-ol wild type nNOS Homo sapiens
0.0367
-
N1-[cis-4'-[(6''-aminopyridin-2''-yl)methyl]pyrrolidin-3'-yl]ethane-1,2-diamine mutant nNOS D597N/M336V Homo sapiens
0.0492
-
3-[cis-4'-[(6''-aminopyridin-2''-yl)methyl]pyrrolidin-3'-ylamino]propan-1-ol mutant nNOS D597N/M336V Homo sapiens
0.08
-
(4S)-N-(4-amino-5-[aminoethyl]aminopentyl)-N''-nitroguanidine wild type eNOS Homo sapiens
0.0852
-
N1-[cis-4'-[(6''-amino-4''-methylpyridin-2''-yl)methyl]pyrrolidin-3'-yl]-N2-(4'-chlorobenzyl)ethane-1,2-diamine wild type eNOS Homo sapiens
0.0952
-
N1-[trans-4'-[(6''-amino-4''-methylpyridin-2''-yl)methyl]pyrrolidin-3'-yl]-N2-(3'-chlorobenzyl)ethane-1,2-diamine wild type eNOS Homo sapiens
0.107
-
L-Nomega-nitroarginine-2,4-L-diaminobutyramide wild type eNOS Homo sapiens
0.11
-
L-Nomega-nitroarginine-(4R)-amino-L-proline amide wild type eNOS Homo sapiens
0.3666
-
3-[cis-4'-[(6''-aminopyridin-2''-yl)methyl]pyrrolidin-3'-ylamino]propan-1-ol wild type eNOS Homo sapiens
0.4167
-
N1-[cis-4'-[(6''-aminopyridin-2''-yl)methyl]pyrrolidin-3'-yl]ethane-1,2-diamine wild type eNOS Homo sapiens