Proteins > Nitric oxide synthase, inducible
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Nitric oxide synthase, inducible
A nitric oxide synthase, inducible that is encoded in the genome of human. [PRO:WCB, UniProtKB:P35228]
Synonyms
EC 1.14.13.39;
Hepatocyte NOS;
HEP-NOS;
Inducible NO synthase;
Inducible NOS;
iNOS;
NOS type II;
Peptidyl-cysteine S-nitrosylase NOS2
Research
Bioassay Publications (39)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 5 (12.82) | 18.2507 |
| 2000's | 26 (66.67) | 29.6817 |
| 2010's | 6 (15.38) | 24.3611 |
| 2020's | 2 (5.13) | 2.80 |
Compounds (34)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drugs with Other Measurements
[no title available]Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
Antiglioma Activity of Aryl and Amido-Aryl Acetamidine Derivatives Targeting iNOS: Synthesis and Biological Evaluation.ACS medicinal chemistry letters, , Jul-09, Volume: 11, Issue:7, 2020
Synthesis, biological evaluation, and docking studies of N-substituted acetamidines as selective inhibitors of inducible nitric oxide synthase.Journal of medicinal chemistry, , Mar-12, Volume: 52, Issue:5, 2009
Anchored plasticity opens doors for selective inhibitor design in nitric oxide synthase.Nature chemical biology, , Volume: 4, Issue:11, 2008
Structure-activity relationships of potent, selective inhibitors of neuronal nitric oxide synthase based on the 6-phenyl-2-aminopyridine structure.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
2-aminopyridines as highly selective inducible nitric oxide synthase inhibitors. Differential binding modes dependent on nitrogen substitution.Journal of medicinal chemistry, , Jun-03, Volume: 47, Issue:12, 2004
Substituted 2-aminopyridines as inhibitors of nitric oxide synthases.Bioorganic & medicinal chemistry letters, , Sep-04, Volume: 10, Issue:17, 2000
Fluorinated indazoles as novel selective inhibitors of nitric oxide synthase (NOS): synthesis and biological evaluation.Bioorganic & medicinal chemistry, , Sep-01, Volume: 17, Issue:17, 2009
New 2-bromomethyl-8-substituted-benzo[c]chromen-6-ones. Synthesis and biological properties.Bioorganic & medicinal chemistry letters, , Jan-03, Volume: 15, Issue:1, 2005
1,2-Dihydro-4-quinazolinamines: potent, highly selective inhibitors of inducible nitric oxide synthase which show antiinflammatory activity in vivo.Journal of medicinal chemistry, , Mar-13, Volume: 46, Issue:6, 2003
3,4-Dihydro-1-isoquinolinamines: a novel class of nitric oxide synthase inhibitors with a range of isoform selectivity and potency.Bioorganic & medicinal chemistry letters, , Apr-23, Volume: 11, Issue:8, 2001
Substituted 2-aminopyridines as inhibitors of nitric oxide synthases.Bioorganic & medicinal chemistry letters, , Sep-04, Volume: 10, Issue:17, 2000
4,4-Difluorinated analogues of l-arginine and N(G)-hydroxy-l-arginine as mechanistic probes for nitric oxide synthase.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 19, Issue:6, 2009
Reductive heme-dependent activation of the n-oxide prodrug AQ4N by nitric oxide synthase.Journal of medicinal chemistry, , Aug-28, Volume: 51, Issue:16, 2008
N(G)-aminoguanidines from primary amines and the preparation of nitric oxide synthase inhibitors.Journal of medicinal chemistry, , Feb-28, Volume: 51, Issue:4, 2008
N-hydroxyl derivatives of guanidine based drugs as enzymatic NO donors.Bioorganic & medicinal chemistry letters, , Sep-03, Volume: 11, Issue:17, 2001
1,2-Dihydro-4-quinazolinamines: potent, highly selective inhibitors of inducible nitric oxide synthase which show antiinflammatory activity in vivo.Journal of medicinal chemistry, , Mar-13, Volume: 46, Issue:6, 2003
Dihydroquinolines with amine-containing side chains as potent n-NOS inhibitors.Bioorganic & medicinal chemistry letters, , Jun-16, Volume: 13, Issue:12, 2003
Dihydroquinolines as novel n-NOS inhibitors.Bioorganic & medicinal chemistry letters, , Sep-16, Volume: 12, Issue:18, 2002
3,4-Dihydro-1-isoquinolinamines: a novel class of nitric oxide synthase inhibitors with a range of isoform selectivity and potency.Bioorganic & medicinal chemistry letters, , Apr-23, Volume: 11, Issue:8, 2001
1,2,3,4-tetrahydroquinoline-based selective human neuronal nitric oxide synthase (nNOS) inhibitors: lead optimization studies resulting in the identification of N-(1-(2-(methylamino)ethyl)-1,2,3,4-tetrahydroquinolin-6-yl)thiophene-2-carboximidamide as a pJournal of medicinal chemistry, , Mar-22, Volume: 55, Issue:6, 2012
NOpiates: Novel Dual Action Neuronal Nitric Oxide Synthase Inhibitors with μ-Opioid Agonist Activity.ACS medicinal chemistry letters, , Mar-08, Volume: 3, Issue:3, 2012
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
Dihydroquinolines with amine-containing side chains as potent n-NOS inhibitors.Bioorganic & medicinal chemistry letters, , Jun-16, Volume: 13, Issue:12, 2003
Thienopyridines: nitric oxide synthase inhibitors with potent in vivo activity.Bioorganic & medicinal chemistry letters, , Apr-23, Volume: 11, Issue:8, 2001
3,4-Dihydro-1-isoquinolinamines: a novel class of nitric oxide synthase inhibitors with a range of isoform selectivity and potency.Bioorganic & medicinal chemistry letters, , Apr-23, Volume: 11, Issue:8, 2001
Inhibition of inducible nitric oxide synthase by acetamidine derivatives of hetero-substituted lysine and homolysine.Bioorganic & medicinal chemistry letters, , Mar-20, Volume: 10, Issue:6, 2000
Substituted 2-aminopyridines as inhibitors of nitric oxide synthases.Bioorganic & medicinal chemistry letters, , Sep-04, Volume: 10, Issue:17, 2000
2-Iminopyrrolidines as potent and selective inhibitors of human inducible nitric oxide synthase.Journal of medicinal chemistry, , Sep-10, Volume: 41, Issue:19, 1998
N-Phenylamidines as selective inhibitors of human neuronal nitric oxide synthase: structure-activity studies and demonstration of in vivo activity.Journal of medicinal chemistry, , Jul-16, Volume: 41, Issue:15, 1998
Synthesis and evaluation of two positron-labeled nitric oxide synthase inhibitors, S-[11C]methylisothiourea and S-(2-[18F]fluoroethyl)isothiourea, as potential positron emission tomography tracers.Journal of medicinal chemistry, , Dec-20, Volume: 39, Issue:26, 1996
N(delta)-Methylated L-arginine derivatives and their effects on the nitric oxide generating system.Bioorganic & medicinal chemistry, , Mar-01, Volume: 16, Issue:5, 2008
2-Iminopiperidine and other 2-iminoazaheterocycles as potent inhibitors of human nitric oxide synthase isoforms.Journal of medicinal chemistry, , Feb-02, Volume: 39, Issue:3, 1996
Dihydroquinolines with amine-containing side chains as potent n-NOS inhibitors.Bioorganic & medicinal chemistry letters, , Jun-16, Volume: 13, Issue:12, 2003
Dihydroquinolines as novel n-NOS inhibitors.Bioorganic & medicinal chemistry letters, , Sep-16, Volume: 12, Issue:18, 2002
2-Iminopyrrolidines as potent and selective inhibitors of human inducible nitric oxide synthase.Journal of medicinal chemistry, , Sep-10, Volume: 41, Issue:19, 1998
N-Phenylamidines as selective inhibitors of human neuronal nitric oxide synthase: structure-activity studies and demonstration of in vivo activity.Journal of medicinal chemistry, , Jul-16, Volume: 41, Issue:15, 1998
Novel nanomolar imidazo[4,5-b]pyridines as selective nitric oxide synthase (iNOS) inhibitors: SAR and structural insights.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 21, Issue:14, 2011
Discovery of a series of aminopiperidines as novel iNOS inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 18, Issue:1, 2008
5-Fluorinated L-lysine analogues as selective induced nitric oxide synthase inhibitors.Journal of medicinal chemistry, , Feb-12, Volume: 47, Issue:4, 2004
Synthesis of analogs of (1,4)-3- and 5-imino oxazepane, thiazepane, and diazepane as inhibitors of nitric oxide synthases.Bioorganic & medicinal chemistry letters, , Dec-06, Volume: 14, Issue:23, 2004
2-aminopyridines as highly selective inducible nitric oxide synthase inhibitors. Differential binding modes dependent on nitrogen substitution.Journal of medicinal chemistry, , Jun-03, Volume: 47, Issue:12, 2004
Evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2-imines as inhibitors of nitric oxide synthase.Bioorganic & medicinal chemistry letters, , Sep-06, Volume: 14, Issue:17, 2004
1,2-Dihydro-4-quinazolinamines: potent, highly selective inhibitors of inducible nitric oxide synthase which show antiinflammatory activity in vivo.Journal of medicinal chemistry, , Mar-13, Volume: 46, Issue:6, 2003
3,4-Dihydro-1-isoquinolinamines: a novel class of nitric oxide synthase inhibitors with a range of isoform selectivity and potency.Bioorganic & medicinal chemistry letters, , Apr-23, Volume: 11, Issue:8, 2001
Substituted 2-aminopyridines as inhibitors of nitric oxide synthases.Bioorganic & medicinal chemistry letters, , Sep-04, Volume: 10, Issue:17, 2000
Acetamidine lysine derivative, N-(5(S)-amino-6,7-dihydroxyheptyl)ethanimidamide dihydrochloride: a highly selective inhibitor of human inducible nitric oxide synthase.Journal of medicinal chemistry, , Mar-12, Volume: 41, Issue:6, 1998
2-Iminopiperidine and other 2-iminoazaheterocycles as potent inhibitors of human nitric oxide synthase isoforms.Journal of medicinal chemistry, , Feb-02, Volume: 39, Issue:3, 1996
Heteroalicyclic carboxamidines as inhibitors of inducible nitric oxide synthase; the identification of (2R)-2-pyrrolidinecarboxamidine as a potent and selective haem-co-ordinating inhibitor.Bioorganic & medicinal chemistry letters, , May-15, Volume: 21, Issue:10, 2011
Novel nanomolar imidazo[4,5-b]pyridines as selective nitric oxide synthase (iNOS) inhibitors: SAR and structural insights.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 21, Issue:14, 2011
Discovery of a series of aminopiperidines as novel iNOS inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 18, Issue:1, 2008
2-aminopyridines as highly selective inducible nitric oxide synthase inhibitors. Differential binding modes dependent on nitrogen substitution.Journal of medicinal chemistry, , Jun-03, Volume: 47, Issue:12, 2004
Inhibition of inducible nitric oxide synthase by acetamidine derivatives of hetero-substituted lysine and homolysine.Bioorganic & medicinal chemistry letters, , Mar-20, Volume: 10, Issue:6, 2000
Enables
This protein enables 11 target(s):
| Target | Category | Definition |
|---|
| nitric-oxide synthase activity | molecular function | Catalysis of the reaction: L-arginine + n NADPH + n H+ + m O2 = citrulline + nitric oxide + n NADP+. [EC:1.14.13.39, RHEA:19897] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| calmodulin binding | molecular function | Binding to calmodulin, a calcium-binding protein with many roles, both in the calcium-bound and calcium-free states. [GOC:krc] |
| FMN binding | molecular function | Binding to flavin mono nucleotide. Flavin mono nucleotide (FMN) is the coenzyme or the prosthetic group of various flavoprotein oxidoreductase enzymes. [GOC:tb] |
| heme binding | molecular function | Binding to a heme, a compound composed of iron complexed in a porphyrin (tetrapyrrole) ring. [GOC:ai] |
| tetrahydrobiopterin binding | molecular function | Binding to a tetrahydrobiopterin, 5,6,7,8-tetrahydrobiopterin or a derivative thereof; tetrahydrobiopterins are enzyme cofactors that carry electrons in redox reactions. [GOC:BHF, GOC:mah, GOC:rl] |
| arginine binding | molecular function | Binding to 2-amino-5-(carbamimidamido)pentanoic acid. [GOC:BHF, GOC:rl] |
| protein homodimerization activity | molecular function | Binding to an identical protein to form a homodimer. [GOC:jl] |
| metal ion binding | molecular function | Binding to a metal ion. [GOC:ai] |
| flavin adenine dinucleotide binding | molecular function | Binding to FAD, flavin-adenine dinucleotide, the coenzyme or the prosthetic group of various flavoprotein oxidoreductase enzymes, in either the oxidized form, FAD, or the reduced form, FADH2. [GOC:ai, GOC:imk, ISBN:0198506732] |
| NADP binding | molecular function | Binding to nicotinamide-adenine dinucleotide phosphate, a coenzyme involved in many redox and biosynthetic reactions; binding may be to either the oxidized form, NADP+, or the reduced form, NADPH. [GOC:ai] |
Located In
This protein is located in 8 target(s):
| Target | Category | Definition |
|---|
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
| nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| peroxisome | cellular component | A small organelle enclosed by a single membrane, and found in most eukaryotic cells. Contains peroxidases and other enzymes involved in a variety of metabolic processes including free radical detoxification, lipid catabolism and biosynthesis, and hydrogen peroxide metabolism. [GOC:pm, PMID:9302272, UniProtKB-KW:KW-0576] |
| peroxisomal matrix | cellular component | The volume contained within the membranes of a peroxisome; in many cells the matrix contains a crystalloid core largely composed of urate oxidase. [GOC:curators, ISBN:0815316194] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
| cortical cytoskeleton | cellular component | The portion of the cytoskeleton that lies just beneath the plasma membrane. [GOC:mah] |
| perinuclear region of cytoplasm | cellular component | Cytoplasm situated near, or occurring around, the nucleus. [GOC:jid] |
Active In
This protein is active in 3 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
Involved In
This protein is involved in 31 target(s):
| Target | Category | Definition |
|---|
| response to hypoxia | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus indicating lowered oxygen tension. Hypoxia, defined as a decline in O2 levels below normoxic levels of 20.8 - 20.95%, results in metabolic adaptation at both the cellular and organismal level. [GOC:hjd] |
| positive regulation of leukocyte mediated cytotoxicity | biological process | Any process that activates or increases the frequency, rate or extent of leukocyte mediated cytotoxicity. [GOC:add, ISBN:0781735149, PMID:11911826] |
| innate immune response in mucosa | biological process | Any process of the innate immune response that takes place in the mucosal tissues. [GOC:add, PMID:10719665, PMID:15971105] |
| arginine catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of arginine, 2-amino-5-(carbamimidamido)pentanoic acid. [GOC:go_curators] |
| superoxide metabolic process | biological process | The chemical reactions and pathways involving superoxide, the superoxide anion O2- (superoxide free radical), or any compound containing this species. [GOC:jl] |
| nitric oxide biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of nitric oxide, nitrogen monoxide (NO), a colorless gas only slightly soluble in water. [GOC:ai] |
| circadian rhythm | biological process | Any biological process in an organism that recurs with a regularity of approximately 24 hours. [GOC:bf, GOC:go_curators] |
| response to bacterium | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus from a bacterium. [GOC:hb] |
| negative regulation of gene expression | biological process | Any process that decreases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018] |
| peptidyl-cysteine S-nitrosylation | biological process | The covalent addition of a nitric oxide (NO) group to the sulphur (S) atom of a cysteine residue in a protein, to form peptidyl-S-nitrosyl-L-cysteine. [RESID:AA0230] |
| prostaglandin secretion | biological process | The regulated release of a prostaglandin, any of a group of biologically active metabolites which contain a cyclopentane ring, from a cell or a tissue. [GOC:mah] |
| positive regulation of interleukin-6 production | biological process | Any process that activates or increases the frequency, rate, or extent of interleukin-6 production. [GOC:mah] |
| positive regulation of interleukin-8 production | biological process | Any process that activates or increases the frequency, rate, or extent of interleukin-8 production. [GOC:mah] |
| regulation of cell population proliferation | biological process | Any process that modulates the frequency, rate or extent of cell proliferation. [GOC:jl] |
| negative regulation of protein catabolic process | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of protein catabolic process. [GO_REF:0000058, GOC:kmv, GOC:obol, GOC:TermGenie, PMID:24785082] |
| defense response to bacterium | biological process | Reactions triggered in response to the presence of a bacterium that act to protect the cell or organism. [GOC:jl] |
| regulation of cellular respiration | biological process | Any process that modulates the frequency, rate or extent of cellular respiration, the enzymatic release of energy from organic compounds. [GOC:jl] |
| cell redox homeostasis | biological process | Any process that maintains the redox environment of a cell or compartment within a cell. [GOC:ai, GOC:dph, GOC:tb] |
| regulation of insulin secretion | biological process | Any process that modulates the frequency, rate or extent of the regulated release of insulin. [GOC:ai] |
| defense response to Gram-negative bacterium | biological process | Reactions triggered in response to the presence of a Gram-negative bacterium that act to protect the cell or organism. [GOC:ai] |
| positive regulation of killing of cells of another organism | biological process | Any process that activates or increases the frequency, rate or extent of the killing by an organism of cells in another organism. [GOC:ai] |
| cellular response to lipopolysaccharide | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a lipopolysaccharide stimulus; lipopolysaccharide is a major component of the cell wall of gram-negative bacteria. [GOC:mah] |
| cellular response to type II interferon | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an interferon-gamma stimulus. Interferon gamma is the only member of the type II interferon found so far. [GOC:mah] |
| cellular response to xenobiotic stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus from a xenobiotic, a compound foreign to the organism exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:krc, GOC:mah] |
| regulation of cytokine production involved in inflammatory response | biological process | Any process that modulates the frequency, rate or extent of cytokine production involved in inflammatory response. [GOC:TermGenie] |
| negative regulation of blood pressure | biological process | Any process in which the force of blood traveling through the circulatory system is decreased. [GOC:go_curators, GOC:mtg_cardio] |
| response to hormone | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a hormone stimulus. [GOC:jl] |
| nitric oxide mediated signal transduction | biological process | An intracellular signaling cassette that starts with production of nitric oxide, detection by receptors/sensors for nitric oxide (such as soluble guanylyl cyclase/sGC) and ends with the activation of downstream effectors that further transmit the signal within the cell. Nitric oxide transmits its downstream effects through either cyclic GMP (cGMP)-dependent or independent mechanisms. [GOC:jl, PMID:21549190] |
| response to lipopolysaccharide | biological process | Any process that results in a change in state or activity of an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a lipopolysaccharide stimulus; lipopolysaccharide is a major component of the cell wall of gram-negative bacteria. [GOC:add, ISBN:0721601464] |
| inflammatory response | biological process | The immediate defensive reaction (by vertebrate tissue) to infection or injury caused by chemical or physical agents. The process is characterized by local vasodilation, extravasation of plasma into intercellular spaces and accumulation of white blood cells and macrophages. [GO_REF:0000022, ISBN:0198506732] |
| positive regulation of guanylate cyclase activity | biological process | Any process that activates or increases the frequency, rate or extent of guanylate cyclase activity. [GOC:mah] |