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Literature summary for 1.4.3.4 extracted from
- Dual-target-directed drugs that block monoamine oxidase B and adenosine A(2A) receptors for Parkinsons disease (2009), Neurotherapeutics, 6, 141-151.
Application
| Application | Comment | Organism |
|---|---|---|
| drug development | dual-target-directed drugs, compounds that inhibit MAO-B and antagonize A2A receptors, may have value in the management of Parkinson's disease, overview | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| (E)-8-(3-chlorostyryl)caffeine | reversible MAO-B inhibitor, a dual-target-directed drug inhibiting MAO-B and antagonizing A2A receptors | Homo sapiens |  |
| (E)-8-(3-chlorostyryl)caffeine | reversible MAO-B inhibitor, a dual-target-directed drug inhibiting MAO-B and antagonizing A2A receptors | Mus musculus | |
| (E)-8-styrylcaffeine | reversible MAO-B inhibitor, a dual-target-directed drug inhibiting MAO-B and antagonizing A2A receptors | Homo sapiens | |
| (E)-8-styrylcaffeine | reversible MAO-B inhibitor, a dual-target-directed drug inhibiting MAO-B and antagonizing A2A receptors | Mus musculus | |
| 2-[(1E,3E)-4-(3-chlorophenyl)buta-1,3-dien-1-yl]-3,5,7-trimethyl-3H-imidazo[4,5-c]pyridine-4,6(5H,7H)-dione | - |
Homo sapiens | |
| 3,5,7-trimethyl-2-[(1E,3E)-4-phenylbuta-1,3-dien-1-yl]-3H-imidazo[4,5-c]pyridine-4,6(5H,7H)-dione | - |
Homo sapiens | |
| 5,7-diethyl-3-methyl-2-[(1E,3E)-4-phenylbuta-1,3-dien-1-yl]-3H-imidazo[4,5-c]pyridine-4,6(5H,7H)-dione | - |
Homo sapiens | |
| Caffeine | a dual-target-directed drug inhibiting MAO-B and antagonizing A2A receptors | Homo sapiens | |
| Caffeine | a dual-target-directed drug inhibiting MAO-B and antagonizing A2A receptors | Mus musculus | |
| KF-17837 | a dual-target-directed drug inhibiting MAO-B and antagonizing A2A receptors | Homo sapiens | |
| KF-17837 | a dual-target-directed drug inhibiting MAO-B and antagonizing A2A receptors | Mus musculus | |
| KW-6002 | a dual-target-directed drug inhibiting MAO-B and antagonizing A2A receptors | Homo sapiens | |
| KW-6002 | a dual-target-directed drug inhibiting MAO-B and antagonizing A2A receptors | Mus musculus | |
| additional information | inhibitors of MAO-B can be adjunctive drugs to levodopa. Neuroprotective and anti-Parkinsonian effects of A2A receptor antogonistic drugs, overview | Homo sapiens | |
| additional information | inhibitors of MAO-B can be adjunctive drugs to levodopa. Neuroprotective and anti-Parkinsonian effects of A2A receptor antogonistic drugs, overview | Mus musculus | |
| [(E)-1,3-dipropyl-7-methyl-8-(2-(3-thienyl)ethenyl)]xanthine | a dual-target-directed drug inhibiting MAO-B and antagonizing A2A receptors | Homo sapiens | |
| [(E)-1,3-dipropyl-7-methyl-8-(2-(3-thienyl)ethenyl)]xanthine | a dual-target-directed drug inhibiting MAO-B and antagonizing A2A receptors | Mus musculus | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine + H2O + O2 | Mus musculus | 1-methyl-4-phenylpyridinium is the ultimate product | ? | - |
? | |
| 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine + H2O + O2 | Homo sapiens | 1-methyl-4-phenylpyridinium is the ultimate product | ? | - |
? | |
| dopamine + H2O + O2 | Mus musculus | - |
(3,4-dihydroxyphenyl)acetaldehyde + NH3 + H2O2 | - |
? | |
| dopamine + H2O + O2 | Homo sapiens | - |
(3,4-dihydroxyphenyl)acetaldehyde + NH3 + H2O2 | - |
? | |
| additional information | Mus musculus | in the catalytic cycle of MAO-B, one mol each of an iminiumyl intermediate that is hydrolyzed to the aldehyde product and H2O2 are produced for each mol of monoamine substrate oxidized. These catabolic products may be neurotoxic if not rapidly inactivated by centrally located aldehyde dehydrogenase and glutathione peroxidase, respectively | ? | - |
? | |
| additional information | Homo sapiens | in the catalytic cycle of MAO-B, one mol each of an iminiumyl intermediate that is hydrolyzed to the aldehyde product and H2O2 are produced for each mol of monoamine substrate oxidized. These catabolic products may be neurotoxic if not rapidly inactivated by centrally located aldehyde dehydrogenase and glutathione peroxidase, respectively | ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | P27338 | - |
- |
| Mus musculus | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| brain | - |
Mus musculus | - |
| brain | age-related increase in MAO-B activity, whereas MAO-A activity remains constant | Homo sapiens | - |
| striatum | - |
Mus musculus | - |
| striatum | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine + H2O + O2 | - |
Mus musculus | ? | - |
? | |
| 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine + H2O + O2 | - |
Homo sapiens | ? | - |
? | |
| 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine + H2O + O2 | 1-methyl-4-phenylpyridinium is the ultimate product | Mus musculus | ? | - |
? | |
| 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine + H2O + O2 | 1-methyl-4-phenylpyridinium is the ultimate product | Homo sapiens | ? | - |
? | |
| dopamine + H2O + O2 | - |
Mus musculus | (3,4-dihydroxyphenyl)acetaldehyde + NH3 + H2O2 | - |
? | |
| dopamine + H2O + O2 | - |
Homo sapiens | (3,4-dihydroxyphenyl)acetaldehyde + NH3 + H2O2 | - |
? | |
| additional information | in the catalytic cycle of MAO-B, one mol each of an iminiumyl intermediate that is hydrolyzed to the aldehyde product and H2O2 are produced for each mol of monoamine substrate oxidized. These catabolic products may be neurotoxic if not rapidly inactivated by centrally located aldehyde dehydrogenase and glutathione peroxidase, respectively | Mus musculus | ? | - |
? | |
| additional information | in the catalytic cycle of MAO-B, one mol each of an iminiumyl intermediate that is hydrolyzed to the aldehyde product and H2O2 are produced for each mol of monoamine substrate oxidized. These catabolic products may be neurotoxic if not rapidly inactivated by centrally located aldehyde dehydrogenase and glutathione peroxidase, respectively | Homo sapiens | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| MAO-B | - |
Mus musculus |
| MAO-B | - |
Homo sapiens |
| monoamine oxidase B | - |
Mus musculus |
| monoamine oxidase B | - |
Homo sapiens |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0000022 | 0.0000045 | KW-6002 | MAO-B | Homo sapiens | |
| 0.00000274 | - |
5,7-diethyl-3-methyl-2-[(1E,3E)-4-phenylbuta-1,3-dien-1-yl]-3H-imidazo[4,5-c]pyridine-4,6(5H,7H)-dione | MAO-B | Homo sapiens | |
| 0.00003 | 0.000081 | (E)-8-(3-chlorostyryl)caffeine | MAO-B | Homo sapiens | |
| 0.000094 | 0.00286 | (E)-8-styrylcaffeine | MAO-B | Homo sapiens | |
| 0.000104 | - |
2-[(1E,3E)-4-(3-chlorophenyl)buta-1,3-dien-1-yl]-3,5,7-trimethyl-3H-imidazo[4,5-c]pyridine-4,6(5H,7H)-dione | MAO-B | Homo sapiens | |
| 0.000149 | 0.000153 | 3,5,7-trimethyl-2-[(1E,3E)-4-phenylbuta-1,3-dien-1-yl]-3H-imidazo[4,5-c]pyridine-4,6(5H,7H)-dione | MAO-B | Homo sapiens | |
| 0.022 | - |
Caffeine | MAO-B | Homo sapiens | |
General Information
| General Information | Comment | Organism |
|---|---|---|
| malfunction | the first step of the bioactivation of the Parkinsonian-inducing pro-neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine, MPTP, is catalyzed by MAO-B, resulting in the ultimate product, 1-methyl-4-phenylpyridinium, a mitochondrial toxin that causes selective degeneration of nigrostriatal dopaminergic neurons in humans and experimental animals | Mus musculus |
| malfunction | the first step of the bioactivation of the Parkinsonian-inducing pro-neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine, MPTP, is catalyzed by MAO-B, resulting in the ultimate product, 1-methyl-4-phenylpyridinium, a mitochondrial toxin that causes selective degeneration of nigrostriatal dopaminergic neurons in humans and experimental animals | Homo sapiens |
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