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Literature summary for 3.6.5.5 extracted from

  • Otomo, M.; Takahashi, K.; Miyoshi, H.; Osada, K.; Nakashima, H.; Yamaguchi, N.
    Some selective serotonin reuptake inhibitors inhibit dynamin I guanosine triphosphatase (GTPase) (2008), Biol. Pharm. Bull., 31, 1489-1495.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
L-phosphatidylserine binds the pleckstrin homology domain of dynamin and enhances its GTPase activity Mus musculus
phosphatidylinositol-4,5-bisphosphate binds the pleckstrin homology domain of dynamin and enhances its GTPase activity Mus musculus

Cloned(Commentary)

Cloned (Comment) Organism
His-tagged dynamin I is expressed in Escherichia coli Rosetta2 (DE3) cells Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
(1R,2R)-2-(aminomethyl)-N,N-diethyl-1-phenyl-cyclopropane-1-carboxamide milnacipran Mus musculus
(3S-trans)-3-((1,3-benzodioxol-5-yloxy)methyl)-4-(4-fluorophenyl)-piperidine paroxetine Mus musculus
1,2,3,4,10,14b-hexahydro-2-methyldibenzo[c,f]pyrazino[1,2-a]azepine mianserin Mus musculus
1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro[2]benzofuran-5-carbonitrile citalopram Mus musculus
10,11-dihydro-5-[3-(methylamino)propyl]-5H-dibenz[b,f]azepine desipramine Mus musculus
2-((8-chlorodibenzo(b,f)thiepin-10-yl)oxy)-N,N-dimethylethylamine zotepine Mus musculus
3-(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidene)-N-methyl-1-propanamine nortriptyline Mus musculus
3-(2-chloro-10H-phenothiazin-10-yl)-N,N-dimethyl-propan-1-amine chlorpromazine Mus musculus
3-(5,6-dihydrobenzo[b][1]benzazepin-11-yl)-N,N-dimethylpropan-1-amine imipramine Mus musculus
3-(9-chloro-5,6-dihydrobenzo[b][1]benzazepin-11-yl)-N,N-dimethylpropan-1-amine clomipramine Mus musculus
4-[4-(4-chlorophenyl)-4-hydroxy-1-piperidyl]-1-(4-fluorophenyl)-butan-1-one haloperidol Mus musculus
5H-dibenz[b,f]azepine-5-carboxamide carbamazepine Mus musculus
fluvoxamine a noncompetitive inhibitor of dynamin I with respect to GTP and a competitive inhibitor with respect to L-phosphatidylserine Mus musculus
methyl 2-phenyl-2-(2-piperidyl)acetate methylphenidate Mus musculus
myristyl trimethyl ammonium bromide standard inhibitor of dynamin I Mus musculus
N-(2-diethylaminoethyl)-2-methoxy-5-methylsulfonyl-benzamide tiapride Mus musculus
N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]-propan-1-amine fluoxetine Mus musculus
N-methyl-9,10-ethanoanthracene-9(10H)-propanamine maprotiline Mus musculus
N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-sulfamoyl-benzamide sulpiride Mus musculus
sertraline a mixed type inhibitor with respect to both GTP and L-phosphatidylserine Mus musculus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0253
-
GTP in 10 mM Tris-HCl, 10 mM NaCl, 2 mM Mg2+, at 30°C Mus musculus

Organism

Organism UniProt Comment Textmining
Mus musculus
-
-
-

Purification (Commentary)

Purification (Comment) Organism
TALON metal affinity resin column chromatography and MonoQ column chroamtography Mus musculus

Source Tissue

Source Tissue Comment Organism Textmining
neuron neuronal dynamin I plays a critical role in the recycling of synaptic vesicles, and thus in nervous system function Mus musculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
GTP + H2O
-
Mus musculus GDP + phosphate
-
?

Synonyms

Synonyms Comment Organism
Dyn I
-
Mus musculus
dynamin I GTPase
-
Mus musculus
dynamin I guanosine triphosphatase
-
Mus musculus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0073
-
in 10 mM Tris-HCl, 10 mM NaCl, 2 mM Mg2+, at 30°C Mus musculus sertraline
0.0147
-
in 10 mM Tris-HCl, 10 mM NaCl, 2 mM Mg2+, at 30°C Mus musculus fluvoxamine
0.0211
-
in 10 mM Tris-HCl, 10 mM NaCl, 2 mM Mg2+, at 30°C Mus musculus N-methyl-9,10-ethanoanthracene-9(10H)-propanamine
0.0234
-
in 10 mM Tris-HCl, 10 mM NaCl, 2 mM Mg2+, at 30°C Mus musculus (3S-trans)-3-((1,3-benzodioxol-5-yloxy)methyl)-4-(4-fluorophenyl)-piperidine
0.0241
-
in 10 mM Tris-HCl, 10 mM NaCl, 2 mM Mg2+, at 30°C Mus musculus myristyl trimethyl ammonium bromide
0.0299
-
in 10 mM Tris-HCl, 10 mM NaCl, 2 mM Mg2+, at 30°C Mus musculus 3-(9-chloro-5,6-dihydrobenzo[b][1]benzazepin-11-yl)-N,N-dimethylpropan-1-amine
0.0334
-
in 10 mM Tris-HCl, 10 mM NaCl, 2 mM Mg2+, at 30°C Mus musculus N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]-propan-1-amine
0.0372
-
in 10 mM Tris-HCl, 10 mM NaCl, 2 mM Mg2+, at 30°C Mus musculus 2-[(8-chlorodibenzo[b,f]thiepin-10-yl)oxy]-N,N-dimethylethanamine
0.0472
-
in 10 mM Tris-HCl, 10 mM NaCl, 2 mM Mg2+, at 30°C Mus musculus 3-(2-chloro-10H-phenothiazin-10-yl)-N,N-dimethyl-propan-1-amine
0.064
-
in 10 mM Tris-HCl, 10 mM NaCl, 2 mM Mg2+, at 30°C Mus musculus 3-(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidene)-N-methyl-1-propanamine
0.1
-
IC50 above 0.1 mM, in 10 mM Tris-HCl, 10 mM NaCl, 2 mM Mg2+, at 30°C Mus musculus 4-[4-(4-chlorophenyl)-4-hydroxy-1-piperidyl]-1-(4-fluorophenyl)-butan-1-one
0.1
-
IC50 above 0.1 mM, in 10 mM Tris-HCl, 10 mM NaCl, 2 mM Mg2+, at 30°C Mus musculus N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-sulfamoyl-benzamide
0.1
-
IC50 above 0.1 mM, in 10 mM Tris-HCl, 10 mM NaCl, 2 mM Mg2+, at 30°C Mus musculus N-(2-diethylaminoethyl)-2-methoxy-5-methylsulfonyl-benzamide
0.1
-
IC50 above 0.1 mM, in 10 mM Tris-HCl, 10 mM NaCl, 2 mM Mg2+, at 30°C Mus musculus methyl 2-phenyl-2-(2-piperidyl)acetate
0.1
-
IC50 above 0.1 mM, in 10 mM Tris-HCl, 10 mM NaCl, 2 mM Mg2+, at 30°C Mus musculus 3-(5,6-dihydrobenzo[b][1]benzazepin-11-yl)-N,N-dimethylpropan-1-amine
0.1
-
IC50 above 0.1 mM, in 10 mM Tris-HCl, 10 mM NaCl, 2 mM Mg2+, at 30°C Mus musculus 10,11-dihydro-5-[3-(methylamino)propyl]-5H-dibenz[b,f]azepine
0.1
-
IC50 above 0.1 mM, in 10 mM Tris-HCl, 10 mM NaCl, 2 mM Mg2+, at 30°C Mus musculus 1,2,3,4,10,14b-hexahydro-2-methyldibenzo[c,f]pyrazino[1,2-a]azepine
0.1
-
IC50 above 0.1 mM, in 10 mM Tris-HCl, 10 mM NaCl, 2 mM Mg2+, at 30°C Mus musculus 5H-dibenz[b,f]azepine-5-carboxamide
0.1
-
IC50 above 0.1 mM, in 10 mM Tris-HCl, 10 mM NaCl, 2 mM Mg2+, at 30°C Mus musculus (1R,2R)-2-(aminomethyl)-N,N-diethyl-1-phenyl-cyclopropane-1-carboxamide
0.1
-
IC50 above 0.1 mM, in 10 mM Tris-HCl, 10 mM NaCl, 2 mM Mg2+, at 30°C Mus musculus 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro[2]benzofuran-5-carbonitrile