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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
20
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pubmed:dateCreated |
2004-9-16
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pubmed:abstractText |
We previously reported that substrates of semicarbazide-sensitive amine oxidase in combination with low concentrations of vanadate exert potent insulin-like effects. Here we performed homology modeling of the catalytic domain of mouse SSAO/VAP-1 and searched through chemical databases to identify novel SSAO substrates. The modeling of the catalytic domain revealed that aromatic residues Tyr384, Phe389, and Tyr394 define a pocket of stable size that may participate in the binding of apolar substrates. We identified a number of amines as substrates of human, rat, and mouse SSAO. The compounds PD0119035, 2,3-dimethoxy-benzylamine, and C-naphthalen-1-yl-methylamine showed high affinity as substrates of rat SSAO. C-Naphthalen-1-yl-methylamine was the only substrate that showed high affinity for human SSAO. C-Naphthalen-1-yl-methylamine and 4-aminomethyl-benzenesulfonamide showed the highest capacity to stimulate glucose transport in isolated rat adipocytes. The impact of these findings on the development of new treatments for diabetes is discussed.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Amine Oxidase (Copper-Containing),
http://linkedlifedata.com/resource/pubmed/chemical/Amines,
http://linkedlifedata.com/resource/pubmed/chemical/Benzylamines,
http://linkedlifedata.com/resource/pubmed/chemical/Cell Adhesion Molecules,
http://linkedlifedata.com/resource/pubmed/chemical/Glucose,
http://linkedlifedata.com/resource/pubmed/chemical/Insulin,
http://linkedlifedata.com/resource/pubmed/chemical/Methylamines,
http://linkedlifedata.com/resource/pubmed/chemical/Naphthalenes,
http://linkedlifedata.com/resource/pubmed/chemical/Vanadates,
http://linkedlifedata.com/resource/pubmed/chemical/benzylamine,
http://linkedlifedata.com/resource/pubmed/chemical/semicarbazide-sensitive amine...
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
23
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pubmed:volume |
47
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4865-74
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pubmed:dateRevised |
2011-11-17
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pubmed:meshHeading |
pubmed-meshheading:15369390-Adipocytes,
pubmed-meshheading:15369390-Amine Oxidase (Copper-Containing),
pubmed-meshheading:15369390-Amines,
pubmed-meshheading:15369390-Amino Acid Sequence,
pubmed-meshheading:15369390-Animals,
pubmed-meshheading:15369390-Benzylamines,
pubmed-meshheading:15369390-Binding Sites,
pubmed-meshheading:15369390-Biological Transport,
pubmed-meshheading:15369390-Catalytic Domain,
pubmed-meshheading:15369390-Cell Adhesion Molecules,
pubmed-meshheading:15369390-Cells, Cultured,
pubmed-meshheading:15369390-Drug Evaluation, Preclinical,
pubmed-meshheading:15369390-Glucose,
pubmed-meshheading:15369390-Humans,
pubmed-meshheading:15369390-Insulin,
pubmed-meshheading:15369390-Male,
pubmed-meshheading:15369390-Methylamines,
pubmed-meshheading:15369390-Mice,
pubmed-meshheading:15369390-Models, Molecular,
pubmed-meshheading:15369390-Molecular Sequence Data,
pubmed-meshheading:15369390-Naphthalenes,
pubmed-meshheading:15369390-Protein Conformation,
pubmed-meshheading:15369390-Rats,
pubmed-meshheading:15369390-Rats, Wistar,
pubmed-meshheading:15369390-Sequence Homology, Amino Acid,
pubmed-meshheading:15369390-Substrate Specificity,
pubmed-meshheading:15369390-Vanadates
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pubmed:year |
2004
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pubmed:articleTitle |
Exploring the binding mode of semicarbazide-sensitive amine oxidase/VAP-1: identification of novel substrates with insulin-like activity.
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pubmed:affiliation |
Parc Científic de Barcelona and Departament de Bioquímica i Biologia Molecular, Facultat de Biologia, Universitat de Barcelona, Avda. Diagonal 645, E-08028 Barcelona, Spain.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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