1rml

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[[Image:1rml.gif|left|200px]]
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{{Seed}}
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[[Image:1rml.png|left|200px]]
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{{STRUCTURE_1rml| PDB=1rml | SCENE= }}
{{STRUCTURE_1rml| PDB=1rml | SCENE= }}
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'''NMR STUDY OF ACID FIBROBLAST GROWTH FACTOR BOUND TO 1,3,6-NAPHTHALENE TRISULPHONATE, 26 STRUCTURES'''
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===NMR STUDY OF ACID FIBROBLAST GROWTH FACTOR BOUND TO 1,3,6-NAPHTHALENE TRISULPHONATE, 26 STRUCTURES===
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==Overview==
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Recent data show that anti-angiogenesis may provide a promising route to treat cancer. Fibroblast growth factors (FGFs) are powerful angiogenic polypeptides, whose mitogenic activity requires the presence of heparin-like compounds. It has been shown that angiogenesis promoted by FGFs on inhibition by monoclonal antibodies and antisense targeting can also inhibit tumour growth. Derivatives of suramin, a polysulfonated binaphthyl urea and binaphthylsulfonated derivatives of distamycin, suradistas, constitute an important group of potential anti-cancer agents. These compounds compete with heparin in forming tight complexes with FGFs. This inhibits the recognition of these growth factors by their tyrosine kinase membrane receptors thereby suppressing their angiogenic activity. Here we show that 1,3,6-naphthalenetrisulfonate, a common chemical function of the suramins and suradistas with the highest anti-angiogenic activity inhibits the mitogenic activity of acidic fibroblast growth factor, and that this inhibition is relieved by increasing concentrations of heparin in the assay. We have also solved the three-dimensional structure in solution of the protein complexed to this compound. The structural data provide clues that may help in understanding the inhibitory effect of suramins and suradistas, and could contribute to the development of new anti-tumoral drugs.
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The line below this paragraph, {{ABSTRACT_PUBMED_9719643}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 9719643 is the PubMed ID number.
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{{ABSTRACT_PUBMED_9719643}}
==About this Structure==
==About this Structure==
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1RML is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1RML OCA].
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1RML is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1RML OCA].
==Reference==
==Reference==
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[[Category: Growth factor]]
[[Category: Growth factor]]
[[Category: Naphthalene]]
[[Category: Naphthalene]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 07:40:27 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 09:51:37 2008''

Revision as of 06:51, 29 July 2008

Image:1rml.png

Template:STRUCTURE 1rml

NMR STUDY OF ACID FIBROBLAST GROWTH FACTOR BOUND TO 1,3,6-NAPHTHALENE TRISULPHONATE, 26 STRUCTURES

Template:ABSTRACT PUBMED 9719643

About this Structure

1RML is a Single protein structure of sequence from Homo sapiens. Full experimental information is available from OCA.

Reference

Solution structure of acidic fibroblast growth factor bound to 1,3, 6-naphthalenetrisulfonate: a minimal model for the anti-tumoral action of suramins and suradistas., Lozano RM, Jimenez M, Santoro J, Rico M, Gimenez-Gallego G, J Mol Biol. 1998 Sep 4;281(5):899-915. PMID:9719643

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