1hkn
From Proteopedia
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| - | [[Image:1hkn.gif|left|200px]]<br /><applet load="1hkn" size=" | + | [[Image:1hkn.gif|left|200px]]<br /><applet load="1hkn" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="1hkn, resolution 2.00Å" /> | caption="1hkn, resolution 2.00Å" /> | ||
'''A COMPLEX BETWEEN ACIDIC FIBROBLAST GROWTH FACTOR AND 5-AMINO-2-NAPHTHALENESULFONATE'''<br /> | '''A COMPLEX BETWEEN ACIDIC FIBROBLAST GROWTH FACTOR AND 5-AMINO-2-NAPHTHALENESULFONATE'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1HKN is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with N2M as [http://en.wikipedia.org/wiki/ligand ligand]. Known structural/functional Site: <scene name='pdbsite=AC1:N2m Binding Site For Chain D'>AC1</scene>. Full crystallographic information is available from [http:// | + | 1HKN is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=N2M:'>N2M</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Known structural/functional Site: <scene name='pdbsite=AC1:N2m+Binding+Site+For+Chain+D'>AC1</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1HKN OCA]. |
==Reference== | ==Reference== | ||
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[[Category: mitogen]] | [[Category: mitogen]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Feb 3 09:49:56 2008'' |
Revision as of 07:49, 3 February 2008
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A COMPLEX BETWEEN ACIDIC FIBROBLAST GROWTH FACTOR AND 5-AMINO-2-NAPHTHALENESULFONATE
Contents |
Overview
Inhibition of angiogenesis-promoting factors such as fibroblast growth, factors is considered to be a potential procedure for inhibiting solid, tumor growth. Although several peptide-based inhibitors are currently, under study, the development of antiangiogenic compounds of small, molecular size is a pharmacological goal of considerable interest. We have, already shown that certain naphthalene sulfonates constitute minimal, functional substitutes of the antiangiogenic compounds of the suramin and, suradista family. Using those data as a lead, we have carried out a, rational search for new angiogenesis inhibitors that could provide new, pharmacological insights for the development of antiangiogenic treatments., The results of the study strongly underline the relevance of the, stereochemistry for an efficient inhibition of acidic fibroblast growth, factor mitogenic activity by the naphthalene sulfonate family and allow us, to formulate rules to aid in searching for new inhibitors and, pharmaceutical developments. To provide further leads for such, developments and acquire a detailed insight into the basis of the, inhibitory activity of the naphthalene sulfonate derivatives, we solved, the three-dimensional structure of acidic fibroblast growth factor, complexed to 5-amino-2-naphthalenesulfonate, the most pharmacologically, promising of the identified inhibitors. The structure shows that binding, of this compound would hamper the interaction of acidic fibroblast growth, factor with the different components of the cell membrane, mitogenesis-triggering complex.
Disease
Known diseases associated with this structure: Aplasia of lacrimal and salivary glands OMIM:[602115], LADD syndrome OMIM:[602115]
About this Structure
1HKN is a Single protein structure of sequence from Homo sapiens with as ligand. Known structural/functional Site: . Full crystallographic information is available from OCA.
Reference
Leads for development of new naphthalenesulfonate derivatives with enhanced antiangiogenic activity: crystal structure of acidic fibroblast growth factor in complex with 5-amino-2-naphthalene sulfonate., Fernandez-Tornero C, Lozano RM, Redondo-Horcajo M, Gomez AM, Lopez JC, Quesada E, Uriel C, Valverde S, Cuevas P, Romero A, Gimenez-Gallego G, J Biol Chem. 2003 Jun 13;278(24):21774-81. Epub 2003 Apr 3. PMID:12676958
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