1hkn: Difference between revisions
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==Overview== | ==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. | 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:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=602115 602115]], LADD syndrome OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=602115 602115]] | |||
==About this Structure== | ==About this Structure== | ||
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[[Category: mitogen]] | [[Category: mitogen]] | ||
''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 17:19:36 2007'' | ||