1y8e

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VCP:Suramin Complex

File:1y8e.gif


1y8e, resolution 2.2Å

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OverviewOverview

Suramin is a competitive inhibitor of heparin binding to many proteins, including viral envelope proteins, protein tyrosine phosphatases, and, fibroblast growth factors (FGFs). It has been clinically evaluated as a, potential therapeutic in treatment of cancers caused by unregulated, angiogenesis, triggered by FGFs. Although it has shown clinical promise in, treatment of several cancers, suramin has many undesirable side effects., There is currently no experimental structure that reveals the molecular, interactions responsible for suramin inhibition of heparin binding, which, could be of potential use in structure-assisted design of improved, analogues of suramin. We report the structure of suramin, in complex with, the heparin-binding site of vaccinia virus complement control protein, (VCP), which interacts with heparin in a geometrically similar manner to, many FGFs. The larger than anticipated flexibility of suramin manifested, in this structure, and other details of VCP-suramin interactions, might, provide useful structural information for interpreting interactions of, suramin with many proteins.

About this StructureAbout this Structure

1Y8E is a Single protein structure of sequence from Vaccinia virus with SVR as ligand. Full crystallographic information is available from OCA.

ReferenceReference

Structural basis for antagonism by suramin of heparin binding to vaccinia complement protein., Ganesh VK, Muthuvel SK, Smith SA, Kotwal GJ, Murthy KH, Biochemistry. 2005 Aug 16;44(32):10757-65. PMID:16086578

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OCA, Eric Martz