1l7i

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(New page: 200px<br /> <applet load="1l7i" size="450" color="white" frame="true" align="right" spinBox="true" caption="1l7i, resolution 1.80&Aring;" /> '''Crystal Structure o...)
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<applet load="1l7i" size="450" color="white" frame="true" align="right" spinBox="true"
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caption="1l7i, resolution 1.80&Aring;" />
caption="1l7i, resolution 1.80&Aring;" />
'''Crystal Structure of the anti-ErbB2 Fab2C4'''<br />
'''Crystal Structure of the anti-ErbB2 Fab2C4'''<br />
==Overview==
==Overview==
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Shotgun scanning combinatorial mutagenesis was used to study the, antigen-binding site of Fab2C4, a humanized monoclonal antibody fragment, that binds to the extracellular domain of the human oncogene product, ErbB2. Essentially all the residues in the Fab2C4 complementarity, determining regions (CDRs) were alanine-scanned using phage-displayed, libraries that preferentially allowed side-chains to vary as the wild-type, or alanine. A separate homolog-scan was performed using libraries that, allowed side-chains to vary only as the wild-type or a similar amino acid, residue. Following binding selections to isolate functional clones, DNA, sequencing was used to determine the wild-type/mutant ratios at each, varied position, and these ratios were used to assess the contributions of, each side-chain to antigen binding. The alanine-scan revealed that most of, the side-chains that contribute to antigen binding are located in the, heavy chain, and the Fab2C4 three-dimensional structure revealed that, these residues fall into two groups. The first group consists of, solvent-exposed residues which likely make energetically favorable, contacts with the antigen and thus comprise the functional-binding, epitope. The second group consists of buried residues with side-chains, that pack against other CDR residues and apparently act as scaffolding to, maintain the functional epitope in a binding-competent conformation. The, homolog-scan involved subtle mutations, and as a result, only a subset of, the side-chains that were intolerant to alanine substitutions were also, intolerant to homologous substitutions. In particular, the 610 A2, functional epitope surface revealed by alanine-scanning shrunk to only 369, A2 when mapped with homologous substitutions, suggesting that this smaller, subset of side-chains may be involved in more precise contacts with the, antigen. The results validate shotgun scanning as a rapid and accurate, method for determining the functional contributions of individual, side-chains involved in protein-protein interactions.
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Shotgun scanning combinatorial mutagenesis was used to study the antigen-binding site of Fab2C4, a humanized monoclonal antibody fragment that binds to the extracellular domain of the human oncogene product ErbB2. Essentially all the residues in the Fab2C4 complementarity determining regions (CDRs) were alanine-scanned using phage-displayed libraries that preferentially allowed side-chains to vary as the wild-type or alanine. A separate homolog-scan was performed using libraries that allowed side-chains to vary only as the wild-type or a similar amino acid residue. Following binding selections to isolate functional clones, DNA sequencing was used to determine the wild-type/mutant ratios at each varied position, and these ratios were used to assess the contributions of each side-chain to antigen binding. The alanine-scan revealed that most of the side-chains that contribute to antigen binding are located in the heavy chain, and the Fab2C4 three-dimensional structure revealed that these residues fall into two groups. The first group consists of solvent-exposed residues which likely make energetically favorable contacts with the antigen and thus comprise the functional-binding epitope. The second group consists of buried residues with side-chains that pack against other CDR residues and apparently act as scaffolding to maintain the functional epitope in a binding-competent conformation. The homolog-scan involved subtle mutations, and as a result, only a subset of the side-chains that were intolerant to alanine substitutions were also intolerant to homologous substitutions. In particular, the 610 A2 functional epitope surface revealed by alanine-scanning shrunk to only 369 A2 when mapped with homologous substitutions, suggesting that this smaller subset of side-chains may be involved in more precise contacts with the antigen. The results validate shotgun scanning as a rapid and accurate method for determining the functional contributions of individual side-chains involved in protein-protein interactions.
==About this Structure==
==About this Structure==
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1L7I is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with SO4 as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1L7I OCA].
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1L7I is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=SO4:'>SO4</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1L7I OCA].
==Reference==
==Reference==
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Protein complex]]
[[Category: Protein complex]]
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[[Category: Adams, C.W.]]
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[[Category: Adams, C W.]]
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[[Category: Breece, T.N.]]
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[[Category: Breece, T N.]]
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[[Category: Presta, L.G.]]
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[[Category: Presta, L G.]]
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[[Category: Sidhu, S.S.]]
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[[Category: Sidhu, S S.]]
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[[Category: Vajdos, F.F.]]
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[[Category: Vajdos, F F.]]
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[[Category: Vos, A.M.de.]]
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[[Category: Vos, A M.de.]]
[[Category: SO4]]
[[Category: SO4]]
[[Category: fab fragment]]
[[Category: fab fragment]]
[[Category: ig domain]]
[[Category: ig domain]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 17:57:28 2007''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 13:42:10 2008''

Revision as of 11:42, 21 February 2008


1l7i, resolution 1.80Å

Drag the structure with the mouse to rotate

Crystal Structure of the anti-ErbB2 Fab2C4

Overview

Shotgun scanning combinatorial mutagenesis was used to study the antigen-binding site of Fab2C4, a humanized monoclonal antibody fragment that binds to the extracellular domain of the human oncogene product ErbB2. Essentially all the residues in the Fab2C4 complementarity determining regions (CDRs) were alanine-scanned using phage-displayed libraries that preferentially allowed side-chains to vary as the wild-type or alanine. A separate homolog-scan was performed using libraries that allowed side-chains to vary only as the wild-type or a similar amino acid residue. Following binding selections to isolate functional clones, DNA sequencing was used to determine the wild-type/mutant ratios at each varied position, and these ratios were used to assess the contributions of each side-chain to antigen binding. The alanine-scan revealed that most of the side-chains that contribute to antigen binding are located in the heavy chain, and the Fab2C4 three-dimensional structure revealed that these residues fall into two groups. The first group consists of solvent-exposed residues which likely make energetically favorable contacts with the antigen and thus comprise the functional-binding epitope. The second group consists of buried residues with side-chains that pack against other CDR residues and apparently act as scaffolding to maintain the functional epitope in a binding-competent conformation. The homolog-scan involved subtle mutations, and as a result, only a subset of the side-chains that were intolerant to alanine substitutions were also intolerant to homologous substitutions. In particular, the 610 A2 functional epitope surface revealed by alanine-scanning shrunk to only 369 A2 when mapped with homologous substitutions, suggesting that this smaller subset of side-chains may be involved in more precise contacts with the antigen. The results validate shotgun scanning as a rapid and accurate method for determining the functional contributions of individual side-chains involved in protein-protein interactions.

About this Structure

1L7I is a Protein complex structure of sequences from Homo sapiens with as ligand. Full crystallographic information is available from OCA.

Reference

Comprehensive functional maps of the antigen-binding site of an anti-ErbB2 antibody obtained with shotgun scanning mutagenesis., Vajdos FF, Adams CW, Breece TN, Presta LG, de Vos AM, Sidhu SS, J Mol Biol. 2002 Jul 5;320(2):415-28. PMID:12079396

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