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| {{STRUCTURE_1bln| PDB=1bln | SCENE= }} | | {{STRUCTURE_1bln| PDB=1bln | SCENE= }} |
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| '''ANTI-P-GLYCOPROTEIN FAB MRK-16'''
| | ===ANTI-P-GLYCOPROTEIN FAB MRK-16=== |
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| ==Overview==
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| Monoclonal antibody MRK-16 recognizes a discontinuous extracellular epitope on the multidrug resistance-associated ATP-binding cassette transporter, P-glycoprotein. The atomic basis for specificity of this antibody is of interest because of its potential as a modulator of P-glycoprotein activity. The crystal structure of Fab MRK-16 is reported to a resolution of 2.8 A. A structure for a portion of the epitope was derived by comparison to regions of solved structures with similar primary sequence. This has permitted a proposal for the mode of binding of the peptide epitope to the antibody, in which the peptide makes specific contacts with complementarity-determining regions H1, H2, and H3 from the heavy chain and L3 from the light chain. These interactions are consistent with epitope mapping studies and with the observation that MRK-16 is specific for human class I P-glycoprotein. This result identifies side chains in MRK-16 that would be amenable to alteration in antibody engineering experiments to derive improved multidrug resistance inhibitors for clinical use during chemotherapy. In particular, Arg-H97 contacts both Glu-746 and Asp-744 of the peptide, Arg-L96 contacts Asp-743, and Thr-H33 interacts with Thr-747. All of these epitope residues were implicated in mediating specificity by epitope mapping studies.
| | The line below this paragraph, {{ABSTRACT_PUBMED_9738009}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 9738009 is the PubMed ID number. |
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| | {{ABSTRACT_PUBMED_9738009}} |
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| ==About this Structure== | | ==About this Structure== |
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| [[Category: Vasudevan, S.]] | | [[Category: Vasudevan, S.]] |
| [[Category: Immunoglobulin]] | | [[Category: Immunoglobulin]] |
| ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 11:40:27 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jun 30 19:21:19 2008'' |