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Principles and Pitfalls in Designing Site-directed Peptide Ligands by Dr. A. B. Edmundson; D. L. Harris; Z.-C. Fan; L. W. Guddat; B. T. Schley; B. L. Hanson; G. Tribbick; H. M. Geysen is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

What is Principles and Pitfalls in Designing Site-directed Peptide Ligands about?

## Abstract An immunoglobulin light chain dimer with a large generic binding cavity was used as a host molecule for designing a series of peptide guest ligands. In a screening procedure peptides coupled to solid supports were systematically tested for binding activity by enzyme linked immunosorbent assays (ELISA). Key members of the binding series were synthesized in milligram quantities and diffused into crystals of the host molecule for X‐ray analyses. These peptides were incrementally increased in size and affinity until they nearly filled the cavity. Progressive changes in binding patterns were mapped by comparisons of crystallo‐graphically refined structures of 14 peptide–protein complexes at 2.7 Å resolution. These comparisons led to guidelines for ligand design and also suggested ways to modify previously established binding patterns. By manipulating equilibria involving histidine, for example, it was possible to abolish one important intramolecular interaction of the bound ligand and substitute another. These events triggered a change inconformation of the ligand from a compact to an extended form and a comprehensive change in the mode of binding to the protein. In dipeptid

Who reads Principles and Pitfalls in Designing Site-directed Peptide Ligands?

Author

Dr. A. B. Edmundson; D. L. Harris; Z.-C. Fan; L. W. Guddat; B. T. Schley; B. L. Hanson; G. Tribbick; H. M. Geysen

Publisher

John Wiley and Sons; Wiley (John Wiley & Sons); Wiley-Liss Inc; Wiley (ISSN 0887-3585)

Published

1993

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)