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Investigation of the PDZ domain ligand binding site using chemically modified peptides.

Abstract：

:Several chemically modified analogues to a tightly binding ligand for the second PDZ domain of MAGI-3 were synthesized and evaluated for their ability to compete with native peptide ligands. N-methyl scanning of the ligand backbone amides revealed the energetically important hydrogen bonds between the ligand backbone and the PDZ domain. Analogues to the ligand's conserved threonine/serine(-2) residue, involved in a side chain to side chain hydrogen bond with a conserved histidine in the PDZ domain, revealed that the interaction is highly sensitive to the steric structure around the hydroxyl group of this residue. Analogues of the ligand carboxy terminus revealed that the full hydrogen bond network of the GLGF loop is important in ligand binding.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Novak KA,Fujii N,Guy RK

doi

10.1016/s0960-894x(02)00345-1

subject

Has Abstract

pub_date

2002-09-02 00:00:00

pages

2471-4

issue

17

eissn

0960-894X

issn

1464-3405

pii

S0960894X02003451

journal_volume

12

pub_type

杂志文章

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