| Autor: |
Kate L, Wegener, Amy E, McGrath, Nicholas E, Dixon, Aaron J, Oakley, Denis B, Scanlon, Andrew D, Abell, John B, Bruning |
| Rok vydání: |
2018 |
| Předmět: |
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| Zdroj: |
Chemistry (Weinheim an der Bergstrasse, Germany). 24(44) |
| ISSN: |
1521-3765 |
| Popis: |
The human sliding clamp (PCNA) controls access to DNA for many proteins involved in DNA replication and repair. Proteins are recruited to the PCNA surface by means of a short, conserved peptide motif known as the PCNA-interacting protein box (PIP-box). Inhibitors of these essential protein-protein interactions may be useful as cancer therapeutics by disrupting DNA replication and repair in these highly proliferative cells. PIP-box peptide mimetics have been identified as a potentially rapid route to potent PCNA inhibitors. Here we describe the rational design and synthesis of the first PCNA peptidomimetic ligands, based on the high affinity PIP-box sequence from the natural PCNA inhibitor p21. These mimetics incorporate covalent i,i+4 side-chain/side-chain lactam linkages of different lengths, designed to constrain the peptides into the 3 |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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