Drug Design and Synthesis of First in Class PDZ1 Targeting NHERF1 Inhibitors as Anticancer Agents.
ACS Med Chem Lett
; 10(4): 499-503, 2019 Apr 11.
Article
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| MEDLINE
| ID: mdl-30996786
ABSTRACT
Targeted approaches aiming at modulating NHERF1 activity, rather than its overall expression, would be preferred to preserve the normal functions of this versatile protein. We focused our attention on the NHERF1/PDZ1 domain that governs its membrane recruitment/displacement through a transient phosphorylation switch. We herein report the design and synthesis of novel NHERF1 PDZ1 domain inhibitors. These compounds have potential therapeutic value when used in combination with antagonists of ß-catenin to augment apoptotic death of colorectal cancer cells refractory to currently available Wnt/ß-catenin-targeted agents.
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1
Colección:
01-internacional
Banco de datos:
MEDLINE
Idioma:
En
Revista:
ACS Med Chem Lett
Año:
2019
Tipo del documento:
Article
País de afiliación:
Italia