Article
Targeting Oncogenic Src Homology 2 Domain-Containing Phosphatase 2 (SHP2) by Inhibiting Its Protein-Protein Interactions.
Journal of medicinal chemistry - 11 Nov 2021
Bobone Sara, Pannone Luca, Biondi Barbara, Solman Maja, Flex Elisabetta, Canale Viviana Claudia, Calligari Paolo, De Faveri Chiara, Gandini Tommaso, Quercioli Andrea, Torini Giuseppe, Venditti Martina, Lauri Antonella, Fasano Giulia, Hoeksma Jelmer, Santucci Valerio, Cattani Giada, Bocedi Alessio, Carpentieri Giovanna, Tirelli Valentina, Sanchez Massimo, Peggion Cristina, Formaggio Fernando, den Hertog Jeroen, Martinelli Simone, Bocchinfuso Gianfranco, Tartaglia Marco, Stella Lorenzo
Abstract excerpt
We developed a new class of inhibitors of protein-protein interactions of the SHP2 phosphatase, which is pivotal in cell signaling and represents a central target in the therapy of cancer and rare diseases. Currently available SHP2 inhibitors target the catalytic site or an allosteric pocket but lack specificity or are ineffective for disease-associated SHP2 mutants. Considering that pathogenic lesions cause...
Topics
- Animals
- Binding Sites
- Mutation
- Oncogenes
- Protein Binding
- Protein Tyrosine Phosphatase, Non-Receptor Type 11
- Signal Transduction