Structure-activity exploration of a small-molecule allosteric inhibitor of T790M/L858R double mutant EGFR

• Main Authors: Francesca Foschi (Author), Annachiara Tinivella (Author), Valentina Crippa (Author), Luca Pinzi (Author), Luca Mologni (Author), Daniele Passarella (Author), Giulio Rastelli (Author)
• Format: Book
• Published: Taylor & Francis Group, 2023-12-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

EGFR is a protein kinase whose aberrant activity is frequently involved in the development of non-small lung cancer (NSCLC) drug resistant forms. The allosteric inhibition of this enzyme is currently one among the most attractive approaches to design and develop anticancer drugs. In a previous study...