1. Academic Validation
  2. Discovery of Novel KRAS-PDEδ Inhibitors by Fragment-Based Drug Design

Discovery of Novel KRAS-PDEδ Inhibitors by Fragment-Based Drug Design

  • J Med Chem. 2018 Mar 22;61(6):2604-2610. doi: 10.1021/acs.jmedchem.8b00057.
Long Chen 1 Chunlin Zhuang 1 Junjie Lu 1 Yan Jiang 1 Chunquan Sheng 1
Affiliations

Affiliation

  • 1 School of Pharmacy , Second Military Medical University , 325 Guohe Road , Shanghai 200433 , China.
Abstract

Targeting KRAS-PDEδ protein-protein interactions with small molecules represents a promising opportunity for developing novel antitumor agents. However, current KRAS-PDEδ inhibitors are limited by poor cellular antitumor potency and the druggability of the target remains to be validated by new inhibitors. To tackle these challenges, herein, novel, highly potent KRAS-PDEδ inhibitors were identified by fragment-based drug design, providing promising lead compounds or chemical probes for investigating the biological functions and druggability of KRAS-PDEδ interaction.

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