Charlotte Mary Griffiths-Jones

TL;DR: This work resulted in a promising lead compound which exhibits tight and selective binding to KEAP1, and activates the NRF2 antioxidant response in cellular and in vivo models, thereby providing a high quality chemical probe to explore the therapeutic potential of disrupting theKEAP1-NRF2 interaction.

TL;DR: In this article, the authors describe the use of new bicyclic heterocyclic derivative compounds in the treatment of diseases, e.g. cancer, and their use in pharmaceutical compositions.

TL;DR: Structural-based drug design guided by structural information from X-ray crystallography, computational studies, and NMR solution conformational analysis was successfully applied to a fragment-derived lead resulting in AT-IAP, a potent, orally bioavailable, dual antagonist of XIAP and cIAP1 and a structurally novel chemical probe for IAP biology.

TL;DR: A detailed account of the medicinal chemistry campaign leading to the KEAP1-NRF2 molecule is presented, which included exploration and optimization of protein-ligand interactions in three energetic "hot spots" identified by fragment screening.

TL;DR: In this article, the authors proposed new bicyclic heterocyclic derivative compounds of Formula (I), which are inhibitors of FGFR, VEGFR or PDGFR.