CHEMICAL BIOLOGY-Oriented Targeted Therapeutics


Chemical Biology I Targeted Protein Degradation I Covalent Drug I Bioconjugation

Co-crystal structure of EGFR bound to JBJ-09-063

An allosteric inhibitor against the therapy- resistant mutant forms of EGFR in non-small  cell lung cancer. 

C To, T S Beyett, J Jang, W W Feng, M Bahcall, H M Haikala, B H Shin, D E Heppner, J K Rana, B A Leeper, K M Soroko, M J Poitras, P C Gokhale, Y Kobayashi, K Wahid, K J Kurppa, T W Gero, M D Cameron, A Ogino, M Mushajiang, C Xu, Y Zhang, D A Scott, M J Eck, N S Gray, P A Jänne

Nature Cancer (2022) 3, 401-417.

Grapical abstract of the paper, Mutant-Selective Allosteric EGFR Degraders are Effective Against a Broad Range of Drug-Resistant Mutations

Mutant‐Selective Allosteric EGFR Degraders are Effective Against a Broad Range of Drug‐Resistant Mutations.  

J Jang, C To, D J H De Clercq, E Park, C M Ponthier, B H Shin, M Mushajiang, R P Nowak, E S Fischer, M J Eck, P A Jänne,* N S Gray* 

Angew. Chem. Int. Ed. (2020) 59, 14481–14489.

Grapical abstract of the paper, Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor

Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor

C To, J Jang, T Chen, E Park, M Mushajiang, D J H De Clercq, M D Cameron, D E Heppner, A Yang, S E Dahlberg, K-K Wong, M J Eck, N S Gray,* P A Jänne* 

Cancer Discov. (2019) 9, 926-943.