Nature Communications (Nov 2019)
Modulating multi-functional ERK complexes by covalent targeting of a recruitment site in vivo
- Tamer S. Kaoud,
- William H. Johnson,
- Nancy D. Ebelt,
- Andrea Piserchio,
- Diana Zamora-Olivares,
- Sabrina X. Van Ravenstein,
- Jacey R. Pridgen,
- Ramakrishna Edupuganti,
- Rachel Sammons,
- Micael Cano,
- Mangalika Warthaka,
- Matthew Harger,
- Clint D. J. Tavares,
- Jihyun Park,
- Mohamed F. Radwan,
- Pengyu Ren,
- Eric V. Anslyn,
- Kenneth Y. Tsai,
- Ranajeet Ghose,
- Kevin N. Dalby
Affiliations
- Tamer S. Kaoud
- Division of Chemical Biology and Medicinal Chemistry, The University of Texas at Austin
- William H. Johnson
- Division of Chemical Biology and Medicinal Chemistry, The University of Texas at Austin
- Nancy D. Ebelt
- Division of Chemical Biology and Medicinal Chemistry, The University of Texas at Austin
- Andrea Piserchio
- Department of Chemistry and Biochemistry, The City College of New York
- Diana Zamora-Olivares
- Department of Chemistry, The University of Texas at Austin
- Sabrina X. Van Ravenstein
- Division of Chemical Biology and Medicinal Chemistry, The University of Texas at Austin
- Jacey R. Pridgen
- Division of Chemical Biology and Medicinal Chemistry, The University of Texas at Austin
- Ramakrishna Edupuganti
- Division of Chemical Biology and Medicinal Chemistry, The University of Texas at Austin
- Rachel Sammons
- Division of Chemical Biology and Medicinal Chemistry, The University of Texas at Austin
- Micael Cano
- Division of Chemical Biology and Medicinal Chemistry, The University of Texas at Austin
- Mangalika Warthaka
- Division of Chemical Biology and Medicinal Chemistry, The University of Texas at Austin
- Matthew Harger
- Biomedical Engineering Department, The University of Texas at Austin
- Clint D. J. Tavares
- Department of Cancer Biology, Dana-Farber Cancer Institute and Department of Cell Biology, Harvard Medical School
- Jihyun Park
- The University of Texas MD Anderson Cancer Center
- Mohamed F. Radwan
- Department of Pharmaceutical Chemistry, Faculty of Pharmacy, King Abdulaziz University
- Pengyu Ren
- Biomedical Engineering Department, The University of Texas at Austin
- Eric V. Anslyn
- Department of Chemistry, The University of Texas at Austin
- Kenneth Y. Tsai
- Moffitt Cancer Center
- Ranajeet Ghose
- Department of Chemistry and Biochemistry, The City College of New York
- Kevin N. Dalby
- Division of Chemical Biology and Medicinal Chemistry, The University of Texas at Austin
- DOI
- https://doi.org/10.1038/s41467-019-12996-8
- Journal volume & issue
-
Vol. 10,
no. 1
pp. 1 – 15
Abstract
The ERK signalling pathway is activated in many cancers, however ERK1 and ERK2 are difficult to target pharmacologically. Here, the authors identify a small molecule inhibitor that binds covalently to the D-recruitment site of ERK and induces cell death and reduces tumour growth in mice.
