Natarajan, Amarnath
Mayo Clinic
Eppley Institute for Research in Cancer and Allied Diseases, University of Nebraska Medical Center, Omaha, NE 68198, USA.
Citations 2
A Selective MAP3K1 Inhibitor Facilitates Discovery of NPM1 as a Member of the Network
Boghean, Lidia , Singh, Sarbjit , Mangalaparthi, Kiran K. , Kizhake, Smitha , Umeta, Lelisse T. , Grothaus, Paul G., Pandey, Akhilesh , Natarajan, Amarnath , Pandey, Akhilesh , Natarajan, Amarnath , Wishka, Donn G.
Molecules | May 1, 2025 | Volume: 30 | Issue: 9 | Pages: 2001
The quinoxaline core is found in several biologically active compounds, with Erdafitinib being the first FDA-approved quinoxaline derivative that targets a kinase and exhibits anti-cancer properties. We previously reported a quinoxaline analog (84) that displayed anti-cancer effects by inhibiting IKKβ, a key kinase in the NFκB pathway. Here, we present the synthesis of a regioisomer (51-106) and its characterization as a selective MAP3K1 inhibitor with improved metabolic stability and oral bioavailability. We used the small molecule MAP3K1 inhibitor in a proteomics study that identified NPM1 as a member of the MAP3K1 network.
Fluorescence based live cell imaging identifies exon 14 skipped hepatocyte growth factor receptor (MET) degraders
Yang, Lin , Lin, Wan-Hsin, Feathers, Ryan W. , Ayers-Ringler, Jennifer , Tolosa, Ezequiel J. , Kizhake, Amritha G., Kizhake, Smitha , Kubica, Sydney P., Boghean, Lidia , Naldrett, Michael J. , Rana, Sandeep , Schaefer-Klein, Janet, Roden, Anja C. , Kosari, Farhad , Anastasiadis, Panos Z. , Feathers, Ryan, Tolosa, Ezequiel, Roden, Anja, Natarajan, Amarnath , Mallareddy, Jayapal Reddy , Lin, Wan‐Hsin , Alvarez, Sophie , Singh, Sarbjit , Zahid, Muhammad , Borad, Mitesh J. , Natarajan, Amarnath , Mansfield, Aaron S.
RSC Advances | April 4, 2025 | Volume: 15 | Issue: 13 | Pages: 10419-10425
Despite ongoing efforts to employ structure-based methods to discover targeted protein degraders (TPD), the prevailing strategy remains synthesizing a focused set of heterobifunctional compounds and screening them for target protein degradation.