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Towards a RIOK2 Chemical Probe: Cellular Potency Improvement of a Selective 2-(Acylamino)pyridine Series

preprint
submitted on 15.08.2020 and posted on 17.08.2020 by Christopher Wang, Álvaro Lorente-Macías, Carrow Wells, Julie E. Pickett, Alfredo Picado, William Zuercher, Alison Axtman
RIOK2 is an understudied kinase associated with a variety of human cancers including non-small cell lung cancer and glioblastoma. No potent, selective, and cell-active chemical probe currently exists for RIOK2. Such a reagent would expedite research into the biological functions of RIOK2 and validate it as a therapeutic target. Herein, we describe the synthesis of naphthyl-pyridine based compounds that have both improved cellular activity while maintaining selectivity for RIOK2.

Funding

Canada Foundation for Innovation

Eshelman Institute for Innovation

Genome Canada

Innovative Medicines Initiative (EU/EFPIA) [ULTRA-DD grant no. 115766]

Ontario Ministry of Economic Development and Innovation

São Paulo Research Foundation-FAPESP

Wellcome [106169/ZZ14/Z]

NC Biotechnology Center Institutional Support Grant 2018-IDG-1030

National Institutes of Health 1U24DK11604

American Foundation for Pharmaceutical Education (AFPE) Foundation

Spanish MECD (FPU 14/00818)

History

Email Address of Submitting Author

alison.axtman@unc.edu

Institution

University of North Carolina at Chapel Hill

Country

United States

ORCID For Submitting Author

0000-0003-4779-9932

Declaration of Conflict of Interest

no conflict of interest

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