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Strategy for Lead Identification for Understudied Kinases

preprint
submitted on 10.03.2021, 20:16 and posted on 11.03.2021, 11:00 by David Drewry, Joel K. Annor-Gyamfi, Carrow Wells, Julie E. Pickett, Alison Axtman

In our manuscript we outline an approach in which we convert a promiscuous pyrimidine scaffold into narrowly selective, cell-active chemical leads for several understudied kinases, including DRAK1, BMP2K, and MARK4. These chemical tools will allow illumination of the function(s) of these poorly characterized kinases for the first time. Several of the understudied kinases that we inhibit with our pyrimidine-based compounds are also implicated in neurodegenerative disease, pushing the utility of kinase inhibitors outside of the oncology space and offering opportunities for the validation of therapeutic hypotheses attributed to these kinases.

Funding

NC Biotechnology Center Institutional Support Grant 2018-IDG-1030

NIH 1U24DK116204

NIH U54AG065187

Department of Defense AL190107

ALS Association wa1127

Canada Foundation for Innovation

Eshelman Institute for Innovation

Genome Canada

Innovative Medicines Initiative

Ontario Ministry of Economic Development and Innovation

São Paulo Research Foundation- FAPESP

Wellcome Trust

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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