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Towards a RIOK2 chemical probe: cellular potency improvement of a selective 2-(acylamino)pyridine series.

ABSTRACT: 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 re-search 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 improved cellular activity while maintaining selectivity for RIOK2. While our compounds do not represent RIOK2 chemical probes, they are the best available tool molecules to begin to characterize RIOK2 function in vitro.

SUBMITTER: Wang CB

PROVIDER: S-EPMC8130602 | biostudies-literature | 2021 Jan

REPOSITORIES: biostudies-literature

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Towards a RIOK2 chemical probe: cellular potency improvement of a selective 2-(acylamino)pyridine series.

Wang Christopher B CB Lorente-Macías Álvaro Á Wells Carrow C Pickett Julie E JE Picado Alfredo A Zuercher William J WJ Axtman Alison D AD

RSC medicinal chemistry 20201111 1

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 re-search 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 improved cellular activity while maintaining selectivity for RIOK2. While our compounds ...[more]

PMID: 34046605

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