In vivo screen identifies a SIK inhibitor that induces β cell proliferation through a transient UPR.

TitleIn vivo screen identifies a SIK inhibitor that induces β cell proliferation through a transient UPR.
Publication TypeJournal Article
Year of Publication2021
AuthorsCharbord J, Ren L, Sharma RB, Johansson A, Ågren R, Chu L, Tworus D, Schulz N, Charbord P, Stewart AF, Wang P, Alonso LC, Andersson O
JournalNat Metab
Volume3
Issue5
Pagination682-700
Date Published2021 05
ISSN2522-5812
KeywordsActivating Transcription Factor 6, Animals, Cell Cycle, Cell Proliferation, Drug Evaluation, Preclinical, Endoribonucleases, Gene Expression Profiling, High-Throughput Nucleotide Sequencing, Humans, Insulin-Secreting Cells, Male, Mice, Protein Kinase Inhibitors, Protein-Serine-Threonine Kinases, Signal Transduction, Single-Cell Analysis, Unfolded Protein Response, Zebrafish
Abstract

It is known that β cell proliferation expands the β cell mass during development and under certain hyperglycemic conditions in the adult, a process that may be used for β cell regeneration in diabetes. Here, through a new high-throughput screen using a luminescence ubiquitination-based cell cycle indicator (LUCCI) in zebrafish, we identify HG-9-91-01 as a driver of proliferation and confirm this effect in mouse and human β cells. HG-9-91-01 is an inhibitor of salt-inducible kinases (SIKs), and overexpression of Sik1 specifically in β cells blocks the effect of HG-9-91-01 on β cell proliferation. Single-cell transcriptomic analyses of mouse β cells demonstrate that HG-9-91-01 induces a wave of activating transcription factor (ATF)6-dependent unfolded protein response (UPR) before cell cycle entry. Importantly, the UPR wave is not associated with an increase in insulin expression. Additional mechanistic studies indicate that HG-9-91-01 induces multiple signalling effectors downstream of SIK inhibition, including CRTC1, CRTC2, ATF6, IRE1 and mTOR, which integrate to collectively drive β cell proliferation.

DOI10.1038/s42255-021-00391-x
Alternate JournalNat Metab
PubMed ID34031592
Grant ListR01 DK095140 / DK / NIDDK NIH HHS / United States
R01 DK113300 / DK / NIDDK NIH HHS / United States
R01 DK114686 / DK / NIDDK NIH HHS / United States
U24 DK093000 / DK / NIDDK NIH HHS / United States