Title | In vivo screen identifies a SIK inhibitor that induces β cell proliferation through a transient UPR. |
Publication Type | Journal Article |
Year of Publication | 2021 |
Authors | Charbord 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 |
Journal | Nat Metab |
Volume | 3 |
Issue | 5 |
Pagination | 682-700 |
Date Published | 2021 05 |
ISSN | 2522-5812 |
Keywords | Activating 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. |
DOI | 10.1038/s42255-021-00391-x |
Alternate Journal | Nat Metab |
PubMed ID | 34031592 |
Grant List | R01 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 |