Research
Hormonal
Inhibition of Errα using the synthetic inverse agonist XCT790 reduces PGC-1α-mediated cellular respiration and OXPHOS gene expression in muscle cells.
This study uses a specific drug (XCT790) to block Errα, proving that Errα is necessary for mitochondrial energy production. This supports the hypothesis that activating Errα (rather than blocking it) could be a therapeutic strategy for diabetes.
GoodSupportsHIGH confidence
By using a synthetic inhibitor of Errα, we demonstrated its key role in PGC-1α-mediated effects on gene regulation and cellular respiration.
Why this rating
Clear functional data in cell culture, but not translated to human outcomes.
Source
Errα and Gabpa/b specify PGC-1α-dependent oxidative phosphorylation gene expression that is altered in diabetic muscle
Vamsi K. Mootha et al. · Proceedings of the National Academy of Sciences · 2004
DOI 10.1073/pnas.0401401101
mechanism_onlyCited 679×
Read the paper DOI resolved against Crossref · corpus check 2026-06-10
More from this paper
- Activation of the estrogen-related receptor alpha (Errα) by PGC-1α drives the expression of oxidative phosphorylation (OXPHOS) genes in skeletal muscle, and this pathway is downregulated in diabetic muscle.Good
- Errα and Gabpa form a double-positive-feedback loop with PGC-1α to drive robust expression of mitochondrial genes, and this loop is disrupted in diabetic muscle.Good
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