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@ARTICLE{Papa:646269,
author = {Papa, Christina and Rose, Alina and Martin, Hugo N. G. and
Useini, Abibe and Geier, Florian and Liao, Longsheng and
Rodríguez-Aguilera, Jesús Rafael and Valina-Allo, Philipp
and Hoffmann, Anne and Tvardovskiy, Andrey and Zulfqar,
Faiqa and Zimmerman, Andrea and Schicht, Gerda and Ott,
Fritzi and Körner, Christiane and Engelmann, Beatrice and
Rolle-Kampczyk, Ulrike and von Bergen, Martin and Meier,
Matthias and Bartke, Till and Seehofer, Daniel and Klöting,
Nora and Matz-Soja, Madlen and Damm, Georg and Boeckel,
Jes-Niels and Buescher, Joerg M. and Blüher, Matthias and
Laufs, Ulrich and Bondareva, Olga and Sträter, Norbert and
Künze, Georg and Heiker, John T. and Sheikh, Bilal N.},
title = {{B}empedoic acid directly binds and activates {PPAR}α},
journal = {Cell metabolism},
volume = {xx},
issn = {1550-4131},
address = {Amsterdam [u.a.]},
publisher = {Elsevier},
reportid = {PUBDB-2026-00792},
pages = {S1550413125005492},
year = {2026},
abstract = {Bempedoic acid (BA) is a recently approved drug that lowers
cholesterol and hepatic lipids, yet its mechanism of action
remains incompletely understood. Here, we combine
transcriptomic, biochemical, and structural approaches to
show that BA directly binds to and activates peroxisome
proliferator-activated receptor alpha (PPARα). BA treatment
robustly induced PPARα signaling and fatty acid oxidation
in primary hepatocytes and mouse liver. Through X-ray
crystallography, we uncovered that BA binds to the
ligand-binding domain of PPARα and stabilizes its active
conformation. BA activated PPARα target genes independently
of very-long-chain acyl-coenzyme A (CoA) synthetase
(ACSVL1), the liver-enriched enzyme that converts BA to its
bempedoyl-CoA form. Notably, BA-mediated induction of fatty
acid oxidation required PPARα. Together, this work reveals
direct PPARα activation as a key mechanism of BA action,
providing a molecular basis for its lipid-lowering effects
and suggesting broader therapeutic potential beyond the
liver.},
cin = {EMBL-User},
ddc = {570},
cid = {I:(DE-H253)EMBL-User-20120814},
pnm = {6G3 - PETRA III (DESY) (POF4-6G3)},
pid = {G:(DE-HGF)POF4-6G3},
experiment = {EXP:(DE-H253)P-P14-20150101},
typ = {PUB:(DE-HGF)16},
doi = {10.1016/j.cmet.2025.12.018},
url = {https://bib-pubdb1.desy.de/record/646269},
}