title: Estrogen-related receptor alpha interacts cooperatively with peroxisome proliferator-activated receptor-gamma coactivator-1alpha to regulate osteocalcin gene expression.
abstract: Osteocalcin is one of the most abundant non-collagenous proteins in bone that is commonly used as a preliminary biomarker in bone formation. Osteocalcin also regulates energy metabolism as a hormone. Estrogen-related receptor alpha (ERRα) is primarily thought to regulate energy homeostasis through interacting with peroxisome proliferator-activated receptor gamma coactivator-1α (PGC-1α). Intriguingly, ERRα may play a functional role in bone formation. We have found there are 3 ERRα response elements (ERR response element, ERRE) in the osteocalcin promoter, and ERRα interacted cooperatively with PGC-1α could improve the osteocalcin promoter activity, whereas ERRα specific antagonist, XCT-790, inhibits this enhancement. XCT-790 inhibits osteocalcin and ERRα target gene PDKs expression in osteoblast cells. Thus ERRs might have physiological roles in bone formation and energy metabolism through modulating osteocalcin gene expression.
authors.affiliation: First Affiliated Hospital, Guangzhou University of Chinese Medicine, Guangzhou, 510405, China.
authors.forename: Haibin
authors.initials: H
authors.lastname: Wang
authors.forename: Junjian
authors.initials: J
authors.lastname: Wang
mesh_terms: D020029:Base Pairing / Q000235:genetics; D002460:Cell Line; D005786:Gene Expression Regulation / Q000187:drug effects; D006801:Humans; D009570:Nitriles / Q000494:pharmacology; D010006:Osteoblasts / Q000187:drug effects / Q000378:metabolism; D015675:Osteocalcin / Q000235:genetics* / Q000378:metabolism; D011401:Promoter Regions, Genetic / Q000235:genetics; D011485:Protein Binding / Q000187:drug effects / Q000235:genetics; D012333:RNA, Messenger / Q000235:genetics / Q000378:metabolism; D011960:Receptors, Estrogen / Q000037:antagonists & inhibitors / Q000378:metabolism*; D013844:Thiazoles / Q000494:pharmacology; D014157:Transcription Factors / Q000378:metabolism*; D000097983:ERRalpha Estrogen-Related Receptor
chemical_list: D009570:Nitriles; D015675:Osteocalcin; D012333:RNA, Messenger; D011960:Receptors, Estrogen; D013844:Thiazoles; D014157:Transcription Factors; D000097983:ERRalpha Estrogen-Related Receptor; C488234:XCT790; C111264:peroxisome-proliferator-activated receptor-gamma coactivator-1
keywords: XCT-790; estrogen related receptor alpha; osteocalcin; peroxisome proliferator-activated receptor-gamma coactivator-1 alpha