Hartmann_2021_J.Med.Chem_64_2815

Reference

Title : Combined Cardioprotective and Adipocyte Browning Effects Promoted by the Eutomer of Dual sEH\/PPARgamma Modulator - Hartmann_2021_J.Med.Chem_64_2815
Author(s) : Hartmann M , Bibli SI , Tews D , Ni X , Kircher T , Kramer JS , Kilu W , Heering J , Hernandez-Olmos V , Weizel L , Scriba GKE , Krait S , Knapp S , Chaikuad A , Merk D , Fleming I , Fischer-Posovszky P , Proschak E
Ref : Journal of Medicinal Chemistry , 64 :2815 , 2021
Abstract : The metabolic syndrome (MetS) is a constellation of cardiovascular and metabolic symptoms involving insulin resistance, steatohepatitis, obesity, hypertension, and heart disease, and patients suffering from MetS often require polypharmaceutical treatment. PPARgamma agonists are highly effective oral antidiabetics with great potential in MetS, which promote adipocyte browning and insulin sensitization. However, the application of PPARgamma agonists in clinics is restricted by potential cardiovascular adverse events. We have previously demonstrated that the racemic dual sEH/PPARgamma modulator RB394 (3) simultaneously improves all risk factors of MetS in vivo. In this study, we identify and characterize the eutomer of 3. We provide structural rationale for molecular recognition of the eutomer. Furthermore, we could show that the dual sEH/PPARgamma modulator is able to promote adipocyte browning and simultaneously exhibits cardioprotective activity which underlines its exciting potential in treatment of MetS.
ESTHER : Hartmann_2021_J.Med.Chem_64_2815
PubMedSearch : Hartmann_2021_J.Med.Chem_64_2815
PubMedID: 33620196

Related information

Inhibitor TK90
Structure TK907A7G

Citations formats

Hartmann M, Bibli SI, Tews D, Ni X, Kircher T, Kramer JS, Kilu W, Heering J, Hernandez-Olmos V, Weizel L, Scriba GKE, Krait S, Knapp S, Chaikuad A, Merk D, Fleming I, Fischer-Posovszky P, Proschak E (2021)
Combined Cardioprotective and Adipocyte Browning Effects Promoted by the Eutomer of Dual sEH\/PPARgamma Modulator
Journal of Medicinal Chemistry 64 :2815

Hartmann M, Bibli SI, Tews D, Ni X, Kircher T, Kramer JS, Kilu W, Heering J, Hernandez-Olmos V, Weizel L, Scriba GKE, Krait S, Knapp S, Chaikuad A, Merk D, Fleming I, Fischer-Posovszky P, Proschak E (2021)
Journal of Medicinal Chemistry 64 :2815