Modification of the Orthosteric PPARγ Covalent Antagonist Scaffold Yields an Improved Dual-Site Allosteric Inhibitor

GW9662 and T0070907 are widely used commercially available irreversible antagonists of peroxisome proliferator-activated receptor gamma (PPARγ). These antagonists covalently modify Cys285 located in an orthosteric ligand-binding pocket embedded in the PPARγ ligand-binding domain and are used to bloc...

Celý popis

Uloženo v:
Podrobná bibliografie
Vydáno v:ACS Chem Biol
Hlavní autoři: Brust, Richard, Lin, Hua, Fuhrmann, Jakob, Asteian, Alice, Kamenecka, Theodore M., Kojetin, Douglas J.
Médium: Artigo
Jazyk:Inglês
Vydáno: 2017
Témata:
Article
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC5652320/
https://ncbi.nlm.nih.gov/pubmed/28165718
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acschembio.6b01015
Tagy: Přidat tag
Žádné tagy, Buďte první, kdo otaguje tento záznam!

Podobné jednotky