Structure-based drug design of novel and highly potent pyruvate dehydrogenase kinase inhibitors

[Display omitted] Pyruvate dehydrogenase kinases (PDHKs) are fascinating drug targets for numerous diseases, including diabetes and cancers. In this report, we describe the result of our structure-based drug design from tricyclic lead compounds that led to the discovery of highly potent PDHK2 and PD...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry 2021-12, Vol.52, p.116514-116514, Article 116514
Hauptverfasser:	Bessho, Yuki, Akaki, Tatsuo, Hara, Yoshinori, Yamakawa, Maki, Obika, Shingo, Mori, Genki, Ubukata, Minoru, Yasue, Katsutaka, Nakane, Yoshitomi, Terasako, Yasuo, Orita, Takuya, Doi, Satoki, Iwanaga, Tomoko, Fujishima, Ayumi, Adachi, Tsuyoshi, Ueno, Hiroshi, Motomura, Takahisa
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenosine Triphosphate - chemistry Adenosine Triphosphate - pharmacology Amides - chemistry Amides - pharmacology ATP binding site Dose-Response Relationship, Drug Drug Design Humans Intramolecular pi-pi interaction Molecular Structure Novel ATP lid conformation Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Pyruvate Dehydrogenase Acetyl-Transferring Kinase Pyruvate dehydrogenase kinases (PDHKs) Structure-Activity Relationship Structure-based drug design (SBDD)
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Schreiben Sie den ersten Kommentar!