Discovery of the 3-Amino-1,2,4-triazine-Based Library as Selective PDK1 Inhibitors with Therapeutic Potential in Highly Aggressive Pancreatic Ductal Adenocarcinoma

Discovery of the 3-Amino-1,2,4-triazine-Based Library as Selective PDK1 Inhibitors with Therapeutic Potential in Highly Aggressive Pancreatic Ductal Adenocarcinoma

Pyruvate dehydrogenase kinases (PDKs) are serine/threonine kinases, that are directly involved in altered cancer cell metabolism, resulting in cancer aggressiveness and resistance. Dichloroacetic acid (DCA) is the first PDK inhibitor that has entered phase II clinical; however, several side effects...

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Bibliographic Details
Main Authors: Daniela Carbone, Michele De Franco, Camilla Pecoraro, Davide Bassani, Matteo Pavan, Stella Cascioferro, Barbara Parrino, Girolamo Cirrincione, Stefano Dall’Acqua, Stefano Moro, Valentina Gandin, Patrizia Diana
Format: Article
Language:English
Published: MDPI AG 2023-02-01
Series:International Journal of Molecular Sciences
Subjects:
3-amino-1,2,4-triazine derivatives
bis-indole derivatives
PDK inhibitors
Kras-mutated pancreatic ductal adenocarcinoma
antitumor agents
ligand-based homology modeling
Online Access:https://www.mdpi.com/1422-0067/24/4/3679

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https://www.mdpi.com/1422-0067/24/4/3679

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