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. 2020 Jul 28;26(28):4036–4054. doi: 10.3748/wjg.v26.i28.4036

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©The Author(s) 2020. Published by Baishideng Publishing Group Inc. All rights reserved.

This article is an open-access article which was selected by an in-house editor and fully peer-reviewed by external reviewers. It is distributed in accordance with the Creative Commons Attribution Non Commercial (CC BY-NC 4.0) license, which permits others to distribute, remix, adapt, build upon this work non-commercially, and license their derivative works on different terms, provided the original work is properly cited and the use is non-commercial.

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Mechanism of action of available PAK4-NAMPT dual inhibitor. Dual inhibition of PAK4 and NAMPT using KPT-9274 single agent or in combination with everolimus results in lower case tumor shrinkage. KPT-9274 inhibits NAMPT causing downregulation of NAD and ATP and alteration of cell metabolism. Additionally, KPT-9274 Inhibits PAK4 resulting in downregulation of β-catenin and RICTOR. Downregulation of RICTOR causes the inhibition of mTORC2 implicated in everolimus resistance. R: Resistance; PAK4: p21-activated kinase 4; NAMPT: Nicotinamide Phosphoribosyltransferase; KPT-9274: Available PAK4-NAMPT dual inhibitor; NAD: Nicotine adenine dinucleotide; ATP: Adenosine-triphosphate; RICTOR: Rapamycin-insensitive companion of Tor; mTORC2: Mammalian target of rapamycincomplex 2.