Pillar 1 - FTO (new thread), page-2740

Preprint

The FTO inhibitor Rhein is a promising option for the treatment of multidrug resistance AML
https://www.researchsquare.com/article/rs-3813501/v1

"By using Rhein at low concentrations, it can enhance the anti-tumor effect of azacitidine. Furthermore, our results indicate that Rhein is effective even in resistant cells, suggesting its potential as an ideal therapeutic option for AML patients, especially for patient who can’t benefit from intensive regimen therapy."

I would have thought a reference to Su et al. 2018 somewhere may have been relevant given the hypomethylating agent/FTO connection.

"Our findings suggest that Rhein is a potent inhibitor for studying the effects of RNA methylation on cancer progression and multidrug resistance. In the future, Rhein may be further modified or combined with other chemotherapy drugs to enhance its efficacy. Furthermore, preclinical primary safety evaluations and pharmacokinetic studies of Rhein are urgently needed. Combination therapy using targeted FTO inhibitors and other AML chemotherapy drugs may also hold great promise for the treatment of AML, and is thus a direction worth exploring."

Bisantrene/CS1 may have been a better choice to explore. As stated in Su et al. 2020

"A set of specific or non-specific FTO inhibitors, such as rhein, meclofenamic acid (MA), MO-I-500, fluorescein, and R-2HG,have been identified (Chen et al., 2012; He et al., 2015; Huang et al., 2015; Padariya and Kalathiya, 2016; Singh et al., 2016; Su et al., 2018; Toh et al., 2015; Wang et al., 2015; Zheng et al., 2014). However, all these small molecules are limited in clinical potential due to mild biological function and low sensitivity and/or specificity (Huang et al., 2019)