(n = 10) and PFKFB3 inhibitor PKF-15 intervention group (n = 10) according to random number table method. The AMI model of mice was reproduced by left anterior descending coronary...
Indeed, an ongoing clinical trial is examining the efficacy of a PFKFB3 inhibitor at treating lung cancer36. Given this, how to effectively inhibit PFKFB3 could be key to a better anti-cancer treatment. In the present study, circadian clock control of PFKFB3 expression was established as ...
PFKFB3 INHIBITOR AND METHODS OF USE AS AN ANTI-CANCER THERAPEUTIC A novel compound, (E)-1-(pyridyn-4-yl)-3-(7-(trifluoromethyl)quinolin-2-yl)-prop-2-en-1-one, is provided herein. (E)-1-(pyridyn-4-yl)-3-(7-(trifluoromethyl)quinolin-2-yl)-prop-2-en-1-one is an inhibitor of...
3PO is a potent inhibitor of PFKFB3 but poor water solubility makes this compound clinically unavailable. Other potent and selective inhibitors of PFKFB3, such as PFK15 and PFK-158, are under clinical trials for treating late-stage cancer patients. Recently emerged nanotechnology-based drug ...
[83,84,85]. We also found that PFK-015 exerted a substantially suppressive role in RCC cell proliferation in vitro, showing a similar function to a specific glycolysis inhibitor 2-DG. These results indicated the feasibility of PFKFB3 as a potential target of pRCC intervention therapy, which ...
inhibitor of PFKFB3, PFK-158, displays broad antitumor activity and immunomodulatory effects in multiple human and syngeneic preclinical models.111–113A phase I clinical trial demonstrated that PFK-158 was successfully completed in July 2016. PFK-158 presented safety and anticancer activity in 6 of...
124 Another potent and selective inhibitor of PFKFB3, PFK-158, displays broad antitumor activity and immunomodulatory effects in multiple human and syngeneic preclinical models.111–113 A phase I clinical trial demonstrated that PFK-158 was successfully completed in July 2016. PFK-158 presented safety...
The HER2-positive GC patient samples were used to determine clinical significance. We also measured protein expression and phosphorylation modifications to determine those alterations related to resistance. In vivo studies combining inhibitor of PFKFB3 with trastuzumab corroborated the in vitro findings. ...
Thus, combining PFK158 with one of the existing Akt/mTOR inhibitors could be a novel therapeutic approach for EC patients who did not derive clinical benefit from monotherapy with Akt/mTOR pathway inhibitor. In cancer cells, increased DNA repair capacity can reverse the DNA damage, which is ...
However, the status of this trial initiated in 2014 is currently unknown. In 2018, a phenylsulfonamide salicylic acid-derived small-molecule inhibitor, KAN0438241, that showed selectivity only for the PFKFB3 kinase domain was identified [26]. An esterified derivative, KAN0438757, showed ...