2021
DOI: 10.3390/cancers13071538
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Abstract: The phosphatidylinositol-3-kinase (PI3K) pathway plays a central role in the regulation of several signalling cascades which regulate biological processes such as cellular growth, survival, proliferation, motility and angiogenesis. The hyperactivation of this pathway is linked to tumour progression and is one of the most common events in human cancers. Additionally, aberrant activation of the PI3K pathway has been demonstrated to limit the effectiveness of a number of anti-tumour agents paving the way for the … Show more

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Cited by 39 publications
(21 citation statements)
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References 192 publications
(261 reference statements)
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“…Another phase 1b study of the miransertib next-generation inhibitor ARQ 751 (vevorisertib, NCT02761694) as a single agent or in combination with either paclitaxel or fulvestrant in patients with advanced solid tumors with PIK3CA/AKT/PTEN mutations was recently completed, although results are not yet available. The pan-inhibitor MK2206 remains the most prominent of the allosteric inhibitors; however, others such as TAS-117 have also shown promising effects [ 109 , 116 , 117 ].…”
Section: Currently Available Inhibitors Acting On Akt and Mtor In Breast Cancermentioning
confidence: 99%
See 1 more Smart Citation
“…Another phase 1b study of the miransertib next-generation inhibitor ARQ 751 (vevorisertib, NCT02761694) as a single agent or in combination with either paclitaxel or fulvestrant in patients with advanced solid tumors with PIK3CA/AKT/PTEN mutations was recently completed, although results are not yet available. The pan-inhibitor MK2206 remains the most prominent of the allosteric inhibitors; however, others such as TAS-117 have also shown promising effects [ 109 , 116 , 117 ].…”
Section: Currently Available Inhibitors Acting On Akt and Mtor In Breast Cancermentioning
confidence: 99%
“…The most frequently observed side effects included headache, fatigue, and erythema (skin rash). In particular, the use of MTOR inhibitors was associated with a higher risk of developing hypertriglyceridemia, hypercholesterolemia, and hyperglycemia [ 116 , 127 , 128 , 129 ]. Future studies should take into account the improvement of clinical benefits together with reduced risk of adverse events.…”
Section: Currently Available Inhibitors Acting On Akt and Mtor In Breast Cancermentioning
confidence: 99%
“…Multitargeting drugs have the potential advantage of eliciting synergistic effects, especially for cancer [ 43 ]. As targeted therapies have progressed, multiple PI3K/mTOR dual inhibitors have entered clinical trials and have shown good therapeutic effects [ 44 47 ]. We present evidence that taxifolin is a promising dual-targeting molecule that can inhibit both mTOR and PI3K.…”
Section: Discussionmentioning
confidence: 99%
“…In fact, this highly active pro-survival pathway is sustained by considerable positive feedback [ 39 ], as also demonstrated by the failure of PI3K/Akt inhibitors as monotherapy in most clinical trials [ 40 , 41 ]. Thus, cancer cells adapt very rapidly to PI3K inhibition, mainly due to feedback signals leading to activation or enhanced expression of growth factor receptors, such as IR/IRS1/IGF-1R, which, in turn, reactivate PI3K [ 42 , 43 ].…”
Section: Discussionmentioning
confidence: 99%