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Cited by 157 publications
(230 citation statements)
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References 49 publications
(51 reference statements)
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“…In accordance with the major theme of this review, a recent study demonstrated that combination of SET targeting and tyrosine kinase inhibitor provides an effective therapeutic approach in human T-cell acute lymphoblastic leukemia [34]. Apart of small-molecules targeting the PIPs, the novel series of orally bioavailable and nontoxic PP2A reactivator molecules with profound in vivo therapeutic activities in KRAS mutant lung cancers and castration-resistant prostate cancer [47,48], provide a very encouraging example that PP2A indeed is druggable [14,39]. In the context of this review, these small-molecule PP2A activators were recently shown to transform the cytostatic MEK inhibitor responses to cytotoxic, and to greatly promote in vivo therapeutic effects of MEK inhibitor AZD6244 in two KRAS mutant lung cancer xenograft models [15].…”
Section: Therapeutic Targeting Of Pp2amentioning
confidence: 64%
“…In accordance with the major theme of this review, a recent study demonstrated that combination of SET targeting and tyrosine kinase inhibitor provides an effective therapeutic approach in human T-cell acute lymphoblastic leukemia [34]. Apart of small-molecules targeting the PIPs, the novel series of orally bioavailable and nontoxic PP2A reactivator molecules with profound in vivo therapeutic activities in KRAS mutant lung cancers and castration-resistant prostate cancer [47,48], provide a very encouraging example that PP2A indeed is druggable [14,39]. In the context of this review, these small-molecule PP2A activators were recently shown to transform the cytostatic MEK inhibitor responses to cytotoxic, and to greatly promote in vivo therapeutic effects of MEK inhibitor AZD6244 in two KRAS mutant lung cancer xenograft models [15].…”
Section: Therapeutic Targeting Of Pp2amentioning
confidence: 64%
“…1A) would compromise BBB permeability, and eventually CNS availability, of the SMAPs as compared to tricyclics. We therefore started by investigating the in vitro BBB passage of NZ-8-061 (a.k.a DT-061) that has been widely used in cancers outside the CNS (Sangodkar et al, 2017;McClinch et al, 2018). Quantified by HPLC-MS/MS, NZ-8-061 was found to cross the artificial BBB (Le Joncour et al, 2019), consisting of murine brain microcapillary endothelial cells and astrocytes ( Fig.…”
Section: Development Of Blood-brain Barrier Permeable Small Molecule mentioning
confidence: 99%
“…As a pharmacologic control, U87MG, U118, or A172 cells were also treated with increasing doses of TRC-766, a structurally similar but biologically inactive derivate of SMAPs ( Supplementary Fig. 3A) (Sangodkar et al, 2017;McClinch et al, 2018).…”
Section: Nz-8-061 Potently Inhibits the Viability Of Gb Cells With Hementioning
confidence: 99%
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“…Subsequent reengineering of these compounds eliminated their CNS effects while retaining and/or even enhancing their anticancer activity. In this issue, Sangodkar et al (15) now show that these reengineered compounds, termed small molecule activators of PP2A (SMAPs), share the ability to activate PP2A. Biochemical studies identified the PP2A A subunit as the primary target of SMAPs, specifically the centrally located HEAT repeats five to eight.…”
Section: Smaps: New Kids In Townmentioning
confidence: 99%