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Phosphatase inhibition by LB-100 enhances BMN-111 stimulation of bone growth.
Shuhaibar LC, Kaci N, Egbert JR, Horville T, Loisay L, Vigone G, Uliasz TF, Dambroise E, Swingle MR, Honkanen RE, Biosse Duplan M, Jaffe LA, Legeai-Mallet L. Shuhaibar LC, et al. JCI Insight. 2021 May 10;6(9):e141426. doi: 10.1172/jci.insight.141426. JCI Insight. 2021. PMID: 33986191 Free PMC article.
Here, because FGFR3 signaling decreases NPR2 activity by dephosphorylating the NPR2 protein, we tested whether a phosphatase inhibitor (LB-100) could enhance BMN-111-stimulated bone growth in ACH. Measurements of cGMP production in chondrocytes of living tibias, and …
Here, because FGFR3 signaling decreases NPR2 activity by dephosphorylating the NPR2 protein, we tested whether a phosphatase inhibitor (L …
Inhibition of PP2A with LB-100 Enhances Efficacy of CAR-T Cell Therapy Against Glioblastoma.
Cui J, Wang H, Medina R, Zhang Q, Xu C, Indig IH, Zhou J, Song Q, Dmitriev P, Sun MY, Guo L, Wang Y, Rosenblum JS, Kovach JS, Gilbert MR, Zhuang Z. Cui J, et al. Cancers (Basel). 2020 Jan 6;12(1):139. doi: 10.3390/cancers12010139. Cancers (Basel). 2020. PMID: 31935881 Free PMC article.
Our studies demonstrate that LB-100 enhanced anti-CAIX CAR-T cell treatment efficacy in vitro and in vivo. Our findings demonstrate the role of LB-100 in augmenting the cytotoxic activity of anti-CAIX CAR-T cells and underscore the synergistic therapeu …
Our studies demonstrate that LB-100 enhanced anti-CAIX CAR-T cell treatment efficacy in vitro and in vivo. Our findings demons …
LB-100, a novel Protein Phosphatase 2A (PP2A) inhibitor, sensitizes malignant meningioma cells to the therapeutic effects of radiation.
Ho WS, Sizdahkhani S, Hao S, Song H, Seldomridge A, Tandle A, Maric D, Kramp T, Lu R, Heiss JD, Camphausen K, Gilbert MR, Zhuang Z, Park DM. Ho WS, et al. Cancer Lett. 2018 Feb 28;415:217-226. doi: 10.1016/j.canlet.2017.11.035. Epub 2017 Dec 2. Cancer Lett. 2018. PMID: 29199006 Free PMC article.
Also, LB-100 decreased activation of STAT3 and expression of its downstream proteins. In vivo, LB-100 and RT combined treatment prolonged the survival of mice with xenografts compared to RT alone. ...
Also, LB-100 decreased activation of STAT3 and expression of its downstream proteins. In vivo, LB-100 and RT com …
LB-100 sensitizes hepatocellular carcinoma cells to the effects of sorafenib during hypoxia by activation of Smad3 phosphorylation.
Fu QH, Zhang Q, Zhang JY, Sun X, Lou Y, Li GG, Chen ZL, Bai XL, Liang TB. Fu QH, et al. Tumour Biol. 2016 Jun;37(6):7277-86. doi: 10.1007/s13277-015-4560-2. Epub 2015 Dec 14. Tumour Biol. 2016. PMID: 26666823
Here, we tested whether LB-100 could sensitize HCC to the effects of sorafenib. Intriguingly, LB-100 enhanced the effects of sorafenib in HCC cells only during hypoxic environments. LB-100 dramatically increased intracellular p-Smad3 leve …
Here, we tested whether LB-100 could sensitize HCC to the effects of sorafenib. Intriguingly, LB-100 enhanced th …
The Antitumor Drug LB-100 Is a Catalytic Inhibitor of Protein Phosphatase 2A (PPP2CA) and 5 (PPP5C) Coordinating with the Active-Site Catalytic Metals in PPP5C.
D'Arcy BM, Swingle MR, Papke CM, Abney KA, Bouska ES, Prakash A, Honkanen RE. D'Arcy BM, et al. Mol Cancer Ther. 2019 Mar;18(3):556-566. doi: 10.1158/1535-7163.MCT-17-1143. Epub 2019 Jan 24. Mol Cancer Ther. 2019. PMID: 30679389 Free PMC article.
LB-100 is an experimental cancer therapeutic with cytotoxic activity against cancer cells in culture and antitumor activity in animals. ...Rather, the premise for LB-100 targeting PP2AC is derived from studies that measure phosphate released from a pho …
LB-100 is an experimental cancer therapeutic with cytotoxic activity against cancer cells in culture and antitumor activity in …
Eprenetapopt (APR-246) and Azacitidine in TP53-Mutant Myelodysplastic Syndromes.
Sallman DA, DeZern AE, Garcia-Manero G, Steensma DP, Roboz GJ, Sekeres MA, Cluzeau T, Sweet KL, McLemore A, McGraw KL, Puskas J, Zhang L, Yao J, Mo Q, Nardelli L, Al Ali NH, Padron E, Korbel G, Attar EC, Kantarjian HM, Lancet JE, Fenaux P, List AF, Komrokji RS. Sallman DA, et al. J Clin Oncol. 2021 May 10;39(14):1584-1594. doi: 10.1200/JCO.20.02341. Epub 2021 Jan 15. J Clin Oncol. 2021. PMID: 33449813 Free PMC article. Clinical Trial.
The phosphatase inhibitor LB-100 creates neoantigens in colon cancer cells through perturbation of mRNA splicing.
Dias MH, Liudkovska V, Montenegro Navarro J, Giebel L, Champagne J, Papagianni C, Bleijerveld OB, Velds A, Agami R, Bernards R, Cieśla M. Dias MH, et al. EMBO Rep. 2024 Apr 10. doi: 10.1038/s44319-024-00128-3. Online ahead of print. EMBO Rep. 2024. PMID: 38600345 Free article.
LB-100 has proven effective in pre-clinical models in combination with immunotherapy, but the molecular underpinnings of this synergy remain understood poorly. ...Altered phosphorylation endows LB-100-treated colorectal adenocarcinoma cells with differ …
LB-100 has proven effective in pre-clinical models in combination with immunotherapy, but the molecular underpinnings of this …
PP2A inhibition by LB-100 protects retinal pigment epithelium cells from UV radiation via activation of AMPK signaling.
Li XF, Li SY, Dai CM, Li JC, Huang DR, Wang JY. Li XF, et al. Biochem Biophys Res Commun. 2018 Nov 17;506(1):73-80. doi: 10.1016/j.bbrc.2018.10.077. Epub 2018 Oct 16. Biochem Biophys Res Commun. 2018. PMID: 30340831
Conversely, AMPK inhibition, by AMPKalpha1-shRNA, -CRISPR/Cas9 knockout or -T172A mutation, almost blocked LB-100-induced RPE cytoprotection against UVR. Importantly, CRISPR/Cas9-mediated PP2A knockout mimicked and nullified LB-100-induced anti-UVR act …
Conversely, AMPK inhibition, by AMPKalpha1-shRNA, -CRISPR/Cas9 knockout or -T172A mutation, almost blocked LB-100-induced RPE …
An LC-MS/MS method for simultaneous determination of LB-100 and its active metabolite, endothall, in human plasma.
Feng Y, Massarelli E, Forman E, Kovach JS, Salgia R, Synold TW. Feng Y, et al. Bioanalysis. 2023 Sep;15(17):1095-1107. doi: 10.4155/bio-2023-0078. Epub 2023 Aug 16. Bioanalysis. 2023. PMID: 37584370
Intra- and inter-assay precision and accuracy were within 11%. LB-100 and endothall recoveries were 78.7 and 86.7%, respectively. The validated LC-MS/MS method enabled the accurate measurement of LB-100 and endothall in patient samples from an ongoing …
Intra- and inter-assay precision and accuracy were within 11%. LB-100 and endothall recoveries were 78.7 and 86.7%, respective …
Therapeutic targeting of PP2A.
O'Connor CM, Perl A, Leonard D, Sangodkar J, Narla G. O'Connor CM, et al. Int J Biochem Cell Biol. 2018 Mar;96:182-193. doi: 10.1016/j.biocel.2017.10.008. Epub 2017 Oct 26. Int J Biochem Cell Biol. 2018. PMID: 29107183 Free PMC article. Review.
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