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9 Diseases |  |
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14 News |  |
- | MLN8054 / Takeda
Journal: Helicobacter pylori VacA-induced mitochondrial damage in the gastric pit cells of the antrum and therapeutic rescue. (Pubmed Central) - Nov 13, 2024
MLN8054 was effective in VacA-treated and Hp-infected hAGOs and mice, highlighting hAGOs as a promising drug-screening model. These findings suggest that mitochondrial quality control may serve as a promising therapeutic target for Hp VacA-mediated toxicity and disease progression.
- MLN8054 / Takeda
PRIMARY CILIA OF SYSTEMIC SCLEROSIS (SSC) DERMAL FIBROBLASTS ARE DISRUPTED BY DOWNREGULATION OF CAVEOLIN-1 AND ABERRANT ACTIVITY OF AURORA A KINASE, INDEPENDENT OF TRANSFORMING GROWTH FACTOR BETA (South Hall 2B) - Feb 13, 2024 - Abstract #SSWC2024SSWC_459;
activation can shorten PC via a non-canonical pathway involving ROCK2, this is not responsible for the short cilia phenotype in SSc. These findings support the notion that SSc profibrotic activation may involve mechanisms beyond TGF?, and highlight the potential significance of Caveolin-1 and AURKA in modulating PC length as contributors to profibrotic activation, and potential therapeutic targets for tissue fibrosis.
- MLN8054 / Takeda
Systemic Sclerosis (SSc) Dermal Fibroblasts Show Shortened Primary Cilia Due to Aberrant Aurora a Kinase Activation Independently of Transforming Growth Factor ? Signalling (Poster Hall; in person) - Sep 23, 2023 - Abstract #ACRConvergence2023ACR_Convergence_3069;
These findings support the notion that SSc profibrotic activation may involve mechanisms beyond TGF?, and highlight the potential significance of Caveolin-1 and AURKA in modulating PC length as contributors to profibrotic activation, and potential therapeutic targets for tissue fibrosis. SD208 (1
- MLN8054 / Takeda
Phenotypic profiling of Aurora inhibitors using the OncoPanelTMplatform (Section 17; Poster Board #24) - Mar 14, 2023 - Abstract #AACR2023AACR_4940;
SD208 (1 Activity of the AurA-selective inhibitor, MLN8054, was also evaluated in the Eurofins Discovery BioMAP
- | MLN8054 / Takeda
Journal: Phosphorylation, Mg-ADP, and Inhibitors Differentially Shape the Conformational Dynamics of the A-Loop of Aurora-A. (Pubmed Central) - Sep 19, 2021
In the closed states, binding of CD532 and MLN8054 inhibitors has the effect of increasing the distance of the N- and C-lobes of the kinase domain of Aurora-A, and the angle analysis between those two lobes during MD simulations showed that the N- and C-lobes are kept more open in presence of CD532, compared to MLN8054. As the A-loop is a common feature of Aurora protein kinases, our studies provide a general description of the conformational dynamics of this structure upon phosphorylation and different ligands binding.
- | MLN8054 / Takeda
Journal: Aurora A inhibition disrupts chromosome condensation and spindle assembly during the first embryonic division in pigs. (Pubmed Central) - Dec 23, 2020
Then, the potential role of Aurora A was further evaluated using a highly selective Aurora A inhibitor, MLN8054, during this mitotic progression in pig embryos...Further subcellular structure examination showed that Aurora A inhibition not only led to the failure of spindle microtubule assembly, but also resulted in severe defects in chromosome condensation, accompanied by an obvious decrease in p-TACC3(S558) expression during the prophase of the first mitosis. Together, these results illustrated that Aurora A is crucial for both spindle assembly and chromosome condensation during the first mitotic division in pig embryos, and that the regulation of Aurora A may be associated with its effects on p-TACC3(S558) expression.
- | mitoxantrone / Generic mfg., MLN8054 / Takeda
Journal: Integrating Differential Gene Expression Analysis with Perturbagen-Response Signatures May Identify Novel Therapies for Thyroid-Associated Orbitopathy. (Pubmed Central) - Sep 12, 2020
Combining disease expression signatures with LINCS small molecule prediction software can identify promising preclinical drug candidates for TAO. These findings may offer insight into future potential therapeutic options for TAO and demonstrate a streamlined model to predict drug candidates for other diseases.
- | tozasertib (MK-0457) / Vertex, Merck (MSD)
Journal: RIPK1-dependent cell death: a novel target of the Aurora kinase inhibitor Tozasertib (VX-680). (Pubmed Central) - Sep 18, 2019
The potency ranking of the newly derived Tozasertib analogues and their specificity profile, as observed in cellular assays, coincide with ADP-Glo recombinant kinase activity assays. Overall, we show that Tozasertib not only targets Aurora kinases but also RIPK1 independently, and that we could generate analogues with increased selectivity to RIPK1 or Aurora kinases, respectively.
- MLN8054 / Takeda
Enrollment change, Metastases: A Phase 1 Trial of Extended MLN8054 Dosing in Patients With Advanced Malignancies (clinicaltrials.gov) - Sep 19, 2013
P1, N=44, Terminated, Sponsor: Millennium Pharmaceuticals, Inc.
Overall, we show that Tozasertib not only targets Aurora kinases but also RIPK1 independently, and that we could generate analogues with increased selectivity to RIPK1 or Aurora kinases, respectively. N=60 --> 44