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- | A 443654 / AbbVie
Journal: 5,7-Dihydroxy-4-Methylcoumarin enhances osteogenesis and ameliorates osteoporosis via the AKT1 pathway. (Pubmed Central) - Feb 23, 2025
Co-treatment with the AKT1 inhibitor A-443654 abolished the anti-osteoporotic effects of D4M. These findings demonstrate that D4M enhances osteoblast differentiation and mitigates osteoporosis through its interaction with AKT1, suggesting its potential as a therapeutic agent for treating osteoporosis.
- | A 443654 / AbbVie
Journal: The effect of AKT inhibition in ?-synuclein-dependent neurodegeneration. (Pubmed Central) - Feb 20, 2025
We observed that administration of the AKT inhibitor, A-443654 led to mild improvements in both survival and motor function in flies expressing human ?-Syn...The protective effects of AKT reduction appear to operate through the fly ortholog of NF-?B, Relish, suggesting a link between AKT and NF-?B in regulating ?-Syn levels. These findings highlight the AKT cascade as a potential therapeutic target for synucleinopathies and provide insights into mechanisms that could be utilized to reduce ?-Syn toxicity in PD and related disorders, such as multiple system atrophy.
- | CHIR-124 / Novartis, Lynparza (olaparib) / Merck (MSD), AstraZeneca, A 443654 / AbbVie
Journal, BRCA Biomarker, PARP Biomarker: A high-throughput approach to identify BRCA1-downregulating compounds to enhance PARP inhibitor sensitivity. (Pubmed Central) - Jul 12, 2024
Three compounds, N-acetyl-N-acetoxy chlorobenzenesulfonamide (NANAC), A-443654, and CHIR-124, were validated to reduce BRCA1 protein levels and sensitize breast cancer cells to the toxic effects of olaparib. These results suggest that BRCA1-HiBiT reporter cells hold promise in developing agents to improve the clinical utility of PARPi.
- | OTS167 / OncoTherapy, A 443654 / AbbVie
Journal, Cancer stem: AI identifies potent inducers of breast cancer stem cell differentiation based on adversarial learning from gene expression data. (Pubmed Central) - May 3, 2024
Experimental validation in MDA-MB-231 and MCF7 cells demonstrated the efficacy of five out of six tested molecules among those scored highest by the model. In particular, the efficacy of triptolide, OTS-167, quinacrine, granisetron and A-443654 offer a potential avenue for targeted therapies against breast CSCs.
- A 443654 / AbbVie
Exploring the Potential of Akt Modulator A-443654 as a Therapeutic Approach for Parkinson's Disease: Insights from Drosophila melanogaster Models (WCC Halls A-C) - Nov 3, 2023 - Abstract #Neuroscience2023NEUROSCIENCE_11571;
Our findings provide evidence that the Akt modulator A-443654 may hold potential as a treatment for PD, as demonstrated in the enhanced longevity in the fly models subjected to ?-synuclein toxicity. These results serve as a pilot study for further exploration in mouse models of PD, paving the way for future investigation of a promising direction of therapeutic intervention for PD.
- | Rubraca (rucaparib) / Pharma& Schweiz, A 443654 / AbbVie
Journal: Constructing a prognostic model for head and neck squamous cell carcinoma based on glucose metabolism related genes. (Pubmed Central) - Oct 29, 2023
Our study highlights the significant association of five prognosis-related genes (MTHFD2, CDKN2A, TPM2, MPZ, and DNMT1) with HNSC. These findings provide further evidence of the crucial role of GMRGs in HNSC.
- | Journal, IO biomarker: Predicting response of immunotherapy and targeted therapy and prognosis characteristics for renal clear cell carcinoma based on m1A methylation regulators. (Pubmed Central) - Aug 9, 2023
Finally, polymerase chain reaction (PCR) showed the expression of YTHN6-Methyladenosine RNA Binding Protein 1[YTHDF1], TRNA Methyltransferase 61B [TRMT61B], TRNA Methyltransferase 10C [TRMT10C] and AlkB Homolog 1[ALKBH1] in ccRCC cell lines. To sum up, the prognosis risk model we created not only has good predictive value, but also can provide guidance for accurately predicting the prognosis of ccRCC.
- | A 443654 / AbbVie
Journal: Eurycomanone stimulates bone mineralization in zebrafish larvae and promotes osteogenic differentiation of mesenchymal stem cells by upregulating AKT/GSK-3?/?-catenin signaling. (Pubmed Central) - Jul 17, 2023
To sum up, the prognosis risk model we created not only has good predictive value, but also can provide guidance for accurately predicting the prognosis of ccRCC. Eventually in vitro, the effect of EN on cell viability, osteogenesis activities were investigated in human bone marrow mesenchymal stem cells (hMSCs) and C3H10
- | A 443654 / AbbVie
Biomarker, Journal, Tumor mutational burden, IO biomarker, Immunomodulating: A risk model constructed using 14 N-methyladenosine-related lncRNAs as a new prognostic marker that correlates with the immunomodulatory effect and drug sensitivity in colorectal cancer. (Pubmed Central) - Jul 12, 2023
We constructed a risk model based on 14 mA-related lncRNAs that could predict the prognosis of patients with CRC and provided additional therapeutic ideas for their treatment. These findings may additionally serve as a foundation for further studies on regulating CRC via mA-related lncRNAs.
- | A 443654 / AbbVie
Biomarker, Journal, IO biomarker: Bioinformatics prediction and experimental verification identify cuproptosis-related lncRNA as prognosis biomarkers of hepatocellular carcinoma. (Pubmed Central) - Jul 10, 2023
And proliferative, migratory and invasion abilities of HCC cell were restrained via silencing CAlncRNAs expression in vitro. In summary, we built a CAlncRNAs-based risk score model, which can be a candidate for HCC patients prognostic prediction and offer some useful information for immunotherapies.
- | A 443654 / AbbVie
Biomarker, Journal: System analysis based on the pyroptosis-related genes identifies GSDMC as a novel therapy target for pancreatic adenocarcinoma. (Pubmed Central) - Oct 13, 2022
Our result suggest that GSDMC may promote the proliferation and migration of PAAD cell lines. These findings may provide new insights into the roles of pyroptosis-related genes in PAAD, and offer new therapeutic targets for the treatment of PAAD.
- | Journal, Gene Signature, PARP Biomarker, IO biomarker: Machine Learning Screens Potential Drugs Targeting a Prognostic Gene Signature Associated With Proliferation in Hepatocellular Carcinoma. (Pubmed Central) - Jul 17, 2022
The five-gene signature associated with proliferation can be used for survival prediction and risk stratification for HCC patients. Potential drugs targeting this gene signature deserve further attention in the treatment of HCC.
- | Biomarker, Journal: Integrative pharmacogenomics revealed three subtypes with different immune landscapes and specific therapeutic responses in lung adenocarcinoma. (Pubmed Central) - Jul 15, 2022
Finally, our study provided subtype-guided personalized treatment strategies: Immune checkpoint blockers (ICBs), doxorubicin, tipifarnib, AZ628, and AZD6244 were for S-Ⅰ; Cisplatin, camptothecin, roscovitine, and A.443654 were for S-Ⅱ; Docetaxel, paclitaxel, vinorelbine, and BIBW2992 were for S-III. We provided a novel molecular classification strategy and revealed three pharmacogenomics-based subtypes for LUAD patients, which uncovered potential subtype-related and patient-specific therapeutic strategies.
- | Preclinical, Journal, Tumor Mutational Burden, Tumor microenvironment: Prognostic Value of Drug Targets Predicted Using Deep Bioinformatic Analysis of m6A-Associated lncRNA-Based Pancreatic Cancer Model Characteristics and Its Tumour Microenvironment. (Pubmed Central) - May 14, 2022
Eight sensitive drugs were screened: ABT.888, ATRA, AP.24534, AG.014699, ABT.263, axitinib, A.443654, and A.770041. We screened m6A-related lncRNAs using bioinformatics, constructed a prognosis-related model, explored TMB and immune function differences in pancreatic cancer, and identified potential therapeutic agents, providing a foundation for further studies of pancreatic cancer diagnosis and treatment.
- | Biomarker, Journal, IO biomarker: Identification of Fatty Acid Metabolism-Related lncRNAs as Biomarkers for Clinical Prognosis and Immunotherapy Response in Patients With Lung Adenocarcinoma. (Pubmed Central) - Apr 26, 2022
We constructed a 7-lncRNA prognostic model to predict the OS of patients with LUAD. In addition, the predictive nomogram model based on our established seven fatty acid metabolism-related lncRNA signatures provides better clinical value than that of the traditional TNM staging system in predicting the prognosis of patients with LUAD and presents new insights for personalized treatment.
- | cisplatin / Generic mfg., temozolomide / Generic mfg.
Journal, IO biomarker: The Role of m5C-Related lncRNAs in Predicting Overall Prognosis and Regulating the Lower Grade Glioma Microenvironment. (Pubmed Central) - Apr 5, 2022
The high-risk group was more sensitive to anti-CTLA4 therapy and to compounds including Temozolomide, Bleomycin, Cisplatin, Cyclopamine, A.443654 (Akt inhibitor), AZD6482 (PI3K inhibitor), GDC0941(PI3K inhibitor), and metformin. We present for the first time a m5C-related lncRNA signature for lower grade glioma patient prognosis and therapy response prediction with validated performance, providing a promising target for future research.
- | A 443654 / AbbVie
Journal: The AKT modulator A-443654 reduces α-synuclein expression and normalizes ER stress and autophagy. (Pubmed Central) - Nov 29, 2021
A-443654 also decreased the expression of DCLK1, an inhibitor of α-synuclein lysosomal degradation. Our study identifies A-443654 and AKT inhibition as a potential strategy for reducing SNCA expression and preventing PD pathology.
- | bicalutamide / Generic mfg.
Journal, PD(L)-1 Biomarker, IO biomarker: Comprehensive Analysis Identifies Potential Ferroptosis-Associated mRNA Therapeutic Targets in Ovarian Cancer. (Pubmed Central) - Mar 23, 2021
Our study characterized two ferroptosis-related subtypes with distinct prognosis and tumor immune features, which could assist clinicians make decisions and individual therapy. Moreover, 15 ferroptosis-related mRNAs were identified, which could become potential therapeutic targets for ovarian cancer.
- | A 443654 / AbbVie
Preclinical, Journal: GPR30-mediated estrogenic regulation of actin polymerization and spatial memory involves SRC-1 and PI3K-mTORC2 in the hippocampus of female mice. (Pubmed Central) - Oct 11, 2020
Moreover, 15 ferroptosis-related mRNAs were identified, which could become potential therapeutic targets for ovarian cancer. Taking together, these results demonstrated that decreased GPR30 induces actin depolymerization through SRC-1 and PI3K/mTORC2 pathways and ultimately impairs learning and memory, indicating its potential role as a therapeutic target against hippocampus-based, E2-related memory impairments.
- | doxycycline / Generic mfg., Pierre Fabre, gentamicin sulfate / Generic mfg.
Journal: A new advanced in silico drug discovery method for novel coronavirus (SARS-CoV-2) with tensor decomposition-based unsupervised feature extraction. (Pubmed Central) - Sep 30, 2020
Taking together, these results demonstrated that decreased GPR30 induces actin depolymerization through SRC-1 and PI3K/mTORC2 pathways and ultimately impairs learning and memory, indicating its potential role as a therapeutic target against hippocampus-based, E2-related memory impairments. The drugs screened using our strategy may be effective candidates for treating patients with COVID-19.
- | A 443654 / AbbVie
Journal: Aurora kinase A promotes hepatitis B virus replication and expression. (Pubmed Central) - Jul 29, 2020
We found that viral replication in infected or transfected hepatoma cell was markedly inhibited by treatment with A-443654, a specific inhibitor of Akt...Our data indicated that Aurora kinase A enhances viral replication and expression independently of its kinase activity required for mitotic function. Our findings suggest that mitotic kinases, considered to be an attractive target of antitumor agents, also provide a novel target for the development of antiviral therapy.
- | quercetin (LY294002) / Eli Lilly, A 443654 / AbbVie
Journal: MT1-MMP downregulation via the PI3K/Akt signaling pathway is required for the mechanical stretching-inhibited invasion of bone-marrow-derived mesenchymal stem cells. (Pubmed Central) - May 27, 2020
In addition, the upregulation of Akt phosphorylation by a pharmacological activator (SC79) increased MT1-MMP expression and suppressed mechanical stretching-reduced BMSC invasion. Taken together, our results suggest that mechanical stretching inhibits BMSC invasion by downregulating MT1-MMP expression by suppressing the PI3K/Akt signaling pathway.
- | A 443654 / AbbVie
Journal: Nuclear and membrane estrogen receptor antagonists induce similar mTORC2 activation-reversible changes in synaptic protein expression and actin polymerization in the mouse hippocampus. (Pubmed Central) - May 29, 2019
Taken together, our results suggest that mechanical stretching inhibits BMSC invasion by downregulating MT1-MMP expression by suppressing the PI3K/Akt signaling pathway. nERs and mER contribute similarly to the changes in proteins and structures associated with synaptic plasticity, and mTORC2 may be a novel target of hippocampal-dependent dementia such as Alzheimer's disease as proposed by previous studies.