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1d
Integrated multi-omics analysis suggests the involvement of PI3K-Akt/p21 signaling in the anti-colorectal cancer effects of Diaphragma Juglandis Fructus extract. (PubMed, Front Pharmacol)
Functional relevance of AKT signaling was evaluated using siRNA knockdown, MK2206, and SC79...EEDJF exerts anti-colorectal cancer effects in vitro, potentially associated with regulation of PI3K-Akt/p21 signaling. These findings provide a basis for further studies on the bioactive constituents, pharmacological mechanisms, and in vivo efficacy of DJF-derived preparations.
Journal
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EGFR (Epidermal growth factor receptor) • CDKN1A (Cyclin-dependent kinase inhibitor 1A)
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MK-2206
1d
GOLPH3 promotes prostate adenocarcinoma cell proliferation by enhancing PI3K/AKT/mTOR-associated glucose metabolism. (PubMed, Tissue Cell)
GOLPH3, which is overexpressed in PRAD, may enhance glucose metabolic activity in PRAD cells in association with activation of the PI3K/AKT/mTOR pathway, thereby supporting PRAD cell proliferation. These findings provide basic mechanistic evidence for the role of GOLPH3 in PRAD cell metabolism, but further clinical studies are required to determine its prognostic or therapeutic relevance.
Journal
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LDHA (Lactate dehydrogenase A)
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LY294002
1d
MUC1 promotes the proliferation and invasion of lung cancer cells by regulating PI3K/AKT pathway. (PubMed, J Cardiothorac Surg)
Furthermore, the PI3K/AKT inhibitor LY294002 enhanced the effects of sh-MUC1 on the proliferation, apoptosis, migration, invasion and EMT progress, while the activator SC79 partially restored these effects...To conclude, these findings suggested that MUC1 played an important role in lung cancer progression, potentially through the PI3K/AKT pathway. This positioned MUC1 as a molecule worthy of further investigation for its therapeutic potential.
Journal • IO biomarker
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BCL2 (B-cell CLL/lymphoma 2) • MUC1 (Mucin 1) • MMP2 (Matrix metallopeptidase 2) • BAX (BCL2-associated X protein) • CASP3 (Caspase 3) • CASP9 (Caspase 9) • MMP9 (Matrix metallopeptidase 9)
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LY294002
1d
Budget impact analysis of capivasertib as a second-line therapy for advanced breast cancer in the United States. (PubMed, Expert Rev Pharmacoecon Outcomes Res)
These net costs amount to $0.88 per-member-per-month. While introduction of capivasertib could reduce adverse event and follow-up costs, it may result in an overall increase in payers' budget.
Journal • HEOR
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HER-2 (Human epidermal growth factor receptor 2) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog) • AKT1 (V-akt murine thymoma viral oncogene homolog 1)
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HER-2 negative
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Truqap (capivasertib)
2d
FUCA2 Sustains AKT Signaling and Suppresses Senescence by Antagonizing FUT3-Mediated ErbB3 Fucosylation in Lung Adenocarcinoma. (PubMed, Adv Sci (Weinh))
Notably, low-dose Capivasertib, an AKT inhibitor targeting tumors with PIK3CA/AKT1/PTEN mutation(s), induced senescence selectively in FUCA2-high LUAD irrespective of PIK3CA/AKT1/PTEN/TP53 mutational status, and its combination with the nutraceutical senolytic procyanidin C1 achieved potent and low-toxicity suppression of LUAD across multiple preclinical models. Together, our results uncover the FUCA2-ErbB3 fucosylation-AKT pathway as a central regulator of senescence and propose a FUCA2-guided drug repurposing strategy for LUAD.
Journal
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HER-2 (Human epidermal growth factor receptor 2) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3) • FUT3 (Fucosyltransferase 3)
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TP53 mutation • PIK3CA mutation • TP53 wild-type • PTEN mutation
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Truqap (capivasertib)
2d
EIF3B promotes oral squamous cell carcinoma progression via the PI3K/AKT pathway and is negatively regulated by miR-124-3p. (PubMed, Life Sci)
EIF3B activated PI3K/AKT signaling and EMT, both of which were abolished by miR-124-3p or LY294002. These findings define the miR-124-3p/EIF3B/PI3K-AKT axis as a key regulator of OSCC progression and suggest EIF3B as a potential prognostic biomarker and therapeutic target.
Journal
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MIR124-3 (MicroRNA 124-3)
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LY294002
3d
ADGRD1 promotes bladder cancer progression and angiogenesis via the PI3K/AKT/mTOR-mediated pro-angiogenic secretome. (PubMed, Front Oncol)
PI3K/AKT/mTOR pathway activity was examined by Western blot, and its function validated using SC79 (AKT activator) and LY294002 (PI3K inhibitor)...By modulating the PI3K/AKT/mTOR signaling axis and the pro-angiogenic microenvironment, ADGRD1 facilitates tumor growth and neovascularization. ADGRD1 may serve as a promising prognostic biomarker and therapeutic target for advanced BLCA.
Journal
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CXCL8 (Chemokine (C-X-C motif) ligand 8)
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LY294002
3d
Targeting the LY6H-PI3K/AKT autophagy axis suppresses HCC malignancy and reveals a druggable vulnerability. (PubMed, Cell Death Dis)
Functional assays in vitro, along with in vivo experiments utilizing the PI3K inhibitor LY294002, confirm that LY6H promotes HCC cell proliferation through a mechanism involving the PI3K/AKT pathway and autophagy...Immunohistochemical analyses reveal positive correlations among LY6H, ATG3, Beclin1, PI3K, and AKT expression in HCC tissues, and their co-overexpression predicts an adverse prognosis. Collectively, this work uncovers a critical regulatory role of the LY6H-p-PI3K-autophagy axis in HCC progression, elucidates the molecular mechanisms underlying LY6H-mediated oncogenic effects, and identifies NSC243928 as a promising therapeutic candidate for targeting LY6H in HCC.
Journal
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ATG3 (Autophagy Related 3) • BECN1 (Beclin 1)
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LY294002
4d
mTORC1/2 Inhibitor AZD2014 or the Oral AKT Inhibitor AZD5363 for Recurrent Endometrial and Ovarian (clinicaltrials.gov)
P1, N=159, Active, not recruiting, M.D. Anderson Cancer Center | Trial completion date: Jun 2026 --> Jun 2028 | Trial primary completion date: Jun 2026 --> Jun 2028
Trial completion date • Trial primary completion date
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ER (Estrogen receptor) • PGR (Progesterone receptor) • BRCA (Breast cancer early onset) • MUC16 (Mucin 16, Cell Surface Associated)
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BRCA mutation
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Lynparza (olaparib) • Truqap (capivasertib) • vistusertib (AZD2014)
9d
Personalized Targeted IMMUNOtherapy-based Regimens in Recurrent GASTric Adenocarcinoma (IMMUNOGAST) (clinicaltrials.gov)
P2, N=54, Completed, Hospices Civils de Lyon | Unknown status --> Completed | Trial completion date: Oct 2023 --> Jun 2026 | Trial primary completion date: Oct 2023 --> Jun 2026
Trial completion • Trial completion date • Trial primary completion date • Tumor mutational burden
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 overexpression
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Avastin (bevacizumab) • Tecentriq (atezolizumab) • ipatasertib (RG7440)
10d
From 2D to 3D Bioprinted In Vitro Breast Cancer Model: A Comparative Study of Proliferation, Tissue Structure, and mTOR Signaling. (PubMed, MedComm (2020))
In addition, mTOR pathway activity and responsiveness to mTOR inhibitors (rapamycin and ipatasertib) and chemotherapeutic agents (cisplatin) were assessed. Compared with 2D monolayer cultures, 3D TMSs exhibited reduced mTOR signaling activity, which led to significantly decreased sensitivity to mTOR inhibition. These findings indicate that 3D bioprinted breast cancer models recapitulate key structural and signaling features of in situ tumors more accurately than 2D systems, highlighting their potential value for preclinical drug testing and mechanistic studies.
Preclinical • Journal
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CTNNB1 (Catenin (cadherin-associated protein), beta 1) • CDH1 (Cadherin 1) • CDH2 (Cadherin 2)
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cisplatin • ipatasertib (RG7440)