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- | sirolimus / Generic mfg.
Journal: Antascomicin B stabilizes FKBP51-Akt1 complexes as a molecular glue. (Pubmed Central) - Apr 22, 2024
Antascomicin B is a natural product that similarly to the macrolides FK506 and Rapamycin binds to the FK506-binding protein 12 (FKBP12)...Our studies show that molecules with molecular glue-like properties are more prominent in nature than previously thought. We predict the existence of additional 'orphan' molecular glues that evolved to induced ternary protein complexes but where the relevant ternary complex partners are unknown.
- | Journal: Exploring the mechanism of levocarnitine in the treatment of epididymitis based on network pharmacology and molecular docking technology (Pubmed Central) - Apr 19, 2024
We predict the existence of additional 'orphan' molecular glues that evolved to induced ternary protein complexes but where the relevant ternary complex partners are unknown. This study revealed through network pharmacology that levocarnitine may act on multiple signaling pathways by targeting AKT1, HSP90AA1, ALB, CASP3, GSK3B, GSR, etc., thereby potentially exerting therapeutic effects on epididymitis.
- | Journal: Erratum: Overexpressed-eIF3I interacted and activated oncogenic Akt1 is a theranostic target in human hepatocellular carcinoma. (Pubmed Central) - Apr 17, 2024
This study revealed through network pharmacology that levocarnitine may act on multiple signaling pathways by targeting AKT1, HSP90AA1, ALB, CASP3, GSK3B, GSR, etc., thereby potentially exerting therapeutic effects on epididymitis. No abstract available
- | Preclinical, Journal: Protective Effects and Mechanisms of Luteolin against Acute Respiratory Distress Syndrome: Network Pharmacology and In vivo and In vitro Studies. (Pubmed Central) - Apr 15, 2024
No abstract available Luteolin could reduce the production of reactive oxygen species and inflammatory factors by inhibiting the AKT/NF-?B signaling pathway, thus reducing apoptosis and attenuating ARDS.
- | LY294002 / Eli Lilly
Preclinical, Journal, IO biomarker: Daphnetin alleviates silica-induced pulmonary inflammation and fibrosis by regulating the PI3K/AKT1 signaling pathway in mice. (Pubmed Central) - Apr 13, 2024
When the A549 cells were pretreated with LY294002, the protective effect of DAP on silica-induced injury was lost. In conclusion, the results of this study suggest that DAP alleviates pulmonary inflammation and fibrosis induced by silica by modulating the PI3K/AKT1 signaling pathway, and holds promise as a potentially effective treatment for silicosis.
- | Journal: Antidiabetic potency and molecular insights of natural products bearing indole moiety: A systematic bioinformatics investigation targeting AKT1. (Pubmed Central) - Apr 13, 2024
Furthermore, molecular dynamic simulation at 100?ns, physicochemical analysis, pharmacokinetics, toxicity assessment, and drug-likeness evaluation suggested that HERD_A and penerpene PENE_D were the most potent inhibitors against AKT1 compared to koenimbine (most potential based on the recorded IC50 value) and murrayakonine_A (most potential based on the docking score). In summary, HERD_A and/or PENE_D have the potential to be used as alternative therapeutic agent for the treatment of diabetes after some pharmacological investigation.
- ||| ipatasertib (RG7440) / Roche
Trial termination, Metastases: IPATunity150: A Study of Ipatasertib Plus Palbociclib and Fulvestrant Versus Placebo Plus Palbociclib and Fulvestrant in Hormone Receptor Positive and HER2 Negative Locally Advanced Unresectable or Metastatic Breast Cancer (clinicaltrials.gov) - Apr 4, 2024
P3, N=20, Terminated, Sponsor: Hoffmann-La Roche
In summary, HERD_A and/or PENE_D have the potential to be used as alternative therapeutic agent for the treatment of diabetes after some pharmacological investigation. Completed --> Terminated; The decision to not open the Phase III portion was based on a strategic sponsor decision and not driven by any safety concerns.
- | chloroquine phosphate / Generic mfg.
Journal: Oleuropein activates autophagy to circumvent anti-plasmodial defense. (Pubmed Central) - Apr 2, 2024
The findings with MII prompted us to detect the antimalarial activity of OLP in the wild type (3D7), D10-expressing GFP-Atg18 parasite, and chloroquine-resistant (Dd2) parasite...The molecular docking of autophagy-related proteins, investigations with MMI, and parasite inhibition assays indicated that the host activated the autophagy to survive OLP pressure. The challenge model of P.
- || Review, Journal: Targeting the PI3K/AKT signaling pathway in anticancer research: a recent update on inhibitor design and clinical trials (2020-2023). (Pubmed Central) - Apr 1, 2024
Development of PROTACs of PI3K? or AKT helps to reduce off-target toxicities.
- | Journal: Selectivity Studies and Free Energy Calculations of AKT Inhibitors. (Pubmed Central) - Apr 1, 2024
The docking data suggested that AKT1 binding may require residues Asn54, Trp80, Tyr272, Asp274, and Asp292, whereas AKT2 binding would expect residues Phe163 and Glu279, and AKT3 binding would favor residues Glu17, Trp79, Phe306, and Glu295. These findings may help guide AKT1-selective or AKT3-selective molecular design while sparing the inhibition of AKT2 to minimize the cutaneous toxicity.
- | ropivacaine / Generic mfg.
Journal: Ropivacaine as a novel AKT1 specific inhibitor regulates the stemness of breast cancer. (Pubmed Central) - Mar 29, 2024
These findings may help guide AKT1-selective or AKT3-selective molecular design while sparing the inhibition of AKT2 to minimize the cutaneous toxicity. Our finding revealed that local anesthetic ropivacaine attenuated breast cancer stemness through AKT1/GGT1/NF-?B signaling pathway, suggesting the potential clinical value of ropivacaine in breast cancer treatment.
- || Review, Journal, Metastases: Best of the year: Advanced breast cancer in 2023. (Pubmed Central) - Mar 27, 2024
- | Preclinical, Journal: Investigating the structural basis of piperine targeting AKT1 against prostate cancer through in (Pubmed Central) - Mar 26, 2024
Overall, the observed results confirmed the anti-PCa effect of piperine by causing effective DNA damage and proved to be genotoxic in nature against the human PCa. These effects may impede the downstream activities of Akt1 and result in PCa cell growth regression.Communicated by Ramaswamy H. Sarma.
- Potential of AKT1, ERBB2, ESR1, KRAS, PIK3CA and TP53 alterations detected by a new NGS assay on liquid biopsy predictive of early response/resistance to hormonal therapy and CDK4/6 inhibitors. (Exhibition area) - Mar 19, 2024 - Abstract #ESMOBC2024ESMO_BC_320;
- | Journal: Elucidating the anti-hypertensive mechanisms of Uncaria rhynchophylla-Alisma plantago-aquatica L: an integrated network pharmacology, cluster analysis, and molecular docking approach. (Pubmed Central) - Mar 18, 2024
However, the study acknowledges its limitations, including the reliance on in silico analyses and the need for in vivo validation. These findings pave the way for future clinical research, aiming to integrate traditional medicine insights with contemporary scientific approaches for developing innovative hypertension therapies.
- | Journal, BRCA Biomarker, PARP Biomarker: AKT1 interacts with DHX9 to mitigate R-loop-induced replication stress in ovarian cancer. (Pubmed Central) - Mar 18, 2024
Moreover, DHX9 was upregulated in tumors from PARPi-resistant BRCAm HGSOC patients, and high co-expression of DHX9 and AKT1 correlated with worse survival. Together, this study reveals an interaction between AKT1 and DHX9 that facilitates R-loop resolution and identifies combining ATRi and AKTi as a rational treatment strategy for BRCAm HGSOC irrespective of PARPi resistance status.
- | Journal: Molecular docking, ADMET profiling of gallic acid and its derivatives (N-alkyl gallamide) as apoptosis (Pubmed Central) - Mar 15, 2024
The ADMET profile of the N-alkyl gallamide compound is predictable and shows a good profile as a candidate for anticancer drugs. Conclusion N-octyl gallamide, N-ters-butyl gallamide, and N-isoamil gallamide have potential as anti-breast cancer agents.
- | Journal: Cyclocodon lancifolius fruit prolongs the lifespan of Caenorhabditis elegans via antioxidation and regulation of purine metabolism. (Pubmed Central) - Mar 14, 2024
Metabolomics analysis revealed that purine metabolism is a key regulatory pathway for CF to exert anti-aging effects. The present study suggests that C. lancifolius fruit has potential for use as a functional food to enhance antioxidant capacity and delay aging.
- | simvastatin / Generic mfg., lovastatin / Generic mfg., dactinomycin / Generic mfg.
Journal: Statin-Sensitive Akt1/Src/Caveolin-1 Signaling Enhances Oxidative Stress Resistance in Rhabdomyosarcoma. (Pubmed Central) - Mar 13, 2024
Taken together, our findings suggest that the molecularly linked signature formed by Akt1, Src, Cav1, and catalase may represent a prognostic determinant for identifying subgroups of RMS patients with higher probability of recurrence after radiotherapy. Furthermore, statin-induced oxidative stress could represent a treatment option to improve the success of radiotherapy.
- | Journal: Identification of novel AKT1 inhibitors from Sapria himalayana bioactive compounds using structure-based virtual screening and molecular dynamics simulations. (Pubmed Central) - Mar 12, 2024
Furthermore, statin-induced oxidative stress could represent a treatment option to improve the success of radiotherapy. Further, MD simulation and PCA analyses showed
- Piqray (alpelisib) / Novartis, Truqap (capivasertib) / Otsuka, AstraZeneca
Indirect Treatment Comparison of Efficacy and Safety of Capivasertib-Fulvestrant Versus Alpelisib-Fulvestrant for PIK3CA-Altered, HR-Positive, Advanced Breast Cancer after Disease Progression Following Endocrine-Based Therapy () - Mar 8, 2024 - Abstract #ISPOR2024ISPOR_494;
P3
Results indicate that for patients with HR-positive, HER2-negative, PIK3CA -altered aBC capivasertib-fulvestrant has numerically improved PFS and a high probability of being more efficacious than alpelisib-fulvestrant with an overall more favourable safety profile. Results are exploratory and subject to limitations.
- Associations of Renin-Angiotensin-System Inhibitor Use with Brain Insulin Signaling and Neuropathology (Colorado Convention Center | Exhibit Hall B-E) - Mar 8, 2024 - Abstract #AAN2024AAN_2426;
Results are exploratory and subject to limitations. These findings suggest that late-life RAS inhibitor use is associated with less insulin resistance and less accumulation of tau tangles in postmortem brain of older individuals.
- Effects of AKT1, 2, and 3 knock-out by CRISPR-Cas9 in CD133+human melanoma stem cells treated with MEK and AKT inhibitors (Section 54) - Mar 5, 2024 - Abstract #AACR2024AACR_8965;
These findings suggest that late-life RAS inhibitor use is associated with less insulin resistance and less accumulation of tau tangles in postmortem brain of older individuals. Abstract is embargoed at this time.
- Truqap (capivasertib) / Otsuka, AstraZeneca
Mechanisms of acquired resistance to AKT inhibitor capivasertib in AKT1 mutant patient derived breast cancer models (Section 54) - Mar 5, 2024 - Abstract #AACR2024AACR_8963;
Abstract is embargoed at this time. Abstract is embargoed at this time.
- Torisel (temsirolimus) / Pfizer
Temsirolimus (T) in patients (pts) with solid tumors with AKT1/3 amplification (amp) or mutation (mut): Results from the Targeted Agent and Profiling Utilization Registry (TAPUR) Study (Section 48) - Mar 5, 2024 - Abstract #AACR2024AACR_7899;
Abstract is embargoed at this time. Abstract is embargoed at this time.
- ICA-1 / University of South Florida
PKC-?/? signaling is crucial for apoptosis/pyroptosis inhibition and invasiveness of glioblastoma cells through upregulation of ?-catenin, PDK1/Akt1 and Smad cascades via 14-3-3 (Section 16) - Mar 5, 2024 - Abstract #AACR2024AACR_7079;
Intravenous and oral administration of ICA-1S resulted in the reduction of tumor growth by approximately 30% in athymic nude mice for U-87 xenografts. Taken together, these results suggest that not only do aPKCs play a central role in GB progression, invasiveness, and cell survival, but that effective therapeutics can be developed to specifically target oncogenic aPKCs.
- Mychexin (WGI-0301) - Zhejiang Haichang Bio / Tech
Anti-tumor effect of the combination of a lipid nanoparticle suspension of an AKT-1 antisense oligonucleotide (WGI-0301) with tyrosine kinase inhibitors in an orthotopic murine tumor model (Section 25) - Mar 5, 2024 - Abstract #AACR2024AACR_5384;
The combination of WGI-0301 with TKIs demonstrated superior anti-tumor efficacy over TKI monotherapy in the absence of substantial increase in toxicity. This finding warrants further robust clinical investigation in patients with advanced HCC.
- ALTA-2618 / Alterome Therap
Discovery of ALTA-2618, the first allosteric, mutant-selective targeted therapy for AKT1 E17K driven cancers (Section 52) - Mar 5, 2024 - Abstract #AACR2024AACR_4751;
This finding warrants further robust clinical investigation in patients with advanced HCC. Abstract is embargoed at this time.
- enzalutamide capsule / Generic mfg.
Cyclin D1 induces Akt1 activity in RB deficient prostate cancer (Section 13) - Mar 5, 2024 - Abstract #AACR2024AACR_4244;
Curr Med Chem Anticancer Agents 2005; 5:575-892. (2) Stoyanova T, et al.
- Akt1 and Cyclin D1 govern polarity of self-renewing divisions in breast cancer stem cells (Section 10) - Mar 5, 2024 - Abstract #AACR2024AACR_3217;
Cell-Autonomous versus Systemic Akt Isoform Deletions Uncovered New Roles for Akt1 and Akt2 in Breast Cancer. Mol Cell 2020; 80:87-101 e5
- | Journal: Polo-like kinase 4 promotes tumorigenesis and glucose metabolism in glioma by activating AKT1 signaling. (Pubmed Central) - Mar 5, 2024
Additionally, the expression of PLK4 protein exhibited a positive correlation with AKT1 phosphorylation in glioma patient tissues. These findings highlight the pivotal role of PLK4-mediated phosphorylation of AKT1 in glioma tumorigenesis and dysregulation of glucose metabolism.
- | Psoralen / EMD Serono
Journal: Exploring quality evaluation markers of Fructus Psoraleae based on chemometric analysis integrated with network pharmacology. (Pubmed Central) - Mar 4, 2024
These findings highlight the pivotal role of PLK4-mediated phosphorylation of AKT1 in glioma tumorigenesis and dysregulation of glucose metabolism. The study not only provides a reference for the improvement of quality control of FP but also offers a theoretical basis for its further in-depth research in osteoporosis.
- | Journal: WRKY6 transcription factor modulates root potassium acquisition through promoting expression of AKT1 in Arabidopsis. (Pubmed Central) - Feb 28, 2024
Further transcriptome profiling suggested that WRKY6 modulates LK response through a complex regulatory network. Thus, this study unveils a transcription factor that modulates root growth under potassium deficiency conditions by affecting the potassium channel gene AKT1 expression.
- | Truqap (capivasertib) / Otsuka, AstraZeneca
Journal: A gain of function mutation in AKT1 increases hexokinase 2 and diminishes oxidative stress in meningioma. (Pubmed Central) - Feb 26, 2024
Treatment with the conventional drug of choice AZD5363 (a pan AKT inhibitor) enhanced cell death and diminished HK2 levels in AKT1 mutants...By affecting metabolism, inflammation, and redox homeostasis AKT1-E17K confers a survival advantage in meningioma cells. Our findings suggest that targeting AKT-HK2 cross-talk to induce ROS-dependent cell death could be exploited as novel therapeutic approach in meningiomas.
- | Preclinical, Journal: Yangyinghuoxue decoction exerts a treatment effect on hepatic fibrosis by PI3K/AKT pathway in rat model: based on the network pharmacology and molecular docking. (Pubmed Central) - Feb 16, 2024
The mechanisms of YYHXD against liver fibrosis were involved in multiple ingredients, multiple targets and multiple signaling pathways. The PI3K/Akt pathway could be the most important pharmacological mechanism of YYHXD therapy for liver fibrosis.
- |||| Truqap (capivasertib) / Otsuka, AstraZeneca
Trial completion date, Trial primary completion date, Metastases: Capivasertib + CDK4/6i + Fulvestrant for Advanced/Metastatic HR+/HER2- Breast Cancer (CAPItello-292) (clinicaltrials.gov) - Feb 15, 2024
P3, N=895, Recruiting, Sponsor: AstraZeneca
The PI3K/Akt pathway could be the most important pharmacological mechanism of YYHXD therapy for liver fibrosis. Trial completion date: Nov 2028 --> Aug 2029 | Trial primary completion date: Aug 2026 --> Nov 2027
- | Journal: Design, synthesis and anticancer evaluation of some novel 7-hydroxy-4-methyl-3-substituted benzopyran-2-one derivatives. (Pubmed Central) - Feb 14, 2024
Results & Compounds 3b, 3c, 3j, 7 and 8 were the most active. Compounds 3c and 8 showed remarkable inhibitory action against PI3K and Akt-1 enzymes, and both are promising candidates for treatment of breast cancer.
- AKT1, ERBB2, ESR1, KRAS, PIK3CA and TP53 alteration detection by a new ctDNA assay in plasma of patients with hormone receptor positive (HR+)/HER2- advanced Breast Cancer treated with hormonal therapy and CDK4/6 inhibitors (Room Exhibition) - Feb 13, 2024 - Abstract #EBCC2024EBCC_436;
- | Journal: Chinese herb couple against diabetes: integrating network pharmacology and mechanism study. (Pubmed Central) - Feb 12, 2024
Finally, the animal experiments showed that Cassia twig-Astragalus could improve the body weight, blood glucose and glucose tolerance in diabetic rats. After the intervention with Cassia twig-Astragalus, the inflammatory factors (IL-10, TNF-?, IL-6) were significantly improved in diabetic rats, which also effectively reduced TG and TC.Communicated by Ramaswamy H. Sarma.
- || Review, Journal: Mitochondrial Signaling, the Mechanisms of AKI-to-CKD Transition and Potential Treatment Targets. (Pubmed Central) - Feb 10, 2024
We review the recent findings of the development of AKI-to-CKD transition with a focus on mitochondrial disorders in PTCs. We propose that mitochondrial signaling is a key mechanism of the progression of AKI to CKD and potential targeting for treatment.
- | Journal: Insulin-like growth factor 2 mRNA-binding protein 3 enhanced melanoma migration through regulation of AKT1 and RELA expression. (Pubmed Central) - Feb 2, 2024
Human melanoma samples with high IMP-3 levels also showed high HMGA2, AKT1 and RELA expression. Our results show that IMP-3 enhances melanoma cell migration through the regulation of the AKT1 and RELA axis.
- | Journal: Exploring the Potential Role of Massa Medicata Fermentata in Alcoholic Liver Injury Disease Based on Network Pharmacology and Animal Experiments. (Pubmed Central) - Feb 1, 2024
This study serves as a rationale to support MMF in the treatment of ALD and meets the urgent need for clinical treatment of ALD. At the same time, it broadens the scope of clinical application of MMF.
- | Piqray (alpelisib) / Novartis, ICA-1 / University of South Florida
Journal: Dual inhibition of atypical PKC signaling and PI3K/Akt signaling dysregulates c-Myc to induce apoptosis in clear cell Renal Cell Carcinoma. (Pubmed Central) - Jan 30, 2024
Therefore, implementing a combination of Alpelisib and a PKC-? inhibitor is an effective approach to reducing cell proliferation, and invasion that eventually induces apoptosis and may be considered as a potential therapeutic option in ccRCC.
- | Journal: Study of Drug Targets Associated With Oncogenesis and Cancer Cell Survival and the Therapeutic Activity of Engineered Ashwagandha Extract Having Differential Withanolide Constitutions. (Pubmed Central) - Jan 28, 2024
Further in-depth investigations are required to fully explore the potency and pharmacology of this novel extract. This study also highlights the importance of the standardization of herbal extracts to get consistent therapeutic activity for the disease indication.
- || Clinical, Journal: Genetic characterization and mutational profiling of foramen magnum meningiomas: a multi-institutional study. (Pubmed Central) - Jan 26, 2024
These findings provide important insights into the molecular genetics and clinicopathological characteristics of FM meningiomas. The identification of specific genetic alterations associated with tumor location, volume, calcification, histology, and sex at diagnosis may have implications for personalized treatment strategies in the future.
- | Journal: Phellinus linteus activates Treg cells via FAK to promote M2 macrophage polarization in hepatocellular carcinoma. (Pubmed Central) - Jan 23, 2024
Overall, our findings suggest that FAK promotes HCC via Treg cells that polarize macrophages toward the M2 type through specific signaling pathways. PL, acting through FAK, could be a protective therapy against HCC.
- Truqap (capivasertib) / Otsuka, AstraZeneca
Capivasertib in Hormone Receptor-Positive Advanced Breast Cancer () - Jan 22, 2024 - Abstract #YIR2024YIR_37;
PL, acting through FAK, could be a protective therapy against HCC. Capivasertib-fulvestrant therapy resulted in significantly longer progression-free survival than treatment with fulvestrant alone among patients with hormone receptor-positive advanced breast cancer whose disease had progressed during or after previous aromatase inhibitor therapy with or without a CDK4/6 inhibitor.
- | Journal: Akt1 is involved in HCV release by promoting endoplasmic reticulum-to-endosome transition of infectious virions. (Pubmed Central) - Jan 22, 2024
Capivasertib-fulvestrant therapy resulted in significantly longer progression-free survival than treatment with fulvestrant alone among patients with hormone receptor-positive advanced breast cancer whose disease had progressed during or after previous aromatase inhibitor therapy with or without a CDK4/6 inhibitor. Our study demonstrates that Akt1 has an impact on the lipogenesis pathway and plays a critical role in the assembly and secretion of infectious HCV.
- | ipatasertib (RG7440) / Roche
Preclinical, Journal: Discovery of novel Akt1 inhibitors by an ensemble-based virtual screening method, molecular dynamics simulation, and in vitro biological activity testing. (Pubmed Central) - Jan 19, 2024
Our study demonstrates that Akt1 has an impact on the lipogenesis pathway and plays a critical role in the assembly and secretion of infectious HCV. The average binding free energies for the Akt1-CQU, Akt1-Ipatasertib, and Akt1-Hit9 systems were - 34.44, - 63.37, and - 39.14
- | Preclinical, Journal: Hypericum perforatum L. protects against renal function decline in ovariectomy rat model by regulating expressions of NOS3 and AKT1 in AGE-RAGE pathway. (Pubmed Central) - Jan 17, 2024
The average binding free energies for the Akt1-CQU, Akt1-Ipatasertib, and Akt1-Hit9 systems were - 34.44, - 63.37, and - 39.14 Our findings indicated that HPL regulated expression of AKT1 and NOS3 through modulating AGE-RAGE signaling pathway in OVX stimulated rats` renal dysfunction, implicating the potential values of HPL in menopause syndromes therapy.