AKT 

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  • ||||||||||  MK-2206 / Merck (MSD), Mekinist (trametinib) / Novartis, BeiGene
    Preclinical, Journal:  Biological and targeting differences between the rare KRAS A146T and canonical KRAS mutants in gastric cancer models. (Pubmed Central) -  Apr 15, 2024   
    Capivasertib can enhance anti-tumour effects of docetaxel by targeting residual docetaxel-persister cells, independent of PTEN status, to induce apoptosis and DNA damage in part through GSK3?. A deeper genomic and biological characterization of KRAS mutants might sustain the development of more efficient and long-lasting therapeutic options for patients harbouring KRAS-driven GC.
  • ||||||||||  CCT128930 / Otsuka
    Journal:  Structural basis of selective TRPM7 inhibition by the anticancer agent CCT128930. (Pubmed Central) -  Apr 14, 2024   
    Moreover, we demonstrate the principal role of several residues in the VL site enabling CCT to inhibit TRPM7 without impacting the homologous TRPM6 channel. Hence, our results uncover the central role of the VL site for the selective interaction of TRPM7 with small molecules that can be explored in future drug design.
  • ||||||||||  LY294002 / Eli Lilly
    Journal, IO biomarker:  LAMC1 attenuates neuronal apoptosis via FAK/PI3K/AKT signaling pathway after subarachnoid hemorrhage. (Pubmed Central) -  Apr 13, 2024   
    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. Exogenous LAMC1 treatment improved neurological deficits after SAH in rats, and attenuated neuronal apoptosis in both in vitro and in vivo SAH models, at least partially through the FAK/PI3K/AKT pathway.
  • ||||||||||  PCUR-101 / Pellficure
    Enrollment change, Trial termination, Combination therapy, Metastases:  Study of PCUR-101 in Combination With ADT in Patients With mCRPC (clinicaltrials.gov) -  Apr 10, 2024   
    P1,  N=7, Terminated, 
    These results demonstrate that engagement of AKT and ERK signaling pathways facilitates viral infection and may be implicated in WNV pathogenesis. N=48 --> 7 | Recruiting --> Terminated; Business Decision due to insufficient enrollment
  • ||||||||||  Turalio (pexidartinib) / Daiichi Sankyo
    Preclinical, Journal:  Sexually dimorphic effects of pexidartinib on nerve injury-induced neuropathic pain in mice. (Pubmed Central) -  Apr 9, 2024   
    Collectively, these findings demonstrate the presence of considerable sex- and androgen-dependent differences in the etiology of neuropathic pain in spinal microglia and DRG macrophages but not in sciatic nerve macrophages. Given that the mechanisms of neuropathic pain may differ among experimental models and clinical conditions, accumulating several lines of evidence is crucial to comprehensively clarifying the sex-dependent regulatory mechanisms of pain.
  • ||||||||||  Taltorvic (ridaforolimus) / Takeda, Merck (MSD)
    Review, Journal:  Clinical research progress of ridaforolimus (AP23573, MK8668) over the past decade: a systemic review. (Pubmed Central) -  Apr 8, 2024   
    Rapamycin, an established mTOR inhibitor in clinical practice, is widely recognized for its therapeutic efficacy...These trials employed diverse drug combinations, incorporating agents such as ponatinib, bicalutamide, dalotuzumab, MK-2206, MK-0752, and taxanes...Our review encompassed analyses of signaling pathways, ridaforolimus as a single therapeutic agent, its compatibility in combination with other drugs, and an assessment of adverse events (AEs). We conclude by recommending further research to advance our understanding of ridaforolimus's clinical applications.
  • ||||||||||  LY294002 / Eli Lilly, AG-1296 - Friedrich / Schiller University of Jena, Wuhan University, Zhejiang University
    Preclinical, Journal:  PDGF-AA guides cell crosstalk between human dental pulp stem cells in (Pubmed Central) -  Apr 8, 2024   
    These observations indicated that the PI3K/AKT/mTORC1 signalling pathway is involved in MMP9 expression by regulating MMP9 promoter activity via NF-?B in the mammary epithelial cells of dairy cows. This research demonstrated that PDGF-AA can enhance Cx43-mediated GJIC in DPSCs via the PDGFR-?/PI3K/Akt axis, which provides new cues for dental pulp regeneration from the perspective of intercellular communication.
  • ||||||||||  Turalio (pexidartinib) / Daiichi Sankyo
    Journal, Real-world evidence, Real-world:  Real-World Patient Experience of Pexidartinib for Tenosynovial Giant-Cell Tumor. (Pubmed Central) -  Apr 8, 2024   
    Findings from this cross-sectional survey confirmed the benefit of pexidartinib in improving symptoms and functional outcomes among patients with symptomatic TGCTs from the patients' perspective. Future research is warranted to examine the long-term benefit and risk of pexidartinib.
  • ||||||||||  Truqap (capivasertib) / Otsuka, AstraZeneca
    Capivasertib and fulvestrant for patients with aromatase inhibitor-resistant HR+/HER2 (Exhibit Hall) -  Apr 7, 2024 - Abstract #HOPA2024HOPA_383;    
    Future research is warranted to examine the long-term benefit and risk of pexidartinib. To provide a detailed understanding of the safety profile of capivasertib + fulvestrant from the CAPItello-291 study, with a focuson frequent clinically relevant AEs
  • ||||||||||  Epidaza (chidamide) / Chipscreen, Meiji Seika, Eisai, HUYA Bioscience
    Journal, CAR T-Cell Therapy, IO biomarker:  Class I HDAC inhibitors enhance antitumor efficacy and persistence of CAR-T cells by activation of the Wnt pathway. (Pubmed Central) -  Apr 5, 2024   
    These results suggest that the binding of cardiac glycosides to Na+,K+-ATPase negatively regulates the THADA-LAT1 pathway, exerting the anti-proliferative effect in cancer cells. Here, we identify class I histone deacetylase inhibitors (HDACi) as boosters of CAR-T cell function by high-throughput screening of chromatin-modifying drugs, in which M344 and chidamide enhance memory maintenance and resistance to exhaustion of CAR-T cells that induce sustained antitumor efficacy both in
  • ||||||||||  Turalio (pexidartinib) / Daiichi Sankyo
    Journal:  CYP3A Mediates an Unusual C(sp2)-C(sp3) Bond Cleavage via Ipso-Addition of Oxygen in Drug Metabolism. (Pubmed Central) -  Apr 4, 2024   
    CYP3A-mediated ipso-addition is also implicated in the regioselective C-C cleavages of several pexidartinib analogs. The regiospecificity of CYP3A-catalyzed oxygen ipso-addition under environmentally friendly conditions may be attractive and inspire biomimetic or P450-engineering methods to address the challenging task of C-C bond cleavages.
  • ||||||||||  Epidaza (chidamide) / Chipscreen, Meiji Seika, Eisai, HUYA Bioscience
    Journal, IO biomarker:  Matrine Enhances the Antitumor Efficacy of Chidamide in CTCL by Promoting Apoptosis. (Pubmed Central) -  Apr 4, 2024   
    The regiospecificity of CYP3A-catalyzed oxygen ipso-addition under environmentally friendly conditions may be attractive and inspire biomimetic or P450-engineering methods to address the challenging task of C-C bond cleavages. Our data have demonstrated chidamide combined with matrine to exhibit elevated antitumor activity in both CTCL cells and xenograft models of NOD/SCID mice, which may be a potential treatment option for CTCL.
  • ||||||||||  dordaviprone (ONC201) / Chimerix
    Journal, IO biomarker:  Employing Piezoelectric Mg -Doped Hydroxyapatite to Target Death Receptor-Mediated Necroptosis: A Strategy for Amplifying Immune Activation. (Pubmed Central) -  Apr 4, 2024   
    In this study, for the first time, piezoelectrically catalyzed Mg2+-doped hydroxyapatite (Mg-HAP) nanoparticles, which are coated with a mesoporous silica layer and loaded with ONC201 as an agonist to specifically target the death receptor DR5 on tumor cells, ultimately developing an Mg-HAP@MS/ONC201 nanoparticle (MHMO NP) system, are engineered...In summary, a dual-targeting therapy system that targets both tumor cells and the tumor microenvironment under piezoelectric catalysis is designed. This system holds substantial potential for advancements in tumor immunotherapy.
  • ||||||||||  Truqap (capivasertib) / Otsuka, AstraZeneca
    Review, Journal, Metastases:  Capivasertib: A Novel AKT Inhibitor Approved for Hormone-Receptor-Positive, HER-2-Negative Metastatic Breast Cancer. (Pubmed Central) -  Apr 3, 2024   
    Capivasertib is a viable treatment option for patients with PIK3CA/AKT1/PTEN activating mutations following progression on endocrine-based regimens in the metastatic setting or recurrence within 12 months of completing adjuvant therapy. Integration of capivasertib into clinical practice is ongoing; intermittent dosing and favorable toxicity are attractive for future novel combination prospective trials.
  • ||||||||||  Cilcane (cilengitide) / Iceni Pharma, LY294002 / Eli Lilly, Ex-Rad (recilisib) / Onconova
    Journal:  FNDC5 inhibits malignant growth of human cervical cancer cells via restraining PI3K/AKT pathway. (Pubmed Central) -  Apr 1, 2024   
    The effects of FNDC5 were prevented by inhibiting integrin with cilengitide, activating PI3K with recilisib or activating Akt with SC79...PI3K inhibitor LY294002 showed similar effects to FNDC5 in HeLa and SiHa cells...These results indicate that FNDC5 inhibits the malignant phenotype of CxCa cells through restraining PI3K/Akt signaling. Upregulation of FNDC5 may play a beneficial role in retarding the tumor growth of CxCa.