Similar to givinostat, kaempferol exhibited tenable stability in bound form with this acetylation-eraser enzymatic protein. Most importantly, this flavonol demonstrated higher chemical reactivity and, as such, lower kinetic stability than givinostat which is quite important from a pharmacological perspective.
P1/2, N=35, Recruiting, National Institute of Allergy and Infectious Diseases (NIAID) | Trial completion date: Jun 2026 --> Jun 2035 | Trial primary completion date: Jun 2026 --> Jun 2035
6 days ago
Trial completion date • Trial primary completion date
On the other hand, MYBL2 may regulate the expression of cycle protein dependent kinase 1, causing G2M cell cycle arrest. Consequently, the combination of Olaparib and Chidamide synergistically induces cell apoptosis through synthetic lethality and cell cycle arrest to exert an antitumor effect.
7 days ago
Journal • BRCA Biomarker • PARP Biomarker
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BRCA1 (Breast cancer 1, early onset) • MYBL2 (MYB Proto-Oncogene Like 2)
The identification of gene mutations contributed to personalizing treatment strategies and predicting patient outcomes. This study raised the preliminary hypothesis that chidamide-containing front-line therapy might be promising for PTCL patients, which warranted further investigation.
7 days ago
Journal • Real-world evidence
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TP53 (Tumor protein P53) • DNMT3A (DNA methyltransferase 1) • TET2 (Tet Methylcytosine Dioxygenase 2) • RHOA (Ras homolog family member A)
In vivo, we confirmed that entinostat treatment increased the expression of immunecheckpoint ligands and antigen presentation machinery in Myc-driven tumors in a Rb1/Trp53/MycT58A (RPM) SCLC mouse model, while shifting tumors from a neuroendocrine (NE)-high to a NE-low phenotype, and was associated with increased T-cell infiltration Notably, combining entinostat with anti-PD-1 immunotherapy suppresses tumor growth and significantly prolonged survival in RPM allograft models. These findings underscore the potential of entinostat to reprogram the NE status of SCLC, enhance immune checkpoint blockade efficacy, and improve therapeutic outcomes.
8 days ago
Journal • PD(L)-1 Biomarker • IO biomarker
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TP53 (Tumor protein P53) • RB1 (RB Transcriptional Corepressor 1)
Eukaryotic transcriptome sequencing revealed that the combination treatment primarily inhibits tumor cell proliferation by modulating TRKC protein expression and suppressing phosphorylation of the phosphatidylinositol 3-kinase (PI3K)/protein kinase B (AKT)/mammalian target of rapamycin (mTOR) signaling pathway. Therefore, our results indicate that nobiletin, a natural BH3 mimetic, synergizes with vorinostat to regulate both apoptosis and autophagy in NSCLC.