PLK1 inhib 
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  • ||||||||||  Review, Journal:  Comprehensive analysis of PLKs expression and prognosis in breast cancer. (Pubmed Central) -  Oct 8, 2022   
    The PLK1 gene might provide new ideas and evidence for bladder cancer research. For the precise therapy of breast cancers, PLK1 and PLK4 are potential targets, while PLK2, PLK3, and PLK5 are brand-new biomarkers for predicting the prognosis of breast cancer.
  • ||||||||||  gemcitabine / Generic mfg.
    Journal, PD(L)-1 Biomarker, IO biomarker:  Targeting Plk1 sensitizes pancreatic cancer to immune checkpoint therapy. (Pubmed Central) -  Oct 6, 2022   
    Recent work has suggested that Plk1 could be a biomarker of gemcitabine response in pancreatic ductal adenocarcinoma (PDAC)...Inhibition of Plk1 sensitized PDAC to immune checkpoint blockade therapy through activation of an anti-tumor immune response. Together, Plk1 suppresses PDAC progression and inhibits NFκB activity, and targeting Plk1 can potentiate the efficacy of immunotherapy in PDAC.
  • ||||||||||  volasertib (NBL-001) / Oncoheroes, Notable Labs
    Journal:  Transferrin-guided intelligent nanovesicles augment the targetability and potency of clinical PLK1 inhibitor to acute myeloid leukemia. (Pubmed Central) -  Oct 4, 2022   
    PLK1 inhibitor, volasertib (Vol), is among the few molecular targeted drugs granted breakthrough therapy status for AML; however, its fast clearance and dose-limiting toxicity greatly restrain its clinical benefits...The efficacy studies in orthotopic MV-4-11 leukemic model demonstrated that TPVol significantly reduced leukemic cell proportions in periphery blood, bone marrow, liver and spleen, effectively enhanced mouse survival rate, and impeded bone loss. This transferrin-guided nano-delivery of molecular targeted drugs appears to be an interesting strategy towards the development of novel treatments for AML.
  • ||||||||||  Biomarker, Journal:  Eight hub genes as potential biomarkers for breast cancer diagnosis and prognosis: A TCGA-based study. (Pubmed Central) -  Sep 29, 2022   
    Our results shed new light on the critical role of PLK1 in reversing PARPi resistance in KRAS-amplified HGSOC, and offer a new therapeutic strategy for this class of ovarian cancer patients where only limited options currently exist. In view of the results of PPI analysis, which were verified by survival and expression analyses, we conclude that MAD2L1, PLK1, SAA1, CCNB1, SHCBP1, KIF4A, ANLN, and ERCC6L may act as biomarkers for the diagnosis and prognosis in BC patients.
  • ||||||||||  Journal:  A high-throughput drug screen reveals means to differentiate triple-negative breast cancer. (Pubmed Central) -  Sep 29, 2022   
    In addition, the upregulation of genes upon PLK1 inhibition correlates with their expression in normal breast tissue and with better overall survival in breast cancer patients. Our results indicate that differentiation therapy based on PLK1 inhibition is a potential alternative strategy to treat TNBC.
  • ||||||||||  Review, Journal:  Regulation of oocyte maturation: Role of conserved ERK signaling. (Pubmed Central) -  Sep 24, 2022   
    Extracellular signal-regulated kinase (ERK), on the other hand, while activated during oocyte maturation in all species, regulates both species-specific, as well as conserved events among different organisms. In this review, we synthesize the general signaling mechanisms and focus on conserved and distinct functions of ERK signaling pathway during oocyte maturation in mammals, non-mammalian vertebrates, and invertebrates such as Drosophila and Caenorhabditis elegans.
  • ||||||||||  Journal:  Development of ultra-high affinity bivalent ligands targeting the polo-like kinase 1. (Pubmed Central) -  Sep 23, 2022   
    Startlingly, and in contradiction to widely accepted notions of KD-PBD interactions, we have found that full affinities can be retained even with minimal linkers between KD and PBD-binding components. In addition to significantly advancing the development of PBD-binding ligands, our findings may cause a rethinking of the structure - function of Plk1.
  • ||||||||||  Journal:  USP39 facilitates breast cancer cell proliferation through stabilization of FOXM1. (Pubmed Central) -  Sep 21, 2022   
    USP39 is positively correlated with the expression level of FOXM1 in breast cancer cells. In general, our research revealed the USP39-FOXM1 axis as a critical driver of breast cancer cell proliferation and provided a theoretical foundation for targeting the USP39-FOXM1 axis for pancreatic cancer treatment.
  • ||||||||||  doxycycline / Generic mfg.
    Unchecked Cytokinesis Generates Highly Proliferative Mononuclear Cardiomyocytes at the Expense of Contractility (S103BC) -  Sep 18, 2022 - Abstract #AHA2022AHA_6789;    
    Similarly, high-dose doxycycline inducible cardiomyocyte-specific overexpression of both proteins (inducible double transgenic) in the adult heart results in reversible widespread cardiomyocyte mitosis, cardiac enlargement, and contractile failure, while low-dose transient induction also results in significant cardiomyocyte proliferation and lower ejection fraction that is reversible after doxycycline is removed. Collectively, these results demonstrate that cytokinesis failure mediates cardiomyocyte multinucleation and cell cycle exit of postnatal cardiomyocytes but may be a protective mechanism to preserve the contractile function of the myocardium.
  • ||||||||||  Journal:  PLK1-mediated phosphorylation of PPIL2 regulates HR via CtIP. (Pubmed Central) -  Sep 14, 2022   
    Our findings reveal new regulatory complexity in CtIP ubiquitination in DSB repair. We propose that the PPIL2-dependent CtIP ubiquitination prevents CtIP from interacting with DNA, thereby inhibiting HR.
  • ||||||||||  Journal:  SMARCE1 promotes neuroblastoma tumorigenesis through assisting MYCN-mediated transcriptional activation. (Pubmed Central) -  Sep 14, 2022   
    Moreover, we revealed that MYCN directly regulated SMARCE1 transcription through binding to a non-canonical E-box of SMARCE1 promoter, thus enhancing SMARCE1-MYCN cooperativity. These findings establish SMARCE1 is a critical oncogenic factor in neuroblastoma and provide a new potential target for treatment of neuroblastoma with 17q21-ter gain and MYCN amplification.
  • ||||||||||  Herceptin (trastuzumab) / Roche, volasertib (BI 6727) / Oncoheroes, Notable Labs
    Journal:  HER-2-mediated nano-delivery of molecular targeted drug potently suppresses orthotopic epithelial ovarian cancer and metastasis. (Pubmed Central) -  Sep 14, 2022   
    Anti-HER-2 antibody, trastuzumab (Tra), was conjugated onto Vol-loaded polymersomes via click chemistry yielding Tra-PVol with a size of 33 nm and optimally about 5 Tra per polymersome...More interestingly, Tra-PVol was shown to effectively suppress the intraperitoneal metastasis and to markedly prolong the survival time of SKOV-3-Luc tumor-bearing mice. This HER-2 directed molecular therapy emerges as a potential treatment strategy toward EOC.
  • ||||||||||  enzalutamide capsule / Generic mfg.
    Journal:  Reciprocal regulation of CIP2A and AR expression in prostate cancer cells. (Pubmed Central) -  Sep 14, 2022   
    The reduction of CIP2A expression also enhanced the sensitivity of PCa cells toward Enzalutamide treatment...In summary, our data showed the existence of a novel regulation between CIP2A and AR protein levels, which is critical for promoting PCa malignancy. Thus, CIP2A could serve as a therapeutic target for PCa.
  • ||||||||||  cisplatin / Generic mfg.
    Journal, BRCA Biomarker:  BRCA1 transports the DNA damage signal for CDDP-induced centrosome amplification through the centrosomal Aurora A. (Pubmed Central) -  Sep 13, 2022   
    Here, the centrosomal localization of BRCA1 and the kinases involved in centrosome duplication were analyzed in each cell cycle phase after treatment with DNA crosslinker cisplatin (CDDP)...Patient-derived variants and mutations at phosphorylated residues of BRCA1 suppressed the interaction between BRCA1 and Aurora A, as well as the CDDP-induced increase in the centrosomal localization of BRCA1 and Aurora A. These results suggest that CDDP induces the phosphorylation of BRCA1 by ATM in the nucleus and its transport to the cytoplasm, thereby promoting the centrosomal localization Aurora A, which phosphorylates PLK1. The function of BRCA1 in the translocation of the DNA damage signal from the nucleus to the centrosome to induce centrosome amplification after CDDP treatment might support its role as a tumor suppressor.
  • ||||||||||  Journal:  Prdx5 regulates DNA damage response through autophagy-dependent Sirt2-p53 axis. (Pubmed Central) -  Sep 7, 2022   
    Furthermore, we found that exogenous expression of Prdx5 decreased DNA damage and the activation of ATM in Pkd1 mutant renal epithelial cells, suggesting that Prdx5 may play a protective role from DNA damage in cystic renal epithelial cells. This study identified a novel mechanism of Prdx5 in the regulation of DDR through the ATM/p53/Sirt2 signaling cascade.
  • ||||||||||  paclitaxel / Generic mfg.
    Treatment strategies based on the molecular subtypes of transformed small cell lung cancer (t-SCLC) (Exhibition Hall) -  Sep 3, 2022 - Abstract #AACRNCIEORTC2022AACR_NCI_EORTC_465;    
    Our in vitro studies suggest that EGFR-mutant t-SCLC can be classified into subtypes like de novo SCLC. NEUROD1-positive SNU-2962A cell line was sensitive to BET inhibition, whereas YAP1-positive SNU-4505 cell line was only sensitive to paclitaxel, suggesting a subtype-specific therapeutic strategy in t-SCLC.
  • ||||||||||  Polivy (polatuzumab vedotin) / Roche, Adcetris (brentuximab vedotin) / Seagen, Takeda, Rituxan (rituximab) / Biogen, Zenyaku Kogyo, Roche
    Transcriptome and computational analysis assess the anti-tubulin activity of [1,2]oxazole derivatives in lymphoma (Exhibition Hall) -  Sep 3, 2022 - Abstract #AACRNCIEORTC2022AACR_NCI_EORTC_322;    
    Transcriptome changes induced by SIX2-F in lymphoma overlapped with those reported for other microtubule inhibitors. These data, further supported by its docking poses and interactions with the crystal structure of tubulin, validated its activity as anti-tubulin agent and confirmed SIX2-F as promising candidate for further studies for the treatment of refractory lymphomas.
  • ||||||||||  prexasertib (ACR-368) / Acrivon Therap, cofetuzumab pelidotin (ABBV-647) / Pfizer, AbbVie, GSK461364 / GSK
    Journal:  Multiomics characterization implicates PTK7 in ovarian cancer EMT and cell plasticity and offers strategies for therapeutic intervention. (Pubmed Central) -  Aug 22, 2022   
    Furthermore, using high-throughput drug sensitivity testing (525 drugs) we show that targeting PTK7 exhibited synergistic activity with chemotherapeutic agent paclitaxel, CHK1/2 inhibitor prexasertib, and PLK1 inhibitor GSK461364, among others, in OC cells and ex vivo primary samples. Taken together, our study provides unique insight into the function of PTK7, which helps to define its role in mediating aberrant Wnt signaling in ovarian cancer.
  • ||||||||||  Biomarker, Journal, IO biomarker:  ABCD3 is a prognostic biomarker for glioma and associated with immune infiltration: A study based on oncolysis of gliomas. (Pubmed Central) -  Aug 22, 2022   
    Gene sets including the plk1 pathway, tyrobp causal network, ir-damage and cellular response, and interleukin-10 signaling showed significant differential enrichment in the high ABCD3 expression phenotype. Our results suggested that ABCD3 could be a potential biomarker for glioma prognosis and immunotherapy response and also further enriched the theoretical and molecular mechanisms of oncolytic virus treatment for malignant gliomas.