Overexpression of Mct-1 was shown to promote cell proliferation and repress cell apoptosis both in vitro and in vivo. The results of RNA-seq indicated that knockdown of Mct-1 suppressed Yap expression, while the results of the luciferase assay also revealed that Mct-1 increases the activity of the Yap promoter.

2018年2月1日 · Mounting evidence suggests that the Hippo coactivator Yes-associated protein 1 (YAP1) is a major mediator of cancer stem cell (CSC) properties, tumor progression, and therapy resistance as well as often a terminal node of many oncogenic pathways.

5 天之前 · In the nucleus, YAP1 and WWTR1 act as co-activators of transcription factors such as TEAD1/2/3/4 to promote the expression of genes that drive cell proliferation and maintain cell viability 1, 4.

2025年3月17日 · Human monocarboxylate transporters (MCTs) are crucial for tumour cell glycolysis. Inhibiting MCT-mediated lactate transport can suppress the proliferation of solid tumours and enhance the efficacy ...

2024年8月1日 · We report the discovery and characterization of a novel YAP1/TEAD inhibitor MRK-A from an aryl ether chemical series demonstrating potent and specific inhibition of YAP1/TEAD activity. In vivo, MRK-A showed a favorable tolerability profile in mice and demonstrated pharmacokinetics suitable for twice daily oral dosing in preclinical efficacy ...

In the hypoxia microenvironment, hypoxia-inducible factor 1-alpha (HIF1α) binds to the dephosphorylated Yap1 in the cell nuclei to form a complex, which transactivates the target genes responsible for the survival of BMSCs and thus inhibits the apoptosis (Wang et al., 2020).

2021年3月1日 · Collectively, these results indicate that Mct-1 acts as a tumor promoter gene in HCC progression by up-regulating Yap expression and, thus, could serve a novel potential diagnostic and prognostic...

2018年1月1日 · We investigated how selective downregulation of YAP1 would affect the growth of established HCC using optimized Gen2.5 antisense oligonucleotides (ASOs) for mouse YAP1. Here, we describe the antitumor activity of YAP1 ASOs in 2 mouse models of HCC, which appears to be mediated by both tumor autonomous and immune modulatory functions of YAP1.

2021年7月1日 · In this review we are discussing the molecular functions of YAP1 and its roles in cancer, with a focus on the different mechanisms of de-regulation of YAP1 activity in human cancers, including inactivation of upstream Hippo pathway tumor suppressors, regulation by intersecting pathways, miRNAs, and viral oncogenes.

Cell polarization is a crucial developmental process that determines cell differentiation in mouse embryos. During this process, an extensively expressed transcriptional regulator, Yes-associated protein 1 (YAP1), is localized either to the cytoplasm or nucleus via HIPPO signaling. In mouse pre-morula embryos, YAP1 is present in the nuclei of …