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Induction of Invasive Transitional Cell Bladder Carcinoma in Immune Intact Human MUC1 Transgenic Mice: A Model for Immunotherapy Development
Published on: October 30, 2013
N-(3,4-dimethoxyphenethyl)-6-methyl-2,3,4,9-tetrahydro-1H-carbazol-1-amine inhibits bladder cancer progression by
Yusuke Shiraishi1,2, Tomohiko Maehama1, Miki Nishio1
1Division of Molecular and Cellular Biology, Kobe University Graduate School of Medicine, Kobe, Japan.
Abstract:
Bladder cancer (BlC) is the fourth most common cancer in males worldwide, but few systemic chemotherapy options for its effective treatment exist. The development of new molecularly-targeted agents against BlC is therefore an urgent issue. The Hippo signaling pathway, with its upstream LATS kinases and downstream transcriptional co-activators YAP1 and TAZ, plays a pivotal role in diverse cell functions, including cell proliferation. Recent studies have shown that overexpression of YAP1 occurs in advanced BlCs and is associated with poor patient prognosis. Accessing data from our previous screening of a chemical library of compounds targeting the Hippo pathway, we identified DMPCA (N-(3,4-dimethoxyphenethyl)-6-methyl-2,3,4,9-tetrahydro-1H-carbazol-1-amine) as an agent able to induce the phosphorylation of LATS1 and YAP1/TAZ in BlC cells, thereby suppressing their viability both in vitro and in mouse xenografts. Our data indicate that DMPCA has a potent anti-tumor effect, and raise the possibility that this agent may represent a new and effective therapeutic option for BlC.
Insights
A new compound, DMPCA, effectively suppresses bladder cancer (BlC) cell viability by targeting the Hippo signaling pathway. This discovery offers a promising new therapeutic option for advanced BlC.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Bladder cancer (BlC) is a prevalent malignancy in males globally, with limited effective systemic chemotherapy options.
- Overexpression of YAP1, a key component of the Hippo signaling pathway, is linked to advanced BlC and poor patient prognosis.
Purpose of the Study:
- To identify novel molecularly-targeted agents for bladder cancer treatment.
- To investigate the anti-tumor potential of compounds targeting the Hippo signaling pathway in BlC.
Main Methods:
- Screening of a chemical library for compounds targeting the Hippo pathway.
- In vitro and mouse xenograft studies to assess the efficacy of the identified compound, DMPCA.
- Analysis of DMPCA's effect on LATS1 and YAP1/TAZ phosphorylation in BlC cells.
Main Results:
- DMPCA was identified as an agent that induces LATS1 and YAP1/TAZ phosphorylation in BlC cells.
- DMPCA demonstrated significant suppression of BlC cell viability in vitro.
- DMPCA exhibited potent anti-tumor effects in mouse xenograft models.
Conclusions:
- DMPCA shows potent anti-tumor activity against bladder cancer by modulating the Hippo signaling pathway.
- DMPCA represents a potential novel therapeutic agent for the treatment of bladder cancer.
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