Delving into the Latest Updates on AhR Pharmaceuticals, Inc. with Synapse

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Immune System Diseases

Endocrinology and Metabolic Disease

Neoplasms

Small molecule drug

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Disease Domain	Count

Endocrinology and Metabolic Disease	1
Immune System Diseases	1
Neoplasms	1

Top 5 Drug Type	Count

Small molecule drug	1

Top 5 Target	Count

AHR(Aryl hydrocarbon receptor)	1

The aryl hydrocarbon receptor (AhR), a ligand-activated transcription factor mediates many biological processes. Herein, we investigated if 2-(1'H-indole-3'-carbonyl)-thiazole-4-carboxylic acid methyl ester (ITE, an endogenous AhR ligand) regulated proliferation and migration of human ovarian cancer cells via AhR. We found that AhR was widely present in many histotypes of ovarian cancer tissues. ITE suppressed OVCAR-3 cell proliferation and SKOV-3 cell migration in vitro, which were blocked by AhR knockdown. ITE also suppressed OVCAR-3 cell growth in mice. These data suggest that the ITE might potentially be used for therapeutic intervention for at least a subset of human ovarian cancer.

Nature CommunicationsQ1 · CROSS-FIELD

Tryptophan derivatives regulate the transcription of Oct4 in stem-like cancer cells

Q1 · CROSS-FIELD

ArticleOA

Author: Zhao, Qingwei ; Shen, Binghui ; Wang, Ying-Jie ; Song, Jiasheng ; Li, Lanjuan ; Zheng, Min ; Yin, Shengyong ; Zhou, Yanwen ; Zhang, Xiaoqian ; Yao, Hangping ; Zheng, Shusen ; Zhu, Chenggang ; Kang, Bo ; Xu, Xiaowei ; Li, Wenxin ; Yi, Wen ; Cheng, Jie ; Yang, Ying ; Cao, Hongcui ; Li, Jingchao ; Dan, Songsong

AbstractThe aryl hydrocarbon receptor (AhR), a ligand-activated transcription factor that responds to environmental toxicants, is increasingly recognized as a key player in embryogenesis and tumorigenesis. Here we show that a variety of tryptophan derivatives that act as endogenous AhR ligands can affect the transcription level of the master pluripotency factor Oct4. Among them, ITE enhances the binding of the AhR to the promoter of Oct4 and suppresses its transcription. Reduction of endogenous ITE levels in cancer cells by tryptophan deprivation or hypoxia leads to Oct4 elevation, which can be reverted by administration with synthetic ITE. Consequently, synthetic ITE induces the differentiation of stem-like cancer cells and reduces their tumorigenic potential in both subcutaneous and orthotopic xenograft tumour models. Thus, our results reveal a role of tryptophan derivatives and the AhR signalling pathway in regulating cancer cell stemness and open a new therapeutic avenue to target stem-like cancer cells.

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Pipeline

Pipeline Snapshot as of 19 Dec 2024

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

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