Targeting epigenetic and posttranscriptional gene regulation by PSF impairs hormone therapy-refractory cancer growth was written by Takayama, Ken-ichi;Honma, Teruki;Suzuki, Takashi;Kondoh, Yasumitsu;Osada, Hiroyuki;Suzuki, Yutaka;Yoshida, Minoru;Inoue, Satoshi. And the article was included in Cancer Research in 2021.Electric Literature of C10H13N This article mentions the following:
RNA-binding protein PSF functions as an epigenetic modifier by interacting with long noncoding RNAs and the corepressor complex. PSF also promotes RNA splicing events to enhance oncogenic signals. In this study, we conducted an in vitro chem. array screen and identified multiple small mols. that interact with PSF. Several mols. inhibited RNA binding by PSF and decreased prostate cancer cell viability. Among these mols. and its derivatives was a promising mol., Number 10-3 [7,8-dihydroxy-4-(4-methoxyphenyl)chromen-2-one], that was the most effective at blocking PSF RNA-binding ability and suppressing treatment-resistant prostate and breast cancer cell proliferation. Exposure to Number 10-3 inhibited PSF target gene expression at the mRNA level. Treatment with Number 10-3 reversed epigenetically repressed PSF downstream targets, such as cell-cycle inhibitors, at the transcriptional level. Chromatin immunoprecipitation sequencing in prostate cancer cells revealed that Number 10-3 enhances histone acetylation to induce expression of apoptosis as well as cell-cycle inhibitors. Furthermore, Number 10-3 exhibited antitumor efficacy in a hormone therapy-resistant prostate cancer xenograft mouse model, suppressing treatment-resistant tumor growth. Taken together, this study highlights the feasibility of targeting PSF-mediated epigenetic and RNA-splicing activities for the treatment of aggressive cancers. In the experiment, the researchers used many compounds, for example, 3,3-Dimethylindoline (cas: 1914-02-9Electric Literature of C10H13N).
3,3-Dimethylindoline (cas: 1914-02-9) belongs to indole derivatives. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Electric Literature of C10H13N
Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles