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Special Issue "Transcription Factors as Therapeutic Targets"

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 31 March 2018

Special Issue Editor

Guest Editor
Dr. Takaomi Sanda

Cancer Science Institute of Singapore, National University of Singapore/Department of Medicine, Yong Loo Lin School of Medicine, National University of Singapore
Website | E-Mail
Interests: transcription; transcription factor; enhancer; core regulatory circuit; stem cells; hematopoiesis; acute leukemia; T-cell acute lymphoblastic leukemia; oncogene; TAL1

Special Issue Information

Dear Colleagues,

Deregulation of transcription factor genes are frequently observed in various human diseases, such as cancer. Understanding the molecular pathogenesis, as well as the development of therapeutic approaches, are crucial to further advance the treatment outcome. Although the feasibility of transcription factors as therapeutic targets has long been realized, the development of drugs is still very challenging due to several pharmacological and biological reasons. Therefore, an improved knowledge is necessary to make transcription factors “actionable”. This Special Issue aims to provide a forum for the dissemination of the latest information on new approaches and methods targeting transcription factors, and with methods of testing their success in cancer or other human diseases.

Dr. Takaomi Sanda
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All papers will be peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 1800 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • Transcription

  • Transcription factor

  • Enhancer

  • Epigenetics

  • Small-molecules

  • Cancer

  • Immunological diseases

  • Infectious diseases

Published Papers (2 papers)

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Research

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Open AccessArticle Thymoquinone Inhibits the Migration and Invasive Characteristics of Cervical Cancer Cells SiHa and CaSki In Vitro by Targeting Epithelial to Mesenchymal Transition Associated Transcription Factors Twist1 and Zeb1
Molecules 2017, 22(12), 2105; doi:10.3390/molecules22122105
Received: 11 October 2017 / Revised: 27 November 2017 / Accepted: 28 November 2017 / Published: 4 December 2017
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Abstract
Cervical cancer is one of the most common gynecological malignant tumors worldwide, for which chemotherapeutic strategies are limited due to their non-specific cytotoxicity and drug resistance. The natural product thymoquinone (TQ) has been reported to target a vast number of signaling pathways in
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Cervical cancer is one of the most common gynecological malignant tumors worldwide, for which chemotherapeutic strategies are limited due to their non-specific cytotoxicity and drug resistance. The natural product thymoquinone (TQ) has been reported to target a vast number of signaling pathways in carcinogenesis in different cancers, and hence is regarded as a promising anticancer molecule. Inhibition of epithelial to mesenchymal transition (EMT) regulators is an important approach in anticancer research. In this study, TQ was used to treat the cervical cancer cell lines SiHa and CaSki to investigate its effects on EMT-regulatory proteins and cancer metastasis. Our results showed that TQ has time-dependent and dose-dependent cytotoxic effects, and it also inhibits the migration and invasion processes in different cervical cancer cells. At the molecular level, TQ treatment inhibited the expression of Twist1, Zeb1 expression, and increased E-Cadherin expression. Luciferase reporter assay showed that TQ decreases the Twist1 and Zeb1 promoter activities respectively, indicating that Twist1 and Zeb1 might be the direct target of TQ. TQ also increased cellular apoptosis in some extent, but apoptotic genes/proteins we tested were not significant affected. We conclude that TQ inhibits the migration and invasion of cervical cancer cells, probably via Twist1/E-Cadherin/EMT or/and Zeb1/E-Cadherin/EMT, among other signaling pathways. Full article
(This article belongs to the Special Issue Transcription Factors as Therapeutic Targets)
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Review

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Open AccessFeature PaperReview Taming the Notch Transcriptional Regulator for Cancer Therapy
Molecules 2018, 23(2), 431; doi:10.3390/molecules23020431
Received: 22 January 2018 / Revised: 12 February 2018 / Accepted: 13 February 2018 / Published: 15 February 2018
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Abstract
Notch signaling is a highly conserved pathway in all metazoans, which is deeply involved in the regulation of cell fate and differentiation, proliferation and migration during development. Research in the last decades has shown that the various components of the Notch signaling cascade
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Notch signaling is a highly conserved pathway in all metazoans, which is deeply involved in the regulation of cell fate and differentiation, proliferation and migration during development. Research in the last decades has shown that the various components of the Notch signaling cascade are either upregulated or activated in human cancers. Therefore, its downregulation stands as a promising and powerful strategy for cancer therapy. Here, we discuss the recent advances in the development of small molecule inhibitors, blocking antibodies and oligonucleotides that hinder Notch activity, and their outcome in clinical trials. Although Notch was initially identified as an oncogene, later studies showed that it can also act as a tumor suppressor in certain contexts. Further complexity is added by the existence of numerous Notch family members, which exert different activities and can be differentially targeted by inhibitors, potentially accounting for contradictory data on their therapeutic efficacy. Notably, recent evidence supports the rationale for combinatorial treatments including Notch inhibitors, which appear to be more effective than single agents in fighting cancer. Full article
(This article belongs to the Special Issue Transcription Factors as Therapeutic Targets)
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