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TRPM4 in Cancer—A New Potential Drug Target
Transient receptor potential melastatin 4 (TRPM4) is widely expressed in various organs and associated with cardiovascular and immune diseases. Lately, the interest in studies on TRPM4 in cancer has increased. Thus far, TRPM4 has been investigated in diffuse large B-cell lymphoma, prostate, colorect...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7914809/ https://www.ncbi.nlm.nih.gov/pubmed/33562811 http://dx.doi.org/10.3390/biom11020229 |
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author | Borgström, Anna Peinelt, Christine Stokłosa, Paulina |
author_facet | Borgström, Anna Peinelt, Christine Stokłosa, Paulina |
author_sort | Borgström, Anna |
collection | PubMed |
description | Transient receptor potential melastatin 4 (TRPM4) is widely expressed in various organs and associated with cardiovascular and immune diseases. Lately, the interest in studies on TRPM4 in cancer has increased. Thus far, TRPM4 has been investigated in diffuse large B-cell lymphoma, prostate, colorectal, liver, breast, urinary bladder, cervical, and endometrial cancer. In several types of cancer TRPM4 is overexpressed and contributes to cancer hallmark functions such as increased proliferation and migration and cell cycle shift. Hence, TRPM4 is a potential prognostic cancer marker and a promising anticancer drug target candidate. Currently, the underlying mechanism by which TRPM4 contributes to cancer hallmark functions is under investigation. TRPM4 is a Ca(2+)-activated monovalent cation channel, and its ion conductivity can decrease intracellular Ca(2+) signaling. Furthermore, TRPM4 can interact with different partner proteins. However, the lack of potent and specific TRPM4 inhibitors has delayed the investigations of TRPM4. In this review, we summarize the potential mechanisms of action and discuss new small molecule TRPM4 inhibitors, as well as the TRPM4 antibody, M4P. Additionally, we provide an overview of TRPM4 in human cancer and discuss TRPM4 as a diagnostic marker and anticancer drug target. |
format | Online Article Text |
id | pubmed-7914809 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-79148092021-03-01 TRPM4 in Cancer—A New Potential Drug Target Borgström, Anna Peinelt, Christine Stokłosa, Paulina Biomolecules Review Transient receptor potential melastatin 4 (TRPM4) is widely expressed in various organs and associated with cardiovascular and immune diseases. Lately, the interest in studies on TRPM4 in cancer has increased. Thus far, TRPM4 has been investigated in diffuse large B-cell lymphoma, prostate, colorectal, liver, breast, urinary bladder, cervical, and endometrial cancer. In several types of cancer TRPM4 is overexpressed and contributes to cancer hallmark functions such as increased proliferation and migration and cell cycle shift. Hence, TRPM4 is a potential prognostic cancer marker and a promising anticancer drug target candidate. Currently, the underlying mechanism by which TRPM4 contributes to cancer hallmark functions is under investigation. TRPM4 is a Ca(2+)-activated monovalent cation channel, and its ion conductivity can decrease intracellular Ca(2+) signaling. Furthermore, TRPM4 can interact with different partner proteins. However, the lack of potent and specific TRPM4 inhibitors has delayed the investigations of TRPM4. In this review, we summarize the potential mechanisms of action and discuss new small molecule TRPM4 inhibitors, as well as the TRPM4 antibody, M4P. Additionally, we provide an overview of TRPM4 in human cancer and discuss TRPM4 as a diagnostic marker and anticancer drug target. MDPI 2021-02-05 /pmc/articles/PMC7914809/ /pubmed/33562811 http://dx.doi.org/10.3390/biom11020229 Text en © 2021 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Review Borgström, Anna Peinelt, Christine Stokłosa, Paulina TRPM4 in Cancer—A New Potential Drug Target |
title | TRPM4 in Cancer—A New Potential Drug Target |
title_full | TRPM4 in Cancer—A New Potential Drug Target |
title_fullStr | TRPM4 in Cancer—A New Potential Drug Target |
title_full_unstemmed | TRPM4 in Cancer—A New Potential Drug Target |
title_short | TRPM4 in Cancer—A New Potential Drug Target |
title_sort | trpm4 in cancer—a new potential drug target |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7914809/ https://www.ncbi.nlm.nih.gov/pubmed/33562811 http://dx.doi.org/10.3390/biom11020229 |
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