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Precious Gene: The Application of RET-Altered Inhibitors
The well-known proto-oncogene rearrangement during transfection (RET), also known as ret proto-oncogene Homo sapiens (human), is a rare gene that is involved in the physiological development of some organ systems and can activate various cancers, such as non-small cell lung cancer, thyroid cancer, a...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9784389/ https://www.ncbi.nlm.nih.gov/pubmed/36557971 http://dx.doi.org/10.3390/molecules27248839 |
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author | Gou, Qitao Gan, Xiaochuan Li, Longhao Gou, Qiheng Zhang, Tao |
author_facet | Gou, Qitao Gan, Xiaochuan Li, Longhao Gou, Qiheng Zhang, Tao |
author_sort | Gou, Qitao |
collection | PubMed |
description | The well-known proto-oncogene rearrangement during transfection (RET), also known as ret proto-oncogene Homo sapiens (human), is a rare gene that is involved in the physiological development of some organ systems and can activate various cancers, such as non-small cell lung cancer, thyroid cancer, and papillary thyroid cancer. In the past few years, cancers with RET alterations have been treated with multikinase inhibitors (MKIs). However, because of off-target effects, these MKIs have developed drug resistance and some unacceptable adverse effects. Therefore, these MKIs are limited in their clinical application. Thus, the novel highly potent and RET-specific inhibitors selpercatinib and pralsetinib have been accelerated for approval by the Food and Drug Administration (FDA), and clinical trials of TPX-0046 and zetletinib are underway. It is well tolerated and a potential therapeutic for RET-altered cancers. Thus, we will focus on current state-of-the-art therapeutics with these novel RET inhibitors and show their efficacy and safety in therapy. |
format | Online Article Text |
id | pubmed-9784389 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-97843892022-12-24 Precious Gene: The Application of RET-Altered Inhibitors Gou, Qitao Gan, Xiaochuan Li, Longhao Gou, Qiheng Zhang, Tao Molecules Review The well-known proto-oncogene rearrangement during transfection (RET), also known as ret proto-oncogene Homo sapiens (human), is a rare gene that is involved in the physiological development of some organ systems and can activate various cancers, such as non-small cell lung cancer, thyroid cancer, and papillary thyroid cancer. In the past few years, cancers with RET alterations have been treated with multikinase inhibitors (MKIs). However, because of off-target effects, these MKIs have developed drug resistance and some unacceptable adverse effects. Therefore, these MKIs are limited in their clinical application. Thus, the novel highly potent and RET-specific inhibitors selpercatinib and pralsetinib have been accelerated for approval by the Food and Drug Administration (FDA), and clinical trials of TPX-0046 and zetletinib are underway. It is well tolerated and a potential therapeutic for RET-altered cancers. Thus, we will focus on current state-of-the-art therapeutics with these novel RET inhibitors and show their efficacy and safety in therapy. MDPI 2022-12-13 /pmc/articles/PMC9784389/ /pubmed/36557971 http://dx.doi.org/10.3390/molecules27248839 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/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 (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Review Gou, Qitao Gan, Xiaochuan Li, Longhao Gou, Qiheng Zhang, Tao Precious Gene: The Application of RET-Altered Inhibitors |
title | Precious Gene: The Application of RET-Altered Inhibitors |
title_full | Precious Gene: The Application of RET-Altered Inhibitors |
title_fullStr | Precious Gene: The Application of RET-Altered Inhibitors |
title_full_unstemmed | Precious Gene: The Application of RET-Altered Inhibitors |
title_short | Precious Gene: The Application of RET-Altered Inhibitors |
title_sort | precious gene: the application of ret-altered inhibitors |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9784389/ https://www.ncbi.nlm.nih.gov/pubmed/36557971 http://dx.doi.org/10.3390/molecules27248839 |
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