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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...

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Autores principales: Gou, Qitao, Gan, Xiaochuan, Li, Longhao, Gou, Qiheng, Zhang, Tao
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
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.
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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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