Small-Molecule Inhibitors and Degraders Targeting KRAS-Driven Cancers

Drug resistance continues to be a major problem associated with cancer treatment. One of the primary causes of anticancer drug resistance is the frequently mutated RAS gene. In particular, considerable efforts have been made to treat KRAS-induced cancers by directly and indirectly controlling the ac...

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Autores principales:	Soonsil Hyun, Dongyun Shin
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	RAS KRAS mutant KRAS inhibitors targeted protein degradation (TPD) drug resistance PROTAC Biology (General) QH301-705.5 Chemistry QD1-999
Acceso en línea:	https://doaj.org/article/69812bda3185416abd49d119a6d7fd35
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spelling	oai:doaj.org-article:69812bda3185416abd49d119a6d7fd352021-11-25T17:53:45ZSmall-Molecule Inhibitors and Degraders Targeting KRAS-Driven Cancers10.3390/ijms2222121421422-00671661-6596https://doaj.org/article/69812bda3185416abd49d119a6d7fd352021-11-01T00:00:00Zhttps://www.mdpi.com/1422-0067/22/22/12142https://doaj.org/toc/1661-6596https://doaj.org/toc/1422-0067Drug resistance continues to be a major problem associated with cancer treatment. One of the primary causes of anticancer drug resistance is the frequently mutated RAS gene. In particular, considerable efforts have been made to treat KRAS-induced cancers by directly and indirectly controlling the activity of KRAS. However, the RAS protein is still one of the most prominent targets for drugs in cancer treatment. Recently, novel targeted protein degradation (TPD) strategies, such as proteolysis-targeting chimeras, have been developed to render “undruggable” targets druggable and overcome drug resistance and mutation problems. In this study, we discuss small-molecule inhibitors, TPD-based small-molecule chemicals for targeting RAS pathway proteins, and their potential applications for treating KRAS-mutant cancers. Novel TPD strategies are expected to serve as promising therapeutic methods for treating tumor patients with KRAS mutations.Soonsil HyunDongyun ShinMDPI AGarticleRASKRAS mutantKRAS inhibitorstargeted protein degradation (TPD)drug resistancePROTACBiology (General)QH301-705.5ChemistryQD1-999ENInternational Journal of Molecular Sciences, Vol 22, Iss 12142, p 12142 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	RAS KRAS mutant KRAS inhibitors targeted protein degradation (TPD) drug resistance PROTAC Biology (General) QH301-705.5 Chemistry QD1-999
spellingShingle	RAS KRAS mutant KRAS inhibitors targeted protein degradation (TPD) drug resistance PROTAC Biology (General) QH301-705.5 Chemistry QD1-999 Soonsil Hyun Dongyun Shin Small-Molecule Inhibitors and Degraders Targeting KRAS-Driven Cancers
description	Drug resistance continues to be a major problem associated with cancer treatment. One of the primary causes of anticancer drug resistance is the frequently mutated RAS gene. In particular, considerable efforts have been made to treat KRAS-induced cancers by directly and indirectly controlling the activity of KRAS. However, the RAS protein is still one of the most prominent targets for drugs in cancer treatment. Recently, novel targeted protein degradation (TPD) strategies, such as proteolysis-targeting chimeras, have been developed to render “undruggable” targets druggable and overcome drug resistance and mutation problems. In this study, we discuss small-molecule inhibitors, TPD-based small-molecule chemicals for targeting RAS pathway proteins, and their potential applications for treating KRAS-mutant cancers. Novel TPD strategies are expected to serve as promising therapeutic methods for treating tumor patients with KRAS mutations.
format	article
author	Soonsil Hyun Dongyun Shin
author_facet	Soonsil Hyun Dongyun Shin
author_sort	Soonsil Hyun
title	Small-Molecule Inhibitors and Degraders Targeting KRAS-Driven Cancers
title_short	Small-Molecule Inhibitors and Degraders Targeting KRAS-Driven Cancers
title_full	Small-Molecule Inhibitors and Degraders Targeting KRAS-Driven Cancers
title_fullStr	Small-Molecule Inhibitors and Degraders Targeting KRAS-Driven Cancers
title_full_unstemmed	Small-Molecule Inhibitors and Degraders Targeting KRAS-Driven Cancers
title_sort	small-molecule inhibitors and degraders targeting kras-driven cancers
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/69812bda3185416abd49d119a6d7fd35
work_keys_str_mv	AT soonsilhyun smallmoleculeinhibitorsanddegraderstargetingkrasdrivencancers AT dongyunshin smallmoleculeinhibitorsanddegraderstargetingkrasdrivencancers
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Small-Molecule Inhibitors and Degraders Targeting KRAS-Driven Cancers

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