Resistance to mTORC1 Inhibitors in Cancer Therapy: From Kinase Mutations to Intratumoral Heterogeneity of Kinase Activity.

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Ressource 1Download: 1726078.pdf (1500.46 [Ko])
State: Public
Version: Final published version
Serval ID
serval:BIB_71959E046B2F
Type
Article: article from journal or magazin.
Publication sub-type
Review (review): journal as complete as possible of one specific subject, written based on exhaustive analyses from published work.
Collection
Publications
Institution
Title
Resistance to mTORC1 Inhibitors in Cancer Therapy: From Kinase Mutations to Intratumoral Heterogeneity of Kinase Activity.
Journal
Oxidative medicine and cellular longevity
Author(s)
Faes S., Demartines N., Dormond O.
ISSN
1942-0994 (Electronic)
ISSN-L
1942-0994
Publication state
Published
Issued date
2017
Peer-reviewed
Oui
Volume
2017
Pages
1726078
Language
english
Notes
Publication types: Journal Article ; Review
Publication Status: ppublish
Abstract
Targeting mTORC1 has been thoroughly explored in cancer therapy. Following encouraging preclinical studies, mTORC1 inhibitors however failed to provide substantial benefits in cancer patients. Several resistance mechanisms have been identified including mutations of mTOR and activation of alternate proliferation pathways. Moreover, emerging evidence discloses intratumoral heterogeneity of mTORC1 activity that further contributes to a reduced anticancer efficacy of mTORC1 inhibitors. Genetic heterogeneity as well as heterogeneous conditions of the tumor environment such as hypoxia profoundly modifies mTORC1 activity in tumors and hence influences the response of tumors to mTORC1 inhibitors. Intriguingly, the heterogeneity of mTORC1 activity also occurs towards its substrates at the single cell level, as mutually exclusive pattern of activation of mTORC1 downstream effectors has been reported in tumors. After briefly describing mTORC1 biology and the use of mTORC1 inhibitors in patients, this review will give an overview on concepts of resistance to mTORC1 inhibition in cancer with a particular focus on intratumoral heterogeneity of mTORC1 activity.

Keywords
Animals, Drug Resistance, Neoplasm/drug effects, Drug Resistance, Neoplasm/genetics, Humans, Multiprotein Complexes/antagonists & inhibitors, Multiprotein Complexes/genetics, Mutation/genetics, Neoplasms/drug therapy, Neoplasms/enzymology, Neoplasms/genetics, Protein Kinase Inhibitors/pharmacology, Protein Kinase Inhibitors/therapeutic use, Signal Transduction/drug effects, TOR Serine-Threonine Kinases/antagonists & inhibitors, TOR Serine-Threonine Kinases/genetics
Pubmed
Open Access
Yes
Create date
27/03/2017 18:33
Last modification date
20/08/2019 15:30
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