TRK xDFG Mutations Trigger a Sensitivity Switch from Type I to II Kinase Inhibitors.
Journal
Cancer discovery
ISSN: 2159-8290
Titre abrégé: Cancer Discov
Pays: United States
ID NLM: 101561693
Informations de publication
Date de publication:
01 2021
01 2021
Historique:
received:
01
05
2020
revised:
26
08
2020
accepted:
28
09
2020
pubmed:
3
10
2020
medline:
5
6
2021
entrez:
2
10
2020
Statut:
ppublish
Résumé
On-target resistance to next-generation TRK inhibitors in TRK fusion-positive cancers is largely uncharacterized. In patients with these tumors, we found that TRK xDFG mutations confer resistance to type I next-generation TRK inhibitors designed to maintain potency against several kinase domain mutations. Computational modeling and biochemical assays showed that TRKA
Identifiants
pubmed: 33004339
pii: 2159-8290.CD-20-0571
doi: 10.1158/2159-8290.CD-20-0571
pmc: PMC8012405
mid: NIHMS1634943
doi:
Substances chimiques
Protein Kinase Inhibitors
0
Receptor, trkA
EC 2.7.10.1
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
126-141Subventions
Organisme : NCI NIH HHS
ID : T32 CA160001
Pays : United States
Organisme : NCI NIH HHS
ID : R01 CA181746
Pays : United States
Organisme : NCI NIH HHS
ID : T32 CA009207
Pays : United States
Organisme : NCI NIH HHS
ID : P30 CA008748
Pays : United States
Organisme : NCI NIH HHS
ID : R01 CA204749
Pays : United States
Organisme : NIH HHS
ID : S10 OD023669
Pays : United States
Organisme : NCI NIH HHS
ID : R01 CA226864
Pays : United States
Informations de copyright
©2020 American Association for Cancer Research.
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