Small molecule inhibits T-cell acute lymphoblastic leukaemia oncogenic interaction through conformational modulation of LMO2.
LMO2
T-ALL
drug discovery
leukaemia
protein-protein interaction
Journal
Oncotarget
ISSN: 1949-2553
Titre abrégé: Oncotarget
Pays: United States
ID NLM: 101532965
Informations de publication
Date de publication:
12 May 2020
12 May 2020
Historique:
received:
24
12
2019
accepted:
03
04
2020
entrez:
2
6
2020
pubmed:
2
6
2020
medline:
2
6
2020
Statut:
epublish
Résumé
Ectopic expression in T-cell precursors of LIM only protein 2 (LMO2), a key factor in hematopoietic development, has been linked to the onset of T-cell acute lymphoblastic leukaemia (T-ALL). In the T-ALL context, LMO2 drives oncogenic progression through binding to erythroid-specific transcription factor SCL/TAL1 and sequestration of E-protein transcription factors, normally required for T-cell differentiation. A key requirement for the formation of this oncogenic protein-protein interaction (PPI) is the conformational flexibility of LMO2. Here we identify a small molecule inhibitor of the SCL-LMO2 PPI, which hinders the interaction
Identifiants
pubmed: 32477463
doi: 10.18632/oncotarget.27580
pii: 27580
pmc: PMC7233811
doi:
Types de publication
Journal Article
Langues
eng
Pagination
1737-1748Déclaration de conflit d'intérêts
CONFLICTS OF INTEREST The authors declare no competing interests.
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