A proteolysis-targeting chimera molecule selectively degrades ENL and inhibits malignant gene expression and tumor growth

A proteolysis-targeting chimera molecule selectively degrades ENL and inhibits malignant gene expression and tumor growth

Background: Chromosome translocations involving mixed lineage leukemia 1 (MLL1) cause acute leukemia in most infants and 5–10% children/adults with dismal clinical outcomes. Most frequent MLL1-fusion partners AF4/AFF4, AF9/ENL and ELL, together with CDK9/cyclin-T1, constitute super elongation comple...

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Bibliographic Details
Main Authors: Li, X. (Author), Song, Y. (Author), Wu, F. (Author), Yao, Y. (Author)
Format: Article
Language:English
Published: BioMed Central Ltd 2022
Subjects:
acute myeloid leukemia
AFF4 protein, human
animal
Animals
Cancer therapeutics
carcinogenesis
Carcinogenesis
chemistry
chimera
Chimera
ENL
ENL mutation
gene expression
Gene Expression
genetics
human
Humans
Kidney Neoplasms
kidney tumor
Leukemia, Myeloid, Acute
metabolism
Mice
mixed lineage leukemia protein
MLL1-rearranged leukemia
mouse
Myeloid-Lymphoid Leukemia Protein
nephroblastoma
PROTAC
protein degradation
Proteolysis
transcription elongation factor
Transcriptional Elongation Factors
Wilms Tumor
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