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Small Molecule Induced FLT3 Degradationopen access

Authors
Han, Sun-Young
Issue Date
Mar-2022
Publisher
MDPI
Keywords
fms-like tyrosine kinase 3; target protein degrader; heat shock protein 90; ubiquitin proteasome system
Citation
PHARMACEUTICALS, v.15, no.3
Indexed
SCIE
SCOPUS
Journal Title
PHARMACEUTICALS
Volume
15
Number
3
URI
https://scholarworks.bwise.kr/gnu/handle/sw.gnu/1586
DOI
10.3390/ph15030320
ISSN
1424-8247
Abstract
Target protein degrader is a new paradigm in the small molecule drug discovery field and relates to the term 'event-driven pharmacology'. Fms-like tyrosine kinase 3 (FLT3) is a significant target for treating acute myeloid leukemia (AML). A few FLT3 kinase inhibitors are currently used in the clinic for AML patients. However, resistance to current FLT3 inhibitors has emerged, and strategies to overcome this resistance are required. Small molecules downregulating FLT3 protein level are reported, exhibiting antileukemic effects against AML cell lines. Small molecules with various mechanisms such as Hsp90 inhibition, proteasome inhibition, RET inhibition, and USP10 inhibition are explained. In addition, reports of FLT3 as a client of Hsp90, current knowledge of the ubiquitin proteasome system for FLT3 degradation, the relationship with FLT3 phosphorylation status and susceptibility of FLT3 degradation are discussed.
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