Target intelligence / Profile preview

Gastrointestinal stromal tumor 48 cell line (GIST48)

Target
GIST48
Molecular classification
Other
01

Overview

GIST48 is a human gastrointestinal stromal tumor (GIST) cell line established from a patient whose tumor progressed during imatinib treatment [1, 4]. It is a widely utilized research model for studying secondary resistance to tyrosine kinase inhibitors (TKIs) in GIST [3, 7]. The cell line is characterized by a primary homozygous mutation in KIT exon 11 (V560D) and a secondary heterozygous mutation in KIT exon 17 (D820A), which confers resistance to first-line (imatinib) and second-line (sunitinib) therapies [1, 7]. GIST48 cells are essential for evaluating the efficacy of novel agents, such as the switch-control inhibitor ripretinib, which are designed to target the active and inactive conformations of the KIT kinase domain [12, 14]. It was established by the laboratory of Jonathan Fletcher and has been instrumental in identifying the role of the KIT D820A mutation in clinical resistance [1, 7]. Although GIST48 is a cell line and not a molecular target itself, it serves as a critical platform for investigating the KIT receptor tyrosine kinase's role in oncogenesis and drug resistance [2, 13].

Other names
GIST48GIST-48GIST 48
02

Mechanism of action

Tyrosine kinase inhibition

03

Biological functions

Cell proliferationSignal transductionApoptosis
04

Disease associations

CancerGastrointestinal stromal tumor
05

Safety considerations

Drug resistanceTherapeutic escapeOff-target kinase inhibition
06

Interacting drugs

9 more in the full profile.

07

Biomarkers

KIT exon 11 mutation (V560D)KIT exon 17 mutation (D820A)CD117DOG1

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