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Drug Target Encyclopedia Series (7) — KIT
Release Time：
2025-12-05 10:35
KIT, also known as CD117, is a type III receptor tyrosine kinase and the receptor for stem cell factor (SCF). It plays a crucial role in the development, survival, and function of various cell types, including hematopoietic stem cells, mast cells, melanocytes, and germ cells.
Aberrant KIT signaling is implicated in multiple malignancies, such as:
- Gastrointestinal stromal tumors (GIST) – where activating mutations in KIT are a primary driver
- Systemic mastocytosis
- Melanoma and acute myeloid leukemia (AML)
Targeting KIT has become a paradigm in precision oncology:
- Tyrosine kinase inhibitors (TKIs) – such as imatinib, sunitinib, and avapritinib – are used to inhibit mutant KIT activity in GIST and other cancers.
- Next-generation TKIs – being developed to overcome resistance from secondary mutations (e.g., D816V).
- Antibody-based therapies and CAR-Ts – under investigation to expand the range of KIT-targeting modalities beyond TKIs.
Despite therapeutic advances, resistance to KIT inhibitors remains a clinical challenge—spurring research into combination strategies and novel inhibitors tailored to mutation profiles.
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