c-KIT Small Molecule Inhibitors as a Therapeutic Strategy for Melanoma: Clinical Insights, SAR, and Future Directions
  • Rivonker, Shubham C.
  • Nada, Hossam
  • Cho, Jaemin
  • Kwon, Yong-Jun
  • Lee, Kyeong
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초록

The proto-oncogene c-KIT plays a key role in several cellular processes such as cell growth, survival, and proliferation. The overexpression of c-KIT has been implicated with the pathogenesis of several malignancies, such as gastrointestinal stromal tumors, acute myeloid leukemia (AML), mastocytosis, and melanoma. Mutation of c-KIT has been observed in acral, mucosal, and chronically sun-damaged melanoma subtypes marking it as a key therapeutic target for melanoma. Moreover, the increasing incidence and mortality rate associated with melanoma further marks the importance of developing new therapeutic modalities. Herein, the progress in the design, structure–activity relationship, mechanisms, and development of c-KIT small molecule inhibitors for melanoma is discussed with the aim of guiding future c-KIT-based melanoma therapeutics. © 2025 Elsevier B.V., All rights reserved.

키워드

c-KITmelanomamolecular dockingSARsmall molecule inhibitorsRECEPTOR TYROSINE KINASESTEM-CELL FACTORPHASE-IIPOINT MUTATIONCANCERACTIVATIONEXPRESSIONMUCOSALTARGETGENE
제목
c-KIT Small Molecule Inhibitors as a Therapeutic Strategy for Melanoma: Clinical Insights, SAR, and Future Directions
저자
Rivonker, Shubham C.Nada, HossamCho, JaeminKwon, Yong-JunLee, Kyeong
DOI
10.1002/ardp.70113
발행일
2025-10
유형
Review
저널명
Archiv der Pharmazie
358
10