c-KIT小分子抑制剂作为黑色素瘤的治疗策略:临床见解,SAR和未来方向。

IF 3.6 3区 医学 Q2 CHEMISTRY, MEDICINAL
Shubham C Rivonker, Hossam Nada, Cho Jaemin, Yong-Jun Kwon, Kyeong Lee
{"title":"c-KIT小分子抑制剂作为黑色素瘤的治疗策略:临床见解,SAR和未来方向。","authors":"Shubham C Rivonker, Hossam Nada, Cho Jaemin, Yong-Jun Kwon, Kyeong Lee","doi":"10.1002/ardp.70113","DOIUrl":null,"url":null,"abstract":"<p><p>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.</p>","PeriodicalId":128,"journal":{"name":"Archiv der Pharmazie","volume":"358 10","pages":"e70113"},"PeriodicalIF":3.6000,"publicationDate":"2025-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"c-KIT Small Molecule Inhibitors as a Therapeutic Strategy for Melanoma: Clinical Insights, SAR, and Future Directions.\",\"authors\":\"Shubham C Rivonker, Hossam Nada, Cho Jaemin, Yong-Jun Kwon, Kyeong Lee\",\"doi\":\"10.1002/ardp.70113\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>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.</p>\",\"PeriodicalId\":128,\"journal\":{\"name\":\"Archiv der Pharmazie\",\"volume\":\"358 10\",\"pages\":\"e70113\"},\"PeriodicalIF\":3.6000,\"publicationDate\":\"2025-10-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Archiv der Pharmazie\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1002/ardp.70113\",\"RegionNum\":3,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Archiv der Pharmazie","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1002/ardp.70113","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0

摘要

原癌基因c-KIT在细胞生长、存活和增殖等几个细胞过程中起着关键作用。c-KIT的过表达与多种恶性肿瘤的发病机制有关,如胃肠道间质瘤、急性髓性白血病(AML)、肥大细胞增多症和黑色素瘤。在肢端、粘膜和慢性晒伤黑色素瘤亚型中观察到c-KIT突变,这标志着它是黑色素瘤的关键治疗靶点。此外,与黑色素瘤相关的发病率和死亡率的增加进一步标志着开发新的治疗方式的重要性。本文就c-KIT小分子黑色素瘤抑制剂的设计、构效关系、机制和开发等方面的进展进行综述,以期指导未来基于c-KIT的黑色素瘤治疗。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
c-KIT Small Molecule Inhibitors as a Therapeutic Strategy for Melanoma: Clinical Insights, SAR, and Future Directions.

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.

求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
Archiv der Pharmazie
Archiv der Pharmazie 医学-化学综合
CiteScore
7.90
自引率
5.90%
发文量
176
审稿时长
3.0 months
期刊介绍: Archiv der Pharmazie - Chemistry in Life Sciences is an international journal devoted to research and development in all fields of pharmaceutical and medicinal chemistry. Emphasis is put on papers combining synthetic organic chemistry, structural biology, molecular modelling, bioorganic chemistry, natural products chemistry, biochemistry or analytical methods with pharmaceutical or medicinal aspects such as biological activity. The focus of this journal is put on original research papers, but other scientifically valuable contributions (e.g. reviews, minireviews, highlights, symposia contributions, discussions, and essays) are also welcome.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:604180095
Book学术官方微信