دورية أكاديمية
أعرض في EDS

Drug resistance in targeted cancer therapies with RAF inhibitors.

التفاصيل البيبلوغرافية
العنوان: Drug resistance in targeted cancer therapies with RAF inhibitors.
المؤلفون: Degirmenci U; The Laboratory of Cancer Signaling, National Cancer Centre Singapore, Singapore 169610, Singapore.; Authors contributed equally., Yap J; The Laboratory of Cancer Signaling, National Cancer Centre Singapore, Singapore 169610, Singapore.; The Cancer and Stem Cell Program, Duke-NUS Medical School, Singapore 169857, Singapore.; Authors contributed equally., Sim YRM; The Laboratory of Cancer Signaling, National Cancer Centre Singapore, Singapore 169610, Singapore., Qin S; The Laboratory of Cancer Signaling, National Cancer Centre Singapore, Singapore 169610, Singapore., Hu J; The Laboratory of Cancer Signaling, National Cancer Centre Singapore, Singapore 169610, Singapore.; The Cancer and Stem Cell Program, Duke-NUS Medical School, Singapore 169857, Singapore.
المصدر: Cancer drug resistance (Alhambra, Calif.) [Cancer Drug Resist] 2021 Jun 17; Vol. 4 (3), pp. 665-683. Date of Electronic Publication: 2021 Jun 17 (Print Publication: 2021).
نوع المنشور: Journal Article; Review
اللغة: English
بيانات الدورية: Publisher: OAE Publishing Inc Country of Publication: United States NLM ID: 101738710 Publication Model: eCollection Cited Medium: Internet ISSN: 2578-532X (Electronic) Linking ISSN: 2578532X NLM ISO Abbreviation: Cancer Drug Resist Subsets: PubMed not MEDLINE
أسماء مطبوعة: Original Publication: Alhambra, CA : OAE Publishing Inc., 2018-
مستخلص: Hyperactive RAS/RAF/MEK/ERK signaling has a well-defined role in cancer biology. Targeting this pathway results in complete or partial regression of most cancers. In recent years, cancer genomic studies have revealed that genetic alterations that aberrantly activate the RAS/RAF/MEK/ERK signaling mainly occur on RAF or upstream, which motivated the extensive development of RAF inhibitors for cancer therapy. Currently, the first-generation RAF inhibitors have been approved for treating late-stage cancers with BRAF(V600E) mutations. Although these inhibitors have achieved promising outcomes in clinical treatments, their efficacy is abolished by quick-rising drug resistance. Moreover, cancers with hyperactive RAS exhibit intrinsic resistance to these drugs. To resolve these problems, the second-generation RAF inhibitors have been designed and are undergoing clinical evaluations. Here, we summarize the recent findings from mechanistic studies on RAF inhibitor resistance and discuss the critical issues in the development of next-generation RAF inhibitors with better therapeutic index, which may provide insights for improving targeted cancer therapy with RAF inhibitors.
Competing Interests: All authors declared that there are no conflicts of interest.
(© The Author(s) 2021.)
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فهرسة مساهمة: Keywords: RAF inhibitors; RAF/KSR family kinase; RAS/RAF/MEK/ERK signaling; drug resistance; oncogenic mutation; regulatory spine; targeted therapy
تواريخ الأحداث: Date Created: 20220518 Latest Revision: 20220716
رمز التحديث: 20240628
مُعرف محوري في PubMed: PMC9094075
DOI: 10.20517/cdr.2021.36
PMID: 35582307
قاعدة البيانات: MEDLINE
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