Potent Imidazothiazole-based Inhibitor of BRAF V600E Overcomes Acquired Resistance <i>via</i> Inhibition of RAF Dimerization in PLX4032-resistant Melanoma

Poudel, Muna; Kım, Garam; Bhattarai, Poshan Yugal; Shin, Seung Yong; Zaraei, Seyed–Omar; Oh, Chang‐Hyun; Choi, Hong Seok

doi:10.21873/anticanres.15773

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“…Moreover, the overexpression of RCS2, which is negative regulator of MAPK and AKT signaling, can suppress melanoma growth (41). Additionally, the drug KS28 that inhibit RAF dimer formation correlated with overcoming BRAF inhibitor resistance in melanoma by down-regulating the MEK/ERK pathway (42). However, in this study, we could not find any possibility that the isolated lncRNAs and the molecules that make up the ERK/MAPK signal function as ceRNAs.…”

Section: Discussionmentioning

confidence: 61%

Identification of BRAF Inhibitor Resistance–associated lncRNAs Using Genome-scale CRISPR-Cas9 Transcriptional Activation Screening

WEN,

HAN,

HOSOYA

et al. 2024

Anticancer Res

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Section: Discussionmentioning

confidence: 61%

Identification of BRAF Inhibitor Resistance–associated lncRNAs Using Genome-scale CRISPR-Cas9 Transcriptional Activation Screening

WEN,

HAN,

HOSOYA

et al. 2024

Anticancer Res

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“…The RAS-RAF-MEK-ERK pathway is a potential target for melanoma therapy. Among the RAF kinase subtypes, BRAF is the main activator of the MAPK signaling pathway [ 63 ]. V600E mutated B-RAF is over-activated and over-expressed in some melanoma patients [ 64 ].…”

Section: Bench Study: Exploration Of the Pharmacological Activity Of ...mentioning

confidence: 99%

From Bench to Bedside: What Do We Know about Imidazothiazole Derivatives So Far?

Guo

Zhu

et al. 2023

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Imidazothiazole derivatives are becoming increasingly important in therapeutic use due to their outstanding physiological activities. Recently, applying imidazothiazole as the core, researchers have synthesized a series of derivatives with biological effects such as antitumor, anti-infection, anti-inflammatory and antioxidant effects. In this review, we summarize the main pharmacological effects and pharmacological mechanisms of imidazothiazole derivates; the contents summarized herein are intended to advance the research and rational development of imidazothiazole-based drugs in the future.

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Potent Imidazothiazole-based Inhibitor of BRAF V600E Overcomes Acquired Resistance via Inhibition of RAF Dimerization in PLX4032-resistant Melanoma

Cited by 2 publications

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Identification of BRAF Inhibitor Resistance–associated lncRNAs Using Genome-scale CRISPR-Cas9 Transcriptional Activation Screening

Identification of BRAF Inhibitor Resistance–associated lncRNAs Using Genome-scale CRISPR-Cas9 Transcriptional Activation Screening

From Bench to Bedside: What Do We Know about Imidazothiazole Derivatives So Far?

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