A patent review of RAF kinase inhibitors (2010–2018)

Man, Ruo‐Jun; Zhang, Ya‐Liang; Jiang, Aiqin; Zhu, Hai‐Liang

doi:10.1080/13543776.2019.1651842

Cited by 14 publications

(10 citation statements)

References 99 publications

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“…More recent examples of RAF inhibitors include vemurafenib and dabrafenib, and these inhibitors are far more specific and effective, especially in melanomas which are driven by the BRAF-mutant BRAF V600E . 102 Fu et al used 51 to design analogues, incorporating a pyrazolo [3,4-d]pyrimidine in place of the pyridine (Fig. 14).…”

Section: Rsc Medicinal Chemistry Reviewmentioning

confidence: 99%

Recent developments in anticancer kinase inhibitors based on the pyrazolo[3,4-d]pyrimidine scaffold

Baillache

Unciti‐Broceta

2020

RSC Med. Chem.

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Section: Rsc Medicinal Chemistry Reviewmentioning

confidence: 99%

Recent developments in anticancer kinase inhibitors based on the pyrazolo[3,4-d]pyrimidine scaffold

Baillache

Unciti‐Broceta

2020

RSC Med. Chem.

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“…Therefore, it is speculated that liraglutide can not only activate the ERK1/2 signal pathway and promote the proliferation of β-cells, but also promote the lysis of RKIP, leading to an increase in HCNP, further acting on the cholinergic nervous system and promoting the release of insulin. RKIP can bind to Raf-1 and MEK-1, interfere with the phosphorylation and activation of MEK-1 by Raf-1, further inhibit the ERK1/2 signal pathway, and attenuate cell proliferation (15,16). Zhang et al showed that RKIP is specifically present in pancreatic islet cells using fluorescence double staining, immunohistochemical staining and other techniques, inhibiting the MAPK signal pathway and inhibiting the proliferation of pancreatic β-cells (9).…”

Section: Discussionmentioning

confidence: 99%

Liraglutide inhibits the progression of prediabetes in rats by reducing Raf-1 kinase inhibitor protein

Gao

Guo

et al. 2021

Ann Transl Med

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Background: The cleavage product of Raf-1 kinase inhibitor protein (RKIP), hippocampal cholinergic neurostimulating peptide (HCNP) is involved in the promotion of insulin secretion. Studies have shown that liraglutide can inhibit the progression of prediabetes. This study aims to investigate whether the above effects of liraglutide are related to RKIP and HCNP.Methods: Insulin-1 (INS-1) cells were divided into control group (CON), HCNP group, and HCNP + darifenacin group (H-DAR). The three groups were cultured with Roswell Park Memorial Institute (RPMI) 1640, synthetic HCNP (50 pg/mL) and RPMI 1640, and HCNP + RPMI 1640 + darifenacin respectively. Subsequently, twelve 12-to 14-week-old Otsuka Long-Evans Tokushima Fatty (OLETF) rats were randomly divided into 2 groups: the placebo group (PBO) and the liraglutide treatment group (LIRA). Six Long Evans Tokushima Otsuka (LETO) rats were used as the control group (CON). The LIRA group was given liraglutide 200 μg/kg intraperitoneally twice a day. After 12 weeks, body weight, fasting blood glucose, 2 hours postprandial blood glucose, and insulin resistance index were recorded. Western blot was used to detect expression level of C-RKIP, N-RKIP, and extracellular signal-regulated kinase of phosphorylation (p-ERK). Real-time quantitative polymerase chain reaction (qRT-PCR) to detect pancreatic tissue choline acetyltransferase (ChAT) and M3 cholinergic receptor (M3R) gene expression levels.Results: At glucose concentrations of 5.6 and 16.7 mmol/L, the insulin content in the HCNP group was higher than that in the CON and H-DAR groups (all P<0.01). The body weight and fasting serum insulin (FINS) of rats in the PBO group were higher than those in the LIRA group and the CON group (P<0.01).The relative content of C-RKIP protein in the PBO group was higher than that in the LIRA and CON groups (P<0.01). The relative content of N-RKIP protein and p-ERK protein was lower than that in the LIRA and CON group (P<0.05 and P<0.01, respectively). ChAT and M3R gene expression levels in PBO group were lower than those in LIRA and CON group (P<0.01).Conclusions: Liraglutide promotes the production of HCNP, can increase ChAT activity, activate M3R, and further promote the secretion of insulin.

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“…Mutations on proteins involved in such signaling mechanisms are key drivers of different types of tumor: B-Raf, N-Ras, K-Ras are found in melanoma, colorectal cancer, thyroid cancer and lung cancer, among others [151][152][153]. TKIs were developed in order to specifically inhibit the mutated proteins, i.e., vemurafenib is a small molecule specifically conceived in order to target the B-Raf V600E mutation [154]. These TKIs are associated with high initial response-rates; however, almost all patients experience drug resistance and tumor recurrence, mostly due to the downstream reactivation of the same proliferative pathway [155].…”

Section: Targeting Proliferative Pathwaysmentioning

confidence: 99%

Cancer Stem Cells—Key Players in Tumor Relapse

Marzagalli

Fontana

Raimondi

et al. 2021

Cancers

102

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Tumor relapse and treatment failure are unfortunately common events for cancer patients, thus often rendering cancer an uncurable disease. Cancer stem cells (CSCs) are a subset of cancer cells endowed with tumor-initiating and self-renewal capacity, as well as with high adaptive abilities. Altogether, these features contribute to CSC survival after one or multiple therapeutic approaches, thus leading to treatment failure and tumor progression/relapse. Thus, elucidating the molecular mechanisms associated with stemness-driven resistance is crucial for the development of more effective drugs and durable responses. This review will highlight the mechanisms exploited by CSCs to overcome different therapeutic strategies, from chemo- and radiotherapies to targeted therapies and immunotherapies, shedding light on their plasticity as an insidious trait responsible for their adaptation/escape. Finally, novel CSC-specific approaches will be described, providing evidence of their preclinical and clinical applications.

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A patent review of RAF kinase inhibitors (2010–2018)

Cited by 14 publications

References 99 publications

Recent developments in anticancer kinase inhibitors based on the pyrazolo[3,4-d]pyrimidine scaffold

Recent developments in anticancer kinase inhibitors based on the pyrazolo[3,4-d]pyrimidine scaffold

Liraglutide inhibits the progression of prediabetes in rats by reducing Raf-1 kinase inhibitor protein

Cancer Stem Cells—Key Players in Tumor Relapse

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