Recent advances of RAF (rapidly accelerated fibrosarcoma) inhibitors as anti-cancer agents

Ammar, Usama M.; Abdel‐Maksoud, Mohammed S.; Oh, Chang‐Hyun

doi:10.1016/j.ejmech.2018.09.005

Cited by 39 publications

(20 citation statements)

References 114 publications

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“…Additional anti-cancer targets have been identified that are designed to disrupt cancer cell survival. These include inhibitors of RAF [158,159], IQGAP [160], and dual inhibitors of RAF-MEK-ERK and PI3K/PDK1-AKT pathways [161].…”

Section: Conclusion and Future Perspectivesmentioning

confidence: 99%

Extracellular Signal-Regulated Kinase: A Regulator of Cell Growth, Inflammation, Chondrocyte and Bone Cell Receptor-Mediated Gene Expression

Malemud

2019

IJMS

122

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Extracellular signal-regulated kinase (ERK) is a member of the mitogen-activated protein kinase family of signaling molecules. ERK is predominantly found in two forms, ERK1 (p44) and ERK2 (p42), respectively. There are also several atypical forms of ERK, including ERK3, ERK4, ERK5 and ERK7. The ERK1/2 signaling pathway has been implicated in many and diverse cellular events, including proliferation, growth, differentiation, cell migration, cell survival, metabolism and transcription. ERK1/2 is activated (i.e., phosphorylated) in the cytosol and subsequently translocated to the nucleus, where it activates transcription factors including, but not limited to, ETS, c-Jun, and Fos. It is not surprising that the ERK1/2 signaling cascade has been implicated in many pathological conditions, namely, cancer, arthritis, chronic inflammation, and osteoporosis. This narrative review examines many of the cellular events in which the ERK1/2 signaling cascade plays a critical role. It is anticipated that agents designed to inhibit ERK1/2 activation or p-ERK1/2 activity will be developed for the treatment of those diseases characterized by dysregulated gene expression through ERK1/2 activation.

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Section: Conclusion and Future Perspectivesmentioning

confidence: 99%

Extracellular Signal-Regulated Kinase: A Regulator of Cell Growth, Inflammation, Chondrocyte and Bone Cell Receptor-Mediated Gene Expression

Malemud

2019

IJMS

122

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“…To further investigate the role of GHR in the MAPK pathway, this study also detected the association between GHR reduction and the expression of RAF, as well as MEK. The MAPK signaling cascade is first triggered by RAS G protein activation, activating RAF and further causing mitogen‐activated protein kinase (MAPK) phosphorylation . This signaling pathway regulates cell‐cycle progression and apoptosis in diverse types of cells, and induces events related to both cell proliferation and cell‐cycle arrest .…”

Section: Discussionmentioning

confidence: 99%

Growth hormone receptor promotes breast cancer progression via the BRAF/MEK/ERK signaling pathway

Zhu

et al. 2020

FEBS Open Bio

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Growth hormone receptor (GHR), a member of the class I cytokine receptor family, plays key roles in cancer progression. Recently, GHR has been reported to be associated with breast cancer development, but the molecular mechanism of GHR in this malignancy is not fully understood. To investigate this issue, we stably inhibited GHR in breast cancer cell lines, which were observed to reduce cell proliferation, tumor growth and induction of apoptosis, and arrest the cell‐cycle arrest at the G1–S phase transition. In addition, GHR silencing suppressed the protein levels of B‐Raf proto‐oncogene, serine/threonine kinase (BRAF), Mitogen‐activated protein kinase kinase (MEK) and Extracellular regulated protein kinases (ERK). These findings suggest that GHR may mediate breast cell progression and apoptosis through control of the cell cycle via the BRAF/MEK/ERK signaling pathway.

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“…[ 41 ] It was estimated that there were 18.1 million new cancer cases, resulting in 9.6 million deaths in 2018. [ 41 ] More than 100 drugs have been approved for the treatment of cancer, but most of them have generated drug resistance along with fatal side effects, [ 42,43 ] creating an urgent need for the development of novel anticancer agents. Isatin is an important pharmacophore in the discovery of new anticancer agents, and many anticancer agents which are exemplified by semaxanib, sunitinib, and nintedanib have already been used in clinical practice for the treatment of various cancers including drug‐resistant cancers.…”

Section: Anticancer Activitymentioning

confidence: 99%

Isatin dimers and their biological activities

Zhang

Liu

et al. 2020

Archiv der Pharmazie

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Dimerization is a promising strategy to develop novel drug candidates that could extend the biological spectrum, enhance the activity, overcome drug resistance, as well as improve pharmacological, pharmacokinetic, and physicochemical profiles. Isatin dimers possess a broad spectrum of biological properties and the isatin dimer indirubin has already been used in the clinic, revealing the potential of isatin dimers as putative drugs. This review covers the recent advances of isatin dimers as pharmacologically significant scaffolds and the structure–activity relationship to set up the direction for the design and development of isatin dimers with higher efficiency and lower toxicity.

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Recent advances of RAF (rapidly accelerated fibrosarcoma) inhibitors as anti-cancer agents

Cited by 39 publications

References 114 publications

Extracellular Signal-Regulated Kinase: A Regulator of Cell Growth, Inflammation, Chondrocyte and Bone Cell Receptor-Mediated Gene Expression

Extracellular Signal-Regulated Kinase: A Regulator of Cell Growth, Inflammation, Chondrocyte and Bone Cell Receptor-Mediated Gene Expression

Growth hormone receptor promotes breast cancer progression via the BRAF/MEK/ERK signaling pathway

Isatin dimers and their biological activities

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