Combination of RSK inhibitor LJH-685 and FLT3 inhibitor FF-10101 promoted apoptosis and proliferation inhibition of AML cell lines

Zhang, Sen; Li, Jun; Lu, Zi-Yi; Xue, Yu-Tong; Mu, Xing-Ru; Liu, Yang; Cao, Jiang; Li, Zhenyu; Li, Feng; Xu, Kai-Lin; Wu, Qing-Yun

doi:10.1007/s13402-022-00703-7

Cited by 5 publications

(3 citation statements)

References 36 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Therefore it is necessary to delve deeper into the possible anticancerigenic activity of these compounds. In this way, in this study, the interaction of 19 quinolone derivatives on RSK-4 was evaluated using 6rv2 protein and LJH685 (RSK-4 inhibitor) [39] as a theoretical tool in a Docking model. [41] The results (Table 1 and Figure On the other hand, it is important to mention that there are some reports which suggest that the interaction protein-ligand complex depends on energy levels which may determine their stability.…”

Section: Resultsmentioning

confidence: 99%

“…The interaction of quinone derivatives with RSK-4 was evaluated using 6rv2 [38] protein and LJH685 (2,6-Difluoro-4-[4-[4-(4-methylpiperazin-1-yl)phenyl]pyridin-3-yl]phenol) [39] as theoretical tools. Besides, to evaluate the types of binding energy involved in the interaction of quinolone derivatives with the 6rv2 [40] protein surface, the Docking Server software was used.…”

Section: Ligand-protein Complexmentioning

confidence: 99%

See 1 more Smart Citation

Evaluation of Interaction of Some Quinolone Derivatives on RSK-4 Using a Theoretical Model

Rosas-Nexticapa¹,

Figueroa‐Valverde²,

Alvarez-Ramirez³

et al. 2022

Clin Cancer Investig J

View full text Add to dashboard Cite

Prostate cancer is one of the leading causes of death among men worldwide; Some data suggest that ribosomal S6 p90 kinase (RSK 1-4), which belongs to the group of highly conserved Ser/Thr kinases, has been related to an increase in prostate cancer levels. For this reason, the aim of this study was to evaluate the theoretical interaction of some quinolone derivatives (compounds 1-19) with RSK-4 using 6rv2 protein and RSK-14 inhibitor (LJH685) in a docking model. The results showed that some quinolone derivatives (12, 15, 17, and 18) could interact with the 6rv2 protein surface in a different manner than LJH685. This phenomenon could be translated as greater RSK-14 inhibition, resulting in a decrease in prostate cancer levels. Analyzing these data, these quinolone derivatives could be considered good compounds to treat prostate cancer.

show abstract

Section: Resultsmentioning

confidence: 99%

Section: Ligand-protein Complexmentioning

confidence: 99%

Evaluation of Interaction of Some Quinolone Derivatives on RSK-4 Using a Theoretical Model

Rosas-Nexticapa¹,

Figueroa‐Valverde²,

Alvarez-Ramirez³

et al. 2022

Clin Cancer Investig J

View full text Add to dashboard Cite

show abstract

“…By exploiting structural differences in the NTKD between RSK isoforms, isoform-selective RSK inhibitors can be designed. For example, exposure of A549 lung adenocarcinoma cells to BI-D1870 led to decreased RSK1 protein expression, which was negatively associated with cell migration and proliferation [90] . Nevertheless, BI-D1870 shows irreparable drawbacks, including high clearance, poor drug stability, and a short plasma half-life [78] .…”

Section: Rsk Inhibitorsmentioning

confidence: 99%

Regulation and function of the RSK family in colorectal cancer

Wang,

Han,

Lei

et al. 2024

J Cancer Metastasis Treat

View full text Add to dashboard Cite

P90 Ribosomal S6 Kinases (RSKs) constitute a class of Serine/Threonine (Ser/Thr) protein kinases and play a critical role as downstream targets in the Raf/MEK/ERK signaling pathway. Gaining insight into the biological function of RSK family proteins, given their functions in various tumors, is vital. The RSK family is involved in the regulation of cellular functions including cell proliferation, motility, invasion, and survival. The RSK family comprises four human isoforms (RSK1, RSK2, RSK3, and RSK4). The activation of RSK protein kinases is mediated through direct phosphorylation by extracellular signal-regulated kinase 1/2 (ERK1/2) and phosphoinositide-dependent kinase 1 (PDK1) after the Ras/MAPK (mitogen-activated protein kinase) pathway is activated. Recent evidence suggests that RSK family proteins promote the onset and metastasis of cancer, leading to the association of the protein expression of these kinases with various cancer types, such as colorectal cancer (CRC), breast cancer, lung cancer, kidney cancer, leukemia, esophageal squamous cell carcinoma, ovarian cancer, glioma, and endometrial cancer. In this review, we summarize the latest research on the RSK family, focusing on its role in patients with CRC, along with associated treatment challenges and limitations. This information enhances our comprehension of the regulation and function of RSK family proteins, highlighting their potential as both clinical biomarkers for diagnosing CRC and targets for molecular therapeutic interventions in the future.

show abstract

Understanding mechanisms of resistance to FLT3 inhibitors in adult FLT3-mutated acute myeloid leukemia to guide treatment strategy

Ruglioni,

Crucitta,

Luculli

et al. 2024

Critical Reviews in Oncology/Hematology

View full text Add to dashboard Cite

Combination of RSK inhibitor LJH-685 and FLT3 inhibitor FF-10101 promoted apoptosis and proliferation inhibition of AML cell lines

Cited by 5 publications

References 36 publications

Evaluation of Interaction of Some Quinolone Derivatives on RSK-4 Using a Theoretical Model

Evaluation of Interaction of Some Quinolone Derivatives on RSK-4 Using a Theoretical Model

Regulation and function of the RSK family in colorectal cancer

Understanding mechanisms of resistance to FLT3 inhibitors in adult FLT3-mutated acute myeloid leukemia to guide treatment strategy

Contact Info

Product

Resources

About