RGD Reference Report - NVP-BSK805, an Inhibitor of JAK2 Kinase, Significantly Enhances the Radiosensitivity of Esophageal Squamous Cell Carcinoma in vitro and in vivo. - Rat Genome Database

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NVP-BSK805, an Inhibitor of JAK2 Kinase, Significantly Enhances the Radiosensitivity of Esophageal Squamous Cell Carcinoma in vitro and in vivo.

Authors: Hua, Yuhui  Wang, Weijia  Zheng, Xiaoli  Yang, Ling  Wu, Hongjin  Hu, Zhaoyang  Li, Ying  Yue, Jing  Jiang, Zhenzhen  Zhang, Xiaoyan  Hou, Qiang  Wu, Shixiu 
Citation: Hua Y, etal., Drug Des Devel Ther. 2020 Feb 24;14:745-755. doi: 10.2147/DDDT.S203048. eCollection 2020.
RGD ID: 127285669
Pubmed: PMID:32158193   (View Abstract at PubMed)
PMCID: PMC7047839   (View Article at PubMed Central)
DOI: DOI:10.2147/DDDT.S203048   (Journal Full-text)


Purpose: Radiotherapy is one major curative treatment modality for esophageal squamous cell carcinoma (ESCC) patients. This study aimed to find out small-molecular kinase inhibitors, which can significantly enhance the radiosensitivity of ESCC in vitro and in vivo.
Materials and Methods: Ninety-three kinase inhibitors were tested for their radiosensitizing effect in ESCC cells through high-content screening. The radiosensitizing effect of kinase inhibitors was investigated in vitro by detection of DNA double-strand breaks (DSBs) and clonogenic survival assay. By the establishment of xenograft tumor models in BALB/c nude mice, the radiosensitizing effect of kinase inhibitors was investigated in vivo.
Results: Among the 93 kinase inhibitors tested, we found NVP-BSK805, an inhibitor of JAK2 kinase, significantly radiosensitized ESCC cells through enhancing DSBs, inhibiting DNA damage repair and arresting cell cycle in G2/M or G0/G1 phase. After treatment with NVP-BSK805, ESCC cells showed decreased clonogenic survival and delayed tumor growth in vivo. JAK2 kinase was highly expressed in tumor tissues of ESCC patients, while rarely expressed in matched normal esophageal epithelial tissues. Survival analysis revealed JAK2 kinase as a prognostic factor of ESCC patients treated with chemoradiotherapy.
Conclusion: Our study discovered JAK2 kinase as an attractive target to enhance the radiosensitivity of ESCC cells in vitro and in vivo.

RGD Manual Disease Annotations    Click to see Annotation Detail View
TermQualifierEvidenceWithReferenceNotesSourceOriginal Reference(s)
esophagus squamous cell carcinoma severityIEP 127285669protein:increased phosphorylation:esophagus squamous epithelium (human)RGD 
esophagus squamous cell carcinoma severityISOJAK2 (Homo sapiens)127285669; 127285669protein:increased phosphorylation:esophagus squamous epithelium (human)RGD 

Objects Annotated

Genes (Rattus norvegicus)
Jak2  (Janus kinase 2)

Genes (Mus musculus)
Jak2  (Janus kinase 2)

Genes (Homo sapiens)
JAK2  (Janus kinase 2)


Additional Information