Identification and Kinetic Characterization of Serum- and Glucocorticoid-Regulated Kinase Inhibitors Using a Fluorescence Polarization–Based Assay

Kim, Jeongeun; Kim, Dong‐Hee; Jung, Hyunho; Lee, Jinho; Hong, Victor Sukbong

doi:10.1177/24725552211002465

Cited by 3 publications

(2 citation statements)

References 28 publications

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“…[59] Concomitantly, kinase genes that promote tumor growth, metastasis. [60][61][62] or drug resistance were downregulated. [63] including serum/glucocorticoid regulated kinase 2(SGK2), calcium/calmodulin-dependent protein kinase II alpha (CAMK2A), eph receptor B2(EPHB2) and microtubule-associated serine/threonine kinase 1 (MAST1) which might be regarded as biomarkers for cancer prognosis (Figure 7C).…”

Section: Gene Expression Analysismentioning

confidence: 99%

A Tumoricidal Lipoprotein Complex Electrostatically Stabilized on Mesoporous Silica as Nanotherapeutics and Nanoadjuvant for Potentiating Immunotherapy of Triple Negative Breast Cancer

Pei,

Li,

et al. 2023

Adv Funct Materials

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As the most aggressive subtype, triple‐negative breast cancer (TNBC) without definitive targets represents a high probability of metastasis. Nevertheless, the presence of high‐level tumor‐infiltrating lymphocytes in the TNBC tumor microenvironment (TME) suggests patients may benefit from immunotherapy. In this study, bovine α‐lactalbumin coupled with oleic acid that forms tumoricidal lipid–protein complex (BAMLET) is electrostatically stabilized on the surface of amino‐functionalized mesoporous silica nanoparticles (MSN‐NH2). It is found that MSN‐NH2 may cause partial conformational changes of immobilized proteins due to electrostatic interactions. Therefore, BAMLET covered MSN‐NH2 (BMSN) as a drug cargo that can not only induce selectively oncolytic effect but kill tumor cells with rapid kinetics. Moreover, the hemolytic activity of BMSN conjugated with pre‐formed serum protein corona is largely reduced which may avoid the poor hemocompatibility caused by BAMLET. Furthermore, the in vivo study indicates that the combinational use of drug‐loaded BMSN and immune checkpoint small‐molecule inhibitor can efficiently inhibit the growth of solid TNBC tumors and activate immune response by sufficient infiltration of immune cells in the TME and prevent the seeding of circulating tumor cells. Therefore, the constructed BMSN provides an integrated nanotherapeutics and a nanoadjuvant with superior anticancer performance to combat TNBC.

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Section: Gene Expression Analysismentioning

confidence: 99%

A Tumoricidal Lipoprotein Complex Electrostatically Stabilized on Mesoporous Silica as Nanotherapeutics and Nanoadjuvant for Potentiating Immunotherapy of Triple Negative Breast Cancer

Pei,

Li,

et al. 2023

Adv Funct Materials

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“…Serum and glucocorticoid-regulated protein kinases (SGKs) are serine-threonine protein kinases of the AGC family (protein kinase A, G, C), which are encoded by three genes located on different chromosomes (SGK1, SGK2, and SGK3) [ 13 ]. SGK1 is widely expressed in human body and involved in regulating multiple functions, such as apoptosis, DNA damage, signal transduction, and ion transmembrane transport [ 14 ].…”

Section: Introductionmentioning

confidence: 99%

Upregulation of serum and glucocorticoid-regulated kinase 1 (SGK1) ameliorates doxorubicin-induced cardiotoxic injury, apoptosis, inflammation and oxidative stress by suppressing glucose regulated protein 78 (GRP78)-mediated endoplasmic reticulum stress

Wang

Han

2021

Bioengineered

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The clinical application of doxorubicin (Dox) in tumor chemotherapy is limited by time-dependent and dose-dependent cardiotoxicity. Hence, there is an urgent need to elucidate doxorubicin cardiotoxicity and to solve the difficult problem in clinical application. It has been verified that serum and glucocorticoid-regulated kinase 1 (SGK1) possess cardioprotective effects. Here, H9c2 cells were treated with 1 μM doxorubicin for 24 h to establish doxorubicin cardiotoxicity, so as to determine the biological role of SGK1 in doxorubicin cardiomyopathy and to elucidate the underlying molecular mechanism. SGK1 level in doxorubicin-treated H9c2 cells was assessed by performing Western blot assay and RT-qPCR. CCK-8 assay and TUNEL staining were employed to evaluate the cell viability and cell apoptosis. Besides, apoptosis-related proteins were measured by Western blot assay to analyze cell apoptosis. Additionally, the release of TNF-α, IL-1β, IL-6, and IL-10 and the levels of ROS, MDA, and SOD were detected to reflect inflammation and oxidative stress. Moreover, Western blot assay was adopted for determination of ERS-associated proteins. Results revealed that SGK1 was downregulated in doxorubicin-treated H9c2 cells. Upregulation of SGK1 alleviated doxorubicin-induced cardiotoxic injury, cell apoptosis, inflammation and oxidative stress in H9c2 cells. Moreover, SGK1 overexpression mitigated doxorubicin-induced ERS in H9c2 cells. The suppressing effects of SGK1 on doxorubicin-induced cardiotoxic injury, apoptosis, inflammation, oxidative stress and ERS in H9c2 cells were partially abolished upon GRP78 overexpression. To conclude, upregulation of SGK1 may alleviate doxorubicin cardiotoxicity by repressing GRP78-mediated ERS.

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SGK3 overexpression correlates with a poor prognosis in endoscopically resected superficial esophageal squamous cell neoplasia: A long-term study

Xu¹,

Li²,

Li³

et al. 2023

World J Gastroenterol

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Identification and Kinetic Characterization of Serum- and Glucocorticoid-Regulated Kinase Inhibitors Using a Fluorescence Polarization–Based Assay

Cited by 3 publications

References 28 publications

A Tumoricidal Lipoprotein Complex Electrostatically Stabilized on Mesoporous Silica as Nanotherapeutics and Nanoadjuvant for Potentiating Immunotherapy of Triple Negative Breast Cancer

A Tumoricidal Lipoprotein Complex Electrostatically Stabilized on Mesoporous Silica as Nanotherapeutics and Nanoadjuvant for Potentiating Immunotherapy of Triple Negative Breast Cancer

Upregulation of serum and glucocorticoid-regulated kinase 1 (SGK1) ameliorates doxorubicin-induced cardiotoxic injury, apoptosis, inflammation and oxidative stress by suppressing glucose regulated protein 78 (GRP78)-mediated endoplasmic reticulum stress

SGK3 overexpression correlates with a poor prognosis in endoscopically resected superficial esophageal squamous cell neoplasia: A long-term study

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