Diacylglycerol kinase α-selective inhibitors induce apoptosis and reduce viability of melanoma and several other cancer cell lines.


:Diacylglycerol (DG) kinase (DGK), which phosphorylates DG to generate phosphatidic acid (PA), consists of ten isozymes (α-к). Recently, we identified a novel small molecule inhibitor, CU-3, that selectively inhibits the activity of the α isozyme. In addition, we newly obtained Compound A, which selectively and strongly inhibits type I DGKs (α, β, and γ). In the present study, we demonstrated that both CU-3 and Compound A induced apoptosis (caspase 3/7 activity and DNA fragmentation) and viability reduction of AKI melanoma cells. Liquid chromatography-mass spectrometry revealed that the production of 32:0- and 34:0-PA species was commonly attenuated by CU-3 and Compound A, suggesting that lower levels of these PA molecular species are involved in the apoptosis induction and viability reduction of AKI cells. We determined the effects of the DGKα inhibitors on several other cancer cell lines derived from refractory cancers. In addition to melanoma, the DGKα inhibitors enhanced caspase 3/7 activity and reduced the viability of hepatocellular carcinoma, glioblastoma, and pancreatic cancer cells, but not breast adenocarcinoma cells. Interestingly, Western blot analysis indicated that the DGKα expression levels were positively correlated with the sensitivity to the DGK inhibitors. Because both CU-3 and Compound A induced interleukin-2 production by T cells, it is believed that these two compounds can enhance cancer immunity. Taken together, our results suggest that DGKα inhibitors are promising anticancer drugs.


J Cell Biochem


Yamaki A,Akiyama R,Murakami C,Takao S,Murakami Y,Mizuno S,Takahashi D,Kado S,Taketomi A,Shirai Y,Goto K,Sakane F




Has Abstract


2019-06-01 00:00:00












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    abstract::A23187 stimulates the metabolism of endogenous as well as exogenous arachidonic acid (AA) and eicosapentaenolc acid (EPA) to their corresponding leukotrienes in human neutrophils. In contrast, conflicting results have been obtained concerning the effect of FMLP on the metabolism of these fatty acids. In the present st...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章


    authors: Mahadevappa VG,Powell WS

    更新日期:1989-07-01 00:00:00

  • Transient increase in vimentin phosphorylation and vimentin-HSC70 association in 9L rat brain tumor cells experiencing heat-shock.

    abstract::Characteristic changes in vimentin were studied in 9L rat brain tumor cells treated at 45 degrees C. During heat-shock treatment, vimentin molecules were rapidly phosphorylated and reorganized from a filamentous form into a perinuclear higher-order structure that was less extractable by nonionic detergent. These effec...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章


    authors: Cheng TJ,Lai YK

    更新日期:1994-01-01 00:00:00

  • ClC-3 Promotes Osteogenic Differentiation in MC3T3-E1 Cell After Dynamic Compression.

    abstract::ClC-3 chloride channel has been proved to have a relationship with the expression of osteogenic markers during osteogenesis, persistent static compression can upregulate the expression of ClC-3 and regulate osteodifferentiation in osteoblasts. However, there was no study about the relationship between the expression o...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章


    authors: Wang D,Wang H,Gao F,Wang K,Dong F

    更新日期:2017-06-01 00:00:00

  • Histamine synergistically promotes bFGF-induced angiogenesis by enhancing VEGF production via H1 receptor.

    abstract::Histamine, a major mediator present in mast cells that is released into the extracellular milieu upon degranulation, is well known to possess a wide range of biological activities in several classic physiological and pathological processes. However, whether and how it participates in angiogenesis remains obscure. In t...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章


    authors: Lu Q,Wang C,Pan R,Gao X,Wei Z,Xia Y,Dai Y

    更新日期:2013-05-01 00:00:00

  • Deep integrative analysis of microRNA-mRNA regulatory networks for biomarker and target discovery in chondrosarcoma.

    abstract::Chondrosarcoma (CHS) is a common malignant bone sarcoma and its occurrence increases with age. microRNAs (miRNAs) are a class of noncoding RNAs that participate in various biological processes and disease pathogenesis by targeting functional messenger RNA (mRNA). However, the modulation of miRNAs in CHS remains largel...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章


    authors: Sui J,Liu Q,Zhang H,Kong Y

    更新日期:2019-06-01 00:00:00

  • Basic fibroblast growth factor decreases type V/XI collagen expression in cultured bovine aortic smooth muscle cells.

    abstract::Vascular smooth muscle cells (SMCs), the major cellular constituent of an artery, synthesize the bulk of fibrillar collagens, including type V/XI, which regulates heterotypic collagen fibril assembly. Basic fibroblast growth factor (bFGF) is a heparin-binding polypeptide growth factor that has been implicated in impor...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章


    authors: Kypreos KE,Sonenshein GE

    更新日期:1998-02-01 00:00:00

  • A new role for 5-methoxytryptophol on bone cells function in vitro.

    abstract::The present study investigates the direct action of 5-methoxytryptophol (5-MTX) in both MC3T3-E1 and RAW264.7 cells and compares it with melatonin (MEL), another 5-methoxyindol known to play a significant role on bone metabolism. We first screened increasing doses of both 5-MTX and MEL to determine their effect on met...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章


    authors: Satué M,Ramis JM,del Mar Arriero M,Monjo M

    更新日期:2015-04-01 00:00:00

  • Endogenous peptides profiles of human infantile hemangioma tissue and their clinical significance for treatment.

    abstract::Endogenous peptides play crucial roles in various biological processes. Their effects on the pathogenesis of human infantile hemangioma remains poorly understood. In this study, we construct a comparative peptidomic profiling between human infantile hemangioma tissue and matched normal skin using liquid chromatography...

    journal_title:Journal of cellular biochemistry

    pub_type: 临床试验,杂志文章


    authors: Li Q,Li J,Chen L,Gao Y,Li J

    更新日期:2018-06-01 00:00:00

  • Silencing survivin gene expression promotes apoptosis of human breast cancer cells through a caspase-independent pathway.

    abstract::Survivin is recognized as an attractive target in cancer therapy because of its selective overexpression in the majority of tumors. Upregulated expression of this protein correlates with increased tumor grade, recurrence risk and decreased cancer patients survival. In this study, we assessed the efficacy of two surviv...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章


    authors: Croci DO,Cogno IS,Vittar NB,Salvatierra E,Trajtenberg F,Podhajcer OL,Osinaga E,Rabinovich GA,Rivarola VA

    更新日期:2008-10-01 00:00:00

  • A prognostic 11 long noncoding RNA expression signature for breast invasive carcinoma.

    abstract::Breast cancer, the most common cancer in women worldwide, is associated with high mortality. The long non-coding RNAs (lncRNAs) with a little capacity of coding proteins is playing an increasingly important role in the cancer paradigm. Accumulating evidences demonstrate that lncRNAs have crucial connections with breas...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章


    authors: He Y,Li X,Meng Y,Fu S,Cui Y,Shi Y,Du H

    更新日期:2019-10-01 00:00:00

  • P-Glycoprotein Inhibition Sensitizes Human Breast Cancer Cells to Proteasome Inhibitors.

    abstract::Although effective for the treatment of hematological malignancies, the FDA approved proteasome inhibitors bortezomib and carfilzomib have limited efficacy in solid tumors including triple negative breast cancer (TNBC). Chemotherapy is the only option for treating TNBC due to the absence of specific therapeutic target...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章


    authors: Deshmukh RR,Kim S,Elghoul Y,Dou QP

    更新日期:2017-05-01 00:00:00

  • Interaction of high-density lipoprotein with Trypanosoma brucei: effect of membrane stabilizers.

    abstract::The specific lysis of bloodstream trypanosomes by serum from a nonpermissive mammalian host is the result of interaction between the serum trypanocidal factor (high-density lipoprotein) and the trypanosome surface. The studies described in this paper attempt to define further the mode of action of this cytotoxic lipop...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章


    authors: Rifkin MR

    更新日期:1983-01-01 00:00:00

  • MicroRNA-330 inhibits growth and migration of melanoma A375 cells: In vitro study.

    abstract::Melanoma skin cancer is one of the main causes of male cancer-related deaths worldwide. It has been suggested that miR-330-5p can act as a tumor suppressor in various types of cancers. So, in this study, we replaced miR-330 in melanoma cancer cells by vector-based miR-330 to evaluate the effects of this microRNA on th...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章


    authors: Sehati N,Sadeghie N,Mansoori B,Mohammadi A,Shanehbandi D,Baradaran B

    更新日期:2020-01-01 00:00:00

  • HOXB13 promotes proliferation, migration, and invasion of glioblastoma through transcriptional upregulation of lncRNA HOXC-AS3.

    abstract::HOXB13 exerts a close relation in several human cancers. This study explored the role of HOXB13 in glioblastoma (GBM), a brain tissue with the highest aggressive rate and mortality in adults. Through microarray and immunohistochemistry analyses, HOXB13 was highly expressed in GBM tissues. Furthermore, we showed that h...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章


    authors: Wang X,Sun Y,Xu T,Qian K,Huang B,Zhang K,Song Z,Qian T,Shi J,Li L

    更新日期:2019-09-01 00:00:00

  • Differential expression patterns of specific long noncoding RNAs and competing endogenous RNA network in alopecia areata.

    abstract:BACKGROUND:Long noncoding RNAs (lncRNAs) regulate gene expression by acting with microRNAs (miRNAs) and indirectly interact with messenger RNA (mRNAs). However, the roles of specific lncRNA and its related competing endogenous RNAs (ceRNA) network in alopecia areata (AA) are not fully understood. METHODS:The blood lnc...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章


    authors: Sheng Y,Ma J,Zhao J,Qi S,Hu R,Yang Q

    更新日期:2019-06-01 00:00:00

  • 4S polycyclic aromatic hydrocarbon receptor (glycine N-methyltransferase) and the aryl hydrocarbon receptor nuclear translocator (hypoxia inducible factor-1β) interaction in Chinese hamster ovary and rat hepatoma cells: 4S PAH-R/ARNT hetero-oligomers?

    abstract::Rat CYP1A1 promoter-luciferase, transiently transfected wild-type and 4S PAH receptor (glycine N-methyl transferase, GNMT)-transformed Chinese hamster ovary (CHO) cells were exposed to benzo[a]pyrene and assayed for luciferase activity as an indicator of CYP1A1 promoter activity. CHO cells transformed with the rat 4S ...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章


    authors: Sterling KM

    更新日期:2011-08-01 00:00:00

  • Methylglyoxal and high glucose co-treatment induces apoptosis or necrosis in human umbilical vein endothelial cells.

    abstract::Hyperglycemia and elevation of methylglyoxal (MG) are symptoms of diabetes mellitus (DM). We previously showed that high glucose (HG; 30 mM) or MG (50-400 microM) could induce apoptosis in mammalian cells, but these doses are higher than the physiological concentrations of glucose and MG in the plasma of DM patients. ...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章


    authors: Chan WH,Wu HJ

    更新日期:2008-03-01 00:00:00

  • TNFalpha mediates sepsis-induced impairment of basal and leucine-stimulated signaling via S6K1 and eIF4E in cardiac muscle.

    abstract::Decreased translation initiation adversely impacts protein synthesis and contributes to the myocardial dysfunction produced by sepsis. Therefore, the purpose of the present study was to identify sepsis-induced changes in signal transduction pathways known to regulate translation initiation in cardiac muscle and to det...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章


    authors: Lang CH,Pruznak AM,Frost RA

    更新日期:2005-02-01 00:00:00

  • TGF-beta2 stimulates cranial suture closure through activation of the Erk-MAPK pathway.

    abstract::Cranial sutures are important growth sites of the skull. During suture closure, the dura mater is one of the most important sources of various positive and negative regulatory signals. Previous results indicate that TGF-beta2 from dura mater strongly accelerates suture closure, however, its exact regulatory mechanism ...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章


    authors: Lee SW,Choi KY,Cho JY,Jung SH,Song KB,Park EK,Choi JY,Shin HI,Kim SY,Woo KM,Baek JH,Nam SH,Kim YJ,Kim HJ,Ryoo HM

    更新日期:2006-07-01 00:00:00

  • MicroRNA Profile in Response to Doxorubicin Treatment in Breast Cancer.

    abstract:UNLABELLED:Chemotherapy treatment is the standard in triple negative breast cancers, a cancer subgroup which lacks a specific target. The mechanisms leading to the response, as well as any markers that allow the differentiation between responder and non-responder groups prior to treatment are unknown. In parallel, miRN...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章


    authors: Tormo E,Pineda B,Serna E,Guijarro A,Ribas G,Fores J,Chirivella E,Climent J,Lluch A,Eroles P

    更新日期:2015-09-01 00:00:00

  • Regulation of osteoclastogenesis by gap junction communication.

    abstract::Receptor activator of NF-kappaB ligand (RANKL) is crucial in osteoclastogenesis but signaling events involved in osteoclast differentiation are far from complete and other signals may play a role in osteoclastogenesis. A more direct pathway for cellular crosstalk is provided by gap junction intercellular channel, whic...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章


    authors: Matemba SF,Lie A,Ransjö M

    更新日期:2006-10-01 00:00:00

  • Berberine demonstrates anti-inflammatory properties in Helicobacter pylori-infected mice with chronic gastritis by attenuating the Th17 response triggered by the B cell-activating factor.

    abstract::Berberine (BBR) is an isoquinoline alkaloid derived from various medicinal herbs. Previous studies have suggested that BBR exerts antimicrobial, antitumor, and antidiabetic effects and can be used to treat Helicobacter pylori-induced chronic gastritis. However, the exact mechanism by which BBR inhibits H. pylori infec...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章


    authors: Wu X,Li X,Dang Z,Jia Y

    更新日期:2018-07-01 00:00:00

  • Comparative efficacy and safety of antiplatelet agents in cerebral ischemic disease: A network meta-analysis.

    abstract::We performed a network meta-analysis (NMA) to enhance the corresponding evidence of the relative efficacy and safety of different antiplatelet agents in cerebral ischemic disease. PubMed and EMBASE were searched systematically for relevant studies. Outcomes were compared using odds ratios and 95% credible intervals. E...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章,meta分析


    authors: Wa D,Zhu P,Long Z

    更新日期:2019-06-01 00:00:00

  • TGF-beta control of cell proliferation.

    abstract::This article focuses on recent findings that the type V TGF-beta receptor (TbetaR-V), which co-expresses with other TGF-beta receptors (TbetaR-I, TbetaR-II, and TbetaR-III) in all normal cell types studied, is involved in growth inhibition by IGFBP-3 and TGF-beta and that TGF-beta activity is regulated by two distinct...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章,评审


    authors: Huang SS,Huang JS

    更新日期:2005-10-15 00:00:00

  • Changes in glycoprotein fucosylation in a concanavalin A-resistant variant of a human leukemia cell line (K562).

    abstract::Previous studies from this and other laboratories have shown that variants of tumor cell lines can be selected for resistance to the lytic action of natural killer (NK) cells. One of these (K562-Clone I), when made resistant to the toxic effects of Concanavalin A (Con A-R1), regained its sensitivity to NK. Comparing t...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章


    authors: Bernier LG,Sullivan AK

    更新日期:1988-06-01 00:00:00

  • Role of angiotensin-converting enzyme insertion/deletion polymorphism in sudden cardiac arrest.

    abstract:OBJECTIVE:This study aimed to investigate the relationship between angiotensin-converting enzyme (ACE) insertion/deletion (I/D) polymorphism and to understand sudden cardiac arrest (SCA) in the Chinese population. METHODS:In this study, 232 patients were divided into the SCA group and the coronary disease group with c...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章


    authors: Liu A,Wang S,Zhang C,Sun D,Song X

    更新日期:2019-03-01 00:00:00

  • Paeoniflorin inhibits mast cell-mediated allergic inflammation in allergic rhinitis.

    abstract::Paeoniflorin (PF), one of the main effective ingredients from the root of Paeonia lactiflora Pall., was reported to possess antitumor, anti-inflammatory, and antiallergic properties. However, the roles of PF in activated human mast cell line, HMC-1 cells, have not yet been elucidated. Thus, the aim of this study was t...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章


    authors: Wang G,Cheng N

    更新日期:2018-11-01 00:00:00

  • Evidence for ligand-independent homo-oligomerization of leptin receptor (OB-R) isoforms: a proposed mechanism permitting productive long-form signaling in the presence of excess short-form expression.

    abstract::The adipocyte secreted hormone leptin (OB) and its receptor (OB-R) are key regulators of mammalian body weight homeostasis. Two predominant isoforms of OB-R have been described: long form (OB-R(L)) characterized as a signal transducing receptor that is highly expressed in specific nuclei of the hypothalamus; and a sho...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章


    authors: White DW,Tartaglia LA

    更新日期:1999-05-01 00:00:00

  • Comprehensive analysis of novel three-long noncoding RNA signatures as a diagnostic and prognostic biomarkers of human triple-negative breast cancer.

    abstract::Currently, traditional predictors of prognosis (tumor size, nodal status, progesterone receptor [PR], estrogen receptor [ER], or human epidermal growth factor receptor-2 [HER2]) are insufficient for precise survival prediction for triple-negative breast cancer (TNBC). Long noncoding RNAs (lncRNAs) have been observed t...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章


    authors: Fan CN,Ma L,Liu N

    更新日期:2019-03-01 00:00:00

  • Upregulation of lincRNA-p21 in thoracic aortic aneurysms is involved in the regulation of proliferation and apoptosis of vascular smooth muscle cells by activating TGF-β1 signaling pathway.

    abstract:OBJECTIVE:Long intergenic noncoding RNA-p21 (lincRNA-p21) has been proved in the pathogenesis of aortic aneurysms, while its functionality in thoracic aortic aneurysms (TAA) and the mechanism of function remains unclear. Therefore our study aimed to investigate the role of lincRNA-p21 in TAA. METHODS:Aortic media spec...

    journal_title:Journal of cellular biochemistry

    pub_type: 杂志文章


    authors: Hu W,Wang Z,Li Q,Wang J,Li L,Jiang G

    更新日期:2019-03-01 00:00:00