Abstract：
:Microtubule affinity regulating kinase 4 (MARK4) becomes a unique anti-cancer drug target as its overexpression is responsible for different types of cancers. In quest of novel, effective MARK4 inhibitors, some acridone derivatives were synthesized, characterized and evaluated for inhibitory activity against human MARK4. Among all the synthesized compounds, three (7b, 7d and 7f) were found to have better binding affinity and enzyme inhibition activity in µM range as shown by fluorescence binding, ITC and kinase assays. Here we used functional assays of selected potential lead molecules with commercially available panel of 26 kinases of same family. A distinctive kinase selectivity profile was observed for each compound. The selective compounds were identified with submicromolar cellular activity against MARK4. Furthermore, in vitro antitumor evaluation against cancerous cells (MCF-7 and HepG2) revealed that compounds 7b, 7d and 7f inhibit cell proliferation and predominantly induce apoptosis in MCF-7 cells, with IC50 values of 5.2 ± 1.2 μM, 6.3 ± 1.2 μM, and 5.8 ± 1.4 μM respectively. In addition, these compounds significantly upsurge the oxidative stress in cancerous cells. Our observations support our approach for the synthesis of effective inhibitors against MARK4 that can be taken forward for the development of novel anticancer molecules targeting MARK4.
journal_name
Sci Repjournal_title
Scientific reportsauthors
Voura M,Khan P,Thysiadis S,Katsamakas S,Queen A,Hasan GM,Ali S,Sarli V,Hassan MIdoi
10.1038/s41598-018-38217-8subject
Has Abstractpub_date
2019-02-08 00:00:00pages
1676issue
1issn
2045-2322pii
10.1038/s41598-018-38217-8journal_volume
9pub_type
杂志文章abstract：:Skilled individuals are characterized by fine-tuned perceptual and motor functions. Here, we tested the idea that the sensory and motor functions of highly-trained individuals are coupled. We assessed the relationships among multifaceted somatosensory and motor functions of expert pianists. The results demonstrated a ...
journal_title：Scientific reports
pub_type： 杂志文章
doi：10.1038/srep37632
更新日期：2016-11-25 00:00:00
abstract：:The oceanic connection between the coastal variability along the southwestern African coasts and the linear equatorial dynamics at subseasonal time-scales (<120 days) is examined using a variety of model outputs, ranging from linear to general circulation models. We focus on the equatorially-forced fast and weakly dis...
journal_title：Scientific reports
pub_type： 杂志文章
doi：10.1038/s41598-019-41847-1
更新日期：2019-03-28 00:00:00
abstract：:A correction to this article has been published and is linked from the HTML and PDF versions of this paper. The error has not been fixed in the paper. ...
journal_title：Scientific reports
pub_type： 已发布勘误
doi：10.1038/s41598-018-37593-5
更新日期：2018-12-21 00:00:00
abstract：:Automated patch clamp (APC) instruments enable efficient evaluation of electrophysiologic effects of drugs on human cardiac currents in heterologous expression systems. Differences in experimental protocols, instruments, and dissimilar site procedures affect the variability of IC50 values characterizing drug block pot...
journal_title：Scientific reports
pub_type： 杂志文章
doi：10.1038/s41598-020-62344-w
更新日期：2020-03-27 00:00:00
abstract：:The initiation of polymorphic ventricular tachycardia in long QT syndrome type 2 (LQT2) has been associated with a characteristic ECG pattern of short-long RR intervals. We hypothesize that this characteristic pattern increases APD dispersion in LQT2, thereby promoting arrhythmia. We investigated APD dispersion and it...
journal_title：Scientific reports
pub_type： 杂志文章
doi：10.1038/s41598-019-51230-9
更新日期：2019-10-16 00:00:00
abstract：:A bioresorbable metallic helical stent was explored as a new device opportunity (magnesium scaffold), which can be absorbed by the body without leaving a trace and simultaneously allowing restoration of vasoreactivity with the potential for vessel remodeling. In this study, developed Mg-based helical stent was inserte...
journal_title：Scientific reports
pub_type： 杂志文章
doi：10.1038/s41598-017-01214-4
更新日期：2017-04-26 00:00:00
abstract：:Dengue virus infection is a global threat for which no specific treatment has not been established. Previous reports suggested chrysin and flavanone derivatives were potential flaviviral inhibitors. Here, we reported two halogenated chrysins, abbreviated FV13 and FV14, were highly potent against DENV1-4 and ZIKV infec...
journal_title：Scientific reports
pub_type： 杂志文章
doi：10.1038/s41598-017-14121-5
更新日期：2017-10-20 00:00:00
abstract：:The intermolt crustacean Y-organ (YO) maintains a basal state mediated by pulsatile release of molt inhibiting hormone (MIH), a neuropeptide produced in the eyestalk ganglia, inhibiting YO ecdysteroidogenesis. Reduction of MIH results in YO activation and the animal enters premolt. In the crab, Gecarcinus lateralis, m...
journal_title：Scientific reports
pub_type： 杂志文章
doi：10.1038/s41598-018-25368-x
更新日期：2018-05-09 00:00:00
abstract：:A three dimensional (3D) numerical solution of unsteady, Ag-MgO hybrid nanoliquid flow with heat and mass transmission caused by upward/downward moving of wavy spinning disk has been scrutinized. The magnetic field has been also considered. The hybrid nanoliquid has been synthesized in the presence of Ag-MgO nanoparti...
journal_title：Scientific reports
pub_type： 杂志文章
doi：10.1038/s41598-020-75905-w
更新日期：2020-11-02 00:00:00
abstract：:An amendment to this paper has been published and can be accessed via a link at the top of the paper. ...
journal_title：Scientific reports
pub_type： 已发布勘误
doi：10.1038/s41598-020-68128-6
更新日期：2020-07-06 00:00:00
abstract：:A correction to this article has been published and is linked from the HTML and PDF versions of this paper. The error has been fixed in the paper. ...
journal_title：Scientific reports
pub_type： 已发布勘误
doi：10.1038/s41598-018-24799-w
更新日期：2018-04-19 00:00:00
abstract：:Tumour growth and metastatic colonization is strongly influenced by the tumour stroma, including cancer-associated fibroblasts (CAF). Multipotent mesenchymal stromal cells (MSC) are a possible source of CAF following myofibroblastic differentiation, and we have previously shown that MSC support tumour growth. Triggere...
journal_title：Scientific reports
pub_type： 杂志文章
doi：10.1038/s41598-019-48142-z
更新日期：2019-08-13 00:00:00
abstract：:Studies focusing on biofilm assembly in deep-sea environments are rarely conducted. To examine the effects of substrate type on microbial community assembly, biofilms were developed on different substrates for different durations at two locations in the Red Sea: in a brine pool and in nearby bottom water (NBW) adjacen...
journal_title：Scientific reports
pub_type： 杂志文章
doi：10.1038/srep06647
更新日期：2014-10-17 00:00:00
abstract：:A glassy carbon electrode (GC) immobilized with chitosan (CHI)@reduced graphene (rGO)-polyaniline (PAni)/ferritin (Frt)/glucose oxidase (GOx) bioelectrode was prepared. The prepared electrode was characterized by using cyclic voltammetry (CV), linear sweep voltammetry (LSV) and electrochemical impedance spectroscopy (...
journal_title：Scientific reports
pub_type： 杂志文章
doi：10.1038/s41598-020-67253-6
更新日期：2020-06-26 00:00:00
abstract：:The ability to change the secondary electron emission properties of nitrogen-doped graphene (N-graphene) has been demonstrated. To this end, a novel microwave plasma-enabled scalable route for continuous and controllable fabrication of free-standing N-graphene sheets was developed. High-quality N-graphene with prescri...
journal_title：Scientific reports
pub_type： 杂志文章
doi：10.1038/s41598-020-69844-9
更新日期：2020-08-03 00:00:00
abstract：:Idiopathic pulmonary fibrosis (IPF) is a progressive disease characterized by interstitial remodeling and pulmonary dysfunction. The etiology of IPF is not completely understood but involves pathologic inflammation and subsequent failure to resolve fibrosis in response to epithelial injury. Treatments for IPF are limi...
journal_title：Scientific reports
pub_type： 杂志文章
doi：10.1038/s41598-020-68336-0
更新日期：2020-07-15 00:00:00
abstract：:In order to improve the accuracy and reliability of micropipetting, a method of micro-pipette detection and calibration combining the dynamic pressure monitoring in pipetting process and quantitative identification of pipette volume in image processing was proposed. Firstly, the normalized pressure model for the pipet...
journal_title：Scientific reports
pub_type： 杂志文章
doi：10.1038/s41598-018-24145-0
更新日期：2018-04-10 00:00:00
abstract：:Adverse maternal environments, such as diabetes and obesity, impair placental mitochondrial function, which affects fetal development and offspring long-term health. The underlying mechanisms and effective interventions to abrogate such effect remain unclear. Our previous studies demonstrated impaired mitochondrial bi...
journal_title：Scientific reports
pub_type： 杂志文章
doi：10.1038/s41598-020-65415-0
更新日期：2020-05-20 00:00:00
abstract：:The use of agrochemicals in vegetable production could influence the selection for insecticide resistance in malaria vectors. Unfortunately, there is a dearth of information on the potential contribution of agrochemicals to insecticide resistance in Anopheles mosquitoes breeding on vegetable farms in southern Benin. A...
journal_title：Scientific reports
pub_type： 杂志文章
doi：10.1038/s41598-020-63086-5
更新日期：2020-04-14 00:00:00
abstract：:Concurrent generation and mixing phenomenon of thermoacoustic (TA) and magnetoacoustic (MA) waves in water are predicted and observed. A theory unifying TA and MA is further put forward to analyze it. By scaling down the radio frequency in thermoacoustics to the low mega Hertz range and by incorporating appropriately ...
journal_title：Scientific reports
pub_type： 杂志文章
doi：10.1038/srep11489
更新日期：2015-06-26 00:00:00
abstract：:Multifactorial lifestyle intervention is known to be more effective for ameliorating cognitive decline than single factor intervention; however, the effects of combining exercise with long-chain polyunsaturated fatty acids (LCPUFA) on the elderlies' cognitive function remain unclear. We conducted a randomised, single-...
journal_title：Scientific reports
pub_type： 杂志文章,随机对照试验
doi：10.1038/s41598-020-69560-4
更新日期：2020-07-31 00:00:00
abstract：:Age-related hearing loss (ARHI) is the most common sensory disorder in the elderly. Although telomere attrition has been shown as a determinant in the pathobiology of various age-related diseases, it remains unknown whether telomere length is associated with ARHI. We hypothesized that decreased leukocyte telomere leng...
journal_title：Scientific reports
pub_type： 杂志文章
doi：10.1038/s41598-017-10680-9
更新日期：2017-08-31 00:00:00
abstract：:In the field of correlative microscopy, light and electron microscopy form a powerful combination for morphological analyses in zoology. Due to sample thickness limitations, these imaging techniques often require sectioning to investigate small animals and thereby suffer from various artefacts. A recently introduced n...
journal_title：Scientific reports
pub_type： 杂志文章
doi：10.1038/s41598-020-60977-5
更新日期：2020-03-03 00:00:00
abstract：:Fluid overload (FO) has been shown to adversely affect multiple organs and survival in critically ill patients. Liver transplantation (LT) carries the risk of massive transfusion, which frequently results in FO. We investigated the association of postoperative weight gain with graft failure, early allograft dysfunctio...
journal_title：Scientific reports
pub_type： 杂志文章
doi：10.1038/s41598-019-56543-3
更新日期：2019-12-27 00:00:00
abstract：:Increased p66Shc expression has been associated with diabetic nephropathy (DN). However, whether p66Shc can serve as a potential biomarker for tubular oxidative injury in DN is unknown. We measured the expression of p66Shc in peripheral blood monocytes (PBMs) and renal biopsy tissues from DN patients and then analysed...
journal_title：Scientific reports
pub_type： 杂志文章
doi：10.1038/srep29302
更新日期：2016-07-05 00:00:00
abstract：:Cell motility requires the precise coordination of cell polarization, lamellipodia formation, adhesion, and force generation. LKB1 is a multi-functional serine/threonine kinase that associates with actin at the cellular leading edge of motile cells and suppresses FAK. We sought to understand how LKB1 coordinates these...
journal_title：Scientific reports
pub_type： 杂志文章
doi：10.1038/srep40929
更新日期：2017-01-19 00:00:00
abstract：:Patients hospitalised with COVID-19 have a high mortality. Identification of patients at increased risk of adverse outcome would be important, to allow closer observation and earlier medical intervention for those at risk, and to objectively guide prognosis for friends and family of affected individuals. We conducted ...
journal_title：Scientific reports
pub_type： 杂志文章
doi：10.1038/s41598-020-78505-w
更新日期：2020-12-07 00:00:00
abstract：:A potted experiment with Populus × euramericana 'Neva' was carried out to assess whether there are positive effects of magnetic treatment of saline water (MTSW) on nitrogen metabolism under controlled conditions in a greenhouse. Growth properties, nitrogen contents, enzyme activities and metabolite concentrations were...
journal_title：Scientific reports
pub_type： 杂志文章
doi：10.1038/s41598-019-45719-6
更新日期：2019-07-11 00:00:00
abstract：:We evaluated regression of iris neovascularization (INV) using en-face anterior-segment optical coherence tomography angiography (AS-OCTA) after anti-vascular endothelial growth factor (VEGF) therapy. Seven consecutive eyes with INV were examined before and after anti-VEGF therapy, and all AS-OCTA scans were obtained ...
journal_title：Scientific reports
pub_type： 杂志文章
doi：10.1038/s41598-019-46514-z
更新日期：2019-07-16 00:00:00
abstract：:Fatigue is a very common non-motor symptom in Parkinson disease (PD) patients. It included physical fatigue and mental fatigue. The potential mechanisms of mental fatigue involving serotonergic dysfunction and abnormal iron metabolism are still unknown. Therefore, we evaluated the fatigue symptoms, classified PD patie...
journal_title：Scientific reports
pub_type： 杂志文章
doi：10.1038/s41598-016-0018-z
更新日期：2016-12-21 00:00:00
