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https://www.readbyqxmd.com/read/28536143/aurora-kinase-a-promotes-ar-degradation-via-the-e3-ligase-chip
#1
James M Larner, Sukumar Sarkar, David L Brautigan
Reducing the levels of the androgen receptor (AR) is one of the most viable approaches to combat castration-resistant prostate cancer (CRPC). Previously, we observed that proteasomal-dependent degradation of AR in response to 2-methoxyestradiol (2-ME) depends primarily on the E3 ligase C-terminus of HSP70-interacting protein (STUB1/CHIP). Here, 2-ME stimulation activates CHIP by phosphorylation via Aurora kinase A (AURKA). Aurora A kinase inhibitors and RNAi knockdown of Aurora A transcript selectively blocked CHIP phosphorylation and AR degradation...
May 23, 2017: Molecular Cancer Research: MCR
https://www.readbyqxmd.com/read/28529042/optimization-and-biological-evaluation-of-2-aminobenzothiazole-derivatives-as-aurora-b-kinase-inhibitors
#2
Eun Lee, Ying An, Junhee Kwon, Keun Il Kim, Raok Jeon
A strong relationship between abnormal functions of Aurora kinases and tumorigenesis has been reported for decades. Consequently, Aurora kinases serve as potential targets for anticancer agents. Here, we identified aminobenzothiazole derivatives as novel inhibitors of Aurora B kinase through bioisosteric replacement of the previous inhibitors, aminobenzoxazole derivatives. Most of the urea-linked aminobenzothiazole derivatives showed potent and selective inhibitory activity against Aurora B kinase over Aurora A kinase...
April 6, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28522591/inhibition-of-aurora-a-and-aurora-b-is-required-for-the-sensitivity-of-hpv-driven-cervical-cancers-to-aurora-kinase-inhibitors
#3
David Martin, Sora Fallaha, Martina Proctor, Alexander Stevenson, Lewis Perrin, Nigel McMillan, Brian Gabrielli
The activity and efficacy of Aurora inhibitors have been reported in a wide range of cancer types.   The most prominent Aurora inhibitor is Alisertib, an investigational Aurora inhibitor that has been the subject of more than 30 clinical trials.   Alisertib has inhibitory activity against both Aurora A and B, although it is considered to be primarily an Aurora A inhibitor in vivo.  Here we show that Alisertib inhibits both Aurora A and B in vivo in preclinical models of HPV-driven cervical cancer, and that it is the inhibition of Aurora A and B that provide the selectivity and efficacy of this drug in vivo in this disease setting...
May 18, 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28470610/production-of-protein-kinases-in-e-coli
#4
Charlotte A Dodson
Recombinant protein expression is widely used to generate milligram quantities of protein kinases for crystallographic, enzymatic, or other biophysical assays in vitro. Expression in E. coli is fast, cheap, and reliable. Here I present a detailed protocol for the production of human Aurora-A kinase. I begin with transformation of a suitable plasmid into an expression strain of E. coli, followed by growth and harvesting of bacterial cell cultures. Finally, I describe the purification of Aurora-A to homogeneity using immobilized metal affinity and size exclusion chromatographies...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28465536/metformin-disrupts-malignant-behavior-of-oral-squamous-cell-carcinoma-via-a-novel-signaling-involving-late-sv40-factor-aurora-a
#5
Chang-Han Chen, Hsin-Ting Tsai, Hui-Ching Chuang, Li-Yen Shiu, Li-Jen Su, Tai-Jan Chiu, Sheng-Dean Luo, Fu-Min Fang, Chao-Cheng Huang, Chih-Yen Chien
Conventional therapeutic processes in patient with OSCC are associated with several unfavorable effects leading to patients with poor survival rate. Metformin has been shown to protect against a variety of specific diseases, including cancer. However, the precise roles and mechanisms underlying the therapeutic effects of metformin on OSCC remain elusive. In the current study, in vitro and xenograft model experiments revealed that metformin inhibited growth and metastasis of oral cancer cells. Importantly, metformin-restrained tumorigenesis of oral cancer was accompanied with strong decrease of both Aurora-A and Late SV40 Factor (LSF) expressions...
May 2, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28446271/-expression-of-aurora-family-genes-in-acute-leukemia-and-its-clinical-significance
#6
Zi-Lei Liu, Ying Xing, Tao Li, Chong Wang, Su-Fang Liu, Hua-Yan Zhao, Rong-Hui Zhang, Ya-Jing Ma, Xin-Ye Zhang, Wen-Liang Tian, Liu Liu, Hui Sun, Ling Sun
OBJECTIVE: To explore the mRNA expression of Aurora-A,B,C(AUR-A,B,C) in acute leukemia(AL) and their correlations with the clinical indications. METHODS: The mRNA expression levels of AUR-A,B,C in 73 cases of newly diagnosed AL (untreated group), 20 cases of AL with remission (remission group) and 14 healthy volunteers as control (healthy group) were detected by QRT-PCR, and the difference of expression levels in difference groups, their correlations with clinical indicators and the correlation between the AUR-A,B,C mRNA expression levels themselves were analyzed...
April 2017: Zhongguo Shi Yan Xue Ye Xue za Zhi
https://www.readbyqxmd.com/read/28444399/development-of-a-multipurpose-scaffold-for-the-display-of-peptide-loops
#7
Maxim Rossmann, Sandra J Greive, Tommaso Moschetti, Michael Dinan, Marko Hyvönen
Protein-protein interactions (PPIs) determine a wide range of biological processes and analysis of these dynamic networks is increasingly becoming a mandatory tool for studying protein function. Using the globular ATPase domain of recombinase RadA as a scaffold, we have developed a peptide display system (RAD display), which allows for the presentation of target peptides, protein domains or full-length proteins and their rapid recombinant production in bacteria. The design of the RAD display system includes differently tagged versions of the scaffold, which allows for flexibility in the protein purification method, and chemical coupling for small molecule labeling or surface immobilization...
April 24, 2017: Protein Engineering, Design & Selection: PEDS
https://www.readbyqxmd.com/read/28431392/characterization-of-aurora-a-and-its-impact-on-the-effect-of-cisplatin-based-chemotherapy-in-patients-with-non-small-cell-lung-cancer
#8
Peng Kuang, Zuhua Chen, JiaYuan Wang, Zhentao Liu, Jingyuan Wang, Jing Gao, Lin Shen
BACKGROUND AND OBJECTIVE: Aurora A, as a member of serine/threonine kinase family and a common characteristic of epithelial cancers, plays a critical role in cell mitosis. However, the clinical significance of Aurora A in non-small cell lung cancer (NSCLC) remains undetermined. METHODS: The expression of Aurora A in NSCLC and paired normal adjacent lung tissues was determined by immunohistochemistry, Western blot, and reverse transcriptase polymerase chain reaction...
June 2017: Translational Oncology
https://www.readbyqxmd.com/read/28427193/targeting-high-aurora-kinases-expression-as-an-innovative-therapy-for-hepatocellular-carcinoma
#9
Fuchen Liu, Guangyong Wang, Xiaoqiang Wang, Zhihui Che, Wei Dong, Xinggang Guo, Zhenguang Wang, Ping Chen, Daisen Hou, Qi Zhang, Wenli Zhang, Yida Pan, Dongqin Yang, Hui Liu
The Aurora kinases A and B control tumorigenesis by inhibiting apoptosis and promoting proliferation and metastasis, however, it remains unknown whether Aurora A and B overexpressed concomitantly and its clinical significance in hepatocellular carcinoma (HCC). Here, we obsearved Aurora A and B tended to overexpress parallelly on protein level (r = 0.8679, P < 0.0001) and their co-overexpression (Aurora AHBH), associated with the worst prognosis, was an independent predictor for the survival. Importantly, with the lower IC50 and stronger anti-tumor effect than selective inhibitors, SNS-314, the pan-inhibitor of Aurora kinases, which induced YAP (Yes-associated protein) reduction and resulted in P21 accumulation, significantly promoted the polyploidy (> 4N) formation and apoptosis in HCC...
April 25, 2017: Oncotarget
https://www.readbyqxmd.com/read/28420331/arsenic-treatment-increase-aurora-a-overexpression-through-e2f1-activation-in-bladder-cells
#10
Yu-Ting Kao, Chin-Han Wu, Shan-Ying Wu, Sheng-Hui Lan, Hsiao-Sheng Liu, Ya-Shih Tseng
BACKGROUND: Arsenic is a widely distributed metalloid compound that has biphasic effects on cultured cells. In large doses, arsenic can be toxic enough to trigger cell death. In smaller amounts, non-toxic doses may promote cell proliferation and induces carcinogenesis. Aberration of chromosome is frequently detected in epithelial cells and lymphocytes of individuals from arsenic contaminated areas. Overexpression of Aurora-A, a mitotic kinase, results in chromosomal instability and cell transformation...
April 18, 2017: BMC Cancer
https://www.readbyqxmd.com/read/28410270/the-aurora-kinase-inhibitor-amg-900-increases-apoptosis-and-induces-chemosensitivity-to-anticancer-drugs-in-the-nci-h295-adrenocortical-carcinoma-cell-line
#11
Kleiton S Borges, Augusto F Andrade, Vanessa S Silveira, David S Marco Antonio, Elton J R Vasconcelos, Sonir R R Antonini, Luiz G Tone, Carlos A Scrideli
Adrenocortical tumor (ACT) is a malignancy with a low incidence rate and the current therapy for advanced disease has a limited impact on overall patient survival. A previous study from our group suggested that elevated expression of aurora-A and aurora-B is associated with poor outcome in childhood ACT. Similar results were also reported for adult ACTs. The present in-vitro study shows that AMG 900 inhibits aurora kinases in adrenocortical carcinoma cells. AMG 900 inhibited cell proliferation in NCI-H295 cells as well as in the ACT primary cultures and caused apoptosis in the cell line NCI-H295...
July 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28404933/aurora-a-affects-radiosenstivity-in-cervical-squamous-cell-carcinoma-and-predicts-poor-prognosis
#12
Yuhua Ma, Jie Yang, Ruozheng Wang, Zegao Zhang, Xiaoli Qi, Chunhua Liu, Miaomiao Ma
BACKGROUND: Definitive radiation therapy (RT) (with or without cisplatin-based chemotherapy) is one of the most effective treatments for cervical squamous cell carcinoma (CSCC), but efficacy is limited due to resistance. In the present study, we investigated the relationship between the expression of Aurora kinase A (Aurora-A, AURKA)and response to RT in patients with CSCC. METHODS: The expression of Aurora-A in biopsy specimens of untreated primary tumors in 129 Uyghur patients with CSCC was investigated immunohistochemically...
May 9, 2017: Oncotarget
https://www.readbyqxmd.com/read/28402276/cell-cycle-protein-bora-serves-as-a-novel-poor-prognostic-factor-in-multiple-adenocarcinomas
#13
Qiong-Xia Zhang, Rui Gao, Jin Xiang, Zhong-Yu Yuan, Yuan-Min Qian, Min Yan, Zi-Feng Wang, Quentin Liu, Hai-Dong Zhao, Chang-Hong Liu
Cell cycle protein Bora has been identified to integrate the functions of three major mitotic kinases: Cyclin-dependent kinase-1, Polo-like kinase-1, and Aurora A kinase. Overexpression of Bora disrupts spindle assembly and causes genomic instability. However, the clinical relevance of Bora in cancer remains unclear. In this study, we examined the expression of Bora and its association with clinical characteristics in breast (n = 538), lung (n = 144) and gastric (n = 77) adenocarcinomas. We found that Bora was overexpressed in primary breast cancer tissues compared to paired non-cancerous tissues...
March 28, 2017: Oncotarget
https://www.readbyqxmd.com/read/28389630/identification-of-small-molecule-inhibitors-of-the-aurora-a-tpx2-complex
#14
Italia Anna Asteriti, Frederick Daidone, Gianni Colotti, Serena Rinaldo, Patrizia Lavia, Giulia Guarguaglini, Alessandro Paiardini
Aurora kinases are a family of cell division regulators that govern the correct assembly of a bipolar mitotic spindle and the fidelity of chromosome segregation. Their overexpression is associated with genomic instability and aneuploidy, and is frequently observed in cancer. Accordingly, competitive inhibitors targeting Aurora kinase activity at the ATP-binding site are being investigated for therapeutic purposes. Despite promising pre-clinical data, these molecules display moderate effects in clinical trials and incomplete selectivity, either against distinct family members, or other kinases...
May 9, 2017: Oncotarget
https://www.readbyqxmd.com/read/28358124/domain-specific-interactions-between-mln8237-and-human-serum-albumin-estimated-by-std-and-waterlogsy-nmr-itc-spectroscopic-and-docking-techniques
#15
Hongqin Yang, Jiuyang Liu, Yanmei Huang, Rui Gao, Bin Tang, Shanshan Li, Jiawei He, Hui Li
Alisertib (MLN8237) is an orally administered inhibitor of Aurora A kinase. This small-molecule inhibitor is under clinical or pre-clinical phase for the treatment of advanced malignancies. The present study provides a detailed characterization of the interaction of MLN8237 with a drug transport protein called human serum albumin (HSA). STD and WaterLOGSY nuclear magnetic resonance (NMR)-binding studies were conducted first to confirm the binding of MLN8237 to HSA. In the ligand orientation assay, the binding sites of MLN8237 were validated through two site-specific spy molecules (warfarin sodium and ibuprofen, which are two known site-selective probes) by using STD and WaterLOGSY NMR competition techniques...
March 30, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28342286/switching-aurora-a-kinase-on-and-off-at-an-allosteric-site
#16
REVIEW
Richard Bayliss, Selena G Burgess, Patrick J McIntyre
Protein kinases are central players in the regulation of cell cycle and signalling pathways. Their catalytic activities are strictly regulated through post-translational modifications and protein-protein interactions that control switching between inactive and active states. These states have been studied extensively using protein crystallography, although the dynamic nature of protein kinases makes it difficult to capture all relevant states. Here, we describe two recent structures of Aurora-A kinase that trap its active and inactive states...
March 25, 2017: FEBS Journal
https://www.readbyqxmd.com/read/28337805/defining-the-anti-cancer-activity-of-tricarbonyl-rhenium-complexes-induction-of-g2-m-cell-cycle-arrest-and-blockade-of-aurora-a-kinase-phosphorylation
#17
Peter V Simpson, Ilaria Casari, Silvano Paternoster, Brian W Skelton, Marco Falasca, Massimiliano Massi
Rhenium and ruthenium complexes containing N-heterocylic carbene (NHC) ligands and conjugated to indomethacin were prepared. The anticancer properties were probed against pancreatic cell lines, revealing a remarkable activity of the rhenium fragment as anticancer agent. The ruthenium complexes were found to be inactive against the same pancreatic cancer cell lines, either alone or in conjugation with indomethacin. An in-depth biological study revealed the origin of the anticancer properties of the rhenium tricarbonyl fragment, of which a complete elucidation had yet to be achieved...
May 11, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28298485/mcak-mediated-regulation-of-endothelial-cell-microtubule-dynamics-is-mechanosensitive-to-myosin-ii-contractility
#18
Lauren D'Angelo, Nicole M Myer, Kenneth A Myers
Compliance and dimensionality mechanosensing, the processes by which cells sense the physical attributes of the extracellular matrix (ECM), are known to drive cell branching and shape change largely through a myosin-II-mediated reorganization of the actin and microtubule (MT) cytoskeletons. Subcellular regulation of MT dynamics is spatially controlled through a Rac1-Aurora-A kinase pathway that locally inhibits the MT depolymerizing activity of mitotic centromere-associated kinesin (MCAK), thereby promoting leading-edge MT growth and cell polarization...
May 1, 2017: Molecular Biology of the Cell
https://www.readbyqxmd.com/read/28284839/depletion-of-tumor-suppressor-kank1-induces-centrosomal-amplification-via-hyperactivation-of-rhoa
#19
Jun-Ichiro Suzuki, Badal Chandra Roy, Takunori Ogaeri, Naoto Kakinuma, Ryoiti Kiyama
Chromosome instability, frequently found in cancer cells, is caused by a deficiency in cell division, including centrosomal amplification and cytokinesis failure, and can result in abnormal chromosome content or aneuploidy. The small GTPase pathways have been implicated as important processes in cell division. We found that knockdown of a tumor suppressor protein Kank1 increases the number of cells with a micronucleus or bi-/multi-nuclei, which was likely caused by centrosomal amplification. Kank1 interacts with Daam1, known to bind to and activate a small GTPase, RhoA, in actin assembly...
April 15, 2017: Experimental Cell Research
https://www.readbyqxmd.com/read/28269755/microrna-124-3p-affects-proliferation-migration-and-apoptosis-of-bladder-cancer-cells-through-targeting-aurka
#20
Qiuyue Yuan, Tingge Sun, Feng Ye, Weisheng Kong, Haofan Jin
OBJECTIVE: The aim of this study was to establish the relationship between miR-124-3p and Aurora A kinase (AURKA) in bladder cancer (BC). METHODS: The expressions of miR-124-3p and AURKA in BC tissues and cell lines were detected using RT-PCR and western blot. BC cells were transfected with miR-124-3p mimics and AURKA siRNA. After this cell proliferation, migration, cell cycle and apoptosis were measured using CCK-8, colony formation assay, wound healing assay and cytometry tests...
2017: Cancer Biomarkers: Section A of Disease Markers
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