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https://www.readbyqxmd.com/read/29332582/dual-bace-1-gsk-3%C3%AE-inhibitors-to-combat-alzheimer-s-disease-a-focus-review
#1
Angela Rampa, Silvia Gobbi, Rita Maria Concetta Di Martino, Federica Belluti, Alessandra Bisi
In industrialized countries, Alzheimer's disease represents the most devastating neurodegenerative disorder in elderly people and the search for a disease modifying agent is still justified by this unmet need. Several possible targets have been explored to find an appropriate drug therapy, and in this review dual inhibitors of beta secretase and glycogen synthase kinase 3, recently reported in literature, will be appraised. Applying a ligand-based approach, the triazinone core emerged as a suitable scaffold to simultaneously bind the aspartic dyad of BACE-1 and the ATP site of GSK-3β, leading to a series of small molecules endowed with a balanced micromolar affinity and a promising pharmacokinetic profile...
January 12, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29331585/cathepsin-l-promotes-ionizing-radiation-induced-u251-glioma-cell-migration-and-invasion-through-regulating-the-gsk-3%C3%AE-cux1-pathway
#2
Yao Fei, Yajie Xiong, Xiao Shen, Yifan Zhao, Ying Zhu, Long Wang, Zhongqin Liang
Cathepsin L (CTSL) is a lysosomal cysteine protease overexpressed and secreted by tumor cells. Our previous study found that CTSL was involved in ionizing radiation (IR)-induced epithelial-mesenchymal transition (EMT) and the increase of glioma invasion and migration. However, the mechanisms by which CTSL promoted this IR-induced glioma migration and invasion remained unclear. In this study, we demonstrated that IR reduced glycogen synthase kinase-3β (GSK-3β) activity, via the CTSL-mediated phosphorylation of its serine-9 residue, in U251 cells...
January 10, 2018: Cellular Signalling
https://www.readbyqxmd.com/read/29331582/inositol-polyphosphates-contribute-to-cellular-circadian-rhythms-implications-for-understanding-lithium-s-molecular-mechanism
#3
Heather Wei, Dominic Landgraf, George Wang, Michael J McCarthy
Most living organisms maintain cell autonomous circadian clocks that synchronize critical biological functions with daily environmental cycles. In mammals, the circadian clock is regulated by inputs from signaling pathways including glycogen synthase kinase 3 (GSK3). The drug lithium has actions on GSK3, and also on inositol metabolism. While it is suspected that lithium's inhibition of GSK3 causes rhythm changes, it is not known if inositol polyphosphates can also affect the circadian clock. We examined whether the signaling molecule inositol hexaphosphate (IP6) has effects on circadian rhythms...
January 10, 2018: Cellular Signalling
https://www.readbyqxmd.com/read/29331511/maresin-1-regulates-autophagy-and-inflammation-in-human-periodontal-ligament-cells-through-glycogen-synthase-kinase-3%C3%AE-%C3%AE-catenin-pathway-under-inflammatory-conditions
#4
Li Du, Yucheng Li, Weifeng Liu
OBJECTIVE: Accumulating lines of evidence suggest that maresin 1 (MaR-1) exerts anti-inflammatory effects in many cell types and plays beneficial roles in inflammatory disease, such as peritonitis and colitis. Moreover, it has been demonstrated that MaR-1 play protective roles against localized aggressive periodontitis. However, the function and mechanism of MaR-1 in human periodontal ligament cells (PDL) cells from periodontitis are poorly understood. The present study aimed to clarify the effects and molecular mechanism of MaR-1 in PDL cell survival and inflammation...
December 23, 2017: Archives of Oral Biology
https://www.readbyqxmd.com/read/29329433/rage-mediates-a%C3%AE-accumulation-in-a-mouse-model-of-alzheimer-s-disease-via-modulation-of-%C3%AE-and-%C3%AE-secretase-activity
#5
Fang Fang, Qing Yu, Ottavio Arancio, Doris Chen, Smruti S Gore, Shi Fang Yan, Shirley ShiDu Yan
Receptor for Advanced Glycation End products (RAGE) has been implicated in amyloid β-peptide (Aβ)-induced perturbation relevant to the pathogenesis of Alzheimer's disease (AD). However, whether and how RAGE regulates Aβ metabolism remains largely unknown. Aβ formation arises from aberrant cleavage of amyloid precursor protein (APP) by β- and γ-secretase. To investigate whether RAGE modulates β- and γ-secretase activity potentiating Aβ formation, we generated mAPP mice with genetic deletion of RAGE (mAPP/RO)...
January 10, 2018: Human Molecular Genetics
https://www.readbyqxmd.com/read/29327199/glycogen-synthase-kinase-3%C3%AE-regulates-equilibrium-between-neurogenesis-and-gliogenesis-in-rat-model-of-parkinson-s-disease-a-crosstalk-with-wnt-and-notch-signaling
#6
Sonu Singh, Akanksha Mishra, Sachi Bharti, Virendra Tiwari, Jitendra Singh, Parul, Shubha Shukla
Neurogenesis involves generation of functional newborn neurons from neural stem cells (NSCs). Insufficient formation or accelerated degeneration of newborn neurons may contribute to the severity of motor/nonmotor symptoms of Parkinson's disease (PD). However, the functional role of adult neurogenesis in PD is yet not explored and whether glycogen synthase kinase-3β (GSK-3β) affects multiple steps of adult neurogenesis in PD is still unknown. We investigated the possible underlying molecular mechanism of impaired adult neurogenesis associated with PD...
January 11, 2018: Molecular Neurobiology
https://www.readbyqxmd.com/read/29323740/long-non-coding-rna-asbel-promotes-osteosarcoma-cell-proliferation-migration-and-invasion-by-regulating-microrna-21
#7
Jianhui Zhao, Zhongli Gao, Chao Zhang, Han Wu, Rui Gu, Rui Jiang
Osteosarcoma is the most common malignant bone tumor in children and adolescents with high rate of incidence, high frequency of recurrence and high degree of metastasis. This study aimed to investigate the effects of long noncoding RNA antisense ncRNA in the Abundant in neuroepithelium area (ANA)/B-cell translocation gene 3 (BTG3) locus (lncRNA ASBEL) on the pathogenesis of osteosarcoma. The expression levels of ASBEL in human osteoblast cells and human osteosarcoma cells were evaluated using qRT-PCR. Effects of ASBEL knockdown on cell viability, migration and invasion were detected using trypan blue exclusion assay, cell migration and invasion assay, respectively...
January 11, 2018: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/29319206/butyl-paraben-promotes-apoptosis-in-human-trophoblast-cells-through-increased-oxidative-stress-induced-endoplasmic-reticulum-stress
#8
Changwon Yang, Whasun Lim, Fuller W Bazer, Gwonhwa Song
Butyl paraben (BP) has antimicrobial effects and is widely used as a preservative in cosmetics, foods, and pharmaceuticals. It is also absorbed into various tissues of the human body. It is known that BP is measurable in maternal and fetal tissues during pregnancy, but the effects of BP on placental development, essential for maintaining normal pregnancy, are unclear. Therefore, we investigated the effect of BP on the proliferation, apoptosis, and invasiveness of human trophoblast cells, using an HTR8/SVneo cell line...
January 10, 2018: Environmental Toxicology
https://www.readbyqxmd.com/read/29316328/anti-fibrotic-effects-of-pirfenidone-by-interference-with-the-hedgehog-signalling-pathway-in-patients-with-systemic-sclerosis-associated-interstitial-lung-disease
#9
Hua Xiao, Guang-Feng Zhang, Xiang-Ping Liao, Xiao-Jie Li, Jian Zhang, Haobo Lin, Zhe Chen, Xiao Zhang
AIM: To determine whether pirfenidone attenuates lung fibrosis by interfering with the hedgehog (Hh) signalling pathway in patients with systemic sclerosis-associated interstitial lung disease (SSc-ILD). METHODS: Twenty-five SSc-ILD patients (20 first visit, five who underwent pirfenidone treatment for 6 months) and 10 healthy controls were recruited. Lung tissues were obtained by open-chest surgery, and primary lung fibroblasts were isolated, cultured and stimulated with pirfenidone...
January 7, 2018: International Journal of Rheumatic Diseases
https://www.readbyqxmd.com/read/29310812/pgbr-extract-ameliorates-tnf-%C3%AE-induced-insulin-resistance-in-hepatocytes
#10
Fu-Chih Chen, Kuo-Ping Shen, Jin-Bor Chen, Hui-Li Lin, Chi-Long Hao, Hsueh-Wei Yen, Shyh-Yu Shaw
Pre-germinated brown rice (PGBR) could ameliorate metabolic syndrome, however, not much research estimates the effect of PGBR extract on insulin resistance. The aim of this study is to examine the effects of PGBR extract in TNF-α induced insulin resistance. HepG2 cells, hepatocytes, were cultured in DMEM medium and added with 5 μM insulin or with insulin and 30 ng/ml TNF-α or with insulin, TNF-α and PGBR extract (50, 100, 300 μg/ml). The glucose levels of the medium were decreased by insulin, demonstrating insulin promoted glucose uptake into cell...
January 2018: Kaohsiung Journal of Medical Sciences
https://www.readbyqxmd.com/read/29306837/glycogen-synthase-kinase-3-and-its-inhibitors-potential-target-for-various-therapeutic-conditions
#11
REVIEW
A Prasanth Saraswati, S M Ali Hussaini, Namballa Hari Krishna, Bathini Nagendra Babu, Ahmed Kamal
Glycogen Synthase Kinase-3 (GSK-3) is a serine/threonine kinase which is ubiquitously expressed and is regarded as a regulator for various cellular events and signalling pathways. It exists in two isoforms, GSK-3α and GSK-3β and can phosphorylate a wide range of substrates. Aberrancy in the GSK-3 activity can lead to various diseases like Alzheimer's, diabetes, cancer, neurodegeneration etc., rendering it an attractive target to develop potent and specific inhibitors. The present review focuses on the recent developments in the area of GSK-3 inhibitors and also enlightens its therapeutic applicability in various disease conditions...
December 9, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29305881/liver-carbohydrates-metabolism-a-new-islet-neogenesis-associated-protein-peptide-ingap-pp-target
#12
Hernán Gonzalo Villagarcía, Carolina Lisi Román, María Cecilia Castro, Luisa Arbeláez González, María Teresa Ronco, Daniel Eleazar Francés, María Laura Massa, Bárbara Maiztegui, Luis Emilio Flores, Juan José Gagliardino, Flavio Francini
Islet-Neogenesis Associated Protein-Pentadecapeptide (INGAP-PP) increases β-cell mass and enhances glucose and amino acids-induced insulin secretion. Our aim was to demonstrate its effect on liver metabolism. For that purpose, adult male Wistar rats were injected twice-daily (10 days) with saline solution or INGAP-PP (250 μg). Thereafter, serum glucose, triglyceride and insulin levels were measured and homeostasis model assessment (HOMA-IR) and hepatic insulin sensitivity (HIS) were determined. Liver glucokinase and glucose-6-phosphatase (G-6-Pase) expression and activity, phosphoenolpyruvate carboxykinase (PEPCK) expression, phosphofructokinase-2 (PFK-2) protein content, P-Akt/Akt and glycogen synthase kinase-3β (P-GSK3/GSK3) protein ratios and glycogen deposit were also determined...
January 3, 2018: Peptides
https://www.readbyqxmd.com/read/29302212/ethyl-linoleate-inhibits-%C3%AE-msh-induced-melanogenesis-through-akt-gsk3%C3%AE-%C3%AE-catenin-signal-pathway
#13
Gyeong-A Ko, Somi Kim Cho
Ethyl linoleate is an unsaturated fatty acid used in many cosmetics for its various attributes, such as antibacterial and anti-inflammatory properties and clinically proven to be an effective anti-acne agent. In this study, we investigated the effect of ethyl linoleate on the melanogenesis and the mechanism underlying its action on melanogenesis in B16F10 murine melanoma cells. Our results revealed that ethyl linoleate significantly inhibited melanin content and intracellular tyrosinase activity in α-MSH-induced B16F10 cells, but it did not directly inhibit activity of mushroom tyrosinase...
January 2018: Korean Journal of Physiology & Pharmacology
https://www.readbyqxmd.com/read/29299988/an-overview-of-discovery-of-thiazole-containing-heterocycles-as-potent-gsk-3%C3%AE-inhibitors
#14
Deepika Sharma, Anjleena Malhotra, Ranju Bansal
Glycogen synthase kinase-3 (GSK-3) is a multifunctional serine/threonine (ser/thr) kinase that was originally identified as a regulator of glycogen metabolism and coupled with insulin signaling. Due to multifunctionality of this enzyme, it is found to play an important role in the onset and progression of various human diseases. Thiazole nucleus has received special attention by medicinal chemists because of its wide therapeutic potential. The objective of this review is to cover all the aspects of GSK-3β enzyme including its clinical implications, types of inhibitors with special reference to thiazole as GSK-3β inhibitor...
January 4, 2018: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/29299155/neuroprotection-by-aripiprazole-against-%C3%AE-amyloid-induced-toxicity-by-p-ck2%C3%AE-activation-via-inhibition-of-gsk-3%C3%AE
#15
So Youn Park, Hwa Kyoung Shin, Won Suk Lee, Sun Sik Bae, Koanhoi Kim, Ki Whan Hong, Chi Dae Kim
Psychosis is reported over 30% of patients with Alzheimer's disease (AD) in clinics. Aripiprazole is an atypical antipsychotic drug with partial agonist activity at the D2 dopamine and 5-HT1A receptors with low side-effect profile. We identified aripiprazole is able to overcome the amyloid-β (Aβ)-evoked neurotoxicity and then increase the cell viability. This study elucidated the mechanism(s) by which aripiprazole ameliorates Aβ1-42-induced decreased neurite outgrowth and viability in neuronal cells. Pretreatment with aripiprazole increased Brain-derived neurotrophic factor (BDNF) mRNA and protein expressions in N2a cells...
December 15, 2017: Oncotarget
https://www.readbyqxmd.com/read/29298990/gsk3%C3%AE-negatively-regulates-trax-a-scaffold-protein-implicated-in-mental-disorders-for-nhej-mediated-dna-repair-in-neurons
#16
Ting Chien, Yu-Ting Weng, Shu-Yung Chang, Hsing-Lin Lai, Feng-Lan Chiu, Hung-Chih Kuo, De-Maw Chuang, Yijuang Chern
Translin-associated protein X (TRAX) is a scaffold protein with various functions and has been associated with mental illnesses, including schizophrenia. We have previously demonstrated that TRAX interacts with a Gsα protein-coupled receptor, the A2A adenosine receptor (A2AR), and mediates the function of this receptor in neuritogenesis. In addition, stimulation of the A2AR markedly ameliorates DNA damage evoked by elevated oxidative stress in neurons derived from induced pluripotent stem cells (iPSCs). Here, we report that glycogen synthase kinase 3 beta (GSK3β) and disrupted-in-schizophrenia 1 (DISC1) are two novel interacting proteins of TRAX...
January 3, 2018: Molecular Psychiatry
https://www.readbyqxmd.com/read/29298849/pathologic-thr175-tau-phosphorylation-in-cte-and-cte-with-als
#17
Alexander J Moszczynski, Wendy Strong, Kathy Xu, Ann McKee, Arthur Brown, Michael J Strong
OBJECTIVE: To investigate whether chronic traumatic encephalopathy (CTE) and CTE with amyotrophic lateral sclerosis (CTE-ALS) exhibit features previously observed in other tauopathies of pathologic phosphorylation of microtubule-associated protein tau at Thr175 (pThr175 tau) and Thr231 (pThr231 tau), and glycogen synthase kinase-3β (GSK3β) activation, and whether these pathologic features are a consequence of traumatic brain injury (TBI). METHODS: Tau isoform expression was assayed by western blot in 6 stage III CTE cases...
January 3, 2018: Neurology
https://www.readbyqxmd.com/read/29298655/fisetin-attenuates-akt-associated-growth-promoting-events-in-aflatoxinb1-induced-hepatocellular-carcinoma
#18
Brajesh Kumar Maurya, Surendra Kumar Trigun
Recently we have reported that Fisetin, a natural flavonol, is able to regress Aflatoxin-B1 (AFB1) induced hepatocellular carcinoma (HCC) by suppressing reactive oxygen species (ROS) led pro-inflammatory factors in rats. In the current study, we aimed to delineate whether Fisetin does so by modulating the cell growth promoting signaling cascade in HCC. The reciprocal interplay of 3-phosphoinositol kinase (PI3K) vs phosphatase and tensin homologue deleted on chromosome 10 (PTEN) displays Akt, a protein kinase B, to get phosphorylated at Thr308 by a 3-phosphoinositol dependent kinase 1 (PDK1)...
December 29, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29291576/lithium-promotes-the-production-of-reactive-oxygen-species-via-gsk-3%C3%AE-tsc2-tor-signaling-in-the-gill-of-zebrafish-danio-rerio
#19
Dongwu Liu, Lili Gao, Zhuangzhuang Zhang, Shiyi Tao, Qiuxiang Pang, Ao Li, Hongkuan Deng, Hairui Yu
In this study, the mechanism that lithium (Li) promotes the production of reactive oxygen species (ROS) via the glycogen synthase kinase-3β (GSK-3β)/tuberous sclerosis complex 2 (TSC2)/target of rapamycin (TOR) signaling was investigated in the gill of zebrafish (Danio rerio). After the zebrafish were treated by 25 and 50 mg/L Li+, the mRNA expression of GSK-3β and TSC2 was inhibited, but the expression of TOR was induced in the gill of zebrafish. The levels of hydrogen peroxide (H2O2), superoxide anion (O2·-), and hydroxy radical (·OH) as well as the activity of superoxide dismutase (SOD) were increased, while the activities of catalase (CAT), glutathione peroxidase (GSH-PX), and peroxidase (POD) were decreased by 25 and 50 mg/L Li+ treatments...
December 28, 2017: Chemosphere
https://www.readbyqxmd.com/read/29291430/the-potential-benefit-of-combined-versus-monotherapy-of-coenzyme-q10-and-fluoxetine-on-depressive-like-behaviors-and-intermediates-coupled-to-gsk-3%C3%AE-in-rats
#20
Sally A Abuelezz, Nevien Hendawy, Yosra Magdy
As a part of the serotoninergic dysfunction implicated in neurobiology of depression, evidence has focused on serotonin (5-HT) receptors downstream signaling intermediates including glycogen synthase kinase-3β (GSK-3β), cAMP response element binding protein (CREB) and brain derived neurotrophic factor (BDNF). Our team previously reported that coenzyme Q10 (CoQ10) exerted antidepressant-like effect in rats exposed to chronic unpredictable mid stress (CUMS) via elevating serotonin levels. However, the effect of CoQ10 has not been elucidated in downstream signaling molecules mediating 5HT receptors' effect involved in depressive disorder hitherto...
December 29, 2017: Toxicology and Applied Pharmacology
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