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https://www.readbyqxmd.com/read/28445786/metallo-%C3%AE-lactamase-inhibitors-by-bioisosteric-replacement-preparation-activity-and-binding
#1
Susann Skagseth, Sundus Akhter, Marianne H Paulsen, Zeeshan Muhammad, Silje Lauksund, Ørjan Samuelsen, Hanna-Kirsti S Leiros, Annette Bayer
Bacterial resistance is compromising the use of β-lactam antibiotics including carbapenems. The main resistance mechanism against β-lactams is hydrolysis of the β-lactam ring mediated by serine- or metallo-β-lactamases (MBLs). Although several inhibitors of MBLs have been reported, none has been developed into a clinically useful inhibitor. Mercaptocarboxylic acids are among the most prominent scaffolds reported as MBL inhibitors. In this study, the carboxylate group of mercaptocarboxylic acids was replaced with bioisosteric groups like phosphonate esters, phosphonic acids and NH-tetrazoles...
April 14, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28445592/polo-like-kinase-1-is-a-proviral-host-factor-for-hepatitis-b-virus-replication
#2
Ahmed M Diab, Adrien Foca, Floriane Fusil, Thomas Lahlali, Pascal Jalaguier, Fouzia Amirache, Lia N'Guyen, Nathalie Isorce, François-Loïc Cosset, Fabien Zoulim, Ourania M Andrisani, David Durantel
Chronic Hepatitis B Virus (HBV) infection is a major risk factor for hepatocellular carcinoma (HCC) and current treatments for CHB and HCC are perfectible. Herein, we identified cellular Serine/Threonine Polo-like-kinase 1 (PLK1) as a positive effector of HBV replication. The aim of this study was to demonstrate the proviral role of PLK1 in HBV biosynthesis and validate PLK1 inhibition a potential antiviral strategy. To this end, we employed physiologically relevant HBV infection models of Primary Human Hepatocytes (PHH) and differentiated HepaRG cells, in conjunction with pharmacologic PLK1 inhibitors, siRNA-mediated knockdown, and overexpression of constitutively active PLK1 (PLK1(CA) )...
April 26, 2017: Hepatology: Official Journal of the American Association for the Study of Liver Diseases
https://www.readbyqxmd.com/read/28445254/the-clinical-features-treatment-and-prognosis-of-primary-mediastinal-malignant-melanoma-a-case-report
#3
ZiHai Li, Hui Jia, Baijiang Zhang, Yongming Zhang, Hui Li, Pingping Song
RATIONALE: Primary malignant melanoma (MM) of the mediastinum is exceedingly rare; a review of the English-language literature reveals only a small number of case reports. In this paper, we discuss a case of primary mediastinal MM and present a review of the relevant literature on its clinical features and treatment. PATIENT CONCERNS: A 52-year-old male presenting with back pain was admitted to our hospital for treatment. Imaging examination revealed an anterior mediastinal mass and no evidence of other metastatic or primary lesions...
April 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28445029/nhs-esters-as-versatile-reactivity-based-probes-for-mapping-proteome-wide-ligandable-hotspots
#4
Carl C Ward, Jordan I Kleinman, Daniel K Nomura
Most of the proteome is considered undruggable oftentimes hindering translational efforts for drug discovery. Identifying previously unknown druggable hotspots in proteins would enable strategies for pharmacologically interrogating these sites with small-molecules. Activity-based protein profiling (ABPP) has arisen as a powerful chemoproteomic strategy that uses reactivity-based chemical probes to map reactive, functional, and ligandable hotspots in complex proteomes, which has enabled inhibitor discovery against various therapeutic protein targets...
April 26, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/28444861/lncrna-malat1-is-dysregulated-in-diabetic-nephropathy-and-involved-in-high-glucose-induced-podocyte-injury-via-its-interplay-with-%C3%AE-catenin
#5
Mengsi Hu, Rong Wang, Xiaobing Li, Minghua Fan, Jiangong Lin, Junhui Zhen, Liqun Chen, Zhimei Lv
Metastasis associated lung adenocarcinoma transcript 1(MALAT1) is a long non-coding RNA, broadly expressed in mammalian tissues including kidney and up-regulated in a variety of cancer cells. To date, its functions in podocytes are largely unknown. β-catenin is a key mediator in the canonical and non-canonical Wnt signalling pathway; its aberrant expression promotes podocyte malfunction and albuminuria, and contributes to kidney fibrosis. In this study, we found that MALAT1 levels were increased in kidney cortices from C57BL/6 mice with streptozocin (STZ)-induced diabetic nephropathy, and dynamically regulated in cultured mouse podocytes stimulated with high glucose, which showed a trend from rise to decline...
April 26, 2017: Journal of Cellular and Molecular Medicine
https://www.readbyqxmd.com/read/28444301/soybean-nima-related-kinase1-promotes-plant-growth-and-improves-salt-and-cold-tolerance
#6
Wen-Jia Pan, Jian-Jun Tao, Tong Cheng, Ming Shen, Jin-Biao Ma, Wan-Ke Zhang, Qin Lin, Biao Ma, Shou-Yi Chen, Jin-Song Zhang
NEK (NIMA-related kinase) is known as a family of serine/threonine kinases which mainly participate in microtubule-related mitotic events in fungi, mammals and other eukaryotes. Our previous studies found that Arabidopsis NEK6 plays an important role in plant response to abiotic stress. We further investigated roles of NEK family in soybean and found that at least eight members can respond to abiotic stresses. Among them, only GmNEK1, a novel NEK member which is distantly-related to Arabidopsis NEK6, enhanced plant growth and promoted salt and cold tolerance in transgenic Arabidopsis plants...
April 21, 2017: Plant & Cell Physiology
https://www.readbyqxmd.com/read/28442992/genetic-deletion-of-akt3-induces-an-endophenotype-reminiscent-of-psychiatric-manifestations-in-mice
#7
Yan Bergeron, Geneviève Bureau, Marie-Élaine Laurier-Laurin, Eric Asselin, Guy Massicotte, Michel Cyr
The protein kinase B (PKB/Akt), found in three distinctive isoforms (PKBα/Akt1, PKBβ/Akt2, PKBγ/Akt3), is implicated in a variety of cellular processes such as cell development, growth and survival. Although Akt3 is the most expressed isoform in the brain, its role in cerebral functions is still unclear. In the present study, we investigated the behavioral, electrophysiological and biochemical consequences of Akt3 deletion in mice. Motor abilities, spatial navigation, recognition memory and LTP are intact in the Akt3 knockout (KO) mice...
2017: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/28442745/phosphorylation-of-the-mitochondrial-autophagy-receptor-nix-enhances-its-interaction-with-lc3-proteins
#8
Vladimir V Rogov, Hironori Suzuki, Mija Marinković, Verena Lang, Ryuichi Kato, Masato Kawasaki, Maja Buljubašić, Matilda Šprung, Natalia Rogova, Soichi Wakatsuki, Anne Hamacher-Brady, Volker Dötsch, Ivan Dikic, Nathan R Brady, Ivana Novak
The mitophagy receptor Nix interacts with LC3/GABARAP proteins, targeting mitochondria into autophagosomes for degradation. Here we present evidence for phosphorylation-driven regulation of the Nix:LC3B interaction. Isothermal titration calorimetry and NMR indicate a ~100 fold enhanced affinity of the serine 34/35-phosphorylated Nix LC3-interacting region (LIR) to LC3B and formation of a very rigid complex compared to the non-phosphorylated sequence. Moreover, the crystal structure of LC3B in complex with the Nix LIR peptide containing glutamic acids as phosphomimetic residues and NMR experiments revealed that LIR phosphorylation stabilizes the Nix:LC3B complex via formation of two additional hydrogen bonds between phosphorylated serines of Nix LIR and Arg11, Lys49 and Lys51 in LC3B...
April 25, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28442665/the-amino-acid-at-position-624-in-the-glycoprotein-of-sftsv-severe-fever-with-thrombocytopenia-virus-plays-a-critical-role-in-low-ph-dependent-cell-fusion-activity
#9
Yoshimi Tsuda, Manabu Igarashi, Ryo Ito, Sanae Nishio, Kenta Shimizu, Kumiko Yoshimatsu, Jiro Arikawa
Severe fever with thrombocytopenia syndrome virus (SFTSV) is a novel phlebovirus responsible for causing an emerging zoonotic disease. We previously established subclones from SFTSV strain YG1 based on differences in low-pH-dependent cell fusion activities and found two amino acid substitutions, Y328H and R624W, in the envelope glycoprotein (GP) of high fusion subclones. In this study, we show that transiently expressed GP with the R624W mutation, but not the Y328H mutation, induced cell fusion under acidic conditions...
2017: Biomedical Research
https://www.readbyqxmd.com/read/28442545/peroxisome-proliferator-activated-receptor-%C3%AE-agonists-attenuate-biofilm-formation-by-pseudomonas-aeruginosa
#10
Brahmchetna Bedi, Nicholas M Maurice, Vincent T Ciavatta, K Sabrina Lynn, Zhihong Yuan, Samuel A Molina, Myungsoo Joo, William R Tyor, Joanna B Goldberg, Michael H Koval, C Michael Hart, Ruxana T Sadikot
Pseudomonas aeruginosa is a significant contributor to recalcitrant multidrug- resistant infections, especially in immunocompromised and hospitalized patients. The pathogenic profile of P. aeruginosa is related to its ability to secrete a variety of virulence factors and to promote biofilm formation. Quorum sensing (QS) is a mechanism wherein P. aeruginosa secretes small diffusible molecules, specifically acyl homo serine lactones, such as N-(3-oxo-dodecanoyl)-l-homoserine lactone (3O-C12-HSL), that promote biofilm formation and virulence via interbacterial communication...
April 25, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28442507/protein-kinase-stk25-aggravates-the-severity-of-non-alcoholic-fatty-pancreas-disease-in-mice
#11
Esther Nunez Duran, Belen Chanclon, Silva Sütt, Joana Real, Hanns-Ulrich Marschall, Ingrid Wernstedt-Asterholm, Emelie Cansby, Margit Mahlapuu
Characterising the molecular networks that negatively regulate pancreatic β-cell function is essential for understanding the underlying pathogenesis and developing new treatment strategies for type 2 diabetes. We recently identified serine/threonine protein kinase 25 (STK25) as a critical regulator of ectopic fat storage, meta-inflammation, and fibrosis in liver and skeletal muscle. Here, we assessed the role of STK25 in control of progression of non-alcoholic fatty pancreas disease in the context of chronic exposure to dietary lipids in mice...
April 25, 2017: Journal of Endocrinology
https://www.readbyqxmd.com/read/28442503/molecular-pathways-targeting-the-protein-kinase-wee1-in-cancer
#12
Jill J J Geenen, Jan H M Schellens
Wee1 is a protein kinase that regulates the G2 checkpoint and prevents entry into mitosis in response to DNA damage. Cyclin-dependent kinases (CDKs) are a family of 14 serine/threonine protein kinases, which coordinate the progression through the cell cycle. The Cdc2/cyclin B complex controls the progression from G2 into mitosis. There are two mechanisms by which the G2 checkpoint is initiated in response to DNA damage: phosphorylation of Cdc25c by CHK1 and of Wee1 kinase, which phosphorylates Cdc2. Blockade at the G2 checkpoint is especially important for p53 mutant cells because these tumors mainly rely on DNA repair at the G2 checkpoint...
April 25, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/28442472/functional-and-metabolomic-consequences-of-atp-dependent-potassium-channel-inactivation-in-human-islets
#13
Changhong Li, Amanda M Ackermann, Kara E Boodhansingh, Tricia R Bhatti, Chengyang Liu, Jonathan Schug, Nicolai Doliba, Bing Han, Karen E Cosgrove, Indraneel Banerjee, Franz M Matschinsky, Itzhak Nissim, Klaus H Kaestner, Ali Naji, N Scott Adzick, Mark J Dunne, Charles A Stanley, Diva D De León
Loss-of-function mutations of β-cell KATP channels cause the most severe form of congenital hyperinsulinism (KATPHI). KATPHI is characterized by fasting and protein-induced hypoglycemia that is unresponsive to medical therapy. For a better understanding of the pathophysiology of KATPHI, we examined cytosolic calcium, insulin secretion, oxygen consumption, and [U-(13)C]glucose metabolism in islets isolated from the pancreases of children with KATPHI who required pancreatectomy. Basal cytosolic calcium ([Ca(2+)] i ) and insulin secretion were higher in KATPHI islets compared to controls...
April 25, 2017: Diabetes
https://www.readbyqxmd.com/read/28442011/-ck2%C3%AE-regulates-the-metastases-and-migration-of-lung-adenocarcinoma-%C3%A2-a549-cell-line-through-pi3k-akt-gsk-3%C3%AE-signal-pathway
#14
Aibing Wu, Mingchun Li, Zongjiong Mai, Shujun Li, Zhixiong Yang
BACKGROUND: Lung cancer is the leading cancer-related death worldwide. Patients with lung cancer mainly died of tumor metastasis and invasion. Protein kinase CK2 is an ubiquitous serine/threonine protein kinase and is frequently upregulated in various human tumors. This study aims to explore the effect and molecular mechanism of the invasion and migration of lung adenocarcinoma A549 cells after knock-down of CK2α expression. METHODS: The pSilencerTM 4.1-siCK2α-eGFP of lentiviral-mediated shRNA was constructed...
April 20, 2017: Zhongguo Fei Ai za Zhi, Chinese Journal of Lung Cancer
https://www.readbyqxmd.com/read/28441528/phosphorylation-of-neurog3-links-endocrine-differentiation-to-the-cell-cycle-in-pancreatic-progenitors
#15
Nicole A J Krentz, Dennis van Hoof, Zhongmei Li, Akie Watanabe, Mei Tang, Cuilan Nian, Michael S German, Francis C Lynn
During pancreatic development, proliferating pancreatic progenitors activate the proendocrine transcription factor neurogenin 3 (NEUROG3), exit the cell cycle, and differentiate into islet cells. The mechanisms that direct robust NEUROG3 expression within a subset of progenitor cells control the size of the endocrine population. Here we demonstrate that NEUROG3 is phosphorylated within the nucleus on serine 183, which catalyzes its hyperphosphorylation and proteosomal degradation. During progression through the progenitor cell cycle, NEUROG3 phosphorylation is driven by the actions of cyclin-dependent kinases 2 and 4/6 at G1/S cell-cycle checkpoint...
April 24, 2017: Developmental Cell
https://www.readbyqxmd.com/read/28441042/aberrantly-expressed-long-noncoding-rnas-in-recurrent-implantation-failure-a-microarray-related-study
#16
Li-Juan Fan, Hong-Jing Han, Jing Guan, Xiao-Wei Zhang, Qing-Hua Cui, Huan Shen, Cheng Shi
Long noncoding RNAs (lncRNAs) are a class of noncoding RNAs longer than 200 nucleotides. They were long regarded as transcription noise for their low expression and non-protein coding features. Recent published reports indicate that lncRNAs are involved in virtually every aspect of human biology. We aimed to profile the endometrial lncRNA expression pattern in women with recurrent implantation failure (RIF) and predict the function of the genes of the dysregulated lncRNA transcripts. Endometrial samples (24) were collected during window of implantation (14 RIF women and 10 women who conceived after embryo transfer)...
April 25, 2017: Systems Biology in Reproductive Medicine
https://www.readbyqxmd.com/read/28440900/phosphoglycerate-dehydrogenase-phgdh-deficiency-without-epilepsy-mimicking-primary-microcephaly
#17
Antoine Poli, Yoann Vial, Damien Haye, Sandrine Passemard, Manuel Schiff, Hala Nasser, Catherine Delanoe, Emma Cuadro, Rémi Kom, Narcisse Elanga, Anne Favre, Séverine Drunat, Alain Verloes
Phosphoglycerate dehydrogenase (PHGDH) deficiency (OMIM 256520) is a rare autosomal recessive disorder of serine synthesis, with mostly severe congenital microcephaly, caused by mutations in the PHGDH gene. Fourteen patients reported to date show severe, early onset, drug resistant epilepsy. In a cohort of patients referred for primary microcephaly, compound heterozygosity for two unreported variants in PHGDG was identified by exome sequencing in a pair of sibs who died aged 4.5 months and 4.5 years. They had severe neurological involvement with congenital microcephaly, disorganized EEG, and progressive spasticity, but never had seizures...
April 25, 2017: American Journal of Medical Genetics. Part A
https://www.readbyqxmd.com/read/28440887/microrna-regulation-of-extracellular-matrix-components-in-the-process-of-atherosclerotic-plaque-destabilization
#18
REVIEW
Michal Kowara, Agnieszka Cudnoch-Jedrzejewska, Grzegorz Opolski, Pawel Wlodarski
The process of atherosclerotic plaque destabilization, leading to myocardial infarction, is still not fully understood. The pathway - composed of structural and regulatory proteins of the extracellular matrix (ECM) such as collagen, elastin, small leucine-rich proteoglycans, metalloproteinases, cathepsins and serine proteases - is one potential way of atherosclerotic plaque destabilization. The expression of these proteins is controlled by different microRNA molecules. The goal of this paper is to summarize the current investigations and knowledge about ECM in the process of atherosclerotic plaque destabilization, giving special attention to epigenetic expression regulation by microRNA...
April 25, 2017: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/28440748/palmitoylated-scp1-is-targeted-to-the-plasma-membrane-and-negatively-regulates-angiogenesis
#19
Peng Liao, Weichao Wang, Yu Li, Rui Wang, Jiali Jin, Weijuan Pang, Yunfei Chen, Mingyue Shen, Xinbo Wang, Dongyang Jiang, Jinjiang Pang, Mingyao Liu, Xia Lin, Xin-Hua Feng, Ping Wang, Xin Ge
SCP1 as a nuclear transcriptional regulator acts globally to silence neuronal genes and to affect the dephosphorylation of RNA Pol ll. However, we report the first finding and description of SCP1 as a plasma membrane-localized protein in various cancer cells using EGFP- or other epitope-fused SCP1. Membrane-located SCP1 dephosphorylates AKT at serine 473, leading to the abolishment of serine 473 phosphorylation that results in suppressed angiogenesis and a decreased risk of tumorigenesis. Consistently, we observed increased AKT phosphorylation and angiogenesis followed by enhanced tumorigenesis in Ctdsp1 (which encodes SCP1) gene - knockout mice...
March 31, 2017: ELife
https://www.readbyqxmd.com/read/28439875/epigenetic-repression-of-mir-375-is-the-dominant-mechanism-for-constitutive-activation-of-the-pdpk1-rps6ka3-signalling-axis-in-multiple-myeloma
#20
Shotaro Tatekawa, Yoshiaki Chinen, Masaki Ri, Tomoko Narita, Yuji Shimura, Yayoi Matsumura-Kimoto, Taku Tsukamoto, Tsutomu Kobayashi, Eri Kawata, Nobuhiko Uoshima, Tomohiko Taki, Masafumi Taniwaki, Hiroshi Handa, Shinsuke Iida, Junya Kuroda
Cytogenetic/molecular heterogeneity is the hallmark of multiple myeloma (MM). However, we recently showed that the serine/threonine kinase PDPK1 and its substrate RPS6KA3 (also termed RSK2) are universally active in MM, and play pivotal roles in myeloma pathophysiology. In this study, we assessed involvement of aberrant miR-375 repression in PDPK1 overexpression in MM. An analysis of plasma cells from 30 pre-malignant monoclonal gammopathies of undetermined significance and 73 MM patients showed a significant decrease in miR-375 expression in patient-derived plasma cells regardless of the clinical stage, compared to normal plasma cells...
April 25, 2017: British Journal of Haematology
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