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Drug Target Insights

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https://www.readbyqxmd.com/read/27812281/immunoinformatics-approach-in-designing-epitope-based-vaccine-against-meningitis-inducing-bacteria-streptococcus-pneumoniae-neisseria-meningitidis-and-haemophilus-influenzae-type-b
#1
Hilyatuz Zahroh, Ahmad Ma'rup, Usman Sumo Friend Tambunan, Arli Aditya Parikesit
Meningitis infection is one of the major threats during Hajj season in Mecca. Meningitis vaccines are available, but their uses are limited in some countries due to religious reasons. Furthermore, they only give protection to certain serogroups, not to all types of meningitis-inducing bacteria. Recently, research on epitope-based vaccines has been developed intensively. Such vaccines have potential advantages over conventional vaccines in that they are safer to use and well responded to the antibody. In this study, we developed epitope-based vaccine candidates against various meningitis-inducing bacteria, including Streptococcus pneumoniae, Neisseria meningitidis, and Haemophilus influenzae type b...
2016: Drug Target Insights
https://www.readbyqxmd.com/read/27660406/effects-and-safety-of-linagliptin-as-an-add-on-therapy-in-advanced-stage-diabetic-nephropathy-patients-taking-renin-angiotensin-aldosterone-system-blockers
#2
Yuichiro Ueda, Hiroki Ishii, Taisuke Kitano, Mitsutoshi Shindo, Haruhisa Miyazawa, Kiyonori Ito, Keiji Hirai, Yoshio Kaku, Honami Mori, Taro Hoshino, Susumu Ookawara, Masafumi Kakei, Kaoru Tabei, Yoshiyuki Morishita
BACKGROUND: We investigated the effects and safety of linagliptin as an add-on therapy in patients with advanced-stage diabetic nephropathy (DMN) taking renin-angiotensin-aldosterone system (RAAS) blockers. METHOD: Twenty advanced-stage DMN patients (estimated glomerular filtration rate (eGFR): 24.5 ± 13.4 mL/min/1.73 m(2)) taking RAAS blockers were administered 5 mg/day linagliptin for 52 weeks. Changes in glucose and lipid metabolism and renal function were evaluated...
2016: Drug Target Insights
https://www.readbyqxmd.com/read/27279734/gentamicin-impregnated-collagen-sponge-effectiveness-in-preventing-sternal-wound-infection-in-high-risk-cardiac-surgery
#3
REVIEW
Filippo Rapetto, Vito D Bruno, Gustavo Guida, Roberto Marsico, Pierpaolo Chivasso, Carlo Zebele
Sternal wound infections represent one of the most frequent complications after cardiac surgery and are associated with high postoperative mortality. Several preventive methods have been introduced, and recently, gentamicin-impregnated collagen sponges (GICSs) have shown a promising effect in reducing the incidence of this type of complications. Gentamicin is an aminoglycoside antibiotic that has been widely used to treat infections caused by multiresistant bacteria; despite its effectiveness, its systemic use carries a risk of toxicity...
2016: Drug Target Insights
https://www.readbyqxmd.com/read/27257369/a-case-of-organizing-pneumonia-op-associated-with-pembrolizumab
#4
Paraskevi Fragkou, Maria Souli, Maria Theochari, Christina Kontopoulou, Stelios Loukides, Anna Koumarianou
Until recently, chemotherapy for metastatic melanoma had disappointing results. The identification of immune checkpoints such as CTLA-4 and PD-1/PD-L1 has led to the development of an array of monoclonal antibodies (Mabs). These immunologic approaches against tumoral cells come with a novel kind of side effects that the clinician needs to be familiarized with. Herein, we report for the first time a case of organizing pneumonia, based on imaging and cytological analyses of bronchoalveolar lavage, possibly associated with the use of pembrolizumab, an anti-PD-1 Mab recently approved for the treatment of metastatic melanoma...
2016: Drug Target Insights
https://www.readbyqxmd.com/read/26966348/brain-histamine-n-methyltransferase-as-a-possible-target-of-treatment-for-methamphetamine-overdose
#5
REVIEW
Junichi Kitanaka, Nobue Kitanaka, F Scott Hall, George R Uhl, Motohiko Takemura
Stereotypical behaviors induced by methamphetamine (METH) overdose are one of the overt symptoms of METH abuse, which can be easily assessed in animal models. Currently, there is no successful treatment for METH overdose. There is increasing evidence that elevated levels of brain histamine can attenuate METH-induced behavioral abnormalities, which might therefore constitute a novel therapeutic treatment for METH abuse and METH overdose. In mammals, histamine N-methyltransferase (HMT) is the sole enzyme responsible for degrading histamine in the brain...
2016: Drug Target Insights
https://www.readbyqxmd.com/read/26949333/preliminary-in-vivo-evaluation-of-a-hybrid-armored-vascular-graft-combining-electrospinning-and-additive-manufacturing-techniques
#6
Cristiano Spadaccio, Francesco Nappi, Federico De Marco, Pietro Sedati, Fraser W H Sutherland, Massimo Chello, Marcella Trombetta, Alberto Rainer
In this study, we tested in vivo effectiveness of a previously developed poly-l-lactide/poly-ε-caprolactone armored vascular graft releasing heparin. This bioprosthesis was designed in order to overcome the main drawbacks of tissue-engineered vascular grafts, mainly concerning poor mechanical properties, thrombogenicity, and endothelialization. The bioprosthesis was successfully implanted in an aortic vascular reconstruction model in rabbits. All grafts implanted were patent at four weeks postoperatively and have been adequately populated by endogenous cells without signs of thrombosis or structural failure and with no need of antiplatelet therapy...
2016: Drug Target Insights
https://www.readbyqxmd.com/read/26617459/screening-analogs-of-%C3%AE-og-pocket-binder-as-fusion-inhibitor-of-dengue-virus-2
#7
Usman Sf Tambunan, Hilyatuz Zahroh, Arli A Parikesit, Syarifuddin Idrus, Djati Kerami
Dengue is an infectious disease caused by dengue virus (DENV) and transmitted between human hosts by mosquitoes. Recently, Indonesia was listed as a country with the highest cases of dengue by the Association of Southeast Asian Nations. The current treatment for dengue disease is supportive therapy; there is no antiviral drug available in the market against dengue. Therefore, a research on antiviral drug against dengue is very important, especially to prevent outbreak explosion. In this research, the development of dengue antiviral is performed through the inhibition of n-octyl-β-D-glucoside (β-OG) binding pocket on envelope protein of DENV by using analogs of β-OG pocket binder...
2015: Drug Target Insights
https://www.readbyqxmd.com/read/26609216/management-of-diabetes-associated-with-nephrotic-syndrome-therapeutic-potential-of-dapagliflozin-for-protracted-volume-retention
#8
Toshimi Imai, Tetsu Akimoto, Chiharu Ito, Takahiro Masuda, Daisuke Nagata
A 48-year-old female was admitted to our hospital presenting with a chief complaint of progressive swelling because of diabetic nephrotic syndrome. Dapagliflozin seemed to play a role in accelerating the patient's urinary sodium excretion as well as reducing gross fluid retention despite the fact that her nephrotic condition was resistant to furosemide. Our experience emphasizes a potential novel approach to overcoming loop diuretic resistance using this agent among some subsets of type 2 diabetic subjects complicated with severe volume accumulation...
2015: Drug Target Insights
https://www.readbyqxmd.com/read/26244009/basal-plasma-levels-of-copeptin-are-elevated-in-inactive-inflammatory-bowel-disease-after-bowel-resection
#9
Bodil Ohlsson, Olle Melander
Evidence of interactions between the enteric nervous system, neuropeptides, and the immune system is growing. The aim of this study was to examine basal plasma levels of a variety of peptide precursors in patients with inflammatory bowel disease (IBD). In two middle-aged cohorts, Malmö Preventive Medicine (n = 5,415) and Malmö Diet and Cost Study (n = 6,103), individuals with the diagnosis of IBD were identified. Medical records were scrutinized. Three controls were matched for each patient. Copeptin, midregional fragments of adrenomedullin, pro-atrial natriuretic peptide, and proenkephalin A, as well as N-terminal protachykinin A and proneurotensin were analyzed in the plasma...
2015: Drug Target Insights
https://www.readbyqxmd.com/read/26106261/medicinal-plants-a-potential-source-of-compounds-for-targeting-cell-division
#10
Ihsan N Zulkipli, Sheba R David, Rajan Rajabalaya, Adi Idris
Modern medicinal plant drug discovery has provided pharmacologically active compounds targeted against a multitude of conditions and diseases, such as infection, inflammation, and cancer. To date, natural products from medicinal plants remain a solid niche as a source from which cancer therapies can be derived. Among other properties, one favorable characteristic of an anticancer drug is its ability to block the uncontrollable process of cell division, as cancer cells are notorious for their abnormal cell division...
2015: Drug Target Insights
https://www.readbyqxmd.com/read/25788830/7-ni-and-odq-disturbs-memory-in-the-elevated-plus-maze-morris-water-maze-and-radial-arm-maze-tests-in-mice
#11
Oguz Mutlu, Furuzan Akar, Ipek Komsuoglu Celikyurt, Pelin Tanyeri, Guner Ulak, Faruk Erden
Nitric oxide (NO) is an atypical neurotransmitter that causes changes in cognition. Nitric oxide synthase (NOS) and guanylate cyclase (GC) inhibitors have been shown to exert some effects on cognition in previous studies; however, the findings have been controversial. This study was aimed at understanding the effects of an NOS inhibitor, 7-nitroindazole (7-NI), and a guanylate cyclase inhibitor, 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (ODQ), on spatial memory in modified elevated plus maze (mEPM), Morris water maze (MWM), and radial arm maze (RAM) tests...
2015: Drug Target Insights
https://www.readbyqxmd.com/read/25574133/genome-wide-analysis-of-mycoplasma-hominis-for-the-identification-of-putative-therapeutic-targets
#12
Md Masud Parvege, Monzilur Rahman, Mohammad Shahnoor Hossain
Ever increasing propensity of antibiotic resistance among pathogenic bacteria raises the demand for the development of novel therapeutic agents to control this grave problem. Advances in the field of bioinformatics, genomics, and proteomics have greatly facilitated the discovery of alternative drugs by swift identification of new drug targets. In the present study, we employed comparative genomics and metabolic pathway analysis with an aim of identifying therapeutic targets in Mycoplasma hominis. Our study has revealed 40 annotated metabolic pathways, including five unique pathways of M...
2014: Drug Target Insights
https://www.readbyqxmd.com/read/25452692/the-expression-of-serum-antibodies-against-gonadotropin-releasing-hormone-gnrh1-progonadoliberin-2-luteinizing-hormone-lh-and-related-receptors-in-patients-with-gastrointestinal-dysfunction-or-diabetes-mellitus
#13
Bodil Roth, Kerstin Berntorp, Bodil Ohlsson
Gonadotropin-releasing hormone (GnRH) 1 and 2 and luteinizing hormone (LH) receptors have been described in the gastrointestinal tract. We have previously demonstrated antibodies in serum against GnRH1 in patients with gastrointestinal dysfunction and diabetes mellitus, and antibodies against GnRH receptor, LH, and LH receptor in patients with infertility. The aim of this study was to search for the expression of serum antibodies against GnRH1 with an improved enzyme-linked immune sorbent assay (ELISA), and antibodies against progonadoliberin-2, GnRH2, GnRH receptor, LH, and LH receptor with newly developed ELISAs, in patients with gastrointestinal dysfunction or diabetes mellitus...
2014: Drug Target Insights
https://www.readbyqxmd.com/read/25210423/febuxostat-for-hyperuricemia-in-patients-with-advanced-chronic-kidney-disease
#14
Tetsu Akimoto, Yoshiyuki Morishita, Chiharu Ito, Osamu Iimura, Sadao Tsunematsu, Yuko Watanabe, Eiji Kusano, Daisuke Nagata
Febuxostat is a nonpurine xanthine oxidase (XO) inhibitor, which recently received marketing approval. However, information regarding the experience with this agent among advanced chronic kidney disease (CKD) patients is limited. In the current study, we investigated the effects of oral febuxostat in patients with advanced CKD with asymptomatic hyperuricemia. We demonstrated, for the first time, that not only the serum levels of uric acid (UA) but also those of 8-hydroxydeoxyguanosine, an oxidative stress marker, were significantly reduced after six months of febuxostat treatment, with no adverse events...
2014: Drug Target Insights
https://www.readbyqxmd.com/read/25125971/molecular-and-kinetic-characterization-of-babesia-microti-gray-strain-lactate-dehydrogenase-as-a-potential-drug-target
#15
Patrick Vudriko, Tatsunori Masatani, Shinuo Cao, Mohamad Alla Terkawi, Ketsarin Kamyingkird, Ahmed A Mousa, Paul F Adjou Moumouni, Yoshifumi Nishikawa, Xuenan Xuan
Babesia microti is an emerging zoonotic protozoan organism that causes "malaria-like" symptoms that can be fatal in immunocompromised people. Owing to lack of specific therapeutic regiment against the disease, we cloned and characterized B. microti lactate dehydrogenase (BmLDH) as a potential molecular drug receptor. The in vitro kinetic properties of BmLDH enzyme was evaluated using nicotinamide adenine dinucleotide (NAD(+)) as a co-factor and lactate as a substrate. Inhibitory assay was also done using gossypol as BmLDH inhibitor to determine the inhibitory concentration 50 (IC50)...
2014: Drug Target Insights
https://www.readbyqxmd.com/read/24855335/effects-of-zaprinast-and-rolipram-on-olfactory-and-visual-memory-in-the-social-transmission-of-food-preference-and-novel-object-recognition-tests-in-mice
#16
Furuzan Akar, Oguz Mutlu, Ipek K Celikyurt, Emine Bektas, Mehmet H Tanyeri, Guner Ulak, Pelin Tanyeri, Faruk Erden
The role of phosphodiesterase (PDE) inhibitors in central nervous system has been investigated and shown to stimulate neuronal functions and increase neurogenesis in Alzheimer patients. The aim of this study is to investigate effect of PDE5 inhibitor zaprinast and PDE4 inhibitor rolipram on visual memory in novel object recognition (NOR) test, on olfactory memory in social transmission of food preference (STFP) test, and also on locomotion and anxiety in open field test in naive mice. Male Balb-c mice were treated intraperitoneally (i...
2014: Drug Target Insights
https://www.readbyqxmd.com/read/24634580/the-antidepressant-agomelatine-improves-memory-deterioration-and-upregulates-creb-and-bdnf-gene-expression-levels-in-unpredictable-chronic-mild-stress-ucms-exposed-mice
#17
Esen Gumuslu, Oguz Mutlu, Deniz Sunnetci, Guner Ulak, Ipek K Celikyurt, Naci Cine, Furuzan Akar, Hakan Savlı, Faruk Erden
Agomelatine, a novel antidepressant with established clinical efficacy, acts as an agonist of melatonergic MT1 and MT2 receptors and as an antagonist of 5-HT2C receptors. The present study was undertaken to investigate whether chronic treatment with agomelatine would block unpredictable chronic mild stress (UCMS)-induced cognitive deterioration in mice in passive avoidance (PA), modified elevated plus maze (mEPM), novel object recognition (NOR), and Morris water maze (MWM) tests. Moreover, the effects of stress and agomelatine on brain-derived neurotrophic factor (BDNF) and cyclic adenosine monophosphate (cAMP) response element binding protein (CREB) messenger ribonucleic acid (mRNA) levels in the hippocampus was also determined using quantitative real-time polymerase chain reaction (RT-PCR)...
2014: Drug Target Insights
https://www.readbyqxmd.com/read/24526834/in-silico-molecular-characterization-of-cysteine-protease-yopt-from-yersinia-pestis-by-homology-modeling-and-binding-site-identification
#18
Md Anayet Hasan, S M Alauddin, Mohammad Al Amin, Suza Mohammad Nur, Adnan Mannan
Plague is a major health concern and Yersinia pestis plays the central causal role in this disease. Yersinia pestis has developed resistance against the commonly available drugs. So, it is now a key concern to find a new drug target. Cysteine protease YopT enzyme is an important factor used by Yersinia pestis for pathogenesis in its host and it has the anti-phagocytic function of removal of C-termini lipid modification. The 3D structure of cysteine protease YopT of Yersinia pestis was determined by means of homology modeling through multiple alignments followed by intensive optimization and validation...
2014: Drug Target Insights
https://www.readbyqxmd.com/read/24137050/microscopic-colitis-and-reproductive-factors-related-to-exposure-to-estrogens-and-progesterone
#19
Bodil Roth, Jonas Manjer, Bodil Ohlsson
Microscopic colitis (MC) often debuts around or after menopause and is divided into lymphocytic- and collagenous colitis. The aim of this study was to examine whether factors influencing sex hormone levels differed between subgroups of MC as well as between patients and controls. A self-administered questionnaire about parity was completed which included questions surrounding age at first childbirth, menarche and menopause, the use of oral contraceptives, and hormonal replacement therapy. Patients with lymphocytic colitis had children less often compared to those with collagenous colitis (OR = 0...
2013: Drug Target Insights
https://www.readbyqxmd.com/read/24027419/hsp60-chaperonin-acts-as-barrier-to-pharmacologically-induced-oxidative-stress-mediated-apoptosis-in-tumor-cells-with-differential-stress-response
#20
Upasana Sarangi, Manish Kumar Singh, Kanugovi Vijaya Vittal Abhijnya, Lebaka Prasanna Anjaneya Reddy, Badabagni Siva Prasad, Vikrant Vinay Pitke, Khanderao Paithankar, Amere Subbarao Sreedhar
Mitochondrial functions play a central role in energy metabolism and provide survival fitness to both normal and tumor cells. Mitochondrial chaperonin Hsp60 is involved in both pro- and anti-apoptotic functions, but how Hsp60 senses the mitochondria selective oxidative stress response is unknown. In this study, by using rotenone, an irreversible inhibitor of oxidative phosphorylation against IMR-32 and BC-8 tumor cells containing differential heat shock transcriptional machinery, we studied whether the oxidative stress response is related to Hsp60...
2013: Drug Target Insights
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