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Pancreatic enzyme inhibitor

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https://www.readbyqxmd.com/read/29026467/chromogranin-a-as-a-biochemical-marker-for-neuroendocrine-tumors-a-single-center-experience-at-royal-hospital-oman
#1
Elham S Al-Risi, Fatma S Al-Essry, Waad-Allah S Mula-Abed
OBJECTIVES: To evaluate the significance of serum chromogranin A (CgA) status in patients with and without different neuroendocrine tumors (NETs) by conducting a retrospective assessment of the diagnostic utility and limitations of CgA as a biomarker for NETs in a tertiary care hospital in Oman. METHODS: We conducted a retrospective analysis of CgA requests referred to the Clinical Biochemistry Laboratory, Royal Hospital, Oman over a 24-month period (April 2012 to March 2014)...
September 2017: Oman Medical Journal
https://www.readbyqxmd.com/read/29018784/peroxisome-proliferator-activated-receptor-gamma-inhibits-the-activation-of-stat3-in-cerulein-stimulated-pancreatic-acinar-cells
#2
Kyung Don Ju, Joo Weon Lim, Hyeyoung Kim
Cerulein-induced pancreatitis is similar to human edematous pancreatitis, characterized by the dysregulation of digestive enzyme production, edema formation, and an infiltration of inflammatory cells into the pancreas. We previously showed that the Janus kinase 2 (JAK2)/STAT3 pathway mediates inflammatory signaling in cerulein-stimulated pancreatic acinar cells. PPAR-γ has been implicated in the regulation of inflammatory responses in several cells. In the present study, we investigated the role of PPAR-γ in cerulein-induced activation of JAK2/STAT3 in pancreatic acinar cells...
September 2017: Journal of Cancer Prevention
https://www.readbyqxmd.com/read/28984404/towards-tuneable-retaining-glycosidase-inhibiting-peptides-by-mimicry-of-a-plant-flavonol-warhead
#3
Ryoji Yoshisada, Lieke van Gijzel, Seino A K Jongkees
Retaining glycosidases are an important class of enzymes involved in glycan degradation. In order to better study the role of specific enzymes in deglycosylation processes, and thereby the importance of particular glycosylation patterns, a set of potent inhibitors each specific to a particular glycosidase would be an invaluable toolkit. Towards this goal, we detail here a more in-depth study of a prototypical macrocyclic peptide inhibitor of the model retaining glycosidase human pancreatic α-amylase (HPA)...
October 6, 2017: Chembiochem: a European Journal of Chemical Biology
https://www.readbyqxmd.com/read/28969017/use-of-a-genome-wide-haploid-genetic-screen-to-identify-treatment-predicting-factors-a-proof-of-principle-study-in-pancreatic-cancer
#4
Yuk Ting Ma, Sarah M Leonard, Naheema Gordon, Jennifer Anderton, Claire James, David Huen, Ciaran B Woodman, Daniel H Palmer
The ability to develop a comprehensive panel of treatment predicting factors would significantly improve our ability to stratify patients for cytotoxic or targeted therapies, and prevent patients receiving ineffective treatments. We have investigated if a recently developed genome-wide haploid genetic screen can be used to reveal the critical mediators of response to anticancer therapy. Pancreatic cancer is known to be highly resistant to systemic therapy. Recently epigenetic changes have been shown to be a key determinant in the maintenance of subpopulations of cancer cells with high-level resistance to cytotoxic therapy...
September 8, 2017: Oncotarget
https://www.readbyqxmd.com/read/28963856/dopamine-d2-receptor-signaling-controls-inflammation-in-acute-pancreatitis-via-pp2a-dependent-akt-nf%C3%AE%C2%BAb-signaling-pathway
#5
Xiao Han, Bin Li, Xin Ye, Tunike Mulatibieke, Jianghong Wu, Juanjuan Dai, Deqing Wu, Jianbo Ni, Ruling Zhang, Jing Xue, Rong Wan, Xingpeng Wang, Guoyong Hu
BACKGROUND AND PURPOSE: Dopamine (DA) has multiple anti-inflammatory effects, but its role and molecular mechanism in acute pancreatitis (AP) is unclear. We investigated the role of DA signaling on inflammatory response in AP. EXPERIMENTAL APPROACH: We analyzed the changes of pancreatic dopaminergic system and effects of DA, antagonists and agonists of DA receptor (DRD)1 and 2 in wild-type and pancreas-specific Drd2(-/-) mice with AP (induced by caerulein and lipopolysaccharide or L-Arginine) or in pancreatic acinar cells with or without CCK stimulation...
September 30, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28962872/ucp2-inhibition-induces-ros-akt-mtor-axis-role-of-gapdh-nuclear-translocation-in-genipin-everolimus-anticancer-synergism
#6
Ilaria Dando, Raffaella Pacchiana, Elisa Dalla Pozza, Ivana Cataldo, Stefano Bruno, Paola Conti, Marco Cordani, Anna Grimaldi, Giovanna Butera, Michele Caraglia, Aldo Scarpa, Marta Palmieri, Massimo Donadelli
Several studies indicate that mitochondrial uncoupling protein 2 (UCP2) plays a pivotal role in cancer development by decreasing reactive oxygen species (ROS) produced by mitochondrial metabolism and by sustaining chemoresistance to a plethora of anticancer drugs. Here, we demonstrate that inhibition of UCP2 triggers Akt/mTOR pathway in a ROS-dependent mechanism in pancreatic adenocarcinoma cells. This event reduces the antiproliferative outcome of UCP2 inhibition by genipin, creating the conditions for the synergistic counteraction of cancer cell growth with the mTOR inhibitor everolimus...
September 27, 2017: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/28957862/triglyceride-lowering-trials
#7
Anthony C Keech, Alicia J Jenkins
PURPOSE OF REVIEW: We provide an overview of current evidence about the independent role of high triglyceride levels for cardiovascular risk and for acute pancreatitis. RECENT FINDINGS: Natural experiments of Mendelian randomization have given us a deeper understanding about the molecular pathways involved in triglyceride metabolism. Individuals with low-triglyceride levels generally have lower rates of cardiovascular disease (CVD). There has been a significant growth in the development of new agents that modulate enzymes involved in a variety of aspects of triglyceride packaging into VLDL or chylomicron particles, and triglyceride catabolism...
September 27, 2017: Current Opinion in Lipidology
https://www.readbyqxmd.com/read/28900700/auxiliary-activation-of-the-complement-system-and-its-importance-for-the-pathophysiology-of-clinical-conditions
#8
REVIEW
Markus Huber-Lang, Kristina N Ekdahl, Rebecca Wiegner, Karin Fromell, Bo Nilsson
Activation and regulation of the cascade systems of the blood (the complement system, the coagulation/contact activation/kallikrein system, and the fibrinolytic system) occurs via activation of zymogen molecules to specific active proteolytic enzymes. Despite the fact that the generated proteases are all present together in the blood, under physiological conditions, the activity of the generated proteases is controlled by endogenous protease inhibitors. Consequently, there is remarkable little crosstalk between the different systems in the fluid phase...
September 12, 2017: Seminars in Immunopathology
https://www.readbyqxmd.com/read/28882992/novel-pathways-of-ponatinib-disposition-catalyzed-by-cyp1a1-involving-generation-of-potentially-toxic-metabolites
#9
De Lin, Rumen Kostov, Jeffrey T-J Huang, Colin J Henderson, C Roland Wolf
Ponatinib, a pan-BCR-ABL tyrosine kinase inhibitor for the treatment of chronic myeloid leukemia (CML), causes severe side effects including vascular occlusions, pancreatitis, and liver toxicity, although the underlying mechanisms remain unclear. Modifications of critical proteins through reactive metabolites are thought to be responsible for a number of adverse drug reactions. In vitro metabolite screening of ponatinib with human liver microsomes and glutathione revealed unambiguous signals of ponatinib-glutathione (P-GSH) adducts...
October 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28842394/transforming-growth-factor-%C3%AE-1-activin-receptor-like-kinase-5-mediated-cell-migration-is-dependent-on-the-protein-proteinase-activated-receptor-2-but-not-on-proteinase-activated-receptor-2-stimulated-gq-calcium-signaling
#10
Hendrik Ungefroren, David Witte, Koichiro Mihara, Bernhard H Rauch, Petra Henklein, Olaf Jöhren, Shirin Bonni, Utz Settmacher, Hendrik Lehnert, Morley D Hollenberg, Roland Kaufmann, Frank Gieseler
Transforming growth factor-β (TGF-β), serine proteinases such as trypsin, and proteinase-activated receptor 2 (PAR2) promote tumor development by stimulating invasion and metastasis. Previously, we found that in cancer cells derived from pancreatic ductal adenocarcinoma (PDAC) PAR2 protein is necessary for TGF-β1-dependent cell motility. Here, we show in the same cells that, conversely, the type I TGF-β receptor activin receptor-like kinase 5 is dispensable for trypsin and PAR2 activating peptide (PAR2-AP)-induced migration...
November 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28780468/design-and-synthesis-of-2-6-di-substituted-phenyl-thiazolo-3-2-b-1-2-4-triazoles-as-%C3%AE-glucosidase-and-%C3%AE-amylase-inhibitors-co-relative-pharmacokinetics-and-3d-qsar-and-risk-analysis
#11
Pervaiz Ali Channar, Aamer Saeed, Fayaz Ali Larik, Sajid Rashid, Qaiser Iqbal, Maryam Rozi, Saima Younis, Jamaluddin Mahar
Ten fused heterocyclic derivatives bearing the 2,6-di(subsituted phenyl)thiazolo[3,2-b]-1,2,4-triazoles as central rings were synthesized and structures of the compounds were established by analytical and spectral data using FTIR, EI-MS, (1)H NMR and (13)C NMR techniques. In vitro inhibitory activities of synthesized compounds on α-amylase, α-glucosidase and α-burylcholinesterase (α-BuChE) were evaluated using a purified enzyme assays. Compound 5c demonstrated strong and selective α-amylase inhibitory activity (IC50=1...
October 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28774309/fungal-endophytes-associated-with-viola-odorata-linn-as-bioresource-for-pancreatic-lipase-inhibitors
#12
M Katoch, A Paul, G Singh, S N C Sridhar
BACKGROUND: As per the recent statistical reports of World Health Organisation (WHO), 13% of total global population is obese. Orlistat remains to be the only drug approved for the long term treatment of obesity. Recent findings highlighted severe adverse effects of orlistat that included hepatotoxicity, gall stones, kidney stones and acute pancreatitis. Therefore, search for new drug is required. The investigations based on endophytic natural products would prove pivotal in the global fight against this health issue...
August 3, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28733542/use-of-a-genome-wide-haploid-genetic-screen-to-identify-treatment-predicting-factors-a-proof-of-principle-study-in-pancreatic-cancer
#13
Yuk Ting Ma, Sarah M Leonard, Naheema Gordon, Jennifer Anderton, Claire James, David Huen, Ciaran B Woodman, Daniel H Palmer
The ability to develop a comprehensive panel of treatment predicting factors would significantly improve our ability to stratify patients for cytotoxic or targeted therapies, and prevent patients receiving ineffective treatments. We have investigated if a recently developed genome-wide haploid genetic screen can be used to reveal the critical mediators of response to anticancer therapy. Pancreatic cancer is known to be highly resistant to systemic therapy. Recently epigenetic changes have been shown to be a key determinant in the maintenance of subpopulations of cancer cells with high-level resistance to cytotoxic therapy...
June 29, 2017: Oncotarget
https://www.readbyqxmd.com/read/28733523/preclinical-efficacy-of-the-novel-competitive-nampt-inhibitor-stf-118804-in-pancreatic-cancer
#14
Jair Machado Espindola-Netto, Claudia C S Chini, Mariana Tarragó, Enfeng Wang, Shamit Dutta, Krishnendu Pal, Debabrata Mukhopadhyay, Mauro Sola-Penna, Eduardo N Chini
NAD salvage is one of the pathways used to generate NAD in mammals. Nicotinamide phosphoribosyltransferase (NAMPT), the rate-limiting enzyme in this pathway, uses nicotinamide (NAM) to generate nicotinamide mononucleotide (NMN). NMN is one of the main precursors of NAD synthesis in cells. Our previous study showed the importance of NAMPT in maintaining NAD levels in pancreatic ductal adenocarcinoma cells (PDAC), and that the NAMPT inhibitor FK866 decreased pancreatic cancer growth. We now tested the effect of STF-118804, a new highly specific NAMPT inhibitor, in models of pancreatic ductal adenocarcinoma...
June 29, 2017: Oncotarget
https://www.readbyqxmd.com/read/28720574/fructose-1-6-bisphosphatase-inhibits-erk-activation-and-bypasses-gemcitabine-resistance-in-pancreatic-cancer-by-blocking-iqgap1-mapk-interaction
#15
Xin Jin, Yunqian Pan, Liguo Wang, Tao Ma, Lizhi Zhang, Amy H Tang, Daniel D Billadeau, Heshui Wu, Haojie Huang
Dysregulation of the MAPK pathway correlates with progression of pancreatic ductal adenocarcinoma (PDAC) progression. IQ motif containing GTPase-activating protein 1 (IQGAP1) is a MAPK scaffold that directly regulates the activation of RAF, MEK, and ERK. Fructose-1,6-bisphosphatase (FBP1), a key enzyme in gluconeogenesis, is transcriptionally downregulated in various cancers, including PDAC. Here, we demonstrate that FBP1 acts as a negative modulator of the IQGAP1-MAPK signaling axis in PDAC cells. FBP1 binding to the WW domain of IQGAP1 impeded IQGAP1-dependent ERK1/2 phosphorylation (pERK1/2) in a manner independent of FBP1 enzymatic activity...
August 15, 2017: Cancer Research
https://www.readbyqxmd.com/read/28705641/design-synthesis-biological-evaluation-and-molecular-modelling-studies-of-novel-diaryl-substituted-pyrazolyl-thiazolidinediones-as-potent-pancreatic-lipase-inhibitors
#16
Sridhar S N C, Deendyal Bhurta, Dharmvir Kantiwal, Ginson George, Vikramdeep Monga, Atish T Paul
A series of novel diaryl substituted pyrazolyl 2,4-thiazolidinediones were synthesized via reaction of appropriate pyrazolecarboxaldehydes with 2,4-thiazolidinedione (TZD) and nitrobenzyl substituted 2,4-thiazolidinedione. The resulting compounds were screened in vitro for pancreatic lipase (PL) inhibitory activity. Two assay protocols were performed viz., methods A and B using p-nitrophenyl butyrate and tributyrin as substrates, respectively. Compound 11e exhibited potent PL inhibitory activity (IC50=4.81µM and Xi50=10...
August 15, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28697127/celecoxib-oral-administration-for-prevention-of-post-endoscopic-retrograde-cholangiopancreatography-pancreatitis-a-randomized-prospective-trial
#17
Kunihiro Kato, Masatsugu Shiba, Yuki Kakiya, Hirotsugu Maruyama, Masaki Ominami, Shusei Fukunaga, Satoshi Sugimori, Yasuaki Nagami, Toshio Watanabe, Kazunari Tominaga, Yasuhiro Fujiwara
OBJECTIVES: Rectal nonsteroidal anti-inflammatory drugs have reported promising prophylactic activity in post-endoscopic retrograde cholangiopancreatography (ERCP) pancreatitis (PEP). Conversely, cyclooxygenase-2 enzyme has been suggested to contribute to experimental acute pancreatitis. The aim of this study was to evaluate the efficacy of oral administration of celecoxib, a cyclooxygenase-2 inhibitor, for the prevention of PEP. METHODS: We performed a prospective randomized controlled study...
August 2017: Pancreas
https://www.readbyqxmd.com/read/28685672/micrornas-mediated-mmp-regulation-current-diagnostic-and-therapeutic-strategies-for-metabolic-syndrome
#18
Sharad Saxena, Aditi Jain, Vibha Rani
Metabolic syndrome (MS) is a global socioeconomic problem rapidly progressing in accordance with increasing body mass index (BMI) and age. It is a consortium of risk factors, such as dyslipidaemia, insulin resistance, leptin resistance, reduced adiponectin, glucose intolerance, hyperglycemia, and hypertension. Collectively, these factors accelerate the onset of type 2 diabetes mellitus, cardiovascular disease, stroke, and certain cancers such as breast, liver pancreatic, and colon cancer. Extracellular matrix (ECM) and basement membrane remodeling play a central role during pathogenesis of MS as they regulate diverse cell functions including proliferation, differentiation, and migration...
July 7, 2017: Current Gene Therapy
https://www.readbyqxmd.com/read/28666105/comparison-of-pancreatic-beta-cells-and-alpha-cells-under-hyperglycemia-inverse-coupling-in-pakt-foxo1
#19
Mi-Kyung Kim, Hyun Mi Shin, HyeSook Jung, EunJu Lee, Tae Kyoon Kim, Tae Nyun Kim, Min Jeong Kwon, Soon Hee Lee, Byoung Doo Rhee, Jeong Hyun Park
Type 2 diabetes manifests beta cell deficiencies and alpha cell expansion which is consistent with relative insulin deficiency and glucagon oversecretion. The effects of hyperglycemia on alpha cells are not as understood in comparison to beta cells. Hyperglycemia increases oxidative stress, which induces Akt activation or FoxO activation, depending on cell type. Several studies independently reported that FoxO1 translocations in alpha cells and beta cells were opposite. We compared the responses of pancreatic alpha cells and beta cells against hyperglycemia...
May 19, 2017: Diabetes Research and Clinical Practice
https://www.readbyqxmd.com/read/28604669/structural-and-mechanistic-basis-of-differentiated-inhibitors-of-the-acute-pancreatitis-target-kynurenine-3-monooxygenase
#20
Jonathan P Hutchinson, Paul Rowland, Mark R D Taylor, Erica M Christodoulou, Carl Haslam, Clare I Hobbs, Duncan S Holmes, Paul Homes, John Liddle, Damian J Mole, Iain Uings, Ann L Walker, Scott P Webster, Christopher G Mowat, Chun-Wa Chung
Kynurenine-3-monooxygenase (KMO) is a key FAD-dependent enzyme of tryptophan metabolism. In animal models, KMO inhibition has shown benefit in neurodegenerative diseases such as Huntington's and Alzheimer's. Most recently it has been identified as a target for acute pancreatitis multiple organ dysfunction syndrome (AP-MODS); a devastating inflammatory condition with a mortality rate in excess of 20%. Here we report and dissect the molecular mechanism of action of three classes of KMO inhibitors with differentiated binding modes and kinetics...
June 12, 2017: Nature Communications
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