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Pancreatic enzyme inhibitor

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https://www.readbyqxmd.com/read/29200824/pharmacodynamic-testing-and-new-validated-hplc-method-to-assess-the-interchangeability-between-multi-source-orlistat-capsules
#1
Abdel Naser Zaid, Nihal Zohud, Bushra E'layan, Tasneem Aburadi, Nidal Jaradat, Iyad Ali, Fatima Hussein, Mashhour Ghanem, Aiman Qaddomi, Yara Abu Zaaror
Background: Orlistat is an irreversible inhibitor of the lipase enzyme that prevents trigylcerides from being digested, thereby inhibiting triglyceride hydrolysis and absorption. The resultant reduced calorie uptake enables a positive effect on weight control. Systemic absorption of the drug is, therefore, not necessary for its mode of action. An alternative in vitro study (pharmacodynamic) has been introduced for this drug, as in vivo bioavailability studies are irrelevant with regard to the achievement of the product's intended purposes...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29187880/the-parp-1-inhibitor-olaparib-suppresses-brca1-protein-levels-increases-apoptosis-and-causes-radiation-hypersensitivity-in-brca1-lymphoblastoid-cells
#2
Emma C Bourton, Pia-Amata Ahorner, Piers N Plowman, Sheba Adam Zahir, Hussein Al-Ali, Christopher N Parris
The use of polyADPribose polymerase inhibitors in cancer treatment provides a unique opportunity to target DNA repair processes in cancer cells while leaving normal tissue intact. The PARP-1 enzyme repairs DNA single strand breaks (SSB). Therefore PARP-1 inhibition in BRCA1 negative cancers results in the formation of cytotoxic DNA double strand breaks (DSB) causing synthetic lethality. The use of PARP1 inhibitors is gaining momentum in the treatment of a variety of tumours with BRCA1 involvement including breast, ovarian, pancreatic and prostate cancer...
2017: Journal of Cancer
https://www.readbyqxmd.com/read/29184702/pharmacological-inhibition-of-diacylglycerol-acyltransferase-1-and-insights-into-postprandial-gut-peptide-secretion
#3
Benjamin S Maciejewski, Tara B Manion, Claire M Steppan
AIM: To examine the role that enzyme Acyl-CoA:diacylglycerol acyltransferase-1 (DGAT1) plays in postprandial gut peptide secretion and signaling. METHODS: The standard experimental paradigm utilized to evaluate the incretin response was a lipid challenge. Following a lipid challenge, plasma was collected via cardiac puncture at each time point from a cohort of 5-8 mice per group from baseline at time zero to 10 h. Incretin hormones [glucagon like peptide-1 (GLP-1), peptide tyrosine-tyrosine (PYY) and glucose dependent insulinotropic polypeptide (GIP)] were then quantitated...
November 15, 2017: World Journal of Gastrointestinal Pathophysiology
https://www.readbyqxmd.com/read/29180466/synthetic-lethality-of-parp-inhibitors-in-combination-with-myc-blockade-is-independent-of-brca-status-in-triple-negative-breast-cancer
#4
Jason Pw Carey, Cansu Karakas, Tuyen Bui, Xian Chen, Smruthi Vijayaraghavan, Yang Zhao, Jing Wang, Keith Mikule, Jennifer K Litton, Kelly K Hunt, Khandan Keyomarsi
PARP inhibitors (PARPi) benefit only a fraction of breast cancer patients. Several of those patients exhibit intrinsic/acquired resistance mechanisms that limit efficacy of PARPi monotherapy. Here we show how the efficacy of PARPi in triple-negative breast cancers (TNBC) can be expanded by targeting MYC-induced oncogenic addiction. In BRCA-mutant/sporadic TNBC patients, amplification of the MYC gene is correlated with increased expression of the homologous DNA recombination enzyme RAD51 and tumors overexpressing both genes are associated with worse overall survival...
November 27, 2017: Cancer Research
https://www.readbyqxmd.com/read/29180353/clec16a-nrdp1-and-usp8-form-a-ubiquitin-dependent-tripartite-complex-that-regulates-beta-cell-mitophagy
#5
Gemma Pearson, Biaoxin Chai, Tracy Vozheiko, Xueying Liu, Malathi Kandarpa, Robert C Piper, Scott A Soleimanpour
Mitophagy is a cellular quality control pathway, which is essential to eliminate unhealthy mitochondria. While mitophagy is critical to pancreatic β-cell function, the post-translational signals governing β-cell mitochondrial turnover are unknown. Here we report that ubiquitination is essential for the assembly of a mitophagy regulatory complex, comprised of the E3 ligase Nrdp1, the deubiquitinase enzyme USP8, and Clec16a, a mediator of β-cell mitophagy with unclear function. We discover that the diabetes gene Clec16a encodes an E3 ligase, which promotes non-degradative ubiquitin conjugates to direct its mitophagy effectors and stabilize the Clec16a-Nrdp1-USP8 complex...
November 27, 2017: Diabetes
https://www.readbyqxmd.com/read/29176494/pancreatic-enzyme-replacement-therapy-use-in-infants-with-cystic-fibrosis-diagnosed-by-newborn-screening
#6
Daniel Gelfond, Sonya L Heltshe, Michelle Skalland, James E Heubi, Margaret Kloster, Daniel H Leung, Bonnie W Ramsey, Drucy Borowitz
OBJECTIVES: To describe pancreatic enzyme practices during the first year of life in infants with cystic fibrosis (CF) and evaluate associations between dosing and outcomes, including growth and gastrointestinal symptoms. METHODS: We analyzed data from a subset of infants who were in a prospective cohort study conducted at 28 US CF centers. Anthropometric measurements and medications were recorded at each visit. Diaries with infant diet, pancreatic enzyme replacement therapy (PERT) dosing, stool frequency and consistency and pain were completed by a parent/guardian for three days prior to each visit...
November 15, 2017: Journal of Pediatric Gastroenterology and Nutrition
https://www.readbyqxmd.com/read/29158292/sphingomyelin-metabolism-is-a-regulator-of-kras-function
#7
Dharini van der Hoeven, Kwang-Jin Cho, Yong Zhou, Xiaoping Ma, Wei Chen, Ali Naji, Dina Montufar-Solis, Yan Zuo, Sarah E Kovar, Kandice R Levental, Jeffrey A Frost, Ransome van der Hoeven, John F Hancock
KRAS must localize to the plasma membrane (PM) for biological activity. We show here that multiple acid sphingomyelinase (ASM) inhibitors, including tricyclic antidepressants, mislocalized phosphatidylserine (PtdSer) and KRASG12V from the PM; resulting in abrogation of KRASG12V signaling and potent, selective growth inhibition of mutant KRAS transformed cancer cells. Concordantly, in nude mice, the ASM inhibitor fendiline decreased the rate of growth of oncogenic KRAS-expressing MiaPaCa-2 tumors, but had no effect on the growth of the wild-type KRAS-expressing BxPC-3 tumors...
November 20, 2017: Molecular and Cellular Biology
https://www.readbyqxmd.com/read/29157102/chk1-inhibitor-sch-900776-enhances-the-antitumor-activity-of-mln4924-on-pancreatic-cancer
#8
Jian-Ang Li, Chao Song, Yefei Rong, Tiantao Kuang, Dansong Wang, Xuefeng Xu, Jian Yuan, Kuntian Luo, Bo Qin, Somaira Nowsheen, Zhenkun Lou, Wenhui Lou
MLN4924 inhibits the cullin-RING ligases mediated ubiquitin-proteasome system, and has showed antitumor activities in preclinical studies, but its effects and mechanisms on pancreatic cancer (PC) remains elusive. We found that MLN4924 inhibited the proliferation and clonogenicity of PC cells, caused DNA damage, particularly double-strand breaks, and leaded to Chk1 activation and cell-cycle arrest. Chk1 inhibitor SCH 900776 alone exhibited minimal cytotoxicity, and caused no DNA damage on PC cells. But in the combination therapy, SCH 900776 enhanced the cytotoxicity and DNA damage caused by MLN4924, likely by abrogating G2/M arrest and promoting DNA re-replication...
November 20, 2017: Cell Cycle
https://www.readbyqxmd.com/read/29156703/preclinical-efficacy-of-the-novel-competitive-nampt-inhibitor-stf-118804-in-pancreatic-cancer
#9
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...
October 17, 2017: Oncotarget
https://www.readbyqxmd.com/read/29147551/development-of-proteolytically-stable-n-methylated-peptide-inhibitors-of-aggregation-of-the-amylin-peptide-implicated-in-type-2-diabetes
#10
Idira Obasse, Mark Taylor, Nigel J Fullwood, David Allsop
Islet amyloid polypeptide, also known as amylin, is the main component of the amyloid deposits present in approximately 90% of people with type 2 diabetes mellitus (T2DM). In this disease, amylin aggregates into multimeric β-pleated sheet structures which cause damage to pancreatic islet β-cells. Inhibitors of early-stage amylin aggregation could therefore provide a disease-modifying treatment for T2DM. In this study, overlapping peptides were designed to target the 'binding' region (RLANFLVHSS, residues 11-20) of human amylin, and their effects on amyloid fibril formation were determined by thioflavin-T assay...
December 6, 2017: Interface Focus
https://www.readbyqxmd.com/read/29138810/angiotensin-converting-enzyme-2-angiotensin-1-7-mas-axis-prevents-pancreatic-acinar-cell-inflammatory-response-via-inhibition-of-the-p38-mitogen-activated-protein-kinase-nuclear-factor-%C3%AE%C2%BAb-pathway
#11
Xiaozheng Yu, Lijian Cui, Fei Hou, Xiaoya Liu, Yan Wang, Yan Wen, Cheng Chi, Chunyun Li, Ruixia Liu, Chenghong Yin
The aim of the present study was to investigate the role of the angiotensin-converting enzyme (ACE)2-angiotensin‑(Ang)-(1-7)-Mas axis in the pathogenesis of pancreatitis and the association between this axis and the p38 mitogen-activated protein kinase (p38 MAPK)/nuclear factor (NF-κB) signaling pathway in pancreatic acinar cells. Mouse pancreatic acinar cancer (MPC-83) cells were stimulated with 10 nM caerulein (CAE) to create an in vitro model of acute pancreatitis, and collected for analysis at 2, 6, 12, 24 and 48 h post stimulation...
November 13, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/29119617/computer-aided-design-of-human-sialyltransferase-inhibitors-of-hst8sia-iii
#12
Christopher Dobie, Andrew P Montgomery, Rémi Szabo, Danielle Skropeta, Haibo Yu
Sialyltransferase (ST) upregulation and the resultant hypersialylation of tumour cell surfaces is an established hallmark of many cancers including lung, breast, ovarian, pancreatic and prostate cancer. The role of ST enzymes in tumour cell growth and metastasis, as well as links to multi-drug resistance, has seen ST inhibition emerge as a target for potential antimetastatic cancer treatments. The most potent of these reported inhibitors are transition-state analogues. Although there are several examples of these in the literature, many have suspected poor pharmacokinetic properties and are not readily synthetically accessible...
November 9, 2017: Journal of Molecular Recognition: JMR
https://www.readbyqxmd.com/read/29099132/development-of-an-alphalisa-high-throughput-technique-to-screen-for-small-molecule-inhibitors-targeting-protein-arginine-methyltransferases
#13
Lakshmi Prabhu, Lan Chen, Han Wei, Özlem Demir, Ahmad Safa, Lifan Zeng, Rommie E Amaro, Bert H O'Neil, Zhon-Yin Zhang, Tao Lu
The protein arginine methyltransferase (PRMT) family of enzymes comprises nine family members in mammals. They catalyze arginine methylation, either monomethylation or symmetric/asymmetric dimethylation of histone and non-histone proteins. PRMT methylation of its substrate proteins modulates cellular processes such as signal transduction, transcription, and mRNA splicing. Recent studies have linked overexpression of PRMT5, a member of the PRMT superfamily, to oncogenesis, making it a potential target for cancer therapy...
November 21, 2017: Molecular BioSystems
https://www.readbyqxmd.com/read/29066484/aminoguanidine-ag-induces-induced-both-pro-and-antioxidant-effect-in-ar42j-cells-a-rat-pancreatic-tumor-cell-line
#14
Parimal Chowdhury
Aminoguanidine (AG), a diamine oxidase and a nitric oxide synthase inhibitor, was used in diabetes, thyroid follicular carcinoma, hepatocellular carcinoma, pancreatic cancer xenografts and in breast cancer research. The effects of AG on these pathologic conditions may be related to its regulatory effects on cell proliferation, angiogenesis, and expression of antioxidant enzymes. However, its role as pro and/or anti-oxidant affecting signaling and function in pancreatic tumor cell lines has not been studied...
September 2017: Annals of Clinical and Laboratory Science
https://www.readbyqxmd.com/read/29037686/identification-and-biological-activities-of-carotenoids-from-the-freshwater-alga-oedogonium-intermedium
#15
Na Wang, Yuki Manabe, Tatsuya Sugawara, Nicholas A Paul, Jian Zhao
The chemical and biological properties of carotenoids in the freshwater alga Oedogonium intermedium were investigated in this study. Carotenoids were extracted from the alga by dichloromethane and purified by saponification. The carotenoid content was determined both spectrometrically and by HPLC, the carotenoids identified by HPLC-PDA-APCI-IT-TOF-MS and the extracts analysed for several health-related bioactivities. The crude and saponified extracts contained 3,411.2±20.7 and 2,929.6±5.9µg carotenoids/g dry algal biomass, respectively...
March 1, 2018: Food Chemistry
https://www.readbyqxmd.com/read/29026467/chromogranin-a-as-a-biochemical-marker-for-neuroendocrine-tumors-a-single-center-experience-at-royal-hospital-oman
#16
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
#17
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
#18
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
#19
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
#20
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
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