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Pancreatic enzyme inhibitor

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https://www.readbyqxmd.com/read/29451201/tackling-dipeptidyl-peptidase-iv-in-neurological-disorders
#1
REVIEW
Ghaith Al-Badri, Gian Marco Leggio, Giuseppe Musumeci, Rubina Marzagalli, Filippo Drago, Alessandro Castorina
Dipeptidyl peptidase IV (DPP-IV) is a serine protease best known for its role in inactivating glucagon-like peptide-1 (GLP-1), pituitary adenylate cyclase-activating polypeptide (PACAP) and glucose-dependent insulinotropic peptide (GIP), three stimulators of pancreatic insulin secretion with beneficial effects on glucose disposal. Owing to the relationship between DPP-IV and these peptides, inhibition of DPP-IV enzyme activity is considered as an attractive treatment option for diabetic patients. Nonetheless, increasing studies support the idea that DPP-IV might also be involved in the development of neurological disorders with a neuroinflammatory component, potentially through its non-incretin activities on immune cells...
January 2018: Neural Regeneration Research
https://www.readbyqxmd.com/read/29449808/suppressive-effects-of-clerodendrum-volubile-p-beauv-labiatae-methanolic-extract-and-its-fractions-on-type-2-diabetes-and-its-complications
#2
Ochuko L Erukainure, Rahman M Hafizur, Nurul Kabir, M Iqbal Choudhary, Olubunmi Atolani, Priyanka Banerjee, Robert Preissner, Chika I Chukwuma, Aliyu Muhammad, Eric O Amonsou, Md Shahidul Islam
Type 2 diabetes is the most prominent of all diabetes types, contributing to global morbidity and mortality. Availability and cost of treatment with little or no side effect especially in developing countries, remains a huge burden. This has led to the search of affordable alternative therapies especially from medicinal plants. In this study, the antidiabetic effect of the methanolic extract, dichloromethane (DCM), butanol (BuOH) and aqueous fractions of Clerodendrum volubile leaves were investigated in type 2 diabetic rats for their effect on glucose homeostasis, serum insulin level and hepatic biomarkers, lipid profile, pancreatic redox balance and Ca 2+ levels, and β-cell distribution and function...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29423062/drug-induced-ciliogenesis-in-pancreatic-cancer-cells-is-facilitated-by-the-secreted-atp-purinergic-receptor-signaling-pathway
#3
Niamat Ali Khan, Abhishek D Garg, Patrizia Agostinis, Johannes V Swinnen
Malignant transformation of cells is often accompanied by the loss of the primary cilium, a protruding microtubule-based sensory organelle, suggesting that it plays an "onco-suppressive" role. Therefore, restoration of the primary cilium is being explored as a new therapeutic approach to attenuate tumor growth. Recently, several commonly used chemotherapeutic drugs have been identified to induce the primary cilium in pancreatic cancer cells. The mechanisms by which these drugs re-express the cilium remain, however, enigmatic...
January 9, 2018: Oncotarget
https://www.readbyqxmd.com/read/29412816/tissue-expression-of-dpp-iv-in-obesity-diabetes-and-modulatory-effects-on-peptide-regulation-of-insulin-secretion
#4
Aine M McKillop, Claire L Stevenson, Brian M Moran, Yasser H A Abdel-Wahab, Peter R Flatt
Dipeptidyl peptidase type 4 (DPP-4) inhibitors represent an important class of glucose-lowering drug for type 2 diabetes. DPP-4 enzyme activity has been observed to be significantly altered in type 2 diabetes. Here, the role of DPP-4 was examined in a high fat fed (HFF) mouse model of insulin resistance. HFF mice had an increased bodyweight (p < .01), were hyperglycaemic (p < .01) and hyperinsulinaemic (p < .05). Compared to normal diet, HFF mice exhibited increased plasma DPP-4 activity (p < .01)...
February 2018: Peptides
https://www.readbyqxmd.com/read/29402301/sialylation-of-egfr-by-the-st6gal-i-sialyltransferase-promotes-egfr-activation-and-resistance-to-gefitinib-mediated-cell-death
#5
Colleen M Britain, Andrew T Holdbrooks, Joshua C Anderson, Christopher D Willey, Susan L Bellis
BACKGROUND: The ST6Gal-I sialyltransferase is upregulated in numerous cancers, and high expression of this enzyme correlates with poor patient prognosis in various malignancies, including ovarian cancer. Through its sialylation of a select cohort of cell surface receptors, ST6Gal-I modulates cell signaling to promote tumor cell survival. The goal of the present study was to investigate the influence of ST6Gal-I on another important receptor that controls cancer cell behavior, EGFR. Additionally, the effect of ST6Gal-I on cancer cells treated with the common EGFR inhibitor, gefitinib, was evaluated...
February 5, 2018: Journal of Ovarian Research
https://www.readbyqxmd.com/read/29383542/ulinastatin-protects-against-cvb3-induced-acute-viral-myocarditis-through-nrf2-activation
#6
Fangqiang Song, Fanpo Kong, Hongqing Zhang, Yongqin Zhou, Ming Li
Inflammation and oxidative stress are implicated in the pathogenesis of acute viral myocarditis (AVM). Ulinastantin (UTI), an inhibitor of serine protease widely used in treatment of pancreatitis and various inflammatory disorders, displays cardioprotective properties in experimental animals. Although the specific mechanism through which UTI regulates cardiac function is not well explored, evidence suggests that UTI might activate nuclear factor E2-related factor 2 (Nrf2) signaling. In this study, we investigated the role of Nrf2 in mediating UTI's cardioprotection in a mouse model of AVM...
January 30, 2018: Inflammation
https://www.readbyqxmd.com/read/29370723/isolated-immune-related-pancreatic-exocrine-insufficiency-associated-with-pembrolizumab-therapy
#7
Thiru Prasanna, Catriona M McNeil, Theresa Nielsen, David Parkin
We report a case of isolated immune-related pancreatic exocrine insufficiency in a patient treated with pembrolizumab for metastatic melanoma. This patient presented with explosive diarrhea and was treated with high dose corticosteroids for possible immune-related colitis. However, biopsies from colon and duodenum did not show any histological evidence of colitis/enteritis. Serum amylase and lipase were not elevated. There was no evidence of pancreatitis or pancreatic metastases on imaging. Significantly lower fecal elastase test on two occasions confirmed the diagnosis of pancreatic exocrine insufficiency...
March 2018: Immunotherapy
https://www.readbyqxmd.com/read/29328069/inhibition-of-muc1-biosynthesis-via-threonyl-trna-synthetase-suppresses-pancreatic-cancer-cell-migration
#8
Seung Jae Jeong, Jong Hyun Kim, Beom Jin Lim, Ina Yoon, Ji-Ae Song, Hee-Sun Moon, Doyeun Kim, Dong Ki Lee, Sunghoon Kim
Mucin1 (MUC1), a heterodimeric oncoprotein, containing tandem repeat structures with a high proportion of threonine, is aberrantly overexpressed in many human cancers including pancreatic cancer. Since the overall survival rate of pancreatic cancer patients has remained low for several decades, novel therapeutic approaches are highly needed. Intestinal mucin has been known to be affected by dietary threonine supply since de novo synthesis of mucin proteins is sensitive to luminal threonine concentration. However, it is unknown whether biosynthesis of MUC1 is regulated by threonine in human cancers...
January 12, 2018: Experimental & Molecular Medicine
https://www.readbyqxmd.com/read/29324628/ulinastatin-protects-against-lps-induced-acute-lung-injury-by-attenuating-tlr4-nf-%C3%AE%C2%BAb-pathway-activation-and-reducing-inflammatory-mediators
#9
Chao Cao, Chengfen Yin, Songtao Shou, Jun Wang, Lechang Yu, Xuening Li, Yanfen Chai
Acute lung injury (ALI) and its severe form, acute respiratory distress syndrome (ARDS), remain the leading causes of morbidity and mortality in intensive care units. Ulinastatin (UTI), a serine protease inhibitor, possesses anti-inflammatory properties and has been suggested to modulate lipopolysaccharide (LPS)-induced sepsis; thus, it is now widely used in the treatment of pancreatitis, sepsis, and septic shock. Toll-like receptor 4 (TLR4), an essential LPS signaling receptor, plays a critical role in the activation of innate immunity...
January 10, 2018: Shock
https://www.readbyqxmd.com/read/29306066/synthesis-molecular-docking-and-biological-evaluation-of-some-benzimidazole-derivatives-as-potent-pancreatic-lipase-inhibitors
#10
Emre Menteşe, Fatih Yılmaz, Mustafa Emirik, Serdar Ülker, Bahittin Kahveci
In this study, a new series of benzimidazole and bisbenzimidazole derivatives were prepared via the reaction of iminoester hydrochlorides and o-phenylenediamines and then screened for their lipase inhibition properties. Among the synthesized molecules, compounds 7a, 8a and 8c showed the best inhibitory effect against lipase enzyme with IC50 values of 1.72 ± 0.12 µM, 1.92 ± 0.28 and 0.98 ± 0.07 µM, respectively. Moreover, molecular modeling studies were performed in order to understand to the inhibitory activity of the molecules...
December 28, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29303910/involvement-of-nucleotide-binding-and-oligomerization-domain-like-receptors-in-the-intestinal-injury-of-severe-acute-pancreatitis-in-rats
#11
Shan Xu, Shuqing Wei, Yu Guo, Donglai Cui, Jinfeng Yao
OBJECTIVES: The aim of the study was to observe the role of nucleotide-binding and oligomerization domain (NOD)-like receptors (NLR) in intestinal injury of severe acute pancreatitis (SAP) in rats. METHODS: Severe acute pancreatitis was induced by retrograde infusion of sodium taurocholate into the biliopancreatic duct. Rats were divided into the following 6 groups: sham operation, SAP treated with saline, and SAP treated with interleukin 1β (IL-1β)-converting enzyme inhibitor, killed at 6 or 12 hours after operation...
February 2018: Pancreas
https://www.readbyqxmd.com/read/29295482/lipid-metabolism-and-lipid-droplets-in-pancreatic-cancer-and-stellate-cells
#12
REVIEW
Yoshiaki Sunami, Artur Rebelo, Jörg Kleeff
Pancreatic ductal adenocarcinoma (PDAC) is projected to become the second deadliest cancer by 2030, and the overall 5-year survival rate is currently less than 7%. Cancer cells frequently exhibit reprogramming of their metabolic activity. It is increasingly recognized that aberrant de novo lipid synthesis and reprogrammed lipid metabolism are both associated with the development and progression of various cancers, including pancreatic cancer. In this review, the current knowledge about lipid metabolism and lipid droplets in pancreatic cancer is discussed...
December 23, 2017: Cancers
https://www.readbyqxmd.com/read/29285362/dtcapfs-a-derivative-of-a-novel-human-hormone-peptide-induces-apoptosis-in-cancer-cells-through-a-mechanism-involving-loss-of-golgi-function
#13
Joel Ohana, Uziel Sandler, Gideon Kass, Salomon M Stemmer, Yoram Devary
dTCApFs (Nerofe™) is a 14-amino acid derivative of a longer hormone peptide, tumor-cells apoptosis factor (TCApF), which enters the cells through the T1/ST2 receptor. In the present study, the mechanism of action (MOA) of dTCApFs as an anticancer agent was investigated. Experiments were performed in pancreatic cancer cell lines, and immunofluorescent staining demonstrated that dTCApFs is located in the Golgi apparatus of treated cells. It was also demonstrated in pancreatic, breast and ovarian cell lines that dTCApFs treatment led to Golgi structural changes, loss of Golgi function, and molecular effects associated with endoplasmic reticulum (ER) stress, such as increased levels of C/EBP homologous protein, binding immunoglobulin protein (BiP), phosphorylated inositol-requiring enzyme 1 (pIRE1), and increased phosphorylation of eukaryotic translation initiation factor 2α, and to the generation of reactive oxygen species, which was attenuated by ER stress inhibitors...
December 2017: Molecular and Clinical Oncology
https://www.readbyqxmd.com/read/29243753/extracts-from-the-edible-seaweed-ascophyllum-nodosum-inhibit-lipase-activity-in-vitro-contributions-of-phenolic-and-polysaccharide-components
#14
Ceri Austin, Derek Stewart, J William Allwood, Gordon J McDougall
A polyphenol-rich extract (PRE) from the edible seaweed, Ascophyllum nodosum, inhibited pancreatic lipase activity in an oil-based turbidimetric assay with an IC50 of 200 μg gallic acid equivalents (GAE) perassay) [∼230 μg DW] whereas the known inhibitor, Orlistat, gave an IC50 at 0.4 μg per assay. A phlorotannin-enriched fraction (TRF) purified from the PRE was more potent with an IC50 = 60 μg GAE per assay (∼65 μg DW). When the assay was started by the addition of lipase, both Orlistat and TRF were much less effective which suggests that pre-incubation of enzyme and inhibitor improved inhibition...
December 15, 2017: Food & Function
https://www.readbyqxmd.com/read/29237705/cilia-loss-sensitizes-cells-to-transformation-by-activating-the-mevalonate-pathway
#15
Yue-Zhen Deng, Zhen Cai, Shuo Shi, Hao Jiang, Yu-Rong Shang, Ning Ma, Jing-Jing Wang, Dong-Xian Guan, Tian-Wei Chen, Ye-Fei Rong, Zhen-Yu Qian, Er-Bin Zhang, Dan Feng, Quan-Li Zhou, Yi-Nan Du, Dong-Ping Liu, Xing-Xu Huang, Lu-Ming Liu, Eugene Chin, Dang-Sheng Li, Xiao-Fan Wang, Xue-Li Zhang, Dong Xie
Although cilia loss and cell transformation are frequently observed in the early stage of tumorigenesis, the roles of cilia in cell transformation are unknown. In this study, disrupted ciliogenesis was observed in cancer cells and pancreatic cancer tissues, which facilitated oncogene-induced transformation of normal pancreatic cells (HPDE6C7) and NIH3T3 cells through activating the mevalonate (MVA) pathway. Disruption of ciliogenesis up-regulated MVA enzymes through β catenin-T cell factor (TCF) signaling, which synchronized with sterol regulatory element binding transcription factor 2 (SREBP2), and the regulation of MVA by β-catenin-TCF signaling was recapitulated in a mouse model of pancreatic ductal adenocarcinoma (PDAC) and human PDAC samples...
December 13, 2017: Journal of Experimental Medicine
https://www.readbyqxmd.com/read/29224179/antidiabetic-polypill-improves-central-pathology-and-cognitive-impairment-in-a-mixed-model-of-alzheimer-s-disease-and-type-2-diabetes
#16
Carmen Infante-Garcia, Juan Jose Ramos-Rodriguez, Carmen Hierro-Bujalance, Esperanza Ortegon, Eleanor Pickett, Rosemary Jackson, Fernando Hernandez-Pacho, Tara Spires-Jones, Monica Garcia-Alloza
Type 2 diabetes (T2D) is an important risk factor to suffer dementia, being Alzheimer's disease (AD) as the most common form. Both AD and T2D are closely related to aging and with a growing elderly population it might be of relevance to explore new therapeutic approaches that may slow or prevent central complications associated with metabolic disorders. Therefore, we propose the use of the antidiabetic polypill (PP), a pharmacological cocktail, commonly used by T2D patients that include metformin, aspirin, simvastatin, and an angiotensin-converting enzyme inhibitor...
December 9, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/29200824/pharmacodynamic-testing-and-new-validated-hplc-method-to-assess-the-interchangeability-between-multi-source-orlistat-capsules
#17
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
#18
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
#19
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
#20
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
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