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Pancreatic enzyme inhibitor

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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
#1
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...
August 3, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28774309/fungal-endophytes-associated-with-viola-odorata-linn-as-bioresource-for-pancreatic-lipase-inhibitors
#2
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
#3
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
#4
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
#5
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
#6
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...
June 28, 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
#7
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
#8
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
#9
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
#10
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
https://www.readbyqxmd.com/read/28589038/inhibition-of-%C3%AE-amylases-by-condensed-and-hydrolysable-tannins-focus-on-kinetics-and-hypoglycemic-actions
#11
Camila Gabriel Kato, Geferson de Almeida Gonçalves, Rosely Aparecida Peralta, Flavio Augusto Vicente Seixas, Anacharis Babeto de Sá-Nakanishi, Lívia Bracht, Jurandir Fernando Comar, Adelar Bracht, Rosane Marina Peralta
The aim of the present study was to compare the in vitro inhibitory effects on the salivary and pancreatic α-amylases and the in vivo hypoglycemic actions of the hydrolysable tannin from Chinese natural gall and the condensed tannin from Acacia mearnsii. The human salivary α-amylase was more strongly inhibited by the hydrolysable than by the condensed tannin, with the concentrations for 50% inhibition (IC50) being 47.0 and 285.4 μM, respectively. The inhibitory capacities of both tannins on the pancreatic α-amylase were also different, with IC50 values being 141...
2017: Enzyme Research
https://www.readbyqxmd.com/read/28583846/epigenetic-effects-of-inhibition-of-heat-shock-protein-90-hsp90-in-human-pancreatic-and-colon-cancer
#12
Ganji Purnachandra Nagaraju, Christina Wu, Neha Merchant, Zhengjia Chen, Gregory B Lesinski, Bassel F El-Rayes
Silencing of tumor suppressor and DNA repair genes through methylation plays a role in cancer development, growth and response to therapy in colorectal and pancreatic cancers. Heat shock protein 90 (HSP90) regulates transcription of DNA methyltransferase enzymes (DNMT). In addition, DNMTs are client proteins of HSP90. The aim of this study is to evaluate the effects of HSP90 inhibition on DNA methylation in colorectal and pancreatic cancer cell lines. Our data shows that inhibition of HSP90 using ganetespib resulted in downregulation of mRNA and protein expression of DNMT1, DNMT3A, and DNMT3B in HT-29 and MIA PaCa-2 cell lines...
June 3, 2017: Cancer Letters
https://www.readbyqxmd.com/read/28583043/intracranial-stenting-for-nilotinib-treatment-associated-cerebrovascular-stenosis-in-chronic-myeloid-leukemia
#13
Tomohiko Ozaki, Hajime Nakamura, Nobuyuki Izutsu, Hiroaki Masaie, Jun Ishikawa, Manabu Kinoshita
One of the second-generation tyrosine kinase inhibitors (TKIs), nilotinib, is increasingly used for imatinib-resistant or intolerant chronic myeloid leukemia (CML). Nilotinib is considered well tolerated with few side effects including hyperglycemia, hyperbilirubinemia and elevated levels of pancreatic enzymes. However, there is growing evidence that nilotinib accelerates atherosclerosis and causes peripheral arterial occlusive disease such as stroke, transient ischemic attack (TIA) and cardiovascular diseases...
January 1, 2017: Interventional Neuroradiology
https://www.readbyqxmd.com/read/28576633/design-synthesis-and-biological-evaluation-of-sulfonamide-substituted-diphenylpyrimidine-derivatives-sul-dppys-as-potent-focal-adhesion-kinase-fak-inhibitors-with-antitumor-activity
#14
Menghua Qu, Zhihao Liu, Dan Zhao, Changyuan Wang, Jianbin Zhang, Zeyao Tang, Kexin Liu, Xiaohong Shu, Hong Yuan, Xiaodong Ma
A class of sulfonamide-substituted diphenylpyrimidines (Sul-DPPYs) were synthesized to improve activity against the focal adhesion kinase (FAK). Most of these new Sul-DPPYs displayed moderate activity against the FAK enzyme with IC50 values of less than 100nM; regardless, they could effectively inhibit several classes of refractory cancer cell lines with IC50 values of less than 10µM, including the pancreatic cancer cell lines (AsPC-1, Panc-1 and BxPC-3), the NSCLC-resistant H1975 cell line, and the B lymphocyte cell line (Ramos cells)...
May 20, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28539721/phytochemical-and-biological-evaluations-of-arum-hygrophilum-boiss-araceae
#15
Fatma U Afifi, Violet Kasabri, Simona Litescu, Ismail F Abaza, Khalid Tawaha
BACKGROUND: Arum hygrophilum is a traditional medicinal plant indigenous to Jordan. The present study explores its phytochemistry, antioxidative, antidiabesity, and antiproliferative potentialities. MATERIALS AND METHODS: Column chromatography and HPLC-MS analysis were used for its phytochemical evaluation. Using leaf crude water and ethanol extracts, the antioxidative capacities, their modulation of pancreatic β-cell proliferation, and insulin secretion as well as glucose diffusion and enzymatic bioassays were evaluated...
April 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28507103/nicotinic-acid-phosphoribosyltransferase-regulates-cancer-cell-metabolism-susceptibility-to-nampt-inhibitors-and-dna-repair
#16
Francesco Piacente, Irene Caffa, Silvia Ravera, Giovanna Sociali, Mario Passalacqua, Valerio G Vellone, Pamela Becherini, Daniele Reverberi, Fiammetta Monacelli, Alberto Ballestrero, Patrizio Odetti, Antonia Cagnetta, Michele Cea, Aimable Nahimana, Michel Duchosal, Santina Bruzzone, Alessio Nencioni
In the last decade, substantial efforts have been made to identify NAD(+) biosynthesis inhibitors, specifically against nicotinamide phosphoribosyltransferase (NAMPT), as preclinical studies indicate their potential efficacy as cancer drugs. However, the clinical activity of NAMPT inhibitors has proven limited, suggesting that alternative NAD(+) production routes exploited by tumors confer resistance. Here, we show the gene encoding nicotinic acid phosphoribosyltransferase (NAPRT), a second NAD(+)-producing enzyme, is amplified and overexpressed in a subset of common types of cancer, including ovarian cancer, where NAPRT expression correlates with a BRCAness gene expression signature...
May 15, 2017: Cancer Research
https://www.readbyqxmd.com/read/28500236/identification-of-the-serine-biosynthesis-pathway-as-a-critical-component-of-braf-inhibitor-resistance-of-melanoma-pancreatic-and-non-small-cell-lung-cancer-cells
#17
Kayleigh C Ross, Andrew J Andrews, Christopher D Marion, Timothy J Yen, Vikram Bhattacharjee
Metastatic melanoma cells commonly acquire resistance to BRAF V600E inhibitors (BRAFi). In this study, we identified serine biosynthesis as a critical mechanism of resistance. Proteomic assays revealed differential protein expression of serine biosynthetic enzymes PHGDH, PSPH, and PSAT1 following vemurafenib (BRAFi) treatment in sensitive versus acquired resistant melanoma cells. Ablation of PHGDH via siRNA sensitized acquired resistant cells to vemurafenib. Inhibiting the folate cycle, directly downstream of serine synthesis, with methotrexate also displayed similar sensitization...
August 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28496472/synthesis-and-biological-evaluation-of-n-5-pyridin-2-yl-1-3-4-thiadiazol-2-yl-benzamide-derivatives-as-lipoxygenase-inhibitor-with-potential-anticancer-activity
#18
Alireza Aliabadi, Ahmad Mohammadi-Farani, Sahar Roodabeh, Farahnaz Ahmadi
In the recent years, the role of LOX enzymes in the origin of neoplastic diseases such as colorectal, skin, pancreatic and renal cancers has been confirmed. A new series of 1,3,4-thiadiazole derivatives bearing 2-pyridyl moiety was synthesized and the cytotoxicity of the members of this series was assessed using MTT protocol. Enzyme inhibitory activity of the prepared compounds was also tested against 15-lipoxygenase-1 as a novel target for the discovery of anticancer drugs. PC3, HT29 and SKNMC cell lines were utilized and the obtained results were compared with doxorubicin...
2017: Iranian Journal of Pharmaceutical Research: IJPR
https://www.readbyqxmd.com/read/28486485/hydrogen-peroxide-inhibition-of-bicupin-oxalate-oxidase
#19
John M Goodwin, Hassan Rana, Joan Ndungu, Gaurab Chakrabarti, Ellen W Moomaw
Oxalate oxidase is a manganese containing enzyme that catalyzes the oxidation of oxalate to carbon dioxide in a reaction that is coupled with the reduction of oxygen to hydrogen peroxide. Oxalate oxidase from Ceriporiopsis subvermispora (CsOxOx) is the first fungal and bicupin enzyme identified that catalyzes this reaction. Potential applications of oxalate oxidase for use in pancreatic cancer treatment, to prevent scaling in paper pulping, and in biofuel cells have highlighted the need to understand the extent of the hydrogen peroxide inhibition of the CsOxOx catalyzed oxidation of oxalate...
2017: PloS One
https://www.readbyqxmd.com/read/28450863/the-proteasome-inhibitor-bortezomib-controls-indoleamine-2-3-dioxygenase-1-breakdown-and-restores-immune-regulation-in-autoimmune-diabetes
#20
Giada Mondanelli, Elisa Albini, Maria T Pallotta, Claudia Volpi, Lucienne Chatenoud, Chantal Kuhn, Francesca Fallarino, Davide Matino, Maria L Belladonna, Roberta Bianchi, Carmine Vacca, Silvio Bicciato, Louis Boon, Giovanni Ricci, Ursula Grohmann, Paolo Puccetti, Ciriana Orabona
Bortezomib (BTZ) is a first-in-class proteasome inhibitor approved for the therapy of multiple myeloma that also displays unique regulatory activities on immune cells. The enzyme indoleamine 2,3-dioxygenase 1 (IDO1) is a tryptophan metabolizing enzyme exerting potent immunoregulatory effects when expressed in dendritic cells (DCs), the most potent antigen-presenting cells capable of promoting either immunity or tolerance. We previously demonstrated that, in inflammatory conditions, IDO1 is subjected to proteasomal degradation in DCs, turning these cells from immunoregulatory to immunostimulatory...
2017: Frontiers in Immunology
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