keyword
MENU ▼
Read by QxMD icon Read
search

Pancreatic enzyme inhibitor

keyword
https://www.readbyqxmd.com/read/29863120/glycogen-synthase-kinase-3%C3%AE-activity-plays-a-key-role-in-the-antitumor-effect-of-nafamostat-mesilate-in-pancreatic-cancer-cells
#1
Koichiro Haruki, Hiroaki Shiba, Yohta Shimada, Yoshihiro Shirai, Ryota Iwase, Yuki Fujiwara, Tadashi Uwagawa, Toya Ohashi, Katsuhiko Yanaga
Pancreatic cancer is often resistant to chemotherapy. We previously showed the efficacy of combination treatment using gemcitabine and nafamostat mesilate (FUT-175) for patients with unresectable pancreatic cancer. However, the mechanisms that affect the sensitivity of FUT-175 are not fully understood. The purpose of the present study was to clarify the mechanism of the sensitivity to FUT-175, with a focus on the activity of glycogen synthase kinase-3β (GSK-3β). In vitro, we assessed sensitivity to FUT-175 in human pancreatic cancer cell lines (PANC-1 and MIAPaCa-2) and difference of signaling in these cells by cell proliferation assay, Western blot analysis and microarray...
January 2018: Annals of gastroenterological surgery
https://www.readbyqxmd.com/read/29800677/manduca-sexta-serpin-12-controls-the-prophenoloxidase-activation-system-in-larval-hemolymph
#2
Fan Yang, Yang Wang, Niranji Sumathipala, Xiaolong Cao, Michael R Kanost, Haobo Jiang
Insect prophenoloxidase activation is coordinated by a serine protease network, which is regulated by serine protease inhibitors of the serpin superfamily. The enzyme system also leads to proteolytic processing of a Spätzle precursor. Binding of Spätzle to a Toll receptor turns on a signaling pathway to induce the synthesis of defense proteins. Previous studies of the tobacco hornworm Manduca sexta have revealed key members of the protease cascade, which generates phenoloxidase for melanogenesis and Spätzle to induce immunity-related genes...
August 2018: Insect Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/29792023/fern-9-11-ene-2%C3%AE-3%C3%AE-diol-action-on-insulin-secretion-in-hyperglycemic-conditions
#3
Allisson Jhonatan Gomes Castro, Luisa Helena Cazarolli, Gabrielle Da Luz, Delsi Altenhofen, Hemily Batista Da Silva, Francieli Kanumfre Carvalho, Moacir Geraldo Pizzolatti, Fátima Rmb Silva
The objective of this study was to investigate the effect and the mechanism of action of fernenediol as insulin secretagogue. Wistar rats were treated with 0.1; 1 and 10 mg/kg fernenediol and then induced hyperglycemia by oral glucose. The glycaemia, insulin, LDH, calcium and hepatic glycogen were analyzed. Considering the intestine and pancreas as targets for the triterpene action, the duodenum was used to verify the influence of fernenediol on intestinal glycosidases. Additionally, pancreatic islets were used for studies of 14 C-deoxyglucose uptake and influx of 45 Ca2+ in hyperglycemic medium with/without fernenediol in the presence/absence of an inhibitor/activator of KATP channels, glibenclamide, diazoxide, nifedipine, calcium chelator (BAPTA- AM) and H-89 and ST the inhibitors of the PKA and PKC enzymes...
May 24, 2018: Biochemistry
https://www.readbyqxmd.com/read/29751319/molecular-modelling-and-synthesis-of-spiroimidazolidine-2-4-diones-with-dual-activities-as-hypoglycemic-agents-and-selective-inhibitors-of-aldose-reductase
#4
Manar G Salem, Yasmine M Abdel Aziz, Marwa Elewa, Hosam A Elshihawy, Mohamed M Said
Novel derivatives of spiroimidazolidinedione were synthesized and evaluated as hypoglycemic agents through binding to sulfonylurea receptor 1 (SUR1) in pancreatic beta-cells. Their selectivity index was calculated against both aldehyde reductase (ALR1) and aldose reductase (ALR2). Aldehyde reductase is a key enzyme in the polyol pathway that is involved in the etiology of the secondary diabetic complications. All structures were confirmed by microanalysis and by IR, 1 H NMR, 13 C NMR and EI-MS spectroscopy...
May 2, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29730302/sabellastarte-magnifica-carboxypetidase-inhibitor-the-first-kunitz-inhibitor-simultaneously-interacting-with-carboxypeptidases-and-serine-proteases
#5
Mey Ling Reytor González, Maday Alonso-Del-Rivero Antigua, Lizbeth Hedstrom, Petr Kuzmič, José Ricardo Pires
Multi-domain inhibitors capable to block the activity of different classes of proteases are not very common in nature. However, these kinds of molecules are attractive systems for biomedical or biotechnological applications, where two or more different targets need to be neutralized. SmCI, the Sabellastarte magnifica Carboxypeptidase Inhibitor, is a tri-domain BPTI-Kunitz inhibitor capable to inhibit serine proteases and A-like metallocarboxypeptidases. The BPTI-Kunitz family of proteins includes voltage gated channel blockers and inhibitors of serine proteases...
May 3, 2018: Biochimie
https://www.readbyqxmd.com/read/29626120/a-new-method-for-tumor-imaging-by-targeting-cancer-associated-fibroblasts
#6
Anastasia Loktev, Thomas Lindner, Walter Mier, Jürgen Debus, Annette Altmann, Dirk Jäger, Frederik Giesel, Clemens Kratochwil, Philippe Barthe, Christian Roumestand, Uwe Haberkorn
The tumor stroma, which accounts for a large part of the tumor mass, represents an attractive target for the delivery of diagnostic and therapeutic compounds. Here, the focus is notably on a subpopulation of stromal cells, known as cancer-associated fibroblasts (CAFs), which are present in more than 90% of epithelial carcinomas including pancreatic, colon and breast cancer. CAFs feature a high expression of fibroblast activation protein (FAP), which is not detectable in adult normal tissue but associated with a poor prognosis in cancer patients...
April 6, 2018: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/29609037/%C3%AE-cyano-4-hydroxycinnamate-impairs-pancreatic-cancer-cells-by-stimulating-the-p38-signaling-pathway
#7
Maria Schönrogge, Hagen Kerndl, Xianbin Zhang, Simone Kumstel, Brigitte Vollmar, Dietmar Zechner
Multiple studies are currently targeting dysregulated cancer cell metabolism with distinct combinations of inhibitors. In this study, we evaluated in pancreatic cancer cells metformin, which blocks oxidative phosphorylation, in combination with α-cyano-4-hydroxycinnamate, which has been reported to inhibit the export of lactate from the cytosol. The combination of metformin with α-cyano-4-hydroxycinnamate had a major inhibitory effect on the migration of 6606PDA cells. Monotherapy with α-cyano-4-hydroxycinnamate and especially the combination with metformin also caused significant inhibition of cell proliferation and induced cell death...
July 2018: Cellular Signalling
https://www.readbyqxmd.com/read/29606349/angiogenin-ribonuclease-5-is-an-egfr-ligand-and-a-serum-biomarker-for-erlotinib-sensitivity-in-pancreatic-cancer
#8
Ying-Nai Wang, Heng-Huan Lee, Chao-Kai Chou, Wen-Hao Yang, Yongkun Wei, Chun-Te Chen, Jun Yao, Jennifer L Hsu, Cihui Zhu, Haoqiang Ying, Yuanqing Ye, Wei-Jan Wang, Seung-Oe Lim, Weiya Xia, How-Wen Ko, Xiuping Liu, Chang-Gong Liu, Xifeng Wu, Huamin Wang, Donghui Li, Laura R Prakash, Matthew H Katz, Yaan Kang, Michael Kim, Jason B Fleming, David Fogelman, Milind Javle, Anirban Maitra, Mien-Chie Hung
Pancreatic ribonuclease (RNase) is a secreted enzyme critical for host defense. We discover an intrinsic RNase function, serving as a ligand for epidermal growth factor receptor (EGFR), a member of receptor tyrosine kinase (RTK), in pancreatic ductal adenocarcinoma (PDAC). The closely related bovine RNase A and human RNase 5 (angiogenin [ANG]) can trigger oncogenic transformation independently of their catalytic activities via direct association with EGFR. Notably, high plasma ANG level in PDAC patients is positively associated with response to EGFR inhibitor erlotinib treatment...
April 9, 2018: Cancer Cell
https://www.readbyqxmd.com/read/29594979/anti-inflammatory-and-antioxidant-effects-of-captopril-compared-to-methylprednisolone-in-l-arginine-induced-acute-pancreatitis
#9
Nahla E El-Ashmawy, Naglaa F Khedr, Hoda A El-Bahrawy, Omnia B Hamada
BACKGROUND: Acute pancreatitis (AP) is an inflammatory disease mediated by damage in acinar cells and pancreatic inflammation with infiltration of leukocytes. The pancreatic renin-angiotensin system may play an important role in the pathogenesis of AP. AIM: The present study aimed to investigate the possible protective role of captopril (CAP), an angiotensin-converting enzyme inhibitor, in attenuating L-arginine-induced AP rat model and to elucidate the underlying molecular mechanisms...
June 2018: Digestive Diseases and Sciences
https://www.readbyqxmd.com/read/29582334/acquired-hemophilia-a-associated-with-autoimmune-pancreatitis-with-serum-igg4-elevation
#10
Taisuke Narazaki, Shojiro Haji, Yasuhiro Nakashima, Yasuhiro Tsukamoto, Mariko Tsuda, Akiko Takamatsu, Hirofumi Ohno, Takamitsu Matsushima, Tomoko Matsumoto, Keiji Nogami, Midori Shima, Motoaki Shiratsuchi, Yoshihiro Ogawa
A case of acquired hemophilia A (AHA) that developed in a patient with autoimmune pancreatitis (AIP) is presented. A 64-year-old woman was diagnosed with AIP in 2007. The symptoms resolved with prednisolone (PSL). Although the dose of PSL was tapered to 7.5 mg/day for maintenance, serum IgG4 levels remained high. She suddenly presented with subcutaneous bleeding in 2015. Her activated partial thromboplastin time was prolonged (80.0 s). A mixing test showed an inhibitor pattern, factor VIII (FVIII) activity was less than 1%, and FVIII inhibitor was 290 BU/mL...
March 26, 2018: International Journal of Hematology
https://www.readbyqxmd.com/read/29575187/culex-pipiens-sperm-motility-is-initiated-by-a-trypsin-like-protease-from-male-accessory-glands
#11
Kimberly Stephens, Richard A Cardullo, Catherine D Thaler
In most animals, sperm are stored in a quiescent state in the male reproductive tract and only initiate motility when released into either the female reproductive tract, or, in the case of broadcast spawners, the external environment. Male accessory gland secretions transferred into the female reproductive tract may provide factors that modulate sperm viability and storage, or aid in sperm competition, as well as activate sperm motility. In several insects, serine proteases have been implicated in activating sperm motility...
March 24, 2018: Molecular Reproduction and Development
https://www.readbyqxmd.com/read/29574296/novel-prodrug-prx-p4-003-selectively-activated-by-gut-enzymes-may-reduce-the-risk-of-iatrogenic-addiction-and-abuse
#12
Sandeep T Patil, Ron H Bihovsky, Steven A Smith, William Z Potter, Valentino J Stella
OBJECTIVES: Prescription stimulants are vulnerable to oral and parenteral abuse. Intravenous forms of abuse may be most detrimental due to an enhanced risk of dependence, overdose, and infectious diseases. Our objective was to discover an orally active prodrug of a stimulant that would not be easily converted to its parent when injected, thus hindering intravenous abuse. METHODS: Following an initial analysis of stimulant structures, the fencamfamine isomer [(-)-FCF; (N-ethyl-3-phenylbicyclo[2...
May 1, 2018: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/29573125/risk-of-dipeptidyl-peptidase-4-dpp-4-inhibitors-on-site-specific-cancer-a-systematic-review-and-meta-analysis
#13
REVIEW
Jetty A Overbeek, Marina Bakker, Amber A W A van der Heijden, Myrthe P P van Herk-Sukel, Ron M C Herings, Giel Nijpels
The long-term impact of dipeptidyl peptidase-4 (DPP-4) inhibition is unknown, and there are concerns about the influence of DPP-4 inhibition on carcinogenesis of the pancreas and thyroid. As DPP-4 is a rather unselective enzyme present in many tissues, we focused on all specific cancer types. PubMed and EMBASE were searched between January 2005 and April 2017 to identify studies comparing DPP-4 inhibitors with either placebo or active drugs on cancer risk. Studies were included if they reported on at least one specific cancer outcome and had a follow-up of at least 1 year after start of drug use...
March 23, 2018: Diabetes/metabolism Research and Reviews
https://www.readbyqxmd.com/read/29520731/individualization-of-irinotecan-treatment-a-review-of-pharmacokinetics-pharmacodynamics-and-pharmacogenetics
#14
REVIEW
Femke M de Man, Andrew K L Goey, Ron H N van Schaik, Ron H J Mathijssen, Sander Bins
Since its clinical introduction in 1998, the topoisomerase I inhibitor irinotecan has been widely used in the treatment of solid tumors, including colorectal, pancreatic, and lung cancer. Irinotecan therapy is characterized by several dose-limiting toxicities and large interindividual pharmacokinetic variability. Irinotecan has a highly complex metabolism, including hydrolyzation by carboxylesterases to its active metabolite SN-38, which is 100- to 1000-fold more active compared with irinotecan itself. Several phase I and II enzymes, including cytochrome P450 (CYP) 3A4 and uridine diphosphate glucuronosyltransferase (UGT) 1A, are involved in the formation of inactive metabolites, making its metabolism prone to environmental and genetic influences...
March 8, 2018: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/29506517/rhaponticum-acaule-l-dc-essential-oil-chemical-composition-in-vitro-antioxidant-and-enzyme-inhibition-properties
#15
Habib Mosbah, Hassiba Chahdoura, Jannet Kammoun, Malek Besbes Hlila, Hanen Louati, Saoussen Hammami, Guido Flamini, Lotfi Achour, Boulbaba Selmi
BACKGROUND: α-glucosidase is a therapeutic target for diabetes mellitus (DM) and α-glucosidase inhibitors play a vital role in the treatments for the disease. Furthermore, xanthine oxidase (XO) is a key enzyme that catalyzes hypoxanthine and xanthine to uric acid which at high levels can lead to hyperuricemia which is an important cause of gout. Pancreatic lipase (PL) secreted into the duodenum plays a key role in the digestion and absorption of fats. For its importance in lipid digestion, PL represents an attractive target for obesity prevention...
March 5, 2018: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/29502987/the-prevalence-of-small-intestinal-bacterial-overgrowth-in-non-surgical-patients-with-chronic-pancreatitis-and-pancreatic-exocrine-insufficiency-pei
#16
Hazel M Ní Chonchubhair, Yasir Bashir, Mark Dobson, Barbara M Ryan, Sinead N Duggan, Kevin C Conlon
BACKGROUND: Small intestinal bacterial overgrowth (SIBO) is a condition characterised by symptoms similar to pancreatic exocrine insufficiency (PEI) in chronic pancreatitis patients. SIBO is thought to complicate chronic pancreatitis in up to 92% of cases; however, studies are heterogeneous and protocols non-standardised. SIBO may be determined by measuring lung air-expiration of either hydrogen or methane which are by-products of small bowel bacterial fermentation of intraluminal substrates such as carbohydrates...
February 24, 2018: Pancreatology: Official Journal of the International Association of Pancreatology (IAP) ... [et Al.]
https://www.readbyqxmd.com/read/29486665/mirtazapine-induced-pancreatitis-a-case-report
#17
Riley D Bowers, Sara M Valanejad, Ashley A Holombo
Acute pancreatitis has numerous etiologies, with the most common including gallstones, alcohol abuse, and medications such as angiotensin-converting enzyme (ACE) inhibitors, statins, and diuretics. Mirtazapine has been associated with increased serum cholesterol and serum triglyceride levels. However, few studies have reported dangerously elevated triglyceride levels resulting in acute pancreatitis. This report discusses a case of mirtazapine-induced pancreatitis in a 46-year-old African American female. The patient presented to the emergency department with pancreatitis, presumably alcohol-induced as with a prior admission, but she denied any recent alcohol use...
January 1, 2018: Journal of Pharmacy Practice
https://www.readbyqxmd.com/read/29463644/the-inositol-requiring-enzyme-1-ire1%C3%AE-rnase-inhibitor-4%C3%A2%C2%B58c-is-also-a-potent-cellular-antioxidant
#18
Stanley M H Chan, Mark P Lowe, Ashton Bernard, Alyson A Miller, Terence P Herbert
Inositol-requiring enzyme 1 alpha (IRE1α) is an endoplasmic reticulum (ER)-transmembrane endonuclease that is activated in response to ER stress as part of the unfolded protein response (UPR). Chronic activation of the UPR has been implicated in the pathogenesis of many common diseases including diabetes, cancer, and neurological pathologies such as Huntington's and Alzheimer's disease. 7-Hydroxy-4-methyl-2-oxo-2H-chromene-8-carbaldehyde (4µ8C) is widely used as a specific inhibitor of IRE1α ribonuclease activity (IC50 of 6...
March 9, 2018: Biochemical Journal
https://www.readbyqxmd.com/read/29462900/next-generation-immunotherapy-for-pancreatic-cancer-dna-vaccination-is-seeking-new-combo-partners
#19
REVIEW
Paola Cappello, Claudia Curcio, Giorgia Mandili, Cecilia Roux, Sara Bulfamante, Francesco Novelli
Pancreatic Ductal Adenocarcinoma (PDA) is an almost incurable radio- and chemo-resistant tumor, and its microenvironment is characterized by a strong desmoplastic reaction associated with a significant infiltration of T regulatory lymphocytes and myeloid-derived suppressor cells (Tregs, MDSC). Investigating immunological targets has identified a number of metabolic and cytoskeletal related molecules, which are typically recognized by circulating antibodies. Among these molecules we have investigated alpha-enolase (ENO1), a glycolytic enzyme that also acts a plasminogen receptor...
February 16, 2018: Cancers
https://www.readbyqxmd.com/read/29451201/tackling-dipeptidyl-peptidase-iv-in-neurological-disorders
#20
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
keyword
keyword
86376
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"