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Peptidase inhibitor

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https://www.readbyqxmd.com/read/28087908/-berberine-regulates-glycemia-via-local-inhibition-of-intestinal-dipeptidyl-peptidase-%C3%A2
#1
Jiesheng Wang, Guanhai Dai, Weijia Li
Objective: To investigate the effect of berberine on glycemia regulation in rats with diabetes and the related mechanisms. Methods: Diabetic-like rat model was successfully induced by intraperitoneal injection of streptozotocin in 50 out of 60 male SD rats, which were then randomly divided into 5 groups with 10 rats in each:control group (received vehicle only), positive drug control group (sitagliptin 10 mg·kg(-1)·d(-1)), low-dose berberine group (30 mg·kg(-1)·d(-1)), moderate-dose berberine group (60 mg·kg(-1)·d(-1)), and high-dose berberine group (120 mg·kg(-1)·d(-1))...
May 25, 2016: Zhejiang da Xue Xue Bao. Yi Xue Ban, Journal of Zhejiang University. Medical Sciences
https://www.readbyqxmd.com/read/28086872/dapagliflozin-decreases-small-dense-low-density-lipoprotein-cholesterol-and-increases-high-density-lipoprotein-2-cholesterol-in-patients-with-type-2-diabetes-comparison-with-sitagliptin
#2
Toshiyuki Hayashi, Tomoyasu Fukui, Noriko Nakanishi, Saki Yamamoto, Masako Tomoyasu, Anna Osamura, Makoto Ohara, Takeshi Yamamoto, Yasuki Ito, Tsutomu Hirano
BACKGROUND: The sodium-glucose co-transporter-2 (SGLT-2) inhibitors have been reported to increase both low-density lipoprotein (LDL) and high-density lipoprotein (HDL)-cholesterol (C). This study aimed to determine how SGLT-2 inhibitors affect LDL and HDL-C subspecies. METHODS: This single center, open-label, randomized, prospective study included 80 patients with type 2 diabetes taking prescribed oral hypoglycemic agents. Patients were allocated to receive dapagliflozin (n = 40) or sitagliptin (n = 40) as add-on treatment...
January 13, 2017: Cardiovascular Diabetology
https://www.readbyqxmd.com/read/28078647/sitagliptin-a-review-in-type-2-diabetes
#3
Lesley J Scott
The dipeptidyl peptidase-4 inhibitor sitagliptin (Januvia(®); Glactiv(®); Tesavel(®); Xelevia™) is approved in more than 130 countries worldwide as monotherapy and in combination with other antihyperglycaemic drugs for the treatment of adult patients with type 2 diabetes (T2D). Extensive clinical experience has firmly established the glycaemic efficacy of oral sitagliptin (±other antihyperglycaemic drugs) in a broad spectrum of patients with T2D, including obese, elderly and renally impaired patients and those with established cardiovascular (CV) disease (CVD)...
January 11, 2017: Drugs
https://www.readbyqxmd.com/read/28074857/deubiquitylation-of-hepatitis-b-virus-x-protein-hbx-by-ubiquitin-specific-peptidase-15-usp15-increases-hbx-stability-and-its-transactivation-activity
#4
Zhi-Jun Su, Jia-Shou Cao, Yan-Fang Wu, Wan-Nan Chen, Xinjian Lin, Yun-Li Wu, Xu Lin
Hepatitis B virus X protein (HBx) plays important roles in viral replication and the development of hepatocellular carcinoma. HBx is a rapid turnover protein and ubiquitin-proteasome pathway has been suggested to influence HBx stability as treatment with proteasome inhibitors increases the levels of HBx protein and causes accumulation of the polyubiquitinated forms of HBx. Deubiquitinases (DUBs) are known to act by removing ubiquitin moieties from proteins and thereby reverse their stability and/or activity...
January 11, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28073873/recurrent-angioedema-associated-with-pharmacological-inhibition-of-dipeptidyl-peptidase-iv
#5
Thorbjørn Hermanrud, Anette Bygum, Eva Rye Rasmussen
Angioedema (AE) of the upper airways is a severe and potentially life-threatening condition. The incidence has been increasing in the past two decades, primarily due to increased use of medications inhibiting the degradation of vasoactive peptides. Acquired angioedema related to angiotensin-converting enzyme inhibitors (ACEI-AAE) is well known, but other pharmaceutical agents also affect the degradation of bradykinin and substance P. We present a middle-aged man with recurrent episodes of severe AE of the oral cavity, hypopharynx and larynx due to pharmacological inhibition of dipeptidyl peptidase IV...
January 10, 2017: BMJ Case Reports
https://www.readbyqxmd.com/read/28070831/the-prolyl-oligopeptidase-inhibitor-suam-14746-attenuates-the-proliferation-of-human-breast-cancer-cell-lines-in-vitro
#6
Satoshi Tanaka, Kanayo Suzuki, Minoru Sakaguchi
BACKGROUND: Prolyl oligopeptidase (POP, EC 3.4.1.26) is a serine peptidase that hydrolyzes post-proline peptide bonds in peptides that are <30 amino acids in length. We previously reported that POP inhibition suppressed the growth of NB-1 human neuroblastomas cells and KATO III human gastric cancer cells. POP activity is commonly elevated in many cancers, which includes breast cancer. However, the effect of POP inhibition as a candidate breast cancer therapy is unknown. METHODS: The effects of POP inhibition and knockdown on the proliferation of cultured human estrogen receptor-positive (ER+) MCF7 and T47D, and ER-negative (ER-) MDA-MB-231 breast cancer cell lines and the MCF12A non-tumorigenic epithelial cell line were tested by analyzing their influence on cell proliferation (WST-1 assay), cell viability (trypan blue exclusion assay), and cell cycle arrest (cell cycle analysis, cell cycle regulator proteins expression)...
January 9, 2017: Breast Cancer: the Journal of the Japanese Breast Cancer Society
https://www.readbyqxmd.com/read/28068175/cpg-methylation-signature-predicts-recurrence-in-early-stage-hepatocellular-carcinoma-results-from-a-multicenter-study
#7
Jiliang Qiu, Baogang Peng, Yunqiang Tang, Yeben Qian, Pi Guo, Mengfeng Li, Junhang Luo, Bin Chen, Hui Tang, Canliang Lu, Muyan Cai, Zunfu Ke, Wei He, Yun Zheng, Dan Xie, Binkui Li, Yunfei Yuan
Purpose Early-stage hepatocellular carcinoma (E-HCC) is being diagnosed increasingly, and in one half of diagnosed patients, recurrence will develop. Thus, it is urgent to identify recurrence-related markers. We investigated the effectiveness of CpG methylation in predicting recurrence for patients with E-HCCs. Patients and Methods In total, 576 patients with E-HCC from four independent centers were sorted by three phases. In the discovery phase, 66 tumor samples were analyzed using the Illumina Methylation 450k Beadchip...
January 9, 2017: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
https://www.readbyqxmd.com/read/28065853/sitagliptin-inhibit-human-lymphocytes-proliferation-and-th1-th17-differentiation-in-vitro
#8
Marcelo Maia Pinheiro, Caroline Lais Stoppa, Claudete Justina Valduga, Cristina Eunice Okuyama, Renata Gorjão, Regina Mara Silva Pereira, Susana Nogueira Diniz
Dipeptidyl peptidase-4 (DPP-4) inhibitors are a new class of anti-diabetic agents that are widely used in clinical practice to improve glycemic control in patients with type 2 diabetes. DPP-4 is also known as lymphocyte cell surface protein, CD26, and plays an important role in T-cell immunity. Recent studies suggest that DPP-4 inhibitors improve beta-cell function and attenuate autoimmunity in type 1 diabetic mouse models. To investigate the direct effect of DPP4 in immune response, human peripheral blood mononuclear cells (PBMC) from healthy volunteers were obtained by Ficoll gradient and cultivated in the absence (control) or presence of phytohemagglutinin (PHA), or stimulated with PHA and treated with sitagliptin...
January 5, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28060882/secretion-of-proteases-by-an-opportunistic-fungal-pathogen-scedosporium-aurantiacum
#9
Zhiping Han, Liisa Kautto, Helena Nevalainen
Scedosporium aurantiacum is an opportunistic filamentous fungus increasingly isolated from the sputum of cystic fibrosis patients, and is especially prevalent in Australia. At the moment, very little is known about the infection mechanism of this fungus. Secreted proteases have been shown to contribute to fungal virulence in several studies with other fungi. Here we have compared the profiles of proteases secreted by a clinical isolate Scedosporium aurantiacum (WM 06.482) and an environmental strain (WM 10...
2017: PloS One
https://www.readbyqxmd.com/read/28060721/dppiv-promotes-endometrial-carcinoma-cell-proliferation-invasion-and-tumorigenesis
#10
Xiaoqing Yang, Xinhua Zhang, Rongrong Wu, Qicheng Huang, Yao Jiang, Jianbing Qin, Feng Yao, Guohua Jin, Yuquan Zhang
Dipeptidyl peptidase IV (DPPIV), also known as CD26, is a 110-kDa cell surface glycoprotein expressed in various tissues. DPPIV reportedly plays a direct role in the progression of several human malignancies. DPPIV specific inhibitors are employed as antidiabetics and could potentially be repurposed to enhance anti-tumor immunotherapies. In the present study, we investigated the correlation between DPPIV expression and tumor progression in endometrial carcinoma (EC). DPPIV overexpression altered cell morphology and stimulated cell proliferation, invasion and tumorigenesis in vitro and in vivo...
January 2, 2017: Oncotarget
https://www.readbyqxmd.com/read/28058753/effect-of-gemigliptin-on-glycemic-variability-in-patients-with-type-2-diabetes
#11
Se E Park, Byung W Lee, Jae H Kim, Woo J Lee, Jae H Cho, Chang H Jung, Seung H Lee, Sunghwan Suh, Gwong C Hur, Sung H Kim, Young H Jang, Cheol Y Park
The aim of this study was to evaluate the effect of gemigliptin vs sitagliptin or glimepiride as initial combination therapy with metformin on glycemic variability and to assess the correlation between glycemic variability reduction and the dipeptidyl peptidase-4 (DPP-4) inhibition in patients with type 2 diabetes. This multicenter, randomized, active-controlled, open-label exploratory study included 69 patients with HbA1c >7.5%. Subjects were randomized to receive gemigliptin 50 mg (n = 24), sitagliptin 100 mg (n = 23), or glimepiride 2 mg (n = 22) for 12 weeks...
January 6, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28058750/efficacy-and-safety-of-adding-evogliptin-versus-sitagliptin-in-metformin-treated-patients-with-type-2-diabetes-a-24-week-randomised-controlled-trial-with-open-label-extension
#12
Sang-Mo Hong, Cheol-Young Park, Dong-Min Hwang, Kyung Ah Han, Chang Beom Lee, Choon Hee Chung, Kun-Ho Yoon, Ji-Oh Mok, Kyong Soo Park, Sung-Woo Park
AIMS: This trial consisted of a 24-week multicenter, randomised, double-blind, double-dummy, active-controlled study and a 52-week open label extension study to assess the efficacy and safety of evogliptin, a novel dipeptidyl peptidase-4 inhibitor, compared to sitagliptin in patients with type 2 diabetes who have inadequate glycaemic control with metformin alone. MATERIALS AND METHODS: Adult type 2 diabetes mellitus patients (N = 222) with HbA1c 6.5-11% on stable metformin doses (≥1000 mg/day) were randomised 1:1 to add-on 5 mg evogliptin (N = 112) or 100 mg sitagliptin (N = 110) once daily for 24 weeks...
January 6, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28056431/second-line-initiation-of-insulin-compared-with-dpp-4-inhibitors-after-metformin-monotherapy-is-associated-with-increased-risk-of-all-cause-mortality-cardiovascular-events-and-severe-hypoglycemia
#13
Thomas Nyström, Johan Bodegard, David Nathanson, Marcus Thuresson, Anna Norhammar, Jan W Eriksson
AIMS: The objective of this nationwide study was to compare the risk of all-cause mortality, fatal and nonfatal cardiovascular disease (CVD), and severe hypoglycemia in patients with type 2 diabetes (T2D) on metformin monotherapy treatment starting second-line treatment with either insulin or dipeptidyl peptidase-4 inhibitor (DPP-4i). METHODS: All patients with T2D in Sweden who initiated second-line treatment with insulin or DPP-4i after metformin monotherapy during 2007-2014 identified in the Swedish Prescribed Drug Register were followed for outcome in the Cause of Death and National Patient Registers...
December 19, 2016: Diabetes Research and Clinical Practice
https://www.readbyqxmd.com/read/28056430/the-effects-of-sitagliptin-a-dpp-4-inhibitor-on-cognitive-functions-in-elderly-diabetic-patients-with-or-without-alzheimer-s-disease
#14
Ahmet Turan Isik, Pinar Soysal, Adnan Yay, Cansu Usarel
AIMS: The present study aimed to evaluate effect of sitagliptin, a dipeptidyl peptidase-4 inhibitor (DPP-4I), on cognitive functions in elderly diabetic patients with and without cognitive impairment. METHODS: 253 elderly patients with type 2DM, were enrolled in this prospective and observational study. After comprehensive geriatric assessment, the patients were divided into either sitagliptin or non-sitagliptin group. RESULTS: A total of 205 patients who completed the study (52 with Alzheimer's Disease (AD)) were re-evaluated 6months later...
December 21, 2016: Diabetes Research and Clinical Practice
https://www.readbyqxmd.com/read/28055075/oral-pharmacologic-treatment-of-type-2-diabetes-mellitus-a-clinical-practice-guideline-update-from-the-american-college-of-physicians
#15
Amir Qaseem, Michael J Barry, Linda L Humphrey, Mary Ann Forciea
Description: The American College of Physicians (ACP) developed this guideline to present the evidence and provide clinical recommendations on oral pharmacologic treatment of type 2 diabetes in adults. This guideline serves as an update to the 2012 ACP guideline on the same topic. This guideline is endorsed by the American Academy of Family Physicians. Methods: This guideline is based on a systematic review of randomized, controlled trials and observational studies published through December 2015 on the comparative effectiveness of oral medications for type 2 diabetes...
January 3, 2017: Annals of Internal Medicine
https://www.readbyqxmd.com/read/28039605/pharmacokinetic-characteristics-and-clinical-efficacy-of-an-sglt2-inhibitor-plus-dpp-4-inhibitor-combination-therapy-in-type-2-diabetes
#16
REVIEW
André J Scheen
Type 2 diabetes (T2D) generally requires a combination of several pharmacological approaches to control hyperglycaemia. Combining a sodium-glucose cotransporter type 2 inhibitor (SGLT2I, also known as gliflozin) and a dipeptidyl peptidase-4 inhibitor (DPP-4I, also known as gliptin) appears to be an attractive strategy because of complementary modes of action. This narrative review analyzes the pharmacokinetics and clinical efficacy of different combined therapies with an SGLT2I (canagliflozin, dapagliflozin, empagliflozin, ertugliflozin, ipragliflozin, luseogliflozin, tofogliflozin) and DPP-4I (linagliptin, saxagliptin, sitagliptin, teneligliptin)...
December 30, 2016: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28039172/toward-defining-the-threshold-between-low-and-high-glucose-variability-in-diabetes
#17
Louis Monnier, Claude Colette, Anne Wojtusciszyn, Sylvie Dejager, Eric Renard, Nicolas Molinari, David R Owens
OBJECTIVE: To define the threshold for excess glucose variability (GV), one of the main features of dysglycemia in diabetes. RESEARCH DESIGN AND METHODS: A total of 376 persons with diabetes investigated at the University Hospital of Montpellier (Montpellier, France) underwent continuous glucose monitoring. Participants with type 2 diabetes were divided into several groups-groups 1, 2a, 2b, and 3 (n = 82, 28, 65, and 79, respectively)-according to treatment: 1) diet and/or insulin sensitizers alone; 2) oral therapy including an insulinotropic agent, dipeptidyl peptidase 4 inhibitors (group 2a), or sulfonylureas (group 2b); or 3) insulin...
December 30, 2016: Diabetes Care
https://www.readbyqxmd.com/read/28038943/design-synthesis-and-in-vitro-biological-evaluation-of-oligopeptides-targeting-e-coli-type-i-signal-peptidase-lepb
#18
Maria De Rosa, Lu Lu, Edouard Zamaratski, Natalia Szałaj, Sha Cao, Henrik Wadensten, Lena Lenhammar, Johan Gising, Annette K Roos, Douglas L Huseby, Rolf Larsson, Per E Andrén, Diarmaid Hughes, Peter Brandt, Sherry L Mowbray, Anders Karlén
Type I signal peptidases are potential targets for the development of new antibacterial agents. Here we report finding potent inhibitors of E. coli type I signal peptidase (LepB), by optimizing a previously reported hit compound, decanoyl-PTANA-CHO, through modifications at the N- and C-termini. Good improvements of inhibitory potency were obtained, with IC50s in the low nanomolar range. The best inhibitors also showed good antimicrobial activity, with MICs in the low μg/mL range for several bacterial species...
December 7, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28035985/impact-of-bee-venom-enzymes-on-diseases-and-immune-responses
#19
REVIEW
Md Sakib Hossen, Ummay Mahfuza Shapla, Siew Hua Gan, Md Ibrahim Khalil
Bee venom (BV) is used to treat many diseases and exhibits anti-inflammatory, anti-bacterial, antimutagenic, radioprotective, anti-nociceptive immunity promoting, hepatocyte protective and anti-cancer activity. According to the literature, BV contains several enzymes, including phospholipase A2 (PLA2), phospholipase B, hyaluronidase, acid phosphatase and α-glucosidase. Recent studies have also reported the detection of different classes of enzymes in BV, including esterases, proteases and peptidases, protease inhibitors and other important enzymes involved in carbohydrate metabolism...
December 27, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28029729/combination-treatment-of-dipeptidyl-peptidase-iv-inhibitor-sitagliptin-and-angiotensin-ii-type-1-receptor-blocker-losartan-suppresses-progression-in-a-nondiabetic-rat-model-of-steatohepatitis
#20
Yasushi Okura, Tadashi Namisaki, Kei Moriya, Mitsuteru Kitade, Kosuke Takeda, Kosuke Kaji, Ryuichi Noguchi, Norihisa Nishimura, Kenichiro Seki, Hideto Kawaratani, Hiroaki Takaya, Shinya Sato, Yasuhiko Sawada, Naotaka Shimozato, Masanori Furukawa, Keisuke Nakanishi, Saikawa Soichiro, Takuya Kubo, Kiyoshi Asada, Hitoshi Yoshiji
AIM: Dipeptidyl peptidase-4 (DPP4) inhibitors (DPP4-I) are oral glucose-lowering drugs for type 2 diabetes mellitus. Previously, we demonstrated that DPP4-I (sitagliptin) exerted suppressive effects on experimental liver fibrosis in rats. Blockade of the renin-angiotensin system by angiotensin-II type 1 receptor blocker (ARB: losartan), commonly used in the management of hypertension, has been shown to significantly alleviate hepatic fibrogenesis and carcinogenesis. We aimed to elucidate the effects and possible mechanisms of a sitagliptin + losartan combination on the progression of nondiabetic nonalcoholic steatohepatitis (NASH) in a rat model...
December 28, 2016: Hepatology Research: the Official Journal of the Japan Society of Hepatology
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