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Peptidase inhibitor

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https://www.readbyqxmd.com/read/29331088/significance-of-circulatory-dpp4-activity-in-metabolic-diseases
#1
REVIEW
Titli Nargis, Partha Chakrabarti
Dipeptidyl peptidase 4 (DPP4), also known as CD26 is a type II transmembrane protein that is released from the cell membrane in a nonclassical secretory mechanism. This exopeptidase selectively degrades varieties of substrates including incretin hormones, growth factors, and cytokines. A significant detectable amount of DPP4 activity can be measured in plasma as well as in different tissues such as intestinal epithelium, vascular endothelium, lymphocytes, monocytes, kidney, liver, adipose, lung, thymus, spleen, prostate, etc...
January 13, 2018: IUBMB Life
https://www.readbyqxmd.com/read/29330812/evaluation-of-the-effect-of-alogliptin-on-tissue-characteristics-of-the-carotid-wall-subanalysis-of-the-spead-a-trial
#2
Yoko Irie, Naoto Katakami, Tomoya Mita, Mitsuyoshi Takahara, Taka-Aki Matsuoka, Masahiko Gosho, Hirotaka Watada, Iichiro Shimomura
INTRODUCTION: Ultrasonic tissue characterization of the carotid wall using gray-scale median (GSM) reflects its composition and low-GSM plaque is considered to be unstable. The present study evaluated the effect of alogliptin, a dipeptidyl peptidase-4 inhibitor, on the longitudinal change in GSM, an index of the tissue characteristics of the carotid wall, in patients with type 2 diabetes (T2DM). METHODS: This is a post hoc subanalysis using data obtained from the SPEAD-A trial, a randomized controlled trial that demonstrated the beneficial effect of alogliptin treatment on the progression of carotid intima-media thickness in patients with T2DM with no past history of apparent cardiovascular disease...
January 12, 2018: Diabetes Therapy: Research, Treatment and Education of Diabetes and related Disorders
https://www.readbyqxmd.com/read/29327406/short-and-medium-term-efficacy-of-sodium-glucose-co-transporter-2-sglt-2-inhibitors-a-meta-analysis-of-randomized-clinical-trials
#3
Matteo Monami, Francesco Liistro, Alessia Scatena, Besmir Nreu, Edoardo Mannucci
AIMS: Sodium glucose co-transport-2 (SGLT-2) inhibitors reduce tubular glucose reabsorption, producing a reduction of blood glucose without stimulating insulin release. Aim of this meta-analysis is the systematic collection of available data from randomized trials, in order to establish the durability of the efficacy of SGLT-2 inhibitors on glycemic control and body mass index. METHODS: A meta-analysis was performed including all trials with a duration of at least 12 weeks, comparing SGLT-2 inhibitors with a non-SGLT-2 inhibitor agents in type 2 diabetes...
January 12, 2018: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/29322651/antifungal-dipeptides-incorporating-an-inhibitor-of-homoserine-dehydrogenase
#4
Andrzej S Skwarecki, Marta Schielmann, Dorota Martynow, Marcin Kawczyński, Aleksandra Wiśniewska, Maria J Milewska, Sławomir Milewski
The antifungal activity of 5-hydroxy-4-oxo-l-norvaline (HONV), exhibited under conditions mimicking human serum, may be improved upon incorporation of this amino acid into a dipeptide structure. Several HONV-containing dipeptides inhibited growth of human pathogenic yeasts of the Candida genus in the RPMI-1640 medium, with minimal inhibitory concentration values in the 32 to 64 μg mL-1 range. This activity was not affected by multidrug resistance that is caused by overexpression of genes encoding drug efflux proteins...
January 2018: Journal of Peptide Science: An Official Publication of the European Peptide Society
https://www.readbyqxmd.com/read/29322610/safety-and-efficacy-of-once-weekly-semaglutide-versus-additional-oral-antidiabetic-drugs-in-japanese-subjects-with-inadequately-controlled-t2d-a-randomised-trial
#5
Kohei Kaku, Yuichiro Yamada, Hirotaka Watada, Atsuko Abiko, Tomoyuki Nishida, Jeppe Zacho, Arihiro Kiyosue
AIMS: Semaglutide is a glucagon-like peptide 1 analogue in development for type 2 diabetes (T2D). Safety and efficacy of once-weekly subcutaneous semaglutide as monotherapy or combined with an oral antidiabetic drug (OAD) vs an additional OAD was evaluated in Japanese subjects with T2D inadequately controlled on diet/exercise or OAD monotherapy. METHODS: In this phase 3, open-label trial, adults with T2D were randomised 2:2:1 to semaglutide 0.5 mg or 1.0 mg, or one additional OAD (dipeptidyl peptidase-4 inhibitor, biguanide, sulphonylurea, glinide, α-glucosidase inhibitor or thiazolidinedione) with different modes of action...
January 11, 2018: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/29321664/mitochondrial-fission-and-mitophagy-depend-on-cofilin-mediated-actin-depolymerization-activity-at-the-mitochondrial-fission-site
#6
Guo-Bing Li, Hong-Wei Zhang, Ruo-Qiu Fu, Xiao-Ye Hu, Lei Liu, Yu-Nong Li, Yan-Xia Liu, Xin Liu, Jin-Jiao Hu, Qin Deng, Qing-Song Luo, Rong Zhang, Ning Gao
Mitochondria fission and mitophagy are fundamentally crucial to cellular physiology and play important roles in cancer progression. Developing a comprehensive understanding of the molecular mechanism underlying mitochondrial fission and mitophagy will provide novel strategies for cancer prevention and treatment. Actin has been shown to participate in mitochondrial fission and mitophagy regulation. Cofilin is best known as an actin-depolymerizing factor. However, the molecular mechanism by which cofilin regulates mitochondrial fission and mitophagy remains largely unknown...
January 11, 2018: Oncogene
https://www.readbyqxmd.com/read/29321388/suppression-of-abdominal-aortic-aneurysm-formation-in-mice-by-teneligliptin-a-dipeptidyl-peptidase-4-inhibitor
#7
Yusuke Takahara, Tomotake Tokunou, Toshihiro Ichiki
AIM: Dipeptidyl peptidase-4 (DPP-4) inhibitors lower blood glucose levels through inhibition of incretin degradation, which stimulates insulin secretion. Recent studies reported that DPP-4 inhibitors suppressed atherogenesis in apolipoprotein E-knockout (ApoEKO) mice. In this study, we investigated whether teneligliptin, a DPP-4 inhibitor, affects the development of abdominal aortic aneurysms (AAA) in ApoEKO mice. METHODS: ApoEKO mice were fed a high-fat diet (HFD) and infused with angiotensin (Ang) II by osmotic mini pumps for 4 weeks to induce AAA with (DPP-4i group) or without (control group) teneligliptin administered orally from 1 week before HFD and Ang II infusion to the end of the experiment...
January 10, 2018: Journal of Atherosclerosis and Thrombosis
https://www.readbyqxmd.com/read/29320602/when-metformin-is-not-enough-pros-and-cons-of-sglt2-and-dpp-4-inhibitors-as-a-second-line-therapy
#8
REVIEW
Angelo Avogaro, Elías Delgado, Ildiko Lingvay
The newer oral therapies for type 2 diabetes (T2DM); dipeptidyl peptidase-4 (DPP-4) inhibitors and sodium glucose cotransporter 2 (SGLT2) inhibitors have advantages over older agents. DPP-4 inhibitors are weight neutral, and have few adverse effects. SGLT2 inhibitors have additional benefits; weight loss, blood pressure reduction, cardiovascular risk reduction, and renoprotective effects. SGLT2 inhibitors, have increased risk of urogenital infections and possible risk of "euglycaemic" diabetic ketoacidosis...
January 10, 2018: Diabetes/metabolism Research and Reviews
https://www.readbyqxmd.com/read/29316236/long-term-safety-and-efficacy-of-tofogliflozin-add-on-to-insulin-in-patients-with-type-2-diabetes-results-from-a-52-week-multicenter-randomized-double-blind-open-label-extension-phase-4-study-in-japan-j-step-ins
#9
Yasuo Terauchi, Masahiro Tamura, Masayuki Senda, Ryoji Gunji, Kohei Kaku
AIMS: To evaluate the long-term safety and efficacy of tofogliflozin as an add-on treatment to insulin over 52 weeks. MATERIALS AND METHODS: This 52-week, multicenter, Phase 4 study consisted of a 16-week, randomized, double-blind, placebo-controlled phase and a 36-week open label extension phase (NCT02201004). Japanese patients with type 2 diabetes mellitus aged 20-75 years with suboptimal glycemic control (7.5%-10.5%) on insulin monotherapy (basal-bolus, bolus, premix [low and high], and basal) or on combination therapy of basal insulin and dipeptidyl peptidase-4 inhibitor were eligible for participation...
January 5, 2018: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/29316197/tofogliflozin-decreases-body-fat-mass-and-improves-peripheral-insulin-resistance
#10
Ren Matsuba, Ikuro Matsuba, Mototsugu Shimokawa, Yoshio Nagai, Yasushi Tanaka
The impact of tofogliflozin, a sodium glucose transporter 2 inhibitor, on peripheral glucose uptake in patients with type 2 diabetes mellitus (T2DM) was investigated by the hyperinsulinemic-euglycemic clamp method in a single-arm, open-label study. The following parameters were compared between before and after tofogliflozin administration for 12 weeks in 16 T2DM patients using dipeptidyl peptidase 4 inhibitors: body weight, blood pressure, glucose metabolism, liver function, lipid profile, and body composition...
January 5, 2018: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/29310647/have-dipeptidyl-peptidase-4-inhibitors-ameliorated-the-vascular-complications-of-type-2-diabetes-in-large-scale-trials-the-potential-confounding-effect-of-stem-cell-chemokines
#11
REVIEW
Milton Packer
Drugs that inhibit dipeptidyl peptidase-4 (DPP-4) are conventionally regarded as incretin-based agents that signal through the glucagon-like peptide-1 (GLP-1) receptor. However, inhibition of DPP-4 also potentiates the stem cell chemokine, stromal cell-derived factor-1 (SDF-1), which can promote inflammation, proliferative responses and neovascularization. In large-scale cardiovascular outcome trials, enhanced GLP-1 signaling has reduced the risk of atherosclerotic ischemic events, potentially because GLP-1 retards the growth and increases the stability of atherosclerotic plaques...
January 8, 2018: Cardiovascular Diabetology
https://www.readbyqxmd.com/read/29310393/association-between-dipeptidyl-peptidase-4-inhibitor-drugs-and-risk-of-acute-pancreatitis-a-meta-analysis
#12
Shimin Chen, Enfa Zhao, Wenfei Li, Jiehong Wang
BACKGROUND: Previous studies have reported conflicting results for the relationship between dipeptidyl peptidase-4 (DPP-4) inhibitor drugs and acute pancreatitis. The aim of this study was to investigate the association between DPP-4 inhibitors and an increased risk of acute pancreatitis using meta-analysis. METHODS: We conducted a comprehensive search in PubMed, Embase, Web of Science, and Cochrane library from inception to March 4, 2017. Original articles with data on DPP-4 inhibitors and acute pancreatitis were included...
December 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/29304092/dipeptidyl-peptidase-3-a-novel-protease-from-leishmania-braziliensis
#13
Jenny R Diaz, Cesar A Ramírez, Paola A Nocua, Fanny Guzman, José M Requena, Concepción J Puerta
The increase of leishmaniasis cases worldwide and the emergence of Leishmania strains resistant to current treatments make necessary to find new therapeutic targets. Proteases are appealing drug targets because they play pivotal roles in facilitating parasite survival and promoting pathogenesis. Enzymes belonging to the dipeptidyl peptidase 3 (DPP3) group have been described in different organisms such as mammals, insects and yeast, in which these enzymes have been involved in both protein turnover and protection against oxidative damage...
2018: PloS One
https://www.readbyqxmd.com/read/29301579/linagliptin-and-cardiovascular-outcomes-in-type-2-diabetes-after-acute-coronary-syndrome-or-acute-ischemic-stroke
#14
Yan-Rong Li, Sung-Sheng Tsai, Dong-Yi Chen, Szu-Tah Chen, Jui-Hung Sun, Hung-Yu Chang, Miaw-Jene Liou, Tien-Hsing Chen
BACKGROUND: The cardiovascular safety and efficacy of linagliptin, a dipeptidyl peptidase-4 inhibitor, in patients with type 2 diabetes mellitus (T2DM) after acute coronary syndrome (ACS) or acute ischemic stroke (AIS) are unclear. The aim of our real-world cohort study was to evaluate the cardiovascular outcomes of linagliptin in patients with T2DM after ACS or AIS. METHODS: An open observational noncrossover retrospective cohort study was conducted between June 1, 2012 and December 31, 2013 utilizing Taiwan National Health Insurance Research Database...
January 4, 2018: Cardiovascular Diabetology
https://www.readbyqxmd.com/read/29299596/clinical-and-immunological-profiles-of-14-patients-with-bullous-pemphigoid-without-igg-autoantibodies-to-the-bp180-nc16a-domain
#15
Kenta Nakama, Hiroshi Koga, Norito Ishii, Chika Ohata, Takashi Hashimoto, Takekuni Nakama
Importance: Enzyme-linked immunosorbent assay (ELISA) and/or chemiluminescent enzyme immunoassay (CLEIA) for BP180 noncollagenous 16A (NC16A) extracellular domain is a sensitive diagnostic tool for bullous pemphigoid (BP). However, some patients with BP have negative results for these assays. Objective: To elucidate the clinical and immunological features of patients with BP without antibodies that react to BP180 NC16A. Design, Setting, and Participants: This retrospective case series study included 152 patients who were diagnosed with BP and followed up at the Kurume University Hospital in Japan from 2007 to 2016...
January 3, 2018: JAMA Dermatology
https://www.readbyqxmd.com/read/29288140/inhibition-of-plasmodium-falciparum-cysteine-proteases-by-the-sugarcane-cystatin-canecpi-4
#16
Pollyana M S Melo, Sarah El Chamy Maluf, Mauro F Azevedo, Thaysa Paschoalin, Alexandre Budu, Piero Bagnaresi, Flávio Henrique-Silva, Andrea Soares-Costa, Marcos L Gazarini, Adriana K Carmona
Malaria is a disease caused by Plasmodium parasites that affects hundreds of millions of people. Plasmodium proteases are involved in invasion, erythrocyte egress and degradation of host proteins. Falcipains are well-studied cysteine peptidases located in P. falciparum food vacuoles that participate in hemoglobin degradation. Cystatins are natural cysteine protease inhibitors that are implicated in a wide range of regulatory processes. Here, we report that a cystatin from sugarcane, CaneCPI-4, is selectively internalized into P...
December 26, 2017: Parasitology International
https://www.readbyqxmd.com/read/29285650/synergistic-cytotoxicity-of-the-dipeptidyl-peptidase-iv-inhibitor-gemigliptin-with-metformin-in-thyroid-carcinoma-cells
#17
Si Hyoung Kim, Jun Goo Kang, Chul Sik Kim, Sung-Hee Ihm, Moon Gi Choi, Hyung Joon Yoo, Seong Jin Lee
PURPOSE: The influence of the dipeptidyl peptidase-IV inhibitor, gemigliptin alone or in combination with metformin on survival, proliferation, and migration of thyroid carcinoma cells was investigated. METHODS: SW1736 and TPC-1 human thyroid carcinoma cells were used. RESULTS: Gemigliptin and metformin caused cell death in a dose-dependent manner. In cells treated with both gemigliptin and metformin, compared with metformin alone, all of the combination index values were lower than 1...
December 28, 2017: Endocrine
https://www.readbyqxmd.com/read/29285456/gemigliptin-newer-promising-gliptin-for-type-2-diabetes-mellitus
#18
REVIEW
Manish Gutch, Abhay Joshi, Sukriti Kumar, Avinash Agarwal, Rajendra Kumar Pahan, Syed Mohd Razi
The dipeptidyl peptidase-4 (DPP-4) inhibitors have facilitated the management of type 2 diabetes mellitus (T2DM) owing to their superior efficacy and safety with low incidence of adverse effects. Gemigliptin is a new member of this family of drugs, and studies have revealed certain advantages of gemigliptin use compared to its previous congeners. Besides, this drug has also been studied for the treatment of T2DM as monotherapy, in combination with metformin or other oral antidiabetic drugs and in T2DM with moderate-to-severe renal failure...
November 2017: Indian Journal of Endocrinology and Metabolism
https://www.readbyqxmd.com/read/29283894/incretin-based-drugs-and-the-incidence-of-colorectal-cancer-in-patients-with-type-2-diabetes
#19
Devin Abrahami, Hui Yin, Oriana H Y Yu, Michael N Pollak, Laurent Azoulay
BACKGROUND: Evidence on the safety of the incretin-based drugs (glucagon-like peptide-1 [GLP-1] analogues and dipeptidyl peptidase-4 [DPP-4] inhibitors) with respect to colorectal cancer is contradictory. The objective of this study was to determine whether use of incretin-based drugs is associated with risk of incident colorectal cancer in patients with type 2 diabetes. METHODS: Using data from the United Kingdom Clinical Practice Research Datalink, we identified a cohort of 112,040 patients newly treated with antidiabetic drugs between 1 January 2007 and 31 March 2015...
December 26, 2017: Epidemiology
https://www.readbyqxmd.com/read/29279487/changes-in-antidiabetic-drug-prescription-and-glycemic-control-trends-in-elderly-patients-with-type-2-diabetes-mellitus-from-2005-2013-an-analysis-of-the-national-center-diabetes-database-ncdd-03
#20
Ritsuko Yamamoto-Honda, Yoshihiko Takahashi, Yasumichi Mori, Shigeo Yamashita, Yoko Yoshida, Shoji Kawazu, Yasuhiko Iwamoto, Hiroshi Kajio, Hidekatsu Yanai, Shuichi Mishima, Nobuhiro Handa, Kotaro Shimokawa, Akiko Yoshida, Hiroki Watanabe, Kazuhiko Ohe, Takuro Shimbo, Mitsuhiko Noda
Objective To analyze the changes in the pharmacotherapy and glycemic control trends in elderly patients with type 2 diabetes mellitus (T2DM) in Japan. Materials and Methods We extracted the data of 7,590 patients (5,396 men and 2,194 women; median year of birth: 1945) with T2DM registered in the National Center Diabetes Database for the years 2005 to 2013, and conducted age-stratified (<65, 65-74, and ≥75 years of age) analyses. Results The hemoglobin A1c (HbA1c) levels declined from 2005 to 2013, and for those who received antihyperglycemic drug prescription, the HbA1c levels were lower in the older age group than in the younger age group...
December 27, 2017: Internal Medicine
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