keyword
https://read.qxmd.com/read/38458637/network-based-screening-identifies-sitagliptin-as-an-antitumor-drug-targeting-dendritic-cells
#1
JOURNAL ARTICLE
Ian-Ian Ng, Jiaqi Zhang, Tingzhong Tian, Qi Peng, Zheng Huang, Kaimin Xiao, Xiyue Yao, Lui Ng, Jianyang Zeng, Haidong Tang
BACKGROUND: Dendritic cell (DC)-mediated antigen presentation is essential for the priming and activation of tumor-specific T cells. However, few drugs that specifically manipulate DC functions are available. The identification of drugs targeting DC holds great promise for cancer immunotherapy. METHODS: We observed that type 1 conventional DCs (cDC1s) initiated a distinct transcriptional program during antigen presentation. We used a network-based approach to screen for cDC1-targeting therapeutics...
March 7, 2024: Journal for Immunotherapy of Cancer
https://read.qxmd.com/read/38425117/incretin-therapy-and-insulin-signaling-therapeutic-targets-for-diabetes-and-associated-dementia
#2
JOURNAL ARTICLE
Deepika Joshi
Dementia is the primary cause of disability and dependence among the elderly population worldwide. The population living with dementia is anticipated to double in the next 17 years. Recent studies show the fact that compared to people without diabetes, people with Type 2 Diabetes (T2D) have about a 60% increased chance of developing dementia. In addition to cholinergic function being downregulated, improper insulin signalling also has a negative impact on synaptic plasticity and neuronal survival. Type 2 diabetes and dementia share various similar pathophysiological components...
February 29, 2024: Current Diabetes Reviews
https://read.qxmd.com/read/38390500/stereochemical-insights-into-%C3%AE-amino-n-acylhydrazones-and-their-impact-on-dpp-4-inhibition
#3
JOURNAL ARTICLE
Eduardo Reina, Lucas Silva Franco, Teiliane Rodrigues Carneiro, Eliezer J Barreiro, Lidia Moreira Lima
Dipeptidyl peptidase IV (DPP-4) is a key enzyme that regulates several important biological processes and it is better known to be targeted by gliptins as a modern validated approach for the management of type 2 diabetes mellitus (T2DM). However, new generations of DPP-4 inhibitors capable of controlling inflammatory processes associated with chronic complications of T2DM are still needed. In this scenario, we report here the design by molecular modelling of new β-amino- N -acylhydrazones, their racemic synthesis, chiral resolution, determination of physicochemical properties and their DPP4 inhibitory potency...
February 21, 2024: RSC Advances
https://read.qxmd.com/read/38234208/two-years-with-gioia-effects-of-gliflozins-and-gliptins-on-markers-of-cardiovascular-damage-in-type-2-diabetes-a-prospective-multicentre-quasi-experimental-study-on-sodium-glucose-cotransporter-2-and-dipeptidyl-peptidase-4-inhibitors-in-diabetes-clinical-practice
#4
JOURNAL ARTICLE
Miriam Longo, Paola Caruso, Lorenzo Scappaticcio, Maria Ida Maiorino, Giuseppe Bellastella, Annalisa Capuano, Katherine Esposito, Dario Giugliano
AIM: To assess and compare the metabolic and vascular effectiveness of sodium-glucose cotransporter 2 inhibitors (SGLT-2i) and dipeptidyl peptidase-4 inhibitors (DPP-4i) in the clinical practice of patients with type 2 diabetes in Italy. MATERIALS AND METHODS: GIOIA is a 2-year prospective, multicentre, quasi-experimental study that enrolled patients with type 2 diabetes initiating SGLT-2i or DPP-4i for inadequate glycaemic control [glycated haemoglobin (HbA1c) >7%] between March 2018 and March 2021...
January 17, 2024: Diabetes, Obesity & Metabolism
https://read.qxmd.com/read/38173201/an-update-on-dipeptidyl-peptidase-iv-inhibiting-peptides
#5
JOURNAL ARTICLE
S A Sivaraman, V Sabareesh
Diabetes is a chronic metabolic disorder. According to the International Diabetes Federation, about 537 million people are living with diabetes. The two types of diabetes are type 1 diabetes mellitus (T1DM) and type 2 diabetes mellitus (T2DM), among which the population affected by T2DM is relatively higher. A major reason for T2DM is that insulin stimulation is hampered due to the inactivation of incretin hormones. Dipeptidyl peptidase-IV (DPP-IV) is a serine protease that is directly involved in the inactivation of incretin hormones, e...
January 3, 2024: Current Protein & Peptide Science
https://read.qxmd.com/read/38150199/-real-world-evidence-on-pharmacological-appropriateness-in-type-2-diabetes-mellitus-and-cardiovascular-disease
#6
JOURNAL ARTICLE
Carolina Pintos, Mariana Andrea Burgos, Natalia Inés Pasik, Sofía Piccioli, María Florencia Grande Ratti, María Paula Russo
OBJECTIVE: To estimate the proportion of individuals with established Type 2 Diabetes Mellitus (T2DM) and Cardiovascular Disease (CVD) who are receiving pharmacological anti-diabetic treatment with evidence of cardiovascular benefit at a hospital in Argentina. MATERIALS AND METHODS: Cross-sectional study conducted at the Italian Hospital of Buenos Aires. A consecutive sample of adult patients affiliated with the institutional prepaid health plan active in March 2020, diagnosed with T2DM and established CVD, was included...
December 26, 2023: Revista de la Facultad de Ciencias Médicas
https://read.qxmd.com/read/38078453/comparison-of-teneligliptin-and-other-gliptin-based-regimens-in-addressing-insulin-resistance-and-glycemic-control-in-type-2-diabetic-patients-a-cross-sectional-study
#7
JOURNAL ARTICLE
Harmanjit Singh, Ravi Rohilla, Shivani Jaswal, Mandeep Singla
INTRODUCTION: The objective of this study was to compare the effects of teneligliptin-based regimens and other gliptin-based regimens with respect to insulin resistance and glycemic control in patients with type 2 diabetes mellitus (T2DM). METHODS: We enrolled T2DM subjects, inadequately controlled with metformin and glimepiride and taking one of the gliptins, and divided them into two groups, i.e. group 1 (teneligliptin-based regimens) and group 2 (other gliptin-based regimens)...
November 30, 2023: Expert Review of Endocrinology & Metabolism
https://read.qxmd.com/read/38069109/from-molecular-insights-to-clinical-perspectives-in-drug-associated-bullous-pemphigoid
#8
REVIEW
Belen de Nicolas-Ruanes, Asuncion Ballester-Martinez, Emilio Garcia-Mouronte, Emilio Berna-Rico, Carlos Azcarraga-Llobet, Montserrat Fernandez-Guarino
Bullous pemphigoid (BP), the most common autoimmune blistering disease, is characterized by the presence of autoantibodies targeting BP180 and BP230 in the basement membrane zone. This leads to the activation of complement-dependent and independent pathways, resulting in proteolytic cleavage at the dermoepidermal junction and an eosinophilic inflammatory response. While numerous drugs have been associated with BP in the literature, causality and pathogenic mechanisms remain elusive in most cases. Dipeptidyl peptidase 4 inhibitors (DPP4i), in particular, are the most frequently reported drugs related to BP and, therefore, have been extensively investigated...
November 26, 2023: International Journal of Molecular Sciences
https://read.qxmd.com/read/38032147/gliptin-induced-bullous-pemphigoid
#9
JOURNAL ARTICLE
Maria Ganeva, Tanya Gancheva, Karen Manuelyan, Evgenya Hristakieva
OBJECTIVES: Bullous pemphigoid (BP) is a rare, autoimmune, blistering disease in elderly patients that can be triggered by external factors including drugs. Drug-induced bullous pemphigoid (DIBP) does not always follow a self-limiting course after the withdrawal of the offending drug. Dipeptidyl peptidase-4 (DPP-4) inhibitors or gliptins seem to be associated with a significant risk of inducing BP. CASE PRESENTATION: We report 2 cases of BP attributed to the DPP-4 inhibitor linagliptin...
November 30, 2023: International Journal of Clinical Pharmacology and Therapeutics
https://read.qxmd.com/read/38030058/diabetic-individuals-with-covid-19-exhibit-reduced-efficacy-of-gliptins-in-inhibiting-dipeptidyl-peptidase-4-dpp4-a-suggested-explanation-for-increased-covid-19-susceptibility-in-patients-with-type-2-diabetes-mellitus-t2dm
#10
JOURNAL ARTICLE
José María Mora-Rodríguez, Belén G Sánchez, Alicia Bort, Alba Díaz-Yuste, Rubén Ballester-González, Francisco Arrieta, Alba Sebastián-Martín, Inés Díaz-Laviada
AIMS: Dipeptidyl peptidase 4 (DPP4) has been proposed as a coreceptor for SARS-CoV-2 cellular entry. Considering that type 2 diabetes mellitus (T2DM) has been identified as the most important risk factor for SARS-CoV-2, and that gliptins (DPP4 inhibitors) are a prescribed diabetic treatment, this study aims to unravel the impact of DPP4 in the intersection of T2DM/COVID-19. MATERIALS AND METHODS: We analyzed 189 serum human samples, divided into six clinical groups (controls, T2DM, T2DM + gliptins, COVID-19, COVID-19 + T2DM, and COVID-19 + T2DM + gliptins), measuring DPP4 protein concentration and activity by Western blot, ELISA, and commercial activity kits...
November 27, 2023: Life Sciences
https://read.qxmd.com/read/38002032/-drosophila-as-a-rapid-screening-model-to-evaluate-the-hypoglycemic-effects-of-dipeptidyl-peptidase-4-dpp4-inhibitors-high-evolutionary-conservation-of-dpp4
#11
JOURNAL ARTICLE
Francisco Alejandro Lagunas-Rangel, Sifang Liao, Michael J Williams, Vladimir Trukhan, Robert Fredriksson, Helgi B Schiöth
Dipeptidyl peptidase 4 (DPP4) inhibitors, commonly known as gliptins, have been an integral part of the treatment of type 2 diabetes mellitus (T2DM) for several years. Despite their remarkable efficacy in lowering glucose levels and their compatibility with other hypoglycemic drugs, recent studies have revealed adverse effects, prompting the search for improved drugs within this category, which has required the use of animal models to verify the hypoglycemic effects of these compounds. Currently, in many countries the use of mammals is being significantly restricted, as well as cost prohibitive, and alternative in vivo approaches have been encouraged...
November 12, 2023: Biomedicines
https://read.qxmd.com/read/37986140/risk-of-pancreatitis-and-pancreatic-carcinoma-for-anti-diabetic-medications-findings-from-real-world-safety-data-analysis-and-systematic-review-and-meta-analysis-of-randomized-controlled-trials
#12
JOURNAL ARTICLE
Asif Muhammad, Christy Thomas, Vivekanandan Kalaiselvan, Krishna Undela
BACKGROUND: The existing evidence from pre- and post-marketing studies is conflicting on the risk of pancreatic events for anti-diabetic medications. RESEARCH DESIGN AND METHODS: A retrospective case/non-case study was conducted by using spontaneous reports on pancreatic events for anti-diabetic medications from the FAERS and VigiBase. Proportional Reporting Ratio (PRR), Reporting Odds Ratio (ROR), and Information Component (IC) were calculated by a disproportionality analysis...
November 20, 2023: Expert Opinion on Drug Safety
https://read.qxmd.com/read/37943295/-trigger-factors-associated-with-bullous-autoimmune-dermatoses
#13
REVIEW
Constantin Lütgerath, Christian D Sadik, Nina van Beek
BACKGROUND: Blistering autoimmune dermatoses are a heterogeneous group of rare diseases. Pemphigus diseases are distinguished from pemphigoid diseases as well as dermatitis herpetiformis. In pemphigus diseases, cutaneous blistering is caused by an intraepidermal loss of adhesion between keratinocytes. In pemphigoid diseases, blister formation is due to a subepidermal loss of adhesion of keratinocytes from the basement membrane. OBJECTIVES: This article reviews the most important trigger factors associated with bullous autoimmune dermatoses and discusses their role in their initial manifestation as well as exacerbation...
November 9, 2023: Dermatologie (Heidelb)
https://read.qxmd.com/read/37909618/effect-of-a-combination-of-gliptin-and-metformin-on-serum-vitamin-b12-folic-acid-and-ferritin-levels
#14
JOURNAL ARTICLE
Fevziye Turkoglu Genc, Ahmet Nalbant, Ahmed Cihad Genc, Tezcan Kaya
OBJECTIVE: The primary objective of this study was to explore the impact of metformin and metformin/gliptin combination therapy on the serum concentrations of vitamin B12, ferritin, and folic acid in individuals diagnosed with type 2 diabetes. METHODS: This study included 118 patients, classified into two groups: 59 patients using only metformin and 59 patients using a combination of metformin/gliptin. Among the latter group, 35 patients used vildagliptin/metformin, and 24 used sitagliptin/metformin...
2023: Revista da Associação Médica Brasileira
https://read.qxmd.com/read/37837799/mechanism-of-molecular-interaction-of-sitagliptin-with-human-dpp-4-enzyme-new-insights
#15
JOURNAL ARTICLE
Michelangelo Bauwelz Gonzatti, José Edvar Monteiro Júnior, Antônio José Rocha, Jonathas Sales de Oliveira, Antônio José de Jesus Evangelista, Fátima Morgana Pio Fonseca, Vânia Marilande Ceccatto, Ariclécio Cunha de Oliveira, José Ednésio da Cruz Freire
PURPOSE: Dipeptidyl peptidase 4 (DPP4 ) inactivates a range of bioactive peptides. The cleavage of insulinotropic peptides and glucagon-like peptide 1 (GLP1 ) by DPP4 directly influences glucose homeostasis. This study aimed to describe the mode of interaction between sitagliptin (an antidiabetic drug) and human DPP4 using in silico approaches. MATERIALS AND METHODS: Docking studies were conducted using AutoDock Vina, 2D and 3D schematic drawings were obtained using PoseView and PLIP servers, and the DPP4 -sitagliptin complex was visualized with Pymol software...
September 2023: Advances in Medical Sciences
https://read.qxmd.com/read/37822982/bullous-pemphigoid-triggered-by-dulaglutide-a-case-report-and-a-review-of-the-literature
#16
JOURNAL ARTICLE
Benedetta Sonego, Enrico Zelin, Iris Zalaudek, Nicola di Meo
Bullous pemphigoid (BP) is an autoimmune disease with a chronic relapsing course, predominantly affecting elderly people. Drugs are one of the possible triggers. A class of antidiabetic drugs often associated with the development of BP are inhibitors of dipeptidyl peptidase 4 (DPP-4 inhibitors or gliptins), while less known is the association with glucagon-like-peptide-1 receptor agonists. We describe a case of BP caused by dulaglutide and summarize the other few cases described in the literature. As a class of drugs widely used in clinical practice, it is important to know about this possible adverse event...
September 12, 2023: Dermatology Reports
https://read.qxmd.com/read/37732495/immunomodulatory-activity-of-dipeptidyl-peptidase-4-inhibitors-in-immune-related-diseases
#17
REVIEW
Marija Drakul, Miodrag Čolić
Dipeptidyl peptidase-4 (DPP-4), also known as CD26, is a 110-kDa cell surface glycoprotein with enzymatic and signal transducing activity. DPP-4/CD26 is expressed by a variety of various cells, including CD4+ and CD8+ T cells, B cells, dendritic cells, macrophages, and NK cells. DPP-4 inhibitors (DPP-4i) were introduced to clinics in 2006 as new oral antihyperglycemic drugs approved for type 2 diabetes mellitus treatment. In addition to glucose-lowering effects, emerging data, from clinical studies and their animal models, suggest that DPP-4i could display anti-inflammatory and immunomodulatory effects as well, but the molecular and immunological mechanisms of these actions are insufficiently investigated...
September 21, 2023: European Journal of Immunology
https://read.qxmd.com/read/37642237/effects-of-dipeptidyl-peptidase-4-inhibition-on-the-endothelial-control-of-the-vascular-tone
#18
REVIEW
Joao Carlos Ribeiro-Silva, Vinicius Bermond Marques, Leonardo Dos Santos
Dipeptidyl peptidase 4 (DPP4) is a serine protease known to cleave incretin hormones, which stimulate insulin secretion after food intake, a fact that supported the development of its inhibitors (DPP4i or gliptins) for the treatment of type 2 diabetes mellitus. In addition to their glucose-lowering effects, DPP4i show benefits for the cardiovascular system that could be related, at least in part, to their protective action on vascular endothelium. DPP4i have been associated with the reversal of endothelial dysfunction, an important predictor of cardiovascular events and a hallmark of diseases such as atherosclerosis, diabetes mellitus, hypertension, and heart failure...
October 1, 2023: American Journal of Physiology. Cell Physiology
https://read.qxmd.com/read/37626624/metabolism-and-chemical-degradation-of-new-antidiabetic-drugs-a-review-of-analytical-approaches-for-analysis-of-glutides-and-gliflozins
#19
REVIEW
Anna Gumieniczek, Anna Berecka-Rycerz
The drug metabolism and drug degradation pathways may overlap, resulting in the formation of similar constituents. Therefore, the metabolism data can be helpful for deriving safe levels of degradation impurities and improving the quality of respective pharmaceutical products. The present article contains considerations on possible links between metabolic and degradation pathways for new antidiabetic drugs such as glutides, gliflozins, and gliptins. Special attention was paid to their reported metabolites and identified degradation products...
July 27, 2023: Biomedicines
https://read.qxmd.com/read/37610193/-effects-of-antidiabetic-medications-on-metabolic-associated-fatty-liver-disease
#20
JOURNAL ARTICLE
André J Scheen
Metabolic-Associated Fatty Liver Disease (MAFLD) is a prevalent metabolic complication among patients with obesity and type 2 diabetes, associated with bad prognosis. Classical antidiabetics have little effects on this complication, except pioglitazone that exerts a positive impact but with uncertain safety. Gliptins are almost neutral, whereas glucagon-like peptide-1 receptor agonists showed benefits, the most potent ones being those associated with a greater weight loss such as liraglutide or semaglutide...
August 23, 2023: Revue Médicale Suisse
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