scholarly journals A First Attempt to Identify Repurposable Drugs for Type 2 Diabetes: 3D-Similarity Search and Molecular Docking

2020 ◽  
Vol 3 (1) ◽  
pp. 7
Author(s):  
Daniela Istrate ◽  
Alina Bora ◽  
Luminita Crisan
Keyword(s):  
Type 2 Diabetes ◽  
Similarity Search ◽  
Drug Repositioning ◽  
New Drugs ◽  
Dipeptidyl Peptidase 4 ◽  
The World ◽  
3D Similarity ◽  
Antidiabetic Effects

Drug repositioning involves the investigation of existing drugs for new therapeutic purposes, such as type 2 diabetes. This disease affects the health and quality of life for individuals around the world. Sitagliptin, a highly selective dipeptidyl peptidase-4 (DPP-4) inhibitor, is used to treat type 2 diabetes mellitus by effective fasting and improved glycemic control. Despite this advantage, serious hypersensitivity reactions have been acknowledged for patients receiving sitagliptin. In this context, it is necessary to develop new drugs with enhanced profiles and targeting DPP-4. Sitagliptin, ((2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihidro[1,2,4]triazolo[4,3-A]pirazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine), was used as a query in a 3D-similarity search on the approved DrugBank. Based on the TanimotoCombo parameter, the first 10 approved DrugBank drugs were docked in the 4FFW active site to identify effective antidiabetic effects for possible repurposable drugs marketed with other indications.

scholarly journals Effects of Social Determinants of Health in Progression to Type 2 Diabetes

2021 ◽  
Author(s):  
◽  
Folabi Ariganjoye ◽  
Keyword(s):  
Quality Of Life ◽  
United States ◽  
Type 2 Diabetes ◽  
Social Determinants ◽  
The United States ◽  
Effective Management ◽  
The World ◽  
Longitudinal Association

The prevalence of prediabetes and diabetes in the United States and around the world has increased faster than expected in the last 30 years. The economic burden this costs a nation can be astronomic both in terms of expense and loss in productivity. One-third of U.S. adults, 86 million people, have prediabetes. Effective management is needed that can reach these 86 million, and others at high risk, to reduce their progression to diagnosed Type 2 diabetes. After the literature review, there was not enough literature to support how these led to the progression to diabetes. The abundant literature is centered on how to prevent complications and improve the quality of life of those living with type 2 diabetes. This paper will focus on the longitudinal association between these social determinants and how they may predispose to the progression to Type 2 diabetes.

Incretin-based therapy for treating patients with type 2 diabetes

2011 ◽  
Vol 152 (48) ◽  
pp. 1931-1940 ◽  
Author(s):  
György Jermendy
Keyword(s):  
Type 2 Diabetes ◽  
Clinical Practice ◽  
New Drugs ◽  
Clinical Experiences ◽  
Dipeptidyl Peptidase 4 ◽  
New Class ◽  
Glucagon Like Peptide ◽  
Glucagon Like Peptide 1 ◽  
Near Future

In the last couple of years, a new class of antidiabetic drugs became available for the clinical practice. Due to the intensive research, several new drugs reached the market. Among the incretinmimetics both the GLP-1 (glucagon like peptide-1)-receptor agonist exenatide and the GLP-1-analogue liraglutide can be used for treatment. As for incretin enhancers (dipeptidyl-peptidase-4 [DPP-4]-inhibitors), sitagliptin, vildagliptin and saxagliptin are available in Hungary, linagliptin will be introduced to the market in the near future. In clinical practice, any incretin-based new drugs can be used for treating patients with type 2 diabetes, preferably in combination with metformin. The clinical experiences with these new drugs are reviewed focusing on both the benefits and the potential side-effects of the particular compounds. Orv. Hetil., 2011, 152, 1931–1940.

scholarly journals Mechanisms of macro-, micro- and ultramicroscopic transformation of bodies in diabetes

Morphologia ◽  
2021 ◽  
Vol 15 (3) ◽  
pp. 23-29
Author(s):  
I.I. Savka ◽  
M.N. Tsytovskyi ◽  
G.M. Dmytriv
Keyword(s):  
Quality Of Life ◽  
Type 2 Diabetes ◽  
Diabetes Type 2 ◽  
Diabetes Type ◽  
Clinical Aspects ◽  
Number Of Patients ◽  
The World ◽  
Patients With Diabetes

The study of structural changes of organs and tissues in the context of diabetes is one of the urgent problems of modern medicine. According to WHO, in all countries of the world the number of patients with diabetes exceeds 175 million. According to an expert estimate of the spread of this disease by 2025 will make about 300 million people. More than 1 million people with diabetes have been officially registered in Ukraine. WHO has recognized the disease as a non-communicable epidemic. The dramatic increase in the prevalence of diabetes requires a detailed study of this problem. It is established that the prevalence of diabetes increases among the population of the countries of the world depending on the region, the level of economic development of the country, gender and age. Thus, according to IDF findings, there is a tendency for the highest prevalence of diabetes among the urban (urban) able-bodied population of developing countries in persons between 40 and 59 years of age, approximately equal in both male and female. The number of patients is increasing, mainly due to patients with type 2 diabetes. Type 2 diabetes (type 2 diabetes mellitus) is a severe progressive chronic disease that is an independent risk factor for heart failure (CH) and cardiovascular complications. In the XXI century. the steady growth of type 2 diabetes and the frequency of its serious consequences is of great concern to the world medical community. It is important that at the time of diagnosis of type 2 diabetes, the prevalence of complications leading to a decline in quality of life, early disability and premature death is already high enough. Despite the presence in the fight against this disease effective drugs, modern technologies, new educational and preventive techniques, mankind loses the fight against diabetes year after year, which leads to disability due to its complications, reducing the life expectancy and quality of life of patients, loss working capacity and premature mortality. Thus, the current prevalence and incidence of diabetes and life-threatening complications suggest that there is a non-communicable diabetes epidemic in the world and in Ukraine in particular. The article represents analysis of work of numerous researchers who studied statistіcal, clinical and morphological aspects of the impact of diabetes on cardiovascular system. Main morphogenetic, morphological and clinical aspects of complications of diabetes, pathologies of microcirculation of patients with diabetes were dedicated, what makes possible to predict and detect on the early stages vascular complications in diabetes and to perform effective prevention and treatment.

scholarly journals AMD Annals 2020 - Synopsis on Type 2 Diabetes. Evaluation of AMD quality indicators of type 2 diabetes care in Italy

2021 ◽  
Vol 24 (1) ◽  
pp. 19
Author(s):  
Michelli , A.
Keyword(s):  
Type 2 Diabetes ◽  
Diabetes Care ◽  
Data File ◽  
New Drugs ◽  
Lipid Lowering ◽  
Type2 Diabetes ◽  
Quality Of Diabetes Care ◽  
Hba1c Levels

OBJECTIVE OF THE STUDY The AMD 2020 Annals on Type 2 Diabetes (DM2) set out to show, 2 years after the last evaluation, how the quality of DM2 care has evolved in Italy. DESIGN AND METHODS In order to participate in the initiative, the centers had to be equipped with information systems capable of guaranteeing the standardized extraction of the information necessary for the creation of the AMD Data File. The data analyzed concern socio-de-mographic and clinical characteristics and volume of activity. The selection of indicators is based on Revision 8 of June 2019 (AMD Annals website). RESULTS DM2 patients increased to 473,740 (57.1% M; 42.9% F, 67.4% aged> 65 y). 6% new diagnoses. All monitoring indicators, of favorable and unfavorable outcome, have improved: 52.9% of DM2 have HbA1c levels <= 7.0%(53 mmol/mol), 63.5% have LDL cholesterol values <100 mg / dl, 53,5% have blood pressure levels <140/80 mmHg, 39.9% are obese. The proportion of patients with GFR <60 mL/min*1.73 m2 rose to 29%, and 7.1% had GFR <30 mL / min. Therapy: there is a reduction in the use of sulfonylureas and glinides (19.9%); stable use of insulin; new drugs are increasingly prescribed (DPPIVi:21%; GLP1-RA: 5.9%; SGLT2i: 9.6%). 60.8% are on lipid-lowering treatment, 70% are on antihypertensive therapy, but 48.6% are not on target. Complications: 22% have diabetic retinopathy; 7.5% had myocardial infarction, 2.7 had a stroke, 14.7% had a history of cardiovascular disease. 50.8% of subjects with age>75a have HbA1c levels <= 7.0%(53 mmol/mol), of these 16.3% are treated with drugs that can induce hypoglycemia. Patients with Q Score> 25 are growing (60.3%). CONCLUSIONS The AMD 2020 Annals on DM2 show a marked improvement in all indicators of quality of care, but large areas of undertreatment and other overtreatment remain, and call to action. KEY WORDS AMD Annals; type2 diabetes mellitus; quality of diabetes care in type 2 diabetes patients in Italy; undertreatment; overtreatment.

scholarly journals Incretin mimetics and dipeptidyl peptidase-4 inhibitors: innovative treatment therapies for type 2 diabetes

2008 ◽  
Vol 52 (6) ◽  
pp. 1039-1049 ◽  
Author(s):  
Jaime A. Davidson ◽  
Erika B. Parente ◽  
Jorge L. Gross
Keyword(s):  
Type 2 Diabetes ◽  
Lifestyle Modification ◽  
Fasting Glucose ◽  
Dipeptidyl Peptidase ◽  
New Drugs ◽  
Glucagon Release ◽  
Incretin Mimetics ◽  
Dipeptidyl Peptidase 4 ◽  
Dipeptidyl Peptidase 4 Inhibitors

The prevalence of diabetes and impaired glucose tolerance is predicted to dramatically increase over the next two decades. Clinical therapies for type 2 diabetes mellitus (T2DM) have traditionally included lifestyle modification, oral anti-diabetic agents, and ultimately insulin initiation. In this report, we review the clinical trial results of two innovative T2DM treatment therapies that are based on the glucoregulatory effects of incretin hormones. Incretin mimetics are peptide drugs that mimic several of the actions of glucagon-like peptide-1 (GLP-1) and have been shown to lower glycated hemoglobin (A1C) levels in patients with T2DM. Additionally, incretin mimetics lower postprandial and fasting glucose, suppress elevated glucagon release, and are associated with progressive weight reduction. Dipeptidyl peptidase-4 (DPP-4) inhibitors increase endogenous GLP-1 levels by inhibiting the enzymatic degradation of GLP-1. Clinical studies in patients with T2DM have shown that DPP-4 inhibitors reduce elevated A1C, lower postprandial and fasting glucose, suppress glucagon release, and are weight neutral. Collectively, these new drugs, given in combination with other antidiabetic agents, such as metformin, sulfonylureas, and/or thiazolidinediones, can help restore glucose homeostasis in poorly controlled patients with T2DM.

scholarly journals Drug repurposing: Dipeptidyl peptidase IV (DPP4) inhibitors as potential agents to treat SARS-CoV-2 (2019-nCov) infection

2020 ◽  
Author(s):  
Praveen P. N. Rao ◽  
Amy Trinh Pham ◽  
Arash Shakeri ◽  
Amna El Shatshat ◽  
Yusheng Zhao ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Treatment Options ◽  
Drug Repurposing ◽  
Dipeptidyl Peptidase ◽  
New Drugs ◽  
Viral Protease ◽  
Dipeptidyl Peptidase 4 ◽  
Dpp4 Inhibitors ◽  
Current Outbreak

Abstract The current outbreak of severe acute respiratory distress syndrome (SARS) or nCOVID-19 pandemic, caused by the coronavirus-2 (CoV-2), continues to wreak havoc globally. Unfortunately, there are no concrete treatment options available which has severely hampered the pharmacotherapy of this devastating infection. This calls for an urgent need to consider alternative strategies which can be employed quickly, as discovering new drugs for SARS-CoV-2 infections is a time consuming and expensive proposition. In this regard, drug repurposing is an appealing approach which can provide rapid access to therapeutics with proven record of safety and efficacy. Accordingly, we investigated the drug repurposing potential of a library of dipeptidyl peptidase 4 (DPP4) inhibitors which are currently marketed for type-2 diabetes, to treat SARS-CoV-2 infections. Computational studies were conducted in the crystal structure of the substrate binding site of viral protease, the SARS-CoV-2 Mpro dimer, which led to the identification of three marketed DPP4 inhibitors; gemigliptin, linagliptin and evogliptin exhibiting favorable binding, in the SARS-CoV-2 Mpro dimer, viral protease. These studies support the repurposing of DPP4 class of inhibitors in treating SARS-CoV-2 infections, especially in elderly patients with type-2 diabetes, who are at a greater risk of suffering from increased disease severity and mortality.

BIOBOARD

2019 ◽  
Vol 23 (03) ◽  
pp. 39-44
Keyword(s):  
Type 2 Diabetes ◽  
Influenza Vaccine ◽  
Human Nutrition ◽  
Protein Source ◽  
Asia Pacific ◽  
Tropical Waters ◽  
Glucose Levels ◽  
The World

ASIA-PACIFIC – Quality and quantity of sleep affects behavior, cognition and glucose levels in Asian teens. ASIA-PACIFIC – Quality of overall diet key to lowering type 2 diabetes risk. ASIA-PACIFIC – Toxic bacteria found on microplastics retrieved from tropical waters. ASIA-PACIFIC – New use of anti-parasitic drug to potentially treat cancer. ASIA-PACIFIC – Hassle free influenza vaccine close to reality. REST OF THE WORLD – Bitter rapeseed could be used as protein source for human nutrition.

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