Glucagon-like peptide 1 and inhibitors of dipeptidyl peptidase IV in the treatment of type 2 diabetes mellitus

2004 ◽  
Vol 4 (6) ◽  
pp. 589-596 ◽  
Author(s):  
Jens Juul Holst ◽  
Carolyn F Deacon
2021 ◽  
Vol 11 (5) ◽  

Dipeptidyl peptidase IV is a key regulator of insulin- stimulating hormones, glucagon-like peptide and glucose dependent insulinotrophic polypeptide. Thus it is a promising target for treatment of type 2 Diabetes mellitus. Inhibition of plasma Dipeptidyl peptidase IV enzyme lead to enhanced endogenous glucagon like peptide-1, GIP activity which ultimately results in the potentiating of insulin secretion by pancreatic cell and subsequent lowering blood glucose level, HbA [1c], glucose secretion, liver glucose production. One of the principal goals of diabetes management is to attain haemoglobin HbA [1c] treatment goals and prevent the onset or decrease the rate of occurrence of Microvascular conditions.2, 6 numerous treatment options are available for management of Type 2 Diabetes mellitus, various class of DPP IV inhibitor being explored such as Sitagliptin and Vildagliptin successfully launched. Several other novel DPP IV inhibitors are in pipeline, Unless there are clear contraindications, metformin monotherapy is prescribed, and if HbA [1c] targets are not attained after 3 months, 1 of several classes of agents could be added, such as sulfonylurea’s, Thiazolidinediones, dipeptidyl peptidase-4 inhibitors, - glucagon like peptide-1 receptor agonists, or basal insulin.2,6 Despite the broad range of therapeutic options, the attainment of HbA [1c] goals among patients with diabetes remains challenging, with just slightly more than half (52%) of diabetes patients attaining the common HbA [1c] goal of < 7.0%. The present review summarizes latest preclinical and clinical trial data of different DPP IV inhibitors with a special emphasis on their DPP8/9 fold selectivity and therapeutic advantages over GLP-1 based approach. Keywords: Diabetes 2, Dipeptidyl Peptidase-4, glucose-dependent insulinot


2018 ◽  
Vol 12 (4) ◽  
pp. 202-209 ◽  
Author(s):  
Spyridon N. Karras ◽  
Eleni Rapti ◽  
Theocharis Koufakis ◽  
Angeliki Kyriazou ◽  
Dimitrios G. Goulis ◽  
...  

2012 ◽  
Vol 413 (11-12) ◽  
pp. 1020-1021 ◽  
Author(s):  
Luziane Potrich Bellé ◽  
Paula Eliete Rodrigues Bitencourt ◽  
Karine Santos De Bona ◽  
Rafael Noal Moresco ◽  
Maria Beatriz Moretto

2021 ◽  
Vol 37 (6) ◽  
pp. 74-83
Author(s):  
A.Yu. Gorbunova ◽  
E.P. Sannikova ◽  
I.I. Gubaidullin ◽  
O.M. Ignatova ◽  
M.Yu. Kopaeva ◽  
...  

In addition to the previously developed recombinant modified human glucagon-like peptide 1 (rmglp1, Glypin), a recombinant modified human glucose-dependent insulinotropic peptide (RMGIP) has been obtained. A new universal reverse-phase HPLC technique has been proposed allowing quantitative analysis of rmGlp1 and rmGip separately and as part of a two-component preparation. The data show that the design of recombinant human rmGip according to the Glypine formula makes it possible to produce one-component and two-component preparations containing various rmGip and rmGlp1 protein ratios ranging from 1:0 to 20:1, using cell biomass samples mixed in predetermined proportions. Studies of human rmGip activity in a mouse model revealed reduced specific activity and signs of weak antagonistic effects. In this regard, there is a need for further study of human rmGip activity in a mouse model, including the use of alternative mouse or rat rmGip. type 2 diabetes mellitus; two-component drug, glucose-dependent insulinotropic peptide, glucagon-like peptide-1 The work was supported by the Internal Grant from National Research Center Kurchatov Institute.


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