Incretin-Related Therapies in Type 2 Diabetes: A Practical Overview

Robertson, Carolyn

doi:10.2337/diaspect.24.1.26

Cited by 10 publications

(12 citation statements)

References 70 publications

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“…In recent years, several pharmaceutical agents have been developed for the treatment of this type of diabetes, such as metformin, α ‐glucosidase inhibitors, and thiazolidinediones . Recently, a new class of drugs was introduced into the clinical practice for incretin‐based therapy . The peptide liraglutide belongs to this class.…”

Section: Introductionmentioning

confidence: 99%

Innovative chemical synthesis and conformational hints on the lipopeptide liraglutide

Guryanov

Bondesan²,

Visentini³

et al. 2016

J. Pept. Sci.

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Liraglutide is a new generation lipopeptide drug used for the treatment of type II diabetes. In this work, we describe new approaches for its preparation fully by chemical methods. The key step of these strategies is the synthesis in solution of the Lys/γ-Glu building block, Fmoc-Lys-(Pal-γ-Glu-OtBu)-OH, in which Lys and Glu residues are linked through their side chains and γ-Glu is N(α) -palmitoylated. This dipeptide derivative is then inserted into the peptide sequence on solid phase. As liraglutide is obtained with great purity and high yield, our approach can be particularly attractive for an industrial production. We also report here the results of a circular dichroism conformational analysis in a membrane mimetic environment that offers new insights into the mechanism of action of liraglutide. Copyright © 2016 European Peptide Society and John Wiley & Sons, Ltd.

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Section: Introductionmentioning

confidence: 99%

Innovative chemical synthesis and conformational hints on the lipopeptide liraglutide

Guryanov

Bondesan²,

Visentini³

et al. 2016

J. Pept. Sci.

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“…As previously discussed, there are two classes of incretin-based therapies: dipeptidyl peptidase-4 inhibitors, which include sitagliptin and saxagliptin and are administered orally, and glucagon-like peptide-1 receptor agonists such as exenatide and liraglutide, that are administered subcutaneously. Both categories have been used as monotherapy or in conjunction with other drugs [ 21 ]. In this study, we chose sitagliptin and extended-release exenatide due to availability and to decrease the number of injections to the animals.…”

Section: Discussionmentioning

confidence: 99%

Effects of Incretin Pathway Elements on Bone Properties

Abdi

Pasiou

Konstantopoulos

et al. 2023

Cureus

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Introduction The effects of incretin-based drugs, such as receptor agonists of glucagon-like peptide-1 and inhibitors of dipeptidyl peptidase-4, on bone metabolism are not completely clear yet. The aim of this study is to compare the effects of glucagon-like peptide-1 and inhibitors of dipeptidyl peptidase-4 on the bone to see how different elements of the incretin pathway affect bone quality in terms of biomechanical properties, bone turnover, and mineral properties. Materials and methods Forty 10-week-old Wistar rats were divided into four groups: a control group, a control diabetic group, a diabetic group treated with sitagliptin, and a diabetic group treated with exenatide. Type 2 diabetes was simulated by dietary manipulation in addition to low-dose streptozotocin, and then two different incretin-based drugs were administered. The rats were sacrificed after five weeks of therapeutic treatment. Their serum was analyzed with the enzyme-linked immunosorbent assay (ELISA) method for basic bone turnover markers, and their right femur was subjected to a three-point bending test. Finally, Hematoxylin & Eosin staining, in addition to Raman spectroscopy, were employed to access the collagen and mineral properties of the bone. Results Both incretin-based drugs reduced osteoclast function; however, they were not able to restore osteoblastic function to normal. The net effect on bone strength was surprising: bone elasticity was restored by the antidiabetic treatment, but bone strength deteriorated. Exenatide had a slightly more pronounced effect, which, although not significant, points to the direction that dipeptidyl peptidase-4 (DPP4) may be a linking factor between reduced osteoclastic function and reduced bone formation, as suggested by the literature. Conclusion DPP4 receptors seem to be one of the links between reduced osteoclast function and reduced bone remodeling, so DPP4 inhibition can be more detrimental to the bone than glucagon-like peptide-1 (GLP-1) receptor agonists.

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“…From understanding the mechanism of incretin system action, a new class of drugs has been found—incretin mimetics. Current incretin mimetics medications involve GLP-1 agonists and dipeptidyl peptidase-4 (DPP-4) inhibitors with an ability to potentiate incretin receptor signalling [ 47 , 96 ].…”

Section: Treatment Of Type 2 Diabetes Mellitusmentioning

confidence: 99%

Pharmaceutical Drugs and Natural Therapeutic Products for the Treatment of Type 2 Diabetes Mellitus

et al. 2021

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Type 2 diabetes mellitus (T2DM) is the most widespread form of diabetes, characterized by chronic hyperglycaemia, insulin resistance, and inefficient insulin secretion and action. Primary care in T2DM is pharmacological, using drugs of several groups that include insulin sensitisers (e.g., biguanides, thiazolidinediones), insulin secretagogues (e.g., sulphonylureas, meglinides), alpha-glucosidase inhibitors, and the newest incretin-based therapies and sodium–glucose co-transporter 2 inhibitors. However, their long-term application can cause many harmful side effects, emphasising the importance of the using natural therapeutic products. Natural health substances including non-flavonoid polyphenols (e.g., resveratrol, curcumin, tannins, and lignans), flavonoids (e.g., anthocyanins, epigallocatechin gallate, quercetin, naringin, rutin, and kaempferol), plant fruits, vegetables and other products (e.g., garlic, green tea, blackcurrant, rowanberry, bilberry, strawberry, cornelian cherry, olive oil, sesame oil, and carrot) may be a safer alternative to primary pharmacological therapy. They are recommended as food supplements to prevent and/or ameliorate T2DM-related complications. In the advanced stage of T2DM, the combination therapy of synthetic agents and natural compounds with synergistic interactions makes the treatment more efficient. In this review, both pharmaceutical drugs and selected natural products, as well as combination therapies, are characterized. Mechanisms of their action and possible negative side effects are also provided.

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Incretin-Related Therapies in Type 2 Diabetes: A Practical Overview

Cited by 10 publications

References 70 publications

Innovative chemical synthesis and conformational hints on the lipopeptide liraglutide

Innovative chemical synthesis and conformational hints on the lipopeptide liraglutide

Effects of Incretin Pathway Elements on Bone Properties

Pharmaceutical Drugs and Natural Therapeutic Products for the Treatment of Type 2 Diabetes Mellitus

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