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Glucagon-Like Peptide 1 (GLP-1) Mediated Therapies On Type 2 Diabetes (T2D)

1. Introduction-T2D

Type 2 diabetes (T2D), the major type of diabetes mellitus (DM), is a long term metabolic disorder primarily occurs as a result of obesity and not enough exercise. [1] T2D is characterized by high blood sugar, insulin resistance, and relative lack of insulin. It is reported that T2D could lead to a ten-year-shorter life expectancy. Globally, near to 400 million people are suffering from T2D and the rate is still rising. [2]

2. Introduction-Insulin, GLP1, GLP1R

Insulin is a peptide hormone which plays a crytical role in the progresses of T2D disease. [3] The human insulin gene primarily encodes preproinsulin which is a peptide containing 110 amino acids. Preproinsulin is further processed into proinsulin by removal of the N-terminal signal peptide. Afeter that, three peptides (B chain, A chain and C-peptide) are released by post-translational modification. The human insulin protein is a dimer of the A-chain and B-chain linked by disulfide bonds.

Glucagon-like peptide-1 (GLP-1) is a peptide hormone and an incretin derived from preproglucagon protein which in human is encoded by the GCG gene. GLP-1 can increase insulin secretion and decrease glucagon secretion from the pancreas in a glucose-dependent manner. The human glucagon-like peptide 1 receptor (GLP1R) is G protein-coupled receptor encoded by the GLP1R gene. GLP1R binds GLP-1 and glucagon as its natural endogenous agonists.

The GLP1R system has become an important target for T2D treatment.

3. T2D Therapies-DPP4 Inhibitors, GLP1R Agonists

There are mainly two classes of glucose-lowering therapeutics: dipeptidyl peptidase 4 (DPP-4) inhibitors and GLP1R agonists. Both GLP1R agonists and DPP-4 inhibitors affect glucose control via multiple mechanisms, including increase of glucose-dependent insulin secretion, slowed gastric emptying, and reduction of postprandial glucagon and of food intake. These agents have a lower risk of causing hypoglycemia.

3.1) DPP-4 enzyme inhibitors

DPP-4 protein, also known as adenosine deaminase complexing protein 2 or CD26, is encoded by human DPP4 gene. DPP-4 plays a key role in glucose metabolism. [4] It is associated with the rapid degradation of incretins including GLP-1, which renders GLP-1 a short half-life, namely less than two minutes.

To circumvent the half-life constraint of GLP-1, multiple DPP-4 inhibitors have been developed, such as Sitagliptin, Vildagliptin, Saxagliptin, Linagliptin, Gemigliptin, Anagliptin, Teneligliptin, Alogliptin, Trelagliptin, Omarigliptin (MK-3102), Evogliptin, Dutogliptin etc. These DPP-4 inhibitors prolong and enhance the activity of incretins including GLP-1 through inhibiting the DPP-4 enzyme, which in turn increases glucose-dependent insulin secretion and suppresses inappropriately elevated glucagon secretion.

3.2) GLP1R agonists

GLP-1R agonists mimic the activities of GLP-1. These agents exhibit increased resistance to DPP-4 degradation by virtue of their amino acid sequence and/or through chemical modification, and thus provide pharmacological levels of GLP-1.

There are several approved GLP-1 agonists, such as exenatide, liraglutide, lixisenatide, albiglutide and dulaglutide etc., with more being developed. These agents work in the same pathway as DPP-4 inhibitors but are generally considered more potent.

Stable cells expressing the GLP-1 receptor are a powerful and indispensable tool during the process of screening novel GLP1R agonists.

4. Our Capabilities

We can offer several agents related to research of GLP1-based T2D treatment, including but not limited to the following products. Please contact us for special requirements, we are always happay to provide custom services to assist your research.

cDNAHuman INS ORF clone
Human GCG ORF clone
Human DPP4 cDNA clone
Human GLP1R ORF Clone
shRNAshRNA set against human INS
shRNA set against human GCG
shRNA set against human DPP4
shRNA set against Human GLP1R
3’UTRHuman INS miRNA 3'UTR clone
Human GCG miRNA 3'UTR clone
Human DPP4 miRNA 3'UTR clone
Human GLP1R miRNA 3'UTR clone
Virus particlesHuman INS lentiviral particles
Human GCG lentivirus particles
Human GCG adenoviral particles
Human DPP4 lentivirus particles
Human DPP4 adenoviral particles
Human GLP1R lentivirus particles
Human GLP1R adenoviral particles
Stable cell linesHuman INS stable cell line
Human GCG stable cell line
Human DPP4 stable cell line
Human GLP1R stable cell lines


  1. "Causes of Diabetes". National Institute of Diabetes and Digestive and Kidney Diseases. June 2014. Archived from the original on 2 February 2016. Retrieved 10 February 2016.
  2. Shi, Yuankai; Hu, Frank B (7 June 2014). "The global implications of diabetes and cancer". The Lancet. 383 (9933): 1947–8.doi:10.1016/S0140-6736(14)60886-2. PMID 24910221
  3. Zaccardi F, Webb DR, Yates T, Davies MJ (February 2016). "Pathophysiology of type 1 and type 2 diabetes mellitus: a 90-year perspective.". Postgraduate Medical Journal. 92 (1084): 63–9.doi:10.1136/postgradmedj-2015-133281. PMID 26621825
  4. Barnett A (Nov 2006). "DPP-4 inhibitors and their potential role in the management of type 2 diabetes".International Journal of Clinical Practice. 60 (11): 1454–70. doi:10.1111/j.1742-1241.2006.01178.x.PMID 17073841

For research use only. Not intended for any clinical use.

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