A new orally available glucagon-like peptide-1 receptor agonist, biotinylated exendin-4, displays improved hypoglycemic effects in db/db mice

Jin, Cheng; Chae, Su Young; Son, Sohee; Kim, Tae Hyung; Um, Key An; Youn, Yu Seok; Lee, Seulki; Lee, Kang Choon

doi:10.1016/j.jconrel.2008.09.091

Cited by 58 publications

(56 citation statements)

References 26 publications

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“…The superior glucose-lowering ability of DBP-GLP-1 is likely due to improved intestinal absorption, as the plasma concentration of GLP-1 was found to be markedly increased 30 min after oral administration of DBP-GLP-1. Similar results have also been reported for biotinylated exendin-4 analogs [21].…”

Section: Chemical Modulation Strategysupporting

confidence: 90%

Emerging technologies to achieve oral delivery of GLP-1 and GLP-1 analogs for treatment of type 2 diabetes mellitus (T2DM)

Ma¹,

We²,

Yang³

et al. 2017

Can J Biotech

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Section: Chemical Modulation Strategysupporting

confidence: 90%

Emerging technologies to achieve oral delivery of GLP-1 and GLP-1 analogs for treatment of type 2 diabetes mellitus (T2DM)

Ma¹,

We²,

Yang³

et al. 2017

Can J Biotech

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“…Exendin-4 was conjugated to iron nanoparticles using the side chain of Lys27, which was the dominant reaction site on the peptide for conjugation to nanoparticles. The second potential reaction site on Lys12 side chain is hindered and could not serve as the major reaction site (31,32). The ratio of Cy5.5:exendin-4:nanoparticles was determined as 2.5:5:1 or 2.5:10:1 by spectrophotometric analysis and bicinchoninic acid protein assay.…”

Section: Resultsmentioning

confidence: 99%

GLP-1R–Targeting Magnetic Nanoparticles for Pancreatic Islet Imaging

et al. 2014

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Noninvasive assessment of pancreatic β-cell mass would tremendously aid in managing type 1 diabetes (T1D). Toward this goal, we synthesized an exendin-4 conjugated magnetic iron oxide–based nanoparticle probe targeting glucagon-like peptide 1 receptor (GLP-1R), which is highly expressed on the surface of pancreatic β-cells. In vitro studies in βTC-6, the β-cell line, showed specific accumulation of the targeted probe (termed MN-Ex10-Cy5.5) compared with nontargeted (termed MN-Cy5.5). In vivo magnetic resonance imaging showed a significant transverse relaxation time (T2) shortening in the pancreata of mice injected with the MN-Ex10-Cy5.5 probe compared with control animals injected with the nontargeted probe at 7.5 and 24 h after injection. Furthermore, ΔT2 of the pancreata of prediabetic NOD mice was significantly higher than that of diabetic NOD mice after the injection of MN-Ex10-Cy5.5, indicating the decrease of probe accumulation in these animals due to β-cell loss. Of note, ΔT2 of prediabetic and diabetic NOD mice injected with MN-Cy5.5 was not significantly changed, reflecting the nonspecific mode of accumulation of nontargeted probe. We believe our results point to the potential for using this agent for monitoring the disease development and response of T1D to therapy.

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“…, poly(lactic acid (PLA)), 3 P-gp pump-inhibiting ( e.g. , d-α-tocopheryl PEG succinate (TPGS)), 6 and vitamin 7,8,9,10,11 ( e.g. , biotin, folic acid, vitamin B 12 , and transferrin) ligands.…”

Section: Introductionmentioning

confidence: 99%

Intestinal absorption of fluorescently labeled nanoparticles

Simović

Song

Nann

et al. 2015

Nanomedicine: Nanotechnology, Biology and Medicine

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Characterization of intestinal absorption of nanoparticles is critical in the design of noninvasive anticancer, protein-based, and gene nanoparticle-based therapeutics. Here we demonstrate a general approach for the characterization of the intestinal absorption of nanoparticles and for understanding the mechanisms active in their processing within healthy intestinal cells. It is generally accepted that the cellular processing represents a major drawback of current nanoparticle-based therapeutic systems. In particular, endolysosomal trafficking causes degradation of therapeutic molecules such as proteins, lipids, acid-sensitive anticancer drugs, and genes. To date, investigations into nanoparticle processing within intestinal cells have studied mass transport through Caco-2 cells or everted rat intestinal sac models. We developed an approach to visualize directly the mechanisms of nanoparticle processing within intestinal tissue. These results clearly identify a mechanism by which healthy intestinal cells process nanoparticles and point to the possible use of this approach in the design of noninvasive nanoparticle-based therapies.

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A new orally available glucagon-like peptide-1 receptor agonist, biotinylated exendin-4, displays improved hypoglycemic effects in db/db mice

Cited by 58 publications

References 26 publications

Emerging technologies to achieve oral delivery of GLP-1 and GLP-1 analogs for treatment of type 2 diabetes mellitus (T2DM)

Emerging technologies to achieve oral delivery of GLP-1 and GLP-1 analogs for treatment of type 2 diabetes mellitus (T2DM)

GLP-1R–Targeting Magnetic Nanoparticles for Pancreatic Islet Imaging

Intestinal absorption of fluorescently labeled nanoparticles

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