Previous work has shown that certain β(3)-peptides can effectively mimic the side chain display of an α-helix and inhibit interactions between proteins, both in vitro and in cultured cells. Here we describe a β(3)-peptide analog of GLP-1, CC-3(Act), that interacts with the GLP-1R extracellular domain (nGLP-1R) in vitro in a manner that competes with exendin-4 and induces GLP-1R-dependent cAMP signaling in cultured CHO-K1 cells expressing GLP-1R.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4006878 | PMC |
| http://dx.doi.org/10.1021/ol402568j | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Comprehensive three-dimensional microCT and signaling analysis reveal the teratogenic effect of 2,3,7,8-tetrachlorodibenzo-p-dioxin on craniofacial bone development in mice.
Ecotoxicol Environ Saf
January 2025
Department of Stomatology, the Affiliated Suzhou Hospital of Nanjing Medical University, Suzhou Municipal Hospital, Gusu School, Nanjing Medical University, No. 242, Guangji Road, Suzhou, Jiangsu Province 215000, China. Electronic address:
Exposure to 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) in utero can result in osteogenic defect during palatogenesis, but the effects on other craniofacial bones and underlying mechanisms remain to be characterized. By treating pregnant mice with TCDD (40 μg/kg) at the vital craniofacial patterning stages (embryonic day 8.5, 10.
View Article and Find Full Text PDFToll-like receptor 2/6-stimulated HMC-1 mast cells promote keratinocyte migration in wound healing.
PLoS One
January 2025
Departments of Microbiology, College of Medicine, Ewha Womans University, Seoul, Korea.
Mast cells, immune sentinels that respond to various stimuli in barrier organs, provide defense by expressing pattern recognition receptors, such as Toll-like receptors (TLRs). They may affect inflammatory responses and wound healing. Here, we investigated the effect of TLR2/6-stimulated mast cells on wound healing in keratinocytes.
View Article and Find Full Text PDFHuman P2X4 receptor gating is modulated by a stable cytoplasmic cap and a unique allosteric pocket.
Sci Adv
January 2025
Department of Chemical Physiology & Biochemistry, Oregon Health & Science University, Portland, OR 97239, USA.
P2X receptors (P2XRs) are adenosine 5'-triphosphate (ATP)-gated ion channels comprising homomeric and heteromeric trimers of seven subtypes (P2X1-P2X7) that confer different rates of desensitization. The helical recoil model of P2XR desensitization proposes stability of the cytoplasmic cap sets the rate of desensitization, but timing of its formation is unclear for slow-desensitizing P2XRs. We report cryo-electron microscopy structures of full-length wild-type human P2X4 receptor in apo closed, antagonist-bound inhibited, and ATP-bound desensitized states.
View Article and Find Full Text PDFComparing demographic/clinical characteristics, health care resource utilization, and costs among patients with type 2 diabetes and established atherosclerotic cardiovascular disease with and without the use of cardioprotective medications.
J Manag Care Spec Pharm
January 2025
Joslin Diabetes Center, Sequel Med Tech, Boston, MA.
Background: Type 2 diabetes (T2D) causes increased health care resource utilization (HCRU) and costs in the United States. People with T2D are more likely to have atherosclerotic cardiovascular disease (ASCVD), which is associated with significant morbidity and mortality. Medical associations recommend cardioprotective antidiabetic medications, including sodium-glucose cotransporter-2 inhibitors (SGLT2is) and glucagon-like peptide 1 receptor agonists (GLP-1 RAs), to reduce the risk of cardiovascular events in patients with T2D with established, or a high risk of, ASCVD, but not all eligible patients receive these medications.
View Article and Find Full Text PDFAddition of continuous glucose monitoring to glucagon-like peptide 1 receptor agonist treatment for type 2 diabetes mellitus - An economic evaluation.
J Manag Care Spec Pharm
January 2025
Abbott Diabetes Care, Mississauga, Ontario, Canada.
Background: Both glucagon-like peptide 1 receptor agonists (GLP-1 RAs) and continuous glucose monitoring (CGM) have been shown to improve glycated hemoglobin A1c (A1c) levels among patients with type 2 diabetes mellitus (T2DM). Recently, a US real-world study found statistically significant improvements in A1c levels among patients using GLP-1 RA and a CGM device, compared with a matched cohort receiving only GLP-1 RA.
Objectives: To assess the cost-effectiveness from a US payer perspective of initiating CGM (FreeStyle Libre Systems) in people living with T2DM using a GLP-1 RA therapy, compared with GLP-1 RA alone.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!