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DA-1229, a novel and potent DPP4 inhibitor, improves insulin resistance and delays the onset of diabetes.
TLDR
DA-1229 as a novel and selective DPP4 inhibitor improves the insulin sensitivity in HF mice and delays the onset of diabetes in young db/db mice. Expand
Discovery of DA-1229: a potent, long acting dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes.
A series of β-amino amide containing substituted piperazine-2-one derivatives was synthesized and evaluated as inhibitors of dipeptidyl pepdidase-4 (DPP-4) for the treatment of type 2 diabetes. AsExpand
Two small molecule agonists of glucagon-like peptide-1 receptor modulate the receptor activation response differently.
TLDR
Compounds 2 and B have different modes of action to activate GLP-1R, and it is confirmed that these two compounds increased calcium influx by different patterns in CHO cells expressing GLP -1R. Expand
Hepatic role in an early glucose-lowering effect by a novel dipeptidyl peptidase 4 inhibitor, evogliptin, in a rodent model of type 2 diabetes.
TLDR
It is concluded that the suppression of hepatic gluconeogenesis by evogliptin is followed by preservation of pancreatic islet, leading to remarkable and persistent glucose-lowering effect in HFD/STZ mice. Expand
Glucose exposure pattern determines glucagon-like peptide 1 receptor expression and signaling through endoplasmic reticulum stress in rat insulinoma cells.
TLDR
It is indicated that glucose fluctuation reduces GLP-1R expression through ER stress more profoundly than sustained hyperglycemia, which may contribute to the diminished response of GLp-1. Expand
Differential Protective Effects of Exenatide, an Agonist of GLP-1 Receptor and Piragliatin, a Glucokinase Activator in Beta Cell Response to Streptozotocin-Induced and Endoplasmic Reticulum Stresses
TLDR
This study is the first to observe specific modulation of 14-3-3 isoform in stress-induced beta cell death associated with progressive deterioration of type 2 diabetes and confirms the hypothesis that GKAs protect beta cells by mechanisms distinct from those underlying GLP-1R agonists. Expand
ApCPEB4, a non-prion domain containing homolog of ApCPEB, is involved in the initiation of long-term facilitation
TLDR
The findings suggest that the two different forms of CPEBs play distinct roles in LTF; ApCP EB is required for maintenance of LTF, whereas the ApCPEB4, which lacks a prion-like domain, is requiredfor the initiation of L TF. Expand
SIENG-HUAT KONG*; SOH KHEANG LOH**; ROBERT THOMAS BACHMANN‡; HARYATI ZAINAL** and KAH
Properties of palm kernel shell (PKS) biochar were studied to identify its potential for soil amendment and carbon sequestration. In this study, slow pyrolysis of PKS was conducted using the BiocharExpand
Abstract 4548: The anti-proliferative activity of TAS-108 (a steroid anti-estrogen) is augmented by high ERβ levels in breast cancer cells
TLDR
The findings underscore the molecular role of ERβ in the biology and suggest that promoting ERα/β heterodimerization may be an effective strategy to increase anti-tumor activity in breast cancer. Expand
Abstract 2146: The chemo-preventive effect of ER-β agonist on DMBA induced breast cancers
TLDR
ER-β selective agonists such as diarylpropionitrile (DPN) may inhibit breast cancer cells, and may also prevent tumor initiation or tumor growth of BrC through lowering proliferation and higher apoptosis. Expand