The Insig1/2 loop 1 peptide markedly inhibited IGF1-induced binding of PCK1 to Insig1 (Figure 1d)
- Measure
- percent_inhibition
- Value
- markedly inhibited
- Target
- Homo sapiens
- Assay
- Not reported by source
PMC12677653::PEP000001
Advanced Science · 2025
Sequence evidence
LYPCIDSHLGEPHKFKRE
Insig1/2 loop 1 peptide (143-LYPCIDSHLGEPHKFKRE-160) ... fused with a fragment of transactivator of transcription (TAT) peptide ... Insig1/2 loop1 peptide sequence, RKKRRQRRRLYPCIDSHLGEPHKFKRE
Experimental observations
The Insig1/2 loop 1 peptide markedly inhibited IGF1-induced binding of PCK1 to Insig1 (Figure 1d)
Insig1/2 loop 1 peptide ... inhibited ... Insig1 S207/Insig2 S151 phosphorylation (Figure 1e)
Insig1/2 loop 1 peptide ... inhibited ... SREBP1 activity (Figure 1f)
Insig1/2 loop 1 peptide ... inhibited ... the nuclear accumulation of SREBP1 (Figure 1g)
Insig1/2 loop 1 peptide ... inhibited ... the expression of GPAM (Figure 1h)
Insig1/2 loop 1 peptide ... inhibited ... the expression of FASN (Figure 1i)
Insig1/2 loop 1 peptide reduced the IGF1-induced increase in triglycerides (TGs) (Figure 1j)
Insig1/2 loop 1 peptide ... inhibited the IGF1-induced increase in the proliferation of Huh7 ... cells (Figure 1k)
Insig1/2 loop 1 peptide ... inhibited the IGF1-induced increase in the proliferation of ... Hep3B cells (Figure S1g)
peptide treatment ... induced cell death in HCT116 human colon cancer cells (Figure S1i)
Insig1/2 loop 1 peptide inhibited tumor growth (Figure 3a) and reduced tumor weight (Figure 3b) and volume (Figure 3c)
Insig1/2 loop 1 peptide injection ... prolonged mouse survival (Figure 3e)
combination of lenvatinib and the Insig1/2 loop 1 peptide ... exhibited an additive inhibition of tumor growth (Figure 3a-d)
combination ... prolonged mouse survival time (Figure 3e) compared with lenvatinib or the Insig1/2 loop 1 peptide alone
combination of semaglutide and the Insig1/2 loop 1 peptide demonstrated additive antitumor effects in mice fed a high-fat diet (Figure 5a-c)
combination of semaglutide and the Insig1/2 loop 1 peptide ... prolonged the survival time of mice (Figure 5c)
Intravenous injection of the LNPs with the Insig1/2 loop 1 peptide into mice did not result in obvious adverse effects, as revealed by ... H&E staining ... and blood examination (Figure S4c-k)
Insig1/2 loop 1 peptide reduced Insig1 S207/Insig2 S151 phosphorylation ... in mouse tumors (Figure 4a)
Insig1/2 loop 1 peptide reduced ... SREBP1 expression, and nuclear accumulation ... in mouse tumors (Figure 4a)
Insig1/2 loop 1 peptide reduced ... Ki67 expression ... in mouse tumors (Figure 4a)
Insig1/2 loop 1 peptide reduced lipid accumulation in tumor tissues (Figure 4b,e)
Insig1/2 loop 1 peptide ... induced cell apoptosis in tumor tissues (Figure 4c,d)
high-fat diet enhanced Insig1 S207 and Insig2 S151 phosphorylation ... This enhancement was reduced by treatment with the Insig1/2 loop 1 peptide (Figure 5f)
semaglutide administration decreased high-fat diet-increased lipid levels ... and this reduction was further promoted by combined treatment with the Insig1/2 loop 1 peptide (Figure 5d)
semaglutide administration decreased ... Ki67 expression in tumor tissues ... and this reduction was further promoted by combined treatment with the Insig1/2 loop 1 peptide (Figure 5e)
Insig1/2 loop 1 peptide markedly inhibited IGF1-induced binding of PCK1 to Insig1 ... in Hep3B cells (Figure S1d)
Insig1/2 loop 1 peptide ... inhibited ... Insig1 S207/Insig2 S151 phosphorylation ... in Hep3B cells (Figure S1e)
Insig1/2 loop 1 peptide reduced the IGF1-induced increase in triglycerides (TGs) ... in Hep3B cells (Figure S1f)
peptide treatment inhibited Insig1 S207 phosphorylation ... in HCT116 human colon cancer cells (Figure S1h)
treatment of HCC cells with the peptide inhibited IGF1-induced nuclear translocation of SREBP2 (Figure S2a)
suppressed SREBP2-mediated expression of HMGCS1 (Figure S2b)
suppressed SREBP2-mediated expression of ... LDLR (Figure S2c)
expression of the phosphorylation-mimicking Insig1 S207D mutant ... abrogated the peptide-mediated suppression of ... expression of GPAM (Figure 1l)
expression of the phosphorylation-mimicking Insig1 S207D mutant ... abrogated the peptide-mediated suppression of ... expression of FASN (Figure 1m)
treatment with LNP@Insig1/2 loop 1 peptide did not significantly alter the mRNA expression levels of lipid synthesis genes FASN, GPAM, and HMGCS1, or LDLR (Figure S4l-o)
Insig1/2 loop 1 peptide exhibited much stronger binding affinity for the S90-phosphorylated GST-PCK1 protein than nonphosphorylated GST-PCK1 (Figure 1b,c)
Local peptide labels such as P1, PEP1, or peptide 1 are grouped only within this paper and are not assumed to represent the same molecule across publications.