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Paper-scoped peptide mentionSequence reported

Insig1/2 loop 1 peptide

PMC12677653::PEP000001

Source publication

Inhibition of Tumor Lipogenesis and Growth by Peptide‐Based Targeting of SREBP Activation

Advanced Science · 2025

Sequence status
reported
Standardization
Sequence ready
Source location
text
Activity records
36

Sequence evidence

Reported molecular identity

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

Resolved peptide links

Experimental observations

Records linked to this mention

Metabolic/CardiovascularAntibacterialPositive observation
Record detail

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
Source publication
AnticancerAntibacterialPositive observation
Record detail

Insig1/2 loop 1 peptide ... inhibited the IGF1-induced increase in the proliferation of Huh7 ... cells (Figure 1k)

Measure
percent_inhibition
Value
inhibited
Target
Homo sapiens
Assay
Not reported by source
Source publication
AnticancerAntibacterialPositive observation
Record detail

Insig1/2 loop 1 peptide ... inhibited the IGF1-induced increase in the proliferation of ... Hep3B cells (Figure S1g)

Measure
percent_inhibition
Value
inhibited
Target
Homo sapiens
Assay
Not reported by source
Source publication
AnticancerAntibacterialPositive observation
Record detail

Insig1/2 loop 1 peptide inhibited tumor growth (Figure 3a) and reduced tumor weight (Figure 3b) and volume (Figure 3c)

Measure
percent_inhibition
Value
inhibited tumor growth
Target
Mus musculus
Assay
Not reported by source
Source publication
AnticancerAntibacterialPositive observation
Record detail

combination of lenvatinib and the Insig1/2 loop 1 peptide ... exhibited an additive inhibition of tumor growth (Figure 3a-d)

Measure
percent_inhibition
Value
additive inhibition
Target
Mus musculus
Assay
Not reported by source
Source publication
AnticancerGeneral ToxicPositive observation
Record detail

combination ... prolonged mouse survival time (Figure 3e) compared with lenvatinib or the Insig1/2 loop 1 peptide alone

Measure
survival_rate
Value
prolonged mouse survival time
Target
Mus musculus
Assay
Not reported by source
Source publication
AnticancerAntibacterialPositive observation
Record detail

combination of semaglutide and the Insig1/2 loop 1 peptide demonstrated additive antitumor effects in mice fed a high-fat diet (Figure 5a-c)

Measure
percent_inhibition
Value
additive antitumor effects
Target
Mus musculus
Assay
Not reported by source
Source publication
AnticancerGeneral ToxicPositive observation
Record detail

combination of semaglutide and the Insig1/2 loop 1 peptide ... prolonged the survival time of mice (Figure 5c)

Measure
survival_rate
Value
prolonged the survival time
Target
Mus musculus
Assay
Not reported by source
Source publication
ToxicityGeneral ToxicNegative / threshold
Record detail

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)

Measure
qualitative
Value
no obvious adverse effects
Target
Mus musculus
Assay
Not reported by source
Source publication
Metabolic/CardiovascularAntibacterialPositive observation
Record detail

Insig1/2 loop 1 peptide reduced Insig1 S207/Insig2 S151 phosphorylation ... in mouse tumors (Figure 4a)

Measure
percent_inhibition
Value
reduced
Target
Mus musculus
Assay
Not reported by source
Source publication
Metabolic/CardiovascularAntibacterialPositive observation
Record detail

Insig1/2 loop 1 peptide reduced ... SREBP1 expression, and nuclear accumulation ... in mouse tumors (Figure 4a)

Measure
percent_inhibition
Value
reduced
Target
Mus musculus
Assay
Not reported by source
Source publication
Metabolic/CardiovascularAntibacterialPositive observation
Record detail

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)

Measure
percent_inhibition
Value
reduced
Target
Mus musculus
Assay
Not reported by source
Source publication
Metabolic/CardiovascularAntibacterialPositive observation
Record detail

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)

Measure
percent_inhibition
Value
reduced
Target
Mus musculus
Assay
Not reported by source
Source publication
AnticancerAntibacterialPositive observation
Record detail

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)

Measure
percent_inhibition
Value
reduced
Target
Mus musculus
Assay
Not reported by source
Source publication
Metabolic/CardiovascularAntibacterialPositive observation
Record detail

Insig1/2 loop 1 peptide markedly inhibited IGF1-induced binding of PCK1 to Insig1 ... in Hep3B cells (Figure S1d)

Measure
percent_inhibition
Value
inhibited
Target
Homo sapiens
Assay
Not reported by source
Source publication
Metabolic/CardiovascularAntibacterialPositive observation
Record detail

Insig1/2 loop 1 peptide ... inhibited ... Insig1 S207/Insig2 S151 phosphorylation ... in Hep3B cells (Figure S1e)

Measure
percent_inhibition
Value
inhibited
Target
Homo sapiens
Assay
Not reported by source
Source publication
Metabolic/CardiovascularAntibacterialPositive observation
Record detail

Insig1/2 loop 1 peptide reduced the IGF1-induced increase in triglycerides (TGs) ... in Hep3B cells (Figure S1f)

Measure
percent_inhibition
Value
reduced
Target
Homo sapiens
Assay
Not reported by source
Source publication
Metabolic/CardiovascularAntibacterialPositive observation
Record detail

peptide treatment inhibited Insig1 S207 phosphorylation ... in HCT116 human colon cancer cells (Figure S1h)

Measure
percent_inhibition
Value
inhibited
Target
Homo sapiens
Assay
Not reported by source
Source publication
Metabolic/CardiovascularAntibacterialPositive observation
Record detail

treatment of HCC cells with the peptide inhibited IGF1-induced nuclear translocation of SREBP2 (Figure S2a)

Measure
percent_inhibition
Value
inhibited
Target
Homo sapiens
Assay
Not reported by source
Source publication
Metabolic/CardiovascularAntibacterialPositive observation
Record detail

expression of the phosphorylation-mimicking Insig1 S207D mutant ... abrogated the peptide-mediated suppression of ... expression of GPAM (Figure 1l)

Measure
percent_inhibition
Value
abrogated
Target
Homo sapiens
Assay
Not reported by source
Source publication
Metabolic/CardiovascularAntibacterialPositive observation
Record detail

expression of the phosphorylation-mimicking Insig1 S207D mutant ... abrogated the peptide-mediated suppression of ... expression of FASN (Figure 1m)

Measure
percent_inhibition
Value
abrogated
Target
Homo sapiens
Assay
Not reported by source
Source publication
Metabolic/CardiovascularAntibacterialPositive observation
Record detail

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)

Measure
percent_inhibition
Value
did not significantly alter
Target
Mus musculus
Assay
Not reported by source
Source publication
Metabolic/CardiovascularACE InhibitorPositive observation
Record detail

Insig1/2 loop 1 peptide exhibited much stronger binding affinity for the S90-phosphorylated GST-PCK1 protein than nonphosphorylated GST-PCK1 (Figure 1b,c)

Measure
Kd
Value
much stronger binding affinity
Target
GST-PCK1 pS90
Assay
Not reported by source
Source publication

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.