transcriptional

Transcriptional Intermediary Factor 2 (TIF2) (740-753) is a 14-amino acid peptide coactivator, encompassing residues 740-753 of the TIF-2 protein.

TAT peptide (TFA), a cell-penetrating peptide (GRKKRRQRRRPQ) originating from HIV-1's trans-activating transcriptional activator (Tat), facilitates intracellular delivery [1] [2].

PINT-87aa, an 87-amino acid (aa) peptide encoded by the circular form of the long intergenic non-protein-coding RNA p53-induced transcript (LINC-PINT), directly interacts with the polymerase associated factor complex (PAF1c) to inhibit the transcriptional elongation of multiple oncogenes, effectively suppressing glioblastoma cell proliferation both in vitro and in vivo [1].

PINT-87aa TFA is an 87-amino acid (aa) peptide encoded by the circular form of the long intergenic non-protein-coding RNA p53-induced transcript (LINC-PINT). It interacts directly with the polymerase-associated factor complex (PAF1c) to inhibit the transcriptional elongation of numerous oncogenes, effectively suppressing glioblastoma cell proliferation both in vitro and in vivo [1].

Cys(Npys)-TAT (47-57), a peptide fragment corresponding to the transduction domain of the TAT peptide, contains an activated cysteine residue C and can electrostatically interact with plasmid DNA. Notably, TAT is a small nuclear transcriptional activator protein encoded by HIV-1 [1].

Tat-QFNP12 is a peptide that combines a transcriptional transactivator (Tat) transmembrane domain with an inhibitor targeting the interaction between N-Myc downstream regulated gene 2 (NDRG2) and protein phosphatase Mg2+/Mn2+ dependent 1A (PPM1A). This compound effectively mitigates blood-brain barrier endothelial tight junction disruption caused by elevated levels of matrix metalloproteinase-9 (MMP-9), alleviates cerebral edema, and promotes spontaneous activity along with symmetric limb movement in a mouse model of subarachnoid hemorrhage induced by endovascular puncture. These benefits are observed at a dosage of 20 mg/kg.

The compound 4A7C-301-Nurr1 agonist is a specific agonist for the nuclear receptor-related 1 (Nurr1). By binding to the Nurr1 ligand-binding domain with an IC50 value of 48.22 nM, it enhances the transcriptional activity of both Nurr1-LBD and the full-length Nurr1, as demonstrated in reporter assays using SK-N-BE(2)C human neuroblastoma cells, with EC50 values of 6.53 and 50-70 µM, respectively. Additionally, administration of 4A7C-301-Nurr1 agonist at a dosage of 5 mg/kg per day has been shown to mitigate dopaminergic cell death in the striatum and substantia nigra pars compacta and ameliorate motor and olfactory deficits in mouse models of Parkinson's disease, circumventing the induction of dyskinesia-like behaviors. These models were induced either by the neurotoxin MPTP or by overexpression of α-synuclein.

CEF27, Epstein-Barr Virus BRLF-1 lytic 148-156 acetate corresponding to amino acids 148-156 of the BRLF1. BRLF1 is a transcriptional activator that binds directly to a GC-rich motif present in some Epstein-Barr virus (EBV) lytic gene promoters.

TAT (48-57) (TFA) is a cellular permeability peptide derived from hiv-1 transcriptional activator (TAT) protein residue 48-57.

Cyclo(CLLFVY) is an inhibitor of hypoxia-inducible factor-1 (HIF-1), exhibiting half-maximal inhibitory concentrations (IC50) of 19 μM in U2OS cells and 16 μM in MCF-7 cells. It binds to the PAS-B domain of HIF-1α, inhibiting the dimerization and transcriptional activity of HIF-1. Moreover, cyclo(CLLFVY) downregulates the expression of hypoxia response genes (such as VEGF and CAIX), demonstrating antitumor effects against HIF-1-related cancers.