biostudies-literatureUnknown54(5)Fan GPAC1-R is a recognized preferential receptor for the neuropeptide of pituitary adenylate cyclase-activating polypeptide (PACAP), which mediates neuroprotective and nerve regenerative activities of PACAP. In this study, we found that in both PAC1R-CHO cells with high expression of PAC1R-eGFP and retinal ganglion cells (RGC-5) with the natural expression of PAC1-R, oligo-peptide PACAP(28-38) and the positively charged arginine-rich penetrating peptide TAT, as positive allosteric modulators of PAC1-R, significantly trigger the nuclear translocation of PAC1-R. The chromatin immunoprecipitation (ChIP)-PCR results show that the nuclear translocated PAC1-R binds with the promoter regions of <i>PAC1-R</i> and its specific ligand <i>PACAP</i>. The up-regulated promoter activities of <i>PAC1-R</i> aActa biochimica et biophysica Sinica657-672https://www.ebi.ac.uk/biostudies/studies/S-EPMC9828401biostudies-literaturePositive allosteric regulation of PAC1-R up-regulates PAC1-R and its specific ligand PACAP.PMC9828401Tao ZFan GYu RZhang HChen SfalsePositive allosteric regulation of PAC1-R up-regulates PAC1-R and its specific ligand PACAP.PAC1-R is a recognized preferential receptor for the neuropeptide of pituitary adenylate cyclase-activating polypeptide (PACAP), which mediates neuroprotective and nerve regenerative activities of PACAP. In this study, we found that in both PAC1R-CHO cells with high expression of PAC1R-eGFP and retinal ganglion cells (RGC-5) with the natural expression of PAC1-R, oligo-peptide PACAP(28-38) and the positively charged arginine-rich penetrating peptide TAT, as positive allosteric modulators of PAC1-R, significantly trigger the nuclear translocation of PAC1-R. The chromatin immunoprecipitation (ChIP)-PCR results show that the nuclear translocated PAC1-R binds with the promoter regions of <i>PAC1-R</i> and its specific ligand <i>PACAP</i>. The up-regulated promoter activities of <i>PAC1-R</i> a2022-01-01T00:00:00Z2022 May2025-04-19T04:46:19.177Z2025-02-19T03:26:17.241ZS-EPMC98284013559347110.3724/abbs.2022041