Recombinant Human Pituitary adenylate cyclase-activating polypeptide type I receptor (ADCYAP1R1)

1. These results show that b-arrestin1 and b-arrestin2 exert differential actions on PAC1R internalization and PAC1R-dependent ERK1/2 activation, and suggest that the two b-arrestin isoforms may be involved in fine and precise tuning of the PAC1R signaling pathways. PMID: 29734363
2. Studies suggest that the level of stress and circulating gonadal hormones may differentially regulate the PACAPergic system in males and females to influence anxiety-like behavior and may be one mechanism underlying the discrepancies in human psychiatric disorders. [Review Article] PMID: 28610473
3. These results provide evidence for an association between ADCYAP1R1 and PTSD and indicate that there may indeed be sex differences. PMID: 28746747
4. These findings lead to a model in which E2 induces the expression of ADCYAP1R1 through binding of ERalpha at the ERE as an adaptive response to stress. Inhibition of E2/ERalpha binding to the ERE containing the rs2267735 risk allele results in reduced expression of ADCYAP1R1, diminishing estrogen regulation as an adaptive stress response and increasing risk for PTSD. PMID: 27959335
5. Data suggest that GCGR (glucagon receptor) activation proceeds via a mechanism in which transmembrane helix 6 (TM6) is held in an inactive conformation by a conserved polar core and a hydrophobic lock (involving intracellular loop 3, IC3); mutations in the corresponding polar core of GCGR or PAC1R disrupt these inhibitory elements, allow TM6 to swing outward, and induce constitutive G protein signaling. PMID: 28356352
6. Results confirmed for the first time that doxycycline specially targeted pituitary adenylate cyclase-activating polypeptide (PACAP) receptor type 1 (PAC1) imitating PACAP(30-37) and acted as an enhancer by facilitating the subsequent ligand binding and the activation of PAC1. PMID: 26700245
7. Rsults suggest that impaired contextual conditioning in the hippocampal formation may mediate the association between type I receptor of the pituitary adenylate cyclase activating polypeptideand and posttraumatic stress disorder symptoms. PMID: 25680674
8. Data show that glucocorticoid response genes NR3C1, ADCYAP1R1 and HSD11B2 were relatively hypomethylated whereas FKBP5 was hypermethylated. PMID: 26343289
9. Further investigations of genetic factors for trauma-related psychopathology should include careful assessments of the social environment PMID: 26334183
10. High child stress and an ADCYAP1R1 single-nucleotide polymorphism are associated with reduced bronchodilator response in children with asthma. PMID: 25918834
11. and its receptor (PAC1) are involved in stress response and anxiety. PMID: 23972788
12. association of variants with sudden infant death not supported PMID: 23981011
13. PAC1/PACAP receptor endocytosis contributes to ERK acktivation. PMID: 24696141
14. This review focuses on role of PAC1 receptor in brain development, behavior of transgenic animals and potential implication in human neurodevelopmental disorders. PMID: 24220567
15. PAC1 receptor (ADCYAP1R1) genotype is associated with dark-enhanced startle in both male and female children. PMID: 22776899
16. Individual differences in ADCYAP1R1 genotype may contribute to dysregulated fear circuitry known to play a central role in posttraumatic stress disorder and other anxiety disorders. PMID: 24516127
17. Data indicate that VIP and PACAP increased macrophage resistance to HIV-1 replication by inducing the synthesis of beta-chemokines CCL3 and CCL5 and IL-10 following preferential activation of the receptors VPAC2 and PAC1. PMID: 23818986
18. The findings suggest that the PACAP-PAC1 receptor pathway may play an important role in female human responses to traumatic stress PMID: 23394710
19. ADCYAP1R1 genotype may have a role in post-traumatic stress symptoms in highly traumatized African-American females PMID: 23505260
20. Genetic variation at the ADCYAP1R1 locus interacts with child abuse to shape risk of later posttraumatic stress disorder (PTSD) in women. PMID: 23280952
21. Epigenetic and genetic variants in ADVYAP1R1 are associated with asthma in Puerto Rican children. PMID: 23328528
22. [review] The Adcyap1r1 receptor single nucleotide polymorphism (SNP) is located within a predicted estrogen response element (ERE). PMID: 23147486
23. Conclude that VPAC2/PAC1 receptors require NO in series to effect cutaneous active vasodilation during heat stress in humans. PMID: 22961270
24. The increased expressions of PAC1 receptors on lactating breast may indicate a PACAP38/PAC1 interaction in the mammary gland during lactation. PMID: 22539193
25. PAC1 regulates PYK-2 tyrosine phosphorylation in a calcium-dependent manner in lung cancer cell lines. PMID: 22581436
26. Activation of Sp1 by the Ras/MAPK pathway might participate in neuron specific expression of the PAC1 gene. PMID: 22609358
27. A reported association between rs2267735 and PTSD could not be replicated in either African American or European American females in two large independent samples. PMID: 21912390
28. The present study constitutes the first characterization of the binding domains of PACAP to its specific receptor PAC1 and suggests heterogeneity within the binding mode of peptide ligands to class B GPCRs. PMID: 21185349
29. VPAC2 and/or PAC1 receptor activation is involved in cutaneous active vasodilation in humans. PMID: 20395540
30. Results indicate that VPAC1, but not VPAC2 or PAC1, up-regulation in macrophages is a common mechanism in response to acute and chronic pro-inflammatory stimuli. PMID: 20026142
31. PACAP receptor type 1 mRNA is expressed in the trigeminal, otic and superior cervical ganglia (prejunctional) and cerebral arteries (postjunctional). PMID: 11930171
32. HCT8 human colon tumor cells express PAC1, and PAC1 activation is coupled to adenylate cyclase, increase cytosolic [Ca(2+)](i), and cellular proliferation PMID: 12409223
33. Using GST pull-down assay, ARF6 binds to the hop1 but not the null domain of PAC1 receptor PMID: 12409233
34. receptors were positively coupled to adenylyl cyclase in human lung cancer, but the enzyme activity was impaired as compared to normal lung PMID: 12732341
35. Expression of functional PAC(1), VPAC(1) and VPAC(2) receptors in human prostate as well as its maintenance after malignant transformation PMID: 12948842
36. In colon cancer cell lines, PAC1 is expressed as the SV1 or HIP splice variant and is coupled to the activation only of cAMP but not of intracellular Ca2+. PMID: 14742913
37. PAC(1)-R null variant is the most relevant isoform expressed in human prostaste cancer, and may be related with the events determining the outcome of prostate cancer. PMID: 16372333
38. Stimulation of endogenously expressed PAC1 receptors with PACAP in human neuroblastoma cells increased APPsalpha secretion. PAC1R activation stimulates ERK phosphorylation. PMID: 16401644
39. PAC1-R is the predominant PACAP receptor found in fetuses, and both PAC1-R and VPAC1-R are expressed in the mature cerebellum. PMID: 16572459
40. Data demonstrate that altered neuronal proliferation/apoptosis and disrupted ependymal cilia are the main factors contributing to hydrocephalus in PAC1-overexpressing mice. PMID: 16823490
41. PACAP may regulate the biological release of peptides and serotonin from BON cells PMID: 16888199

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HGNC: 242

OMIM: 102981

KEGG: hsa:117

UniGene: Hs.377783