VPAC and PAC receptors: From ligands to function

Dickson, Louise; Finlayson, Keith

doi:10.1016/j.pharmthera.2008.11.006

Cited by 334 publications

(333 citation statements)

References 322 publications

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“…The EC50 values for PACAP-27 mediated transglutaminase-catalysed amine incorporation (0.08 nM) and protein cross-linking activity (0.4 nM) are in-line with the affinity of PACAP-27 for the PAC1 receptor (Dickson et al, 2006;Dickson and Finlayson, 2009;Harmar et al, 2012). Furthermore, PACAP-27-induced TG2 activity was blocked by the PAC1 receptor antagonist PACAP 6-38 (Robberecht et al, 1992).…”

Section: In Vitro Modulation Of Tg2 Transamidation Activity By the Pasupporting

confidence: 62%

“…The PAC1 receptor is a member of the GPCR superfamily which activates adenylyl cyclase/cAMP/PKA (via Gsprotein coupling) and phospholipase C/DAG/PKC (via Gq-protein coupling) dependent signalling pathways (Dickson and Finlayson, 2009;Vaudry et al, 2009). The PAC1 receptor also triggers the activation of several other protein kinase cascades such as ERK1/2, JNK1/2, p38 MAPK and PKB (Monaghan et al, 2008;May et al, 2010, Castorina et al 2014.…”

Section: Introductionmentioning

confidence: 99%

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Role of transglutaminase 2 in PAC1 receptor mediated protection against hypoxia-induced cell death and neurite outgrowth in differentiating N2a neuroblastoma cells

Algarni

Hargreaves

Dickenson

2017

Biochemical Pharmacology

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Section: In Vitro Modulation Of Tg2 Transamidation Activity By the Pasupporting

confidence: 62%

Section: Introductionmentioning

confidence: 99%

Role of transglutaminase 2 in PAC1 receptor mediated protection against hypoxia-induced cell death and neurite outgrowth in differentiating N2a neuroblastoma cells

Algarni

Hargreaves

Dickenson

2017

Biochemical Pharmacology

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“…PKA is often involved in the signaling triggered by VIP [18]. Our data indicate that the effect of VIP on neuritogenesis and MYCN expression in Kelly and IMR-32 cells, as well as on AKT activity in Kelly cells, is PKA-dependent.…”

Section: Mycn-amplifiedmentioning

confidence: 59%

“…These two receptors bind VIP and PACAP equally and activate mainly the protein kinase A (PKA) and protein kinase C (PKC) signaling pathways, which induce regulation of gene expression [18]. VIP and PACAP are involved in the development of the nervous system.…”

Section: Introductionmentioning

confidence: 99%

VIP and PACAP analogs regulate therapeutic targets in high-risk neuroblastoma cells

et al. 2016

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“…In addition to reducing food intake, icv administration of PACAP modulates autonomic nerve activity (55) as well as hepatic glucose production (60). As a ligand, PACAP binds to three different G protein-coupled receptors, the PAC1 receptor (PAC1R), and the receptors originally discovered as targets of vasoactive intestinal polypeptide (VIP), VPAC1R and VPAC2R (10). Although PACAP stimulates all three receptor subtypes, it has the highest affinity for the PAC1R, whereas VIP is less likely to utilize the PAC1R due to its low binding affinity compared with the VPACRs (18,34).…”

mentioning

confidence: 99%

Intrahypothalamic pituitary adenylate cyclase-activating polypeptide regulates energy balance via site-specific actions on feeding and metabolism

Resch

Maunze

Gerhardt

et al. 2013

American Journal of Physiology-Endocrinology and Metabolism

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Resch JM, Maunze B, Gerhardt AK, Magnuson SK, Phillips KA, Choi S. Intrahypothalamic pituitary adenylate cyclase-activating polypeptide regulates energy balance via site-specific actions on feeding and metabolism. Am J Physiol Endocrinol Metab 305: E1452-E1463, 2013. First published October 22, 2013; doi:10.1152/ajpendo.00293.2013.-Numerous studies have demonstrated that both the hypothalamic paraventricular nuclei (PVN) and ventromedial nuclei (VMN) regulate energy homeostasis through behavioral and metabolic mechanisms. Receptors for pituitary adenylate cyclase-activating polypeptide (PACAP) are abundantly expressed in these nuclei, suggesting PACAP may be critical for the regulation of feeding behavior and body weight. To characterize the unique behavioral and physiological responses attributed to select hypothalamic cell groups, PACAP was site-specifically injected into the PVN or VMN. Overall food intake was significantly reduced by PACAP at both sites; however, meal pattern analysis revealed that only injections into the PVN produced significant reductions in meal size, duration, and total time spent eating. PACAP-mediated hypophagia in both the PVN and VMN was abolished by PAC1R antagonism, whereas pretreatment with a VPACR antagonist had no effect. PACAP injections into the VMN produced unique changes in metabolic parameters, including significant increases in core body temperature and spontaneous locomotor activity that was PAC1R dependent whereas, PVN injections of PACAP had no effect. Finally, PACAP-containing afferents were identified using the neuronal tracer cholera toxin subunit B (CTB) injected unilaterally into the PVN or VMN. CTB signal from PVN injections was colocalized with PACAP mRNA in the medial anterior bed nucleus of the stria terminalis, VMN, and lateral parabrachial nucleus (LPB), whereas CTB signal from VMN injections was highly colocalized with PACAP mRNA in the medial amygdala and LPB. These brain regions are known to influence energy homeostasis perhaps, in part, through PACAP projections to the PVN and VMN.feeding; activity; temperature; hypothalamus; rat PITUITARY ADENYLATE CYCLASE-ACTIVATING polypeptide (PACAP) is a key regulator of several hypothalamic systems, including stress (1), osmoregulation (17), thermoregulation (21), and body weight (27). PACAP was first discovered to influence energy homeostasis through inhibition of feeding in mice following a single intracerebroventricular (icv) injection of the peptide (39). These results combined with reports of dietspecific alterations of PACAP mRNA expression in the hypothalamic ventromedial nuclei (VMN) suggest that PACAP is responsive to nutritional status and directly tied to metabolic systems linked to energy expenditure (27,40). In addition to reducing food intake, icv administration of PACAP modulates autonomic nerve activity (55) as well as hepatic glucose production (60). As a ligand, PACAP binds to three different G protein-coupled receptors, the PAC1 receptor (PAC1R), and the receptors originally discovered as targets...

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VPAC and PAC receptors: From ligands to function

Cited by 334 publications

References 322 publications

Role of transglutaminase 2 in PAC1 receptor mediated protection against hypoxia-induced cell death and neurite outgrowth in differentiating N2a neuroblastoma cells

Role of transglutaminase 2 in PAC1 receptor mediated protection against hypoxia-induced cell death and neurite outgrowth in differentiating N2a neuroblastoma cells

VIP and PACAP analogs regulate therapeutic targets in high-risk neuroblastoma cells

Intrahypothalamic pituitary adenylate cyclase-activating polypeptide regulates energy balance via site-specific actions on feeding and metabolism

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