ParkinsonCanadaV1, PascalFrancis, Corpus, bibRecord, 000460

Pituitary Adenylate Cyclase-Activating Polypeptide: Focus on Structure-Activity Relationships of a Neuroprotective Peptide

Identifieur interne : 000460 ( PascalFrancis/Corpus ); précédent : 000459; suivant : 000461

Pituitary Adenylate Cyclase-Activating Polypeptide: Focus on Structure-Activity Relationships of a Neuroprotective Peptide

Auteurs : S. Bourgault ; D. Vaudry ; A. Dejda ; N. D. Doan ; H. Vaudry ; A. Fournier

Source :

Current medicinal chemistry [ 0929-8673 ] ; 2009.

RBID : Pascal:10-0131039

Descripteurs français

Pascal (Inist)
- Peptide PACAP, Relation structure activité, Neuroprotecteur, Récepteur PAC1, Maladie dégénérative, Pathologie du système nerveux, In vitro, In vivo, Article synthèse, Agoniste, Affinité, Traitement, Neurone, Mécanisme action, Structure secondaire, Sélectivité, Récepteur couplé protéine G.

English descriptors

KwdEn :
- Affinity, Agonist, Degenerative disease, G protein coupled receptor, In vitro, In vivo, Mechanism of action, Nervous system diseases, Neuron, Neuroprotective agent, PAC1 receptor, Pituitary adenylate cyclase activating peptide, Review, Secondary structure, Selectivity, Structure activity relation, Treatment.

Abstract

Pituitary adenylate cyclase-activating polypeptide (PACAP) is a 38-amino acid peptide that was initially isolated from hypothalamus extracts on the basis of its ability to stimulate the production of cAMP in cultured pituitary cells. Recent studies have shown that PACAP exerts potent neuroprotective effects not only in vitro but also in in vivo models of Parkinson's disease, Huntington's disease, traumatic brain injury and stroke. The protective effects of PACAP are based on its capacity to prevent neuronal apoptosis by acting directly on neurons or indirectly through the release of neuroprotective factors by astrocytes. These biological activities are mainly mediated through activation of the PAC 1 receptor which is currently considered as a potential target for the treatment of neurodegenerative diseases. However, the use of native PACAP, the endogenous ligand of PAC1, as an efficient neuroprotective drug is actually limited by its rapid degradation. Moreover, injection of PACAP to human induces peripheral side effects which are mainly mediated through VPAC I and VPAC2 receptors. Strategies to overcome these compromising conditions include the development of metabolically stable analogs of PACAP acting as selective agonists of the PAC1 receptor. This review presents an overview of the structure-activity relationships of PACAP and summarizes the molecular and conformational requirements for activation of PAC1 receptor. The applicability of PACAP analogs as therapeutic agents for treatment of neurodegenerative diseases is also discussed.

Notice en format standard (ISO 2709)

Pour connaître la documentation sur le format Inist Standard.

A01	`01`	`1`		`@0 0929-8673`
A03		`1`		`@0 Curr. med. chem.`
A05				`@2 16`
A06				`@2 33`
A08	`01`	`1`	`ENG`	`@1 Pituitary Adenylate Cyclase-Activating Polypeptide: Focus on Structure-Activity Relationships of a Neuroprotective Peptide`
A11	`01`	`1`		`@1 BOURGAULT (S.)`
A11	`02`	`1`		`@1 VAUDRY (D.)`
A11	`03`	`1`		`@1 DEJDA (A.)`
A11	`04`	`1`		`@1 DOAN (N. D.)`
A11	`05`	`1`		`@1 VAUDRY (H.)`
A11	`06`	`1`		`@1 FOURNIER (A.)`
A14	`01`			`@1 INRS-Institut Armand-Frappier, Institut National de la Recherche Scientifique, 531 boul. des Prairies @2 Ville de Laval, Qc, H7V 1B7 @3 CAN @Z 1 aut. @Z 3 aut. @Z 4 aut. @Z 6 aut.`
A14	`02`			`@1 Laboratoire de Neuroendocrinologie Cellulaire et Moléculaire, INSERM U413, Université de Rouen @2 76821 Mont-Saint-Aignan @3 FRA @Z 1 aut. @Z 2 aut. @Z 5 aut.`
A14	`03`			`@1 International Associated Laboratory Samuel de Champlain (INSERM- INRS) @3 FRA @Z 1 aut. @Z 2 aut. @Z 3 aut. @Z 4 aut. @Z 5 aut. @Z 6 aut.`
A20				`@1 4462-4480`
A21				`@1 2009`
A23	`01`			`@0 ENG`
A43	`01`			`@1 INIST @2 22999 @5 354000171487100080`
A44				`@0 0000 @1 © 2010 INIST-CNRS. All rights reserved.`
A45				`@0 183 ref.`
A47	`01`	`1`		`@0 10-0131039`
A60				`@1 P`
A61				`@0 A`
A64	`01`	`1`		`@0 Current medicinal chemistry`
A66	`01`			`@0 USA`
C01	`01`		`ENG`	@0 Pituitary adenylate cyclase-activating polypeptide (PACAP) is a 38-amino acid peptide that was initially isolated from hypothalamus extracts on the basis of its ability to stimulate the production of cAMP in cultured pituitary cells. Recent studies have shown that PACAP exerts potent neuroprotective effects not only in vitro but also in in vivo models of Parkinson's disease, Huntington's disease, traumatic brain injury and stroke. The protective effects of PACAP are based on its capacity to prevent neuronal apoptosis by acting directly on neurons or indirectly through the release of neuroprotective factors by astrocytes. These biological activities are mainly mediated through activation of the PAC 1 receptor which is currently considered as a potential target for the treatment of neurodegenerative diseases. However, the use of native PACAP, the endogenous ligand of PAC1, as an efficient neuroprotective drug is actually limited by its rapid degradation. Moreover, injection of PACAP to human induces peripheral side effects which are mainly mediated through VPAC I and VPAC2 receptors. Strategies to overcome these compromising conditions include the development of metabolically stable analogs of PACAP acting as selective agonists of the PAC1 receptor. This review presents an overview of the structure-activity relationships of PACAP and summarizes the molecular and conformational requirements for activation of PAC1 receptor. The applicability of PACAP analogs as therapeutic agents for treatment of neurodegenerative diseases is also discussed.
C02	`01`	`X`		`@0 002B02B10`
C02	`02`	`X`		`@0 002B02B09F`
C03	`01`	`X`	`FRE`	`@0 Peptide PACAP @5 01`
C03	`01`	`X`	`ENG`	`@0 Pituitary adenylate cyclase activating peptide @5 01`
C03	`01`	`X`	`SPA`	`@0 Péptido PACAP @5 01`
C03	`02`	`X`	`FRE`	`@0 Relation structure activité @5 02`
C03	`02`	`X`	`ENG`	`@0 Structure activity relation @5 02`
C03	`02`	`X`	`SPA`	`@0 Relación estructura actividad @5 02`
C03	`03`	`X`	`FRE`	`@0 Neuroprotecteur @5 03`
C03	`03`	`X`	`ENG`	`@0 Neuroprotective agent @5 03`
C03	`03`	`X`	`SPA`	`@0 Neuroprotector @5 03`
C03	`04`	`X`	`FRE`	`@0 Récepteur PAC1 @5 04`
C03	`04`	`X`	`ENG`	`@0 PAC1 receptor @5 04`
C03	`04`	`X`	`SPA`	`@0 Receptor PAC1 @5 04`
C03	`05`	`X`	`FRE`	`@0 Maladie dégénérative @5 05`
C03	`05`	`X`	`ENG`	`@0 Degenerative disease @5 05`
C03	`05`	`X`	`SPA`	`@0 Enfermedad degenerativa @5 05`
C03	`06`	`X`	`FRE`	`@0 Pathologie du système nerveux @5 06`
C03	`06`	`X`	`ENG`	`@0 Nervous system diseases @5 06`
C03	`06`	`X`	`SPA`	`@0 Sistema nervioso patología @5 06`
C03	`07`	`X`	`FRE`	`@0 In vitro @5 07`
C03	`07`	`X`	`ENG`	`@0 In vitro @5 07`
C03	`07`	`X`	`SPA`	`@0 In vitro @5 07`
C03	`08`	`X`	`FRE`	`@0 In vivo @5 08`
C03	`08`	`X`	`ENG`	`@0 In vivo @5 08`
C03	`08`	`X`	`SPA`	`@0 In vivo @5 08`
C03	`09`	`X`	`FRE`	`@0 Article synthèse @5 09`
C03	`09`	`X`	`ENG`	`@0 Review @5 09`
C03	`09`	`X`	`SPA`	`@0 Artículo síntesis @5 09`
C03	`10`	`X`	`FRE`	`@0 Agoniste @5 10`
C03	`10`	`X`	`ENG`	`@0 Agonist @5 10`
C03	`10`	`X`	`SPA`	`@0 Agonista @5 10`
C03	`11`	`X`	`FRE`	`@0 Affinité @5 11`
C03	`11`	`X`	`ENG`	`@0 Affinity @5 11`
C03	`11`	`X`	`SPA`	`@0 Afinidad @5 11`
C03	`12`	`X`	`FRE`	`@0 Traitement @5 12`
C03	`12`	`X`	`ENG`	`@0 Treatment @5 12`
C03	`12`	`X`	`SPA`	`@0 Tratamiento @5 12`
C03	`13`	`X`	`FRE`	`@0 Neurone @5 13`
C03	`13`	`X`	`ENG`	`@0 Neuron @5 13`
C03	`13`	`X`	`SPA`	`@0 Neurona @5 13`
C03	`14`	`X`	`FRE`	`@0 Mécanisme action @5 14`
C03	`14`	`X`	`ENG`	`@0 Mechanism of action @5 14`
C03	`14`	`X`	`SPA`	`@0 Mecanismo acción @5 14`
C03	`15`	`X`	`FRE`	`@0 Structure secondaire @5 15`
C03	`15`	`X`	`ENG`	`@0 Secondary structure @5 15`
C03	`15`	`X`	`SPA`	`@0 Estructura secundaria @5 15`
C03	`16`	`X`	`FRE`	`@0 Sélectivité @5 16`
C03	`16`	`X`	`ENG`	`@0 Selectivity @5 16`
C03	`16`	`X`	`SPA`	`@0 Selectividad @5 16`
C03	`17`	`X`	`FRE`	`@0 Récepteur couplé protéine G @5 32`
C03	`17`	`X`	`ENG`	`@0 G protein coupled receptor @5 32`
C03	`17`	`X`	`SPA`	`@0 Receptor acoplado proteína G @5 32`
N21				`@1 081`

Format Inist (serveur)

NO :	PASCAL 10-0131039 INIST
ET :	Pituitary Adenylate Cyclase-Activating Polypeptide: Focus on Structure-Activity Relationships of a Neuroprotective Peptide
AU :	BOURGAULT (S.); VAUDRY (D.); DEJDA (A.); DOAN (N. D.); VAUDRY (H.); FOURNIER (A.)
AF :	INRS-Institut Armand-Frappier, Institut National de la Recherche Scientifique, 531 boul. des Prairies/Ville de Laval, Qc, H7V 1B7/Canada (1 aut., 3 aut., 4 aut., 6 aut.); Laboratoire de Neuroendocrinologie Cellulaire et Moléculaire, INSERM U413, Université de Rouen/76821 Mont-Saint-Aignan/France (1 aut., 2 aut., 5 aut.); International Associated Laboratory Samuel de Champlain (INSERM- INRS)/France (1 aut., 2 aut., 3 aut., 4 aut., 5 aut., 6 aut.)
DT :	Publication en série; Niveau analytique
SO :	Current medicinal chemistry; ISSN 0929-8673; Etats-Unis; Da. 2009; Vol. 16; No. 33; Pp. 4462-4480; Bibl. 183 ref.
LA :	Anglais
EA :	Pituitary adenylate cyclase-activating polypeptide (PACAP) is a 38-amino acid peptide that was initially isolated from hypothalamus extracts on the basis of its ability to stimulate the production of cAMP in cultured pituitary cells. Recent studies have shown that PACAP exerts potent neuroprotective effects not only in vitro but also in in vivo models of Parkinson's disease, Huntington's disease, traumatic brain injury and stroke. The protective effects of PACAP are based on its capacity to prevent neuronal apoptosis by acting directly on neurons or indirectly through the release of neuroprotective factors by astrocytes. These biological activities are mainly mediated through activation of the PAC 1 receptor which is currently considered as a potential target for the treatment of neurodegenerative diseases. However, the use of native PACAP, the endogenous ligand of PAC1, as an efficient neuroprotective drug is actually limited by its rapid degradation. Moreover, injection of PACAP to human induces peripheral side effects which are mainly mediated through VPAC I and VPAC2 receptors. Strategies to overcome these compromising conditions include the development of metabolically stable analogs of PACAP acting as selective agonists of the PAC1 receptor. This review presents an overview of the structure-activity relationships of PACAP and summarizes the molecular and conformational requirements for activation of PAC1 receptor. The applicability of PACAP analogs as therapeutic agents for treatment of neurodegenerative diseases is also discussed.
CC :	002B02B10; 002B02B09F
FD :	Peptide PACAP; Relation structure activité; Neuroprotecteur; Récepteur PAC1; Maladie dégénérative; Pathologie du système nerveux; In vitro; In vivo; Article synthèse; Agoniste; Affinité; Traitement; Neurone; Mécanisme action; Structure secondaire; Sélectivité; Récepteur couplé protéine G
ED :	Pituitary adenylate cyclase activating peptide; Structure activity relation; Neuroprotective agent; PAC1 receptor; Degenerative disease; Nervous system diseases; In vitro; In vivo; Review; Agonist; Affinity; Treatment; Neuron; Mechanism of action; Secondary structure; Selectivity; G protein coupled receptor
SD :	Péptido PACAP; Relación estructura actividad; Neuroprotector; Receptor PAC1; Enfermedad degenerativa; Sistema nervioso patología; In vitro; In vivo; Artículo síntesis; Agonista; Afinidad; Tratamiento; Neurona; Mecanismo acción; Estructura secundaria; Selectividad; Receptor acoplado proteína G
LO :	INIST-22999.354000171487100080
ID :	10-0131039

Links to Exploration step

Pascal:10-0131039

Le document en format XML

<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en" level="a">Pituitary Adenylate Cyclase-Activating Polypeptide: Focus on Structure-Activity Relationships of a Neuroprotective Peptide</title>
<author><name sortKey="Bourgault, S" sort="Bourgault, S" uniqKey="Bourgault S" first="S." last="Bourgault">S. Bourgault</name>
<affiliation><inist:fA14 i1="01"><s1>INRS-Institut Armand-Frappier, Institut National de la Recherche Scientifique, 531 boul. des Prairies</s1>
<s2>Ville de Laval, Qc, H7V 1B7</s2>
<s3>CAN</s3>
<sZ>1 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>6 aut.</sZ>
</inist:fA14>
</affiliation>
<affiliation><inist:fA14 i1="02"><s1>Laboratoire de Neuroendocrinologie Cellulaire et Moléculaire, INSERM U413, Université de Rouen</s1>
<s2>76821 Mont-Saint-Aignan</s2>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>2 aut.</sZ>
<sZ>5 aut.</sZ>
</inist:fA14>
</affiliation>
<affiliation><inist:fA14 i1="03"><s1>International Associated Laboratory Samuel de Champlain (INSERM- INRS)</s1>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>2 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>5 aut.</sZ>
<sZ>6 aut.</sZ>
</inist:fA14>
</affiliation>
</author>
<author><name sortKey="Vaudry, D" sort="Vaudry, D" uniqKey="Vaudry D" first="D." last="Vaudry">D. Vaudry</name>
<affiliation><inist:fA14 i1="02"><s1>Laboratoire de Neuroendocrinologie Cellulaire et Moléculaire, INSERM U413, Université de Rouen</s1>
<s2>76821 Mont-Saint-Aignan</s2>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>2 aut.</sZ>
<sZ>5 aut.</sZ>
</inist:fA14>
</affiliation>
<affiliation><inist:fA14 i1="03"><s1>International Associated Laboratory Samuel de Champlain (INSERM- INRS)</s1>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>2 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>5 aut.</sZ>
<sZ>6 aut.</sZ>
</inist:fA14>
</affiliation>
</author>
<author><name sortKey="Dejda, A" sort="Dejda, A" uniqKey="Dejda A" first="A." last="Dejda">A. Dejda</name>
<affiliation><inist:fA14 i1="01"><s1>INRS-Institut Armand-Frappier, Institut National de la Recherche Scientifique, 531 boul. des Prairies</s1>
<s2>Ville de Laval, Qc, H7V 1B7</s2>
<s3>CAN</s3>
<sZ>1 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>6 aut.</sZ>
</inist:fA14>
</affiliation>
<affiliation><inist:fA14 i1="03"><s1>International Associated Laboratory Samuel de Champlain (INSERM- INRS)</s1>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>2 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>5 aut.</sZ>
<sZ>6 aut.</sZ>
</inist:fA14>
</affiliation>
</author>
<author><name sortKey="Doan, N D" sort="Doan, N D" uniqKey="Doan N" first="N. D." last="Doan">N. D. Doan</name>
<affiliation><inist:fA14 i1="01"><s1>INRS-Institut Armand-Frappier, Institut National de la Recherche Scientifique, 531 boul. des Prairies</s1>
<s2>Ville de Laval, Qc, H7V 1B7</s2>
<s3>CAN</s3>
<sZ>1 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>6 aut.</sZ>
</inist:fA14>
</affiliation>
<affiliation><inist:fA14 i1="03"><s1>International Associated Laboratory Samuel de Champlain (INSERM- INRS)</s1>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>2 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>5 aut.</sZ>
<sZ>6 aut.</sZ>
</inist:fA14>
</affiliation>
</author>
<author><name sortKey="Vaudry, H" sort="Vaudry, H" uniqKey="Vaudry H" first="H." last="Vaudry">H. Vaudry</name>
<affiliation><inist:fA14 i1="02"><s1>Laboratoire de Neuroendocrinologie Cellulaire et Moléculaire, INSERM U413, Université de Rouen</s1>
<s2>76821 Mont-Saint-Aignan</s2>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>2 aut.</sZ>
<sZ>5 aut.</sZ>
</inist:fA14>
</affiliation>
<affiliation><inist:fA14 i1="03"><s1>International Associated Laboratory Samuel de Champlain (INSERM- INRS)</s1>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>2 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>5 aut.</sZ>
<sZ>6 aut.</sZ>
</inist:fA14>
</affiliation>
</author>
<author><name sortKey="Fournier, A" sort="Fournier, A" uniqKey="Fournier A" first="A." last="Fournier">A. Fournier</name>
<affiliation><inist:fA14 i1="01"><s1>INRS-Institut Armand-Frappier, Institut National de la Recherche Scientifique, 531 boul. des Prairies</s1>
<s2>Ville de Laval, Qc, H7V 1B7</s2>
<s3>CAN</s3>
<sZ>1 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>6 aut.</sZ>
</inist:fA14>
</affiliation>
<affiliation><inist:fA14 i1="03"><s1>International Associated Laboratory Samuel de Champlain (INSERM- INRS)</s1>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>2 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>5 aut.</sZ>
<sZ>6 aut.</sZ>
</inist:fA14>
</affiliation>
</author>
</titleStmt>
<publicationStmt><idno type="wicri:source">INIST</idno>
<idno type="inist">10-0131039</idno>
<date when="2009">2009</date>
<idno type="stanalyst">PASCAL 10-0131039 INIST</idno>
<idno type="RBID">Pascal:10-0131039</idno>
<idno type="wicri:Area/PascalFrancis/Corpus">000460</idno>
</publicationStmt>
<sourceDesc><biblStruct><analytic><title xml:lang="en" level="a">Pituitary Adenylate Cyclase-Activating Polypeptide: Focus on Structure-Activity Relationships of a Neuroprotective Peptide</title>
<author><name sortKey="Bourgault, S" sort="Bourgault, S" uniqKey="Bourgault S" first="S." last="Bourgault">S. Bourgault</name>
<affiliation><inist:fA14 i1="01"><s1>INRS-Institut Armand-Frappier, Institut National de la Recherche Scientifique, 531 boul. des Prairies</s1>
<s2>Ville de Laval, Qc, H7V 1B7</s2>
<s3>CAN</s3>
<sZ>1 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>6 aut.</sZ>
</inist:fA14>
</affiliation>
<affiliation><inist:fA14 i1="02"><s1>Laboratoire de Neuroendocrinologie Cellulaire et Moléculaire, INSERM U413, Université de Rouen</s1>
<s2>76821 Mont-Saint-Aignan</s2>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>2 aut.</sZ>
<sZ>5 aut.</sZ>
</inist:fA14>
</affiliation>
<affiliation><inist:fA14 i1="03"><s1>International Associated Laboratory Samuel de Champlain (INSERM- INRS)</s1>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>2 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>5 aut.</sZ>
<sZ>6 aut.</sZ>
</inist:fA14>
</affiliation>
</author>
<author><name sortKey="Vaudry, D" sort="Vaudry, D" uniqKey="Vaudry D" first="D." last="Vaudry">D. Vaudry</name>
<affiliation><inist:fA14 i1="02"><s1>Laboratoire de Neuroendocrinologie Cellulaire et Moléculaire, INSERM U413, Université de Rouen</s1>
<s2>76821 Mont-Saint-Aignan</s2>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>2 aut.</sZ>
<sZ>5 aut.</sZ>
</inist:fA14>
</affiliation>
<affiliation><inist:fA14 i1="03"><s1>International Associated Laboratory Samuel de Champlain (INSERM- INRS)</s1>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>2 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>5 aut.</sZ>
<sZ>6 aut.</sZ>
</inist:fA14>
</affiliation>
</author>
<author><name sortKey="Dejda, A" sort="Dejda, A" uniqKey="Dejda A" first="A." last="Dejda">A. Dejda</name>
<affiliation><inist:fA14 i1="01"><s1>INRS-Institut Armand-Frappier, Institut National de la Recherche Scientifique, 531 boul. des Prairies</s1>
<s2>Ville de Laval, Qc, H7V 1B7</s2>
<s3>CAN</s3>
<sZ>1 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>6 aut.</sZ>
</inist:fA14>
</affiliation>
<affiliation><inist:fA14 i1="03"><s1>International Associated Laboratory Samuel de Champlain (INSERM- INRS)</s1>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>2 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>5 aut.</sZ>
<sZ>6 aut.</sZ>
</inist:fA14>
</affiliation>
</author>
<author><name sortKey="Doan, N D" sort="Doan, N D" uniqKey="Doan N" first="N. D." last="Doan">N. D. Doan</name>
<affiliation><inist:fA14 i1="01"><s1>INRS-Institut Armand-Frappier, Institut National de la Recherche Scientifique, 531 boul. des Prairies</s1>
<s2>Ville de Laval, Qc, H7V 1B7</s2>
<s3>CAN</s3>
<sZ>1 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>6 aut.</sZ>
</inist:fA14>
</affiliation>
<affiliation><inist:fA14 i1="03"><s1>International Associated Laboratory Samuel de Champlain (INSERM- INRS)</s1>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>2 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>5 aut.</sZ>
<sZ>6 aut.</sZ>
</inist:fA14>
</affiliation>
</author>
<author><name sortKey="Vaudry, H" sort="Vaudry, H" uniqKey="Vaudry H" first="H." last="Vaudry">H. Vaudry</name>
<affiliation><inist:fA14 i1="02"><s1>Laboratoire de Neuroendocrinologie Cellulaire et Moléculaire, INSERM U413, Université de Rouen</s1>
<s2>76821 Mont-Saint-Aignan</s2>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>2 aut.</sZ>
<sZ>5 aut.</sZ>
</inist:fA14>
</affiliation>
<affiliation><inist:fA14 i1="03"><s1>International Associated Laboratory Samuel de Champlain (INSERM- INRS)</s1>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>2 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>5 aut.</sZ>
<sZ>6 aut.</sZ>
</inist:fA14>
</affiliation>
</author>
<author><name sortKey="Fournier, A" sort="Fournier, A" uniqKey="Fournier A" first="A." last="Fournier">A. Fournier</name>
<affiliation><inist:fA14 i1="01"><s1>INRS-Institut Armand-Frappier, Institut National de la Recherche Scientifique, 531 boul. des Prairies</s1>
<s2>Ville de Laval, Qc, H7V 1B7</s2>
<s3>CAN</s3>
<sZ>1 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>6 aut.</sZ>
</inist:fA14>
</affiliation>
<affiliation><inist:fA14 i1="03"><s1>International Associated Laboratory Samuel de Champlain (INSERM- INRS)</s1>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>2 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>5 aut.</sZ>
<sZ>6 aut.</sZ>
</inist:fA14>
</affiliation>
</author>
</analytic>
<series><title level="j" type="main">Current medicinal chemistry</title>
<title level="j" type="abbreviated">Curr. med. chem.</title>
<idno type="ISSN">0929-8673</idno>
<imprint><date when="2009">2009</date>
</imprint>
</series>
</biblStruct>
</sourceDesc>
<seriesStmt><title level="j" type="main">Current medicinal chemistry</title>
<title level="j" type="abbreviated">Curr. med. chem.</title>
<idno type="ISSN">0929-8673</idno>
</seriesStmt>
</fileDesc>
<profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Affinity</term>
<term>Agonist</term>
<term>Degenerative disease</term>
<term>G protein coupled receptor</term>
<term>In vitro</term>
<term>In vivo</term>
<term>Mechanism of action</term>
<term>Nervous system diseases</term>
<term>Neuron</term>
<term>Neuroprotective agent</term>
<term>PAC1 receptor</term>
<term>Pituitary adenylate cyclase activating peptide</term>
<term>Review</term>
<term>Secondary structure</term>
<term>Selectivity</term>
<term>Structure activity relation</term>
<term>Treatment</term>
</keywords>
<keywords scheme="Pascal" xml:lang="fr"><term>Peptide PACAP</term>
<term>Relation structure activité</term>
<term>Neuroprotecteur</term>
<term>Récepteur PAC1</term>
<term>Maladie dégénérative</term>
<term>Pathologie du   système nerveux</term>
<term>In vitro</term>
<term>In vivo</term>
<term>Article synthèse</term>
<term>Agoniste</term>
<term>Affinité</term>
<term>Traitement</term>
<term>Neurone</term>
<term>Mécanisme action</term>
<term>Structure secondaire</term>
<term>Sélectivité</term>
<term>Récepteur couplé protéine G</term>
</keywords>
</textClass>
</profileDesc>
</teiHeader>
<front><div type="abstract" xml:lang="en">Pituitary adenylate cyclase-activating polypeptide (PACAP) is a 38-amino acid peptide that was initially isolated from hypothalamus extracts on the basis of its ability to stimulate the production of cAMP in cultured pituitary cells. Recent studies have shown that PACAP exerts potent neuroprotective effects not only in vitro but also in in vivo models of Parkinson's disease, Huntington's disease, traumatic brain injury and stroke. The protective effects of PACAP are based on its capacity to prevent neuronal apoptosis by acting directly on neurons or indirectly through the release of neuroprotective factors by astrocytes. These biological activities are mainly mediated through activation of the PAC 1 receptor which is currently considered as a potential target for the treatment of neurodegenerative diseases. However, the use of native PACAP, the endogenous ligand of PAC1, as an efficient neuroprotective drug is actually limited by its rapid degradation. Moreover, injection of PACAP to human induces peripheral side effects which are mainly mediated through VPAC I and VPAC2 receptors. Strategies to overcome these compromising conditions include the development of metabolically stable analogs of PACAP acting as selective agonists of the PAC1 receptor. This review presents an overview of the structure-activity relationships of PACAP and summarizes the molecular and conformational requirements for activation of PAC1 receptor. The applicability of PACAP analogs as therapeutic agents for treatment of neurodegenerative diseases is also discussed.</div>
</front>
</TEI>
<inist><standard h6="B"><pA><fA01 i1="01" i2="1"><s0>0929-8673</s0>
</fA01>
<fA03 i2="1"><s0>Curr. med. chem.</s0>
</fA03>
<fA05><s2>16</s2>
</fA05>
<fA06><s2>33</s2>
</fA06>
<fA08 i1="01" i2="1" l="ENG"><s1>Pituitary Adenylate Cyclase-Activating Polypeptide: Focus on Structure-Activity Relationships of a Neuroprotective Peptide</s1>
</fA08>
<fA11 i1="01" i2="1"><s1>BOURGAULT (S.)</s1>
</fA11>
<fA11 i1="02" i2="1"><s1>VAUDRY (D.)</s1>
</fA11>
<fA11 i1="03" i2="1"><s1>DEJDA (A.)</s1>
</fA11>
<fA11 i1="04" i2="1"><s1>DOAN (N. D.)</s1>
</fA11>
<fA11 i1="05" i2="1"><s1>VAUDRY (H.)</s1>
</fA11>
<fA11 i1="06" i2="1"><s1>FOURNIER (A.)</s1>
</fA11>
<fA14 i1="01"><s1>INRS-Institut Armand-Frappier, Institut National de la Recherche Scientifique, 531 boul. des Prairies</s1>
<s2>Ville de Laval, Qc, H7V 1B7</s2>
<s3>CAN</s3>
<sZ>1 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>6 aut.</sZ>
</fA14>
<fA14 i1="02"><s1>Laboratoire de Neuroendocrinologie Cellulaire et Moléculaire, INSERM U413, Université de Rouen</s1>
<s2>76821 Mont-Saint-Aignan</s2>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>2 aut.</sZ>
<sZ>5 aut.</sZ>
</fA14>
<fA14 i1="03"><s1>International Associated Laboratory Samuel de Champlain (INSERM- INRS)</s1>
<s3>FRA</s3>
<sZ>1 aut.</sZ>
<sZ>2 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>5 aut.</sZ>
<sZ>6 aut.</sZ>
</fA14>
<fA20><s1>4462-4480</s1>
</fA20>
<fA21><s1>2009</s1>
</fA21>
<fA23 i1="01"><s0>ENG</s0>
</fA23>
<fA43 i1="01"><s1>INIST</s1>
<s2>22999</s2>
<s5>354000171487100080</s5>
</fA43>
<fA44><s0>0000</s0>
<s1>© 2010 INIST-CNRS. All rights reserved.</s1>
</fA44>
<fA45><s0>183 ref.</s0>
</fA45>
<fA47 i1="01" i2="1"><s0>10-0131039</s0>
</fA47>
<fA60><s1>P</s1>
</fA60>
<fA61><s0>A</s0>
</fA61>
<fA64 i1="01" i2="1"><s0>Current medicinal chemistry</s0>
</fA64>
<fA66 i1="01"><s0>USA</s0>
</fA66>
<fC01 i1="01" l="ENG"><s0>Pituitary adenylate cyclase-activating polypeptide (PACAP) is a 38-amino acid peptide that was initially isolated from hypothalamus extracts on the basis of its ability to stimulate the production of cAMP in cultured pituitary cells. Recent studies have shown that PACAP exerts potent neuroprotective effects not only in vitro but also in in vivo models of Parkinson's disease, Huntington's disease, traumatic brain injury and stroke. The protective effects of PACAP are based on its capacity to prevent neuronal apoptosis by acting directly on neurons or indirectly through the release of neuroprotective factors by astrocytes. These biological activities are mainly mediated through activation of the PAC 1 receptor which is currently considered as a potential target for the treatment of neurodegenerative diseases. However, the use of native PACAP, the endogenous ligand of PAC1, as an efficient neuroprotective drug is actually limited by its rapid degradation. Moreover, injection of PACAP to human induces peripheral side effects which are mainly mediated through VPAC I and VPAC2 receptors. Strategies to overcome these compromising conditions include the development of metabolically stable analogs of PACAP acting as selective agonists of the PAC1 receptor. This review presents an overview of the structure-activity relationships of PACAP and summarizes the molecular and conformational requirements for activation of PAC1 receptor. The applicability of PACAP analogs as therapeutic agents for treatment of neurodegenerative diseases is also discussed.</s0>
</fC01>
<fC02 i1="01" i2="X"><s0>002B02B10</s0>
</fC02>
<fC02 i1="02" i2="X"><s0>002B02B09F</s0>
</fC02>
<fC03 i1="01" i2="X" l="FRE"><s0>Peptide PACAP</s0>
<s5>01</s5>
</fC03>
<fC03 i1="01" i2="X" l="ENG"><s0>Pituitary adenylate cyclase activating peptide</s0>
<s5>01</s5>
</fC03>
<fC03 i1="01" i2="X" l="SPA"><s0>Péptido PACAP</s0>
<s5>01</s5>
</fC03>
<fC03 i1="02" i2="X" l="FRE"><s0>Relation structure activité</s0>
<s5>02</s5>
</fC03>
<fC03 i1="02" i2="X" l="ENG"><s0>Structure activity relation</s0>
<s5>02</s5>
</fC03>
<fC03 i1="02" i2="X" l="SPA"><s0>Relación estructura actividad</s0>
<s5>02</s5>
</fC03>
<fC03 i1="03" i2="X" l="FRE"><s0>Neuroprotecteur</s0>
<s5>03</s5>
</fC03>
<fC03 i1="03" i2="X" l="ENG"><s0>Neuroprotective agent</s0>
<s5>03</s5>
</fC03>
<fC03 i1="03" i2="X" l="SPA"><s0>Neuroprotector</s0>
<s5>03</s5>
</fC03>
<fC03 i1="04" i2="X" l="FRE"><s0>Récepteur PAC1</s0>
<s5>04</s5>
</fC03>
<fC03 i1="04" i2="X" l="ENG"><s0>PAC1 receptor</s0>
<s5>04</s5>
</fC03>
<fC03 i1="04" i2="X" l="SPA"><s0>Receptor PAC1</s0>
<s5>04</s5>
</fC03>
<fC03 i1="05" i2="X" l="FRE"><s0>Maladie dégénérative</s0>
<s5>05</s5>
</fC03>
<fC03 i1="05" i2="X" l="ENG"><s0>Degenerative disease</s0>
<s5>05</s5>
</fC03>
<fC03 i1="05" i2="X" l="SPA"><s0>Enfermedad degenerativa</s0>
<s5>05</s5>
</fC03>
<fC03 i1="06" i2="X" l="FRE"><s0>Pathologie du   système nerveux</s0>
<s5>06</s5>
</fC03>
<fC03 i1="06" i2="X" l="ENG"><s0>Nervous system diseases</s0>
<s5>06</s5>
</fC03>
<fC03 i1="06" i2="X" l="SPA"><s0>Sistema nervioso patología</s0>
<s5>06</s5>
</fC03>
<fC03 i1="07" i2="X" l="FRE"><s0>In vitro</s0>
<s5>07</s5>
</fC03>
<fC03 i1="07" i2="X" l="ENG"><s0>In vitro</s0>
<s5>07</s5>
</fC03>
<fC03 i1="07" i2="X" l="SPA"><s0>In vitro</s0>
<s5>07</s5>
</fC03>
<fC03 i1="08" i2="X" l="FRE"><s0>In vivo</s0>
<s5>08</s5>
</fC03>
<fC03 i1="08" i2="X" l="ENG"><s0>In vivo</s0>
<s5>08</s5>
</fC03>
<fC03 i1="08" i2="X" l="SPA"><s0>In vivo</s0>
<s5>08</s5>
</fC03>
<fC03 i1="09" i2="X" l="FRE"><s0>Article synthèse</s0>
<s5>09</s5>
</fC03>
<fC03 i1="09" i2="X" l="ENG"><s0>Review</s0>
<s5>09</s5>
</fC03>
<fC03 i1="09" i2="X" l="SPA"><s0>Artículo síntesis</s0>
<s5>09</s5>
</fC03>
<fC03 i1="10" i2="X" l="FRE"><s0>Agoniste</s0>
<s5>10</s5>
</fC03>
<fC03 i1="10" i2="X" l="ENG"><s0>Agonist</s0>
<s5>10</s5>
</fC03>
<fC03 i1="10" i2="X" l="SPA"><s0>Agonista</s0>
<s5>10</s5>
</fC03>
<fC03 i1="11" i2="X" l="FRE"><s0>Affinité</s0>
<s5>11</s5>
</fC03>
<fC03 i1="11" i2="X" l="ENG"><s0>Affinity</s0>
<s5>11</s5>
</fC03>
<fC03 i1="11" i2="X" l="SPA"><s0>Afinidad</s0>
<s5>11</s5>
</fC03>
<fC03 i1="12" i2="X" l="FRE"><s0>Traitement</s0>
<s5>12</s5>
</fC03>
<fC03 i1="12" i2="X" l="ENG"><s0>Treatment</s0>
<s5>12</s5>
</fC03>
<fC03 i1="12" i2="X" l="SPA"><s0>Tratamiento</s0>
<s5>12</s5>
</fC03>
<fC03 i1="13" i2="X" l="FRE"><s0>Neurone</s0>
<s5>13</s5>
</fC03>
<fC03 i1="13" i2="X" l="ENG"><s0>Neuron</s0>
<s5>13</s5>
</fC03>
<fC03 i1="13" i2="X" l="SPA"><s0>Neurona</s0>
<s5>13</s5>
</fC03>
<fC03 i1="14" i2="X" l="FRE"><s0>Mécanisme action</s0>
<s5>14</s5>
</fC03>
<fC03 i1="14" i2="X" l="ENG"><s0>Mechanism of action</s0>
<s5>14</s5>
</fC03>
<fC03 i1="14" i2="X" l="SPA"><s0>Mecanismo acción</s0>
<s5>14</s5>
</fC03>
<fC03 i1="15" i2="X" l="FRE"><s0>Structure secondaire</s0>
<s5>15</s5>
</fC03>
<fC03 i1="15" i2="X" l="ENG"><s0>Secondary structure</s0>
<s5>15</s5>
</fC03>
<fC03 i1="15" i2="X" l="SPA"><s0>Estructura secundaria</s0>
<s5>15</s5>
</fC03>
<fC03 i1="16" i2="X" l="FRE"><s0>Sélectivité</s0>
<s5>16</s5>
</fC03>
<fC03 i1="16" i2="X" l="ENG"><s0>Selectivity</s0>
<s5>16</s5>
</fC03>
<fC03 i1="16" i2="X" l="SPA"><s0>Selectividad</s0>
<s5>16</s5>
</fC03>
<fC03 i1="17" i2="X" l="FRE"><s0>Récepteur couplé protéine G</s0>
<s5>32</s5>
</fC03>
<fC03 i1="17" i2="X" l="ENG"><s0>G protein coupled receptor</s0>
<s5>32</s5>
</fC03>
<fC03 i1="17" i2="X" l="SPA"><s0>Receptor acoplado proteína G</s0>
<s5>32</s5>
</fC03>
<fN21><s1>081</s1>
</fN21>
</pA>
</standard>
<server><NO>PASCAL 10-0131039 INIST</NO>
<ET>Pituitary Adenylate Cyclase-Activating Polypeptide: Focus on Structure-Activity Relationships of a Neuroprotective Peptide</ET>
<AU>BOURGAULT (S.); VAUDRY (D.); DEJDA (A.); DOAN (N. D.); VAUDRY (H.); FOURNIER (A.)</AU>
<AF>INRS-Institut Armand-Frappier, Institut National de la Recherche Scientifique, 531 boul. des Prairies/Ville de Laval, Qc, H7V 1B7/Canada (1 aut., 3 aut., 4 aut., 6 aut.); Laboratoire de Neuroendocrinologie Cellulaire et Moléculaire, INSERM U413, Université de Rouen/76821 Mont-Saint-Aignan/France (1 aut., 2 aut., 5 aut.); International Associated Laboratory Samuel de Champlain (INSERM- INRS)/France (1 aut., 2 aut., 3 aut., 4 aut., 5 aut., 6 aut.)</AF>
<DT>Publication en série; Niveau analytique</DT>
<SO>Current medicinal chemistry; ISSN 0929-8673; Etats-Unis; Da. 2009; Vol. 16; No. 33; Pp. 4462-4480; Bibl. 183 ref.</SO>
<LA>Anglais</LA>
<EA>Pituitary adenylate cyclase-activating polypeptide (PACAP) is a 38-amino acid peptide that was initially isolated from hypothalamus extracts on the basis of its ability to stimulate the production of cAMP in cultured pituitary cells. Recent studies have shown that PACAP exerts potent neuroprotective effects not only in vitro but also in in vivo models of Parkinson's disease, Huntington's disease, traumatic brain injury and stroke. The protective effects of PACAP are based on its capacity to prevent neuronal apoptosis by acting directly on neurons or indirectly through the release of neuroprotective factors by astrocytes. These biological activities are mainly mediated through activation of the PAC 1 receptor which is currently considered as a potential target for the treatment of neurodegenerative diseases. However, the use of native PACAP, the endogenous ligand of PAC1, as an efficient neuroprotective drug is actually limited by its rapid degradation. Moreover, injection of PACAP to human induces peripheral side effects which are mainly mediated through VPAC I and VPAC2 receptors. Strategies to overcome these compromising conditions include the development of metabolically stable analogs of PACAP acting as selective agonists of the PAC1 receptor. This review presents an overview of the structure-activity relationships of PACAP and summarizes the molecular and conformational requirements for activation of PAC1 receptor. The applicability of PACAP analogs as therapeutic agents for treatment of neurodegenerative diseases is also discussed.</EA>
<CC>002B02B10; 002B02B09F</CC>
<FD>Peptide PACAP; Relation structure activité; Neuroprotecteur; Récepteur PAC1; Maladie dégénérative; Pathologie du   système nerveux; In vitro; In vivo; Article synthèse; Agoniste; Affinité; Traitement; Neurone; Mécanisme action; Structure secondaire; Sélectivité; Récepteur couplé protéine G</FD>
<ED>Pituitary adenylate cyclase activating peptide; Structure activity relation; Neuroprotective agent; PAC1 receptor; Degenerative disease; Nervous system diseases; In vitro; In vivo; Review; Agonist; Affinity; Treatment; Neuron; Mechanism of action; Secondary structure; Selectivity; G protein coupled receptor</ED>
<SD>Péptido PACAP; Relación estructura actividad; Neuroprotector; Receptor PAC1; Enfermedad degenerativa; Sistema nervioso patología; In vitro; In vivo; Artículo síntesis; Agonista; Afinidad; Tratamiento; Neurona; Mecanismo acción; Estructura secundaria; Selectividad; Receptor acoplado proteína G</SD>
<LO>INIST-22999.354000171487100080</LO>
<ID>10-0131039</ID>
</server>
</inist>
</record>

Pour manipuler ce document sous Unix (Dilib)

EXPLOR_STEP=$WICRI_ROOT/Wicri/Canada/explor/ParkinsonCanadaV1/Data/PascalFrancis/Corpus

HfdSelect -h $EXPLOR_STEP/biblio.hfd -nk 000460 | SxmlIndent | more

HfdSelect -h $EXPLOR_AREA/Data/PascalFrancis/Corpus/biblio.hfd -nk 000460 | SxmlIndent | more

Pour mettre un lien sur cette page dans le réseau Wicri

{{Explor lien
   |wiki=    Wicri/Canada
   |area=    ParkinsonCanadaV1
   |flux=    PascalFrancis
   |étape=   Corpus
   |type=    RBID
   |clé=     Pascal:10-0131039
   |texte=   Pituitary Adenylate Cyclase-Activating Polypeptide: Focus on Structure-Activity Relationships of a Neuroprotective Peptide
}}

This area was generated with Dilib version V0.6.29.
Data generation: Thu May 4 22:20:19 2017. Site generation: Fri Dec 23 23:17:26 2022

	La maladie de Parkinson au Canada (serveur d'exploration)
	Attention, ce site est en cours de développement ! Attention, site généré par des moyens informatiques à partir de corpus bruts. Les informations ne sont donc pas validées.

La maladie de Parkinson au Canada (serveur d'exploration)

Pituitary Adenylate Cyclase-Activating Polypeptide: Focus on Structure-Activity Relationships of a Neuroprotective Peptide

Pituitary Adenylate Cyclase-Activating Polypeptide: Focus on Structure-Activity Relationships of a Neuroprotective Peptide

Source :

Descripteurs français

English descriptors

Abstract

Notice en format standard (ISO 2709)

Format Inist (serveur)

Links to Exploration step

Le document en format XML

Pour manipuler ce document sous Unix (Dilib)

Pour mettre un lien sur cette page dans le réseau Wicri