The identification of GPR3 inverse agonist AF64394; The first small molecule inhibitor of GPR3 receptor function

The identification of the novel and selective GPR3 inverse agonist AF64394, the first small molecule inhibitor of GPR3 receptor function, is described. Structure activity relationships and syntheses based around AF64394 are reported. [Display omitted] The identification of the novel and selective GP...

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Published inBioorganic & medicinal chemistry letters Vol. 24; no. 22; pp. 5195 - 5198
Main Authors Jensen, Thomas, Elster, Lisbeth, Nielsen, Søren Møller, Poda, Suresh Babu, Loechel, Frosty, Volbracht, Christiane, Klewe, Ib Vestergaard, David, Laurent, Watson, Stephen P.
Format Journal Article
LanguageEnglish
Published OXFORD Elsevier Ltd 15.11.2014
Elsevier
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Abstract The identification of the novel and selective GPR3 inverse agonist AF64394, the first small molecule inhibitor of GPR3 receptor function, is described. Structure activity relationships and syntheses based around AF64394 are reported. [Display omitted] The identification of the novel and selective GPR3 inverse agonist AF64394, the first small molecule inhibitor of GPR3 receptor function, is described. Structure activity relationships and syntheses based around AF64394 are reported.
AbstractList The identification of the novel and selective GPR3 inverse agonist AF64394, the first small molecule inhibitor of GPR3 receptor function, is described. Structure activity relationships and syntheses based around AF64394 are reported. [Display omitted] The identification of the novel and selective GPR3 inverse agonist AF64394, the first small molecule inhibitor of GPR3 receptor function, is described. Structure activity relationships and syntheses based around AF64394 are reported.
The identification of the novel and selective GPR3 inverse agonist AF64394, the first small molecule inhibitor of GPR3 receptor function, is described. Structure activity relationships and syntheses based around AF64394 are reported.
The identification of the novel and selective GPR3 inverse agonist AF64394, the first small molecule inhibitor of GPR3 receptor function, is described. Structure activity relationships and syntheses based around AF64394 are reported. (C) 2014 Elsevier Ltd. All rights reserved.
Author Jensen, Thomas
Klewe, Ib Vestergaard
Nielsen, Søren Møller
Poda, Suresh Babu
Elster, Lisbeth
Watson, Stephen P.
Loechel, Frosty
David, Laurent
Volbracht, Christiane
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Cites_doi 10.1021/jm900319e
10.1016/j.neuropharm.2011.02.014
10.1021/jm200265b
10.1371/journal.pone.0074680
10.1038/nm.3023
10.1124/jpet.114.213082
10.1371/journal.pone.0004704
10.1111/j.1476-5381.2012.02043.x
10.1074/jbc.M700911200
10.1002/cber.19711040908
10.1016/S1359-6446(05)03386-6
10.1515/znb-1999-0614
10.1186/gb-2002-3-11-research0063
10.1016/S0898-6568(02)00041-4
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Keywords AF64394
GPR12
G protein coupled receptor
Inverse agonist
GPR3
GPR6
Orphan receptor
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References Thathiah, Horré, Snellinx, Vandewyer, Huang, Ciesielska, De Kloe, Munck, De Strooper (b0030) 2013; 19
b0080
b0090
Ruiz-Medina, Ledent, Valverde (b0040) 2011; 61
Abad-Zapatero, Metz (b0095) 2005; 10
b0085
b0050
Attaby, Eldin (b0065) 1999; 54
Ye, Zhang, Wang, Hua, Zhang, Xie (b0010) 2014; 349
Reimlinger, Jacquier, Daunis (b0070) 1971; 104
EP 0728759
Nelson, Sheng (b0025) 2013; 8
Gujjar, El Mazouni, White, White, Creason, Shackleford, Deng, Charman, Bathurst, Burrows, Floyd, Matthews, Buckner, Charman, Phillips, Rathod (b0060) 2011; 54
Joost, Methner, Gloriam, Foord, Blaney, Garland (b0005) 2002; 3
Tanaka, Ishii, Kasai, Yoon, Saeki (b0015) 2007; 282
Valverde, Célérier, Baranyi, Vanderhaeghen, Maldonado, Sperlagh, Vassart, Ledent (b0045) 2009; 4
p 40.
b0075
Uhlenbrock, Gassenhuber, Kostenis (b0020) 2002; 14
Tourino, Valjent, Ruiz-Medina, Herve, Ledent, Valverde (b0035) 2012; 167
Valverde, O (WOS:000265490500015) 2009; 4
Ye, CL (WOS:000336156200008) 2014; 349
Abad-Zapatero, C (WOS:000227936000007) 2005; 10
(000343901400011.1) 1996
Attaby, FA (WOS:000081323700014) 1999; 54
Uhlenbrock, K (WOS:000178523000006) 2002; 14
Ruiz-Medina, J (WOS:000292408200005) 2011; 61
Thathiah, A (WOS:000313230300024) 2013; 19
Tourino, C (WOS:000309396100017) 2012; 167
Gujjar, R (WOS:000291082500020) 2011; 54
Joost, P (WOS:000207582200014) 2002; 3
Nelson, CD (WOS:000326240100115) 2013; 8
Tanaka, S (WOS:000245941000043) 2007; 282
REIMLINGER, H (WOS:A1971K265500007) 1971; 104
Gloriam, DE (WOS:000268139900037) 2009; 52
Ruiz-Medina (10.1016/j.bmcl.2014.09.077_b0040) 2011; 61
Tanaka (10.1016/j.bmcl.2014.09.077_b0015) 2007; 282
Joost (10.1016/j.bmcl.2014.09.077_h0005) 2002; 3
Attaby (10.1016/j.bmcl.2014.09.077_b0065) 1999; 54
Thathiah (10.1016/j.bmcl.2014.09.077_b0030) 2013; 19
Abad-Zapatero (10.1016/j.bmcl.2014.09.077_b0095) 2005; 10
Ye (10.1016/j.bmcl.2014.09.077_b0010) 2014; 349
Uhlenbrock (10.1016/j.bmcl.2014.09.077_b0020) 2002; 14
Reimlinger (10.1016/j.bmcl.2014.09.077_b0070) 1971; 104
Tourino (10.1016/j.bmcl.2014.09.077_b0035) 2012; 167
Valverde (10.1016/j.bmcl.2014.09.077_b0045) 2009; 4
Nelson (10.1016/j.bmcl.2014.09.077_b0025) 2013; 8
Gloriam (10.1016/j.bmcl.2014.09.077_h0010) 2009; 52
10.1016/j.bmcl.2014.09.077_b0055
Gujjar (10.1016/j.bmcl.2014.09.077_b0060) 2011; 54
References_xml – ident: b0080
– volume: 167
  start-page: 892
  year: 2012
  ident: b0035
  publication-title: Br. J. Pharmacol.
  contributor:
    fullname: Valverde
– ident: b0075
– volume: 3
  start-page: 11
  year: 2002
  ident: b0005
  publication-title: Genome Biol.
  contributor:
    fullname: Garland
– volume: 54
  start-page: 3935
  year: 2011
  ident: b0060
  publication-title: J. Med. Chem.
  contributor:
    fullname: Rathod
– ident: b0050
– volume: 104
  start-page: 2702
  year: 1971
  ident: b0070
  publication-title: Chem. Ber.
  contributor:
    fullname: Daunis
– volume: 8
  start-page: e74680
  year: 2013
  ident: b0025
  publication-title: PloS One
  contributor:
    fullname: Sheng
– volume: 61
  start-page: 43
  year: 2011
  ident: b0040
  publication-title: Neuropharmacology
  contributor:
    fullname: Valverde
– volume: 4
  start-page: e4704
  year: 2009
  ident: b0045
  publication-title: PloS One
  contributor:
    fullname: Ledent
– ident: b0090
– volume: 10
  start-page: 464
  year: 2005
  ident: b0095
  publication-title: Drug Discovery Today
  contributor:
    fullname: Metz
– volume: 19
  start-page: 43
  year: 2013
  ident: b0030
  publication-title: Nat. Med.
  contributor:
    fullname: De Strooper
– volume: 54
  start-page: 788
  year: 1999
  ident: b0065
  publication-title: Z. Naturforsch., B
  contributor:
    fullname: Eldin
– volume: 282
  start-page: 10506
  year: 2007
  ident: b0015
  publication-title: J. Biol. Chem.
  contributor:
    fullname: Saeki
– ident: b0085
– volume: 14
  start-page: 941
  year: 2002
  ident: b0020
  publication-title: Cell. Signal.
  contributor:
    fullname: Kostenis
– volume: 349
  start-page: 437
  year: 2014
  ident: b0010
  publication-title: J. Pharmacol. Exp. Ther.
  contributor:
    fullname: Xie
– volume: 52
  start-page: 4429
  year: 2009
  ident: WOS:000268139900037
  article-title: Definition of the G Protein-Coupled Receptor Transmembrane Bundle Binding Pocket and Calculation of Receptor Similarities for Drug Design
  publication-title: JOURNAL OF MEDICINAL CHEMISTRY
  doi: 10.1021/jm900319e
  contributor:
    fullname: Gloriam, DE
– volume: 61
  start-page: 43
  year: 2011
  ident: WOS:000292408200005
  article-title: GPR3 orphan receptor is involved in neuropathic pain after peripheral nerve injury and regulates morphine-induced antinociception
  publication-title: NEUROPHARMACOLOGY
  doi: 10.1016/j.neuropharm.2011.02.014
  contributor:
    fullname: Ruiz-Medina, J
– volume: 54
  start-page: 3935
  year: 2011
  ident: WOS:000291082500020
  article-title: Lead Optimization of Aryl and Aralkyl Amine-Based Triazolopyrimidine Inhibitors of Plasmodium falciparum Dihydroorotate Dehydrogenase with Antimalarial Activity in Mice
  publication-title: JOURNAL OF MEDICINAL CHEMISTRY
  doi: 10.1021/jm200265b
  contributor:
    fullname: Gujjar, R
– volume: 8
  start-page: ARTN e74680
  year: 2013
  ident: WOS:000326240100115
  article-title: GPR3 Stimulates A beta Production via Interactions with APP and beta-Arrestin2
  publication-title: PLOS ONE
  doi: 10.1371/journal.pone.0074680
  contributor:
    fullname: Nelson, CD
– year: 1996
  ident: 000343901400011.1
  publication-title: EP
– volume: 19
  start-page: 43
  year: 2013
  ident: WOS:000313230300024
  article-title: beta-arrestin 2 regulates A beta generation and gamma-secretase activity in Alzheimer's disease
  publication-title: NATURE MEDICINE
  doi: 10.1038/nm.3023
  contributor:
    fullname: Thathiah, A
– volume: 349
  start-page: 437
  year: 2014
  ident: WOS:000336156200008
  article-title: Identification of a Novel Small-Molecule Agonist for Human G Protein-Coupled Receptor 3
  publication-title: JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
  doi: 10.1124/jpet.114.213082
  contributor:
    fullname: Ye, CL
– volume: 3
  start-page: ARTN 0063.1
  year: 2002
  ident: WOS:000207582200014
  article-title: Phylogenetic analysis of 277 human G-protein-coupled receptors as a tool for the prediction of orphan receptor ligands
  publication-title: GENOME BIOLOGY
  contributor:
    fullname: Joost, P
– volume: 4
  start-page: ARTN e4704
  year: 2009
  ident: WOS:000265490500015
  article-title: GPR3 Receptor, a Novel Actor in the Emotional-Like Responses
  publication-title: PLOS ONE
  doi: 10.1371/journal.pone.0004704
  contributor:
    fullname: Valverde, O
– volume: 10
  start-page: 464
  year: 2005
  ident: WOS:000227936000007
  article-title: Ligand efficiency indices as guideposts for drug discovery
  publication-title: DRUG DISCOVERY TODAY
  contributor:
    fullname: Abad-Zapatero, C
– volume: 167
  start-page: 892
  year: 2012
  ident: WOS:000309396100017
  article-title: The orphan receptor GPR3 modulates the early phases of cocaine reinforcement
  publication-title: BRITISH JOURNAL OF PHARMACOLOGY
  doi: 10.1111/j.1476-5381.2012.02043.x
  contributor:
    fullname: Tourino, C
– volume: 14
  start-page: 941
  year: 2002
  ident: WOS:000178523000006
  article-title: Sphingosine 1-phosphate is a ligand of the human gpr3, gpr6 and gpr12 family of constitutively active G protein-coupled receptors
  publication-title: CELLULAR SIGNALLING
  contributor:
    fullname: Uhlenbrock, K
– volume: 54
  start-page: 788
  year: 1999
  ident: WOS:000081323700014
  article-title: Synthesis of pyrimidine, thiazolopyrimidine, pyrimidotriazine and triazolopyrimidine derivatives and their biological evaluation
  publication-title: ZEITSCHRIFT FUR NATURFORSCHUNG SECTION B-A JOURNAL OF CHEMICAL SCIENCES
  contributor:
    fullname: Attaby, FA
– volume: 104
  start-page: 2702
  year: 1971
  ident: WOS:A1971K265500007
  article-title: SYNTHESES WITH HETEROCYCLIC AMINES .6. ADDITIONAL SYNTHESES OF 7-OXO-7.8-DIHYDRO-S-TRIAZOLO[4.3-A]PYRIMIDINES
  publication-title: CHEMISCHE BERICHTE-RECUEIL
  contributor:
    fullname: REIMLINGER, H
– volume: 282
  start-page: 10506
  year: 2007
  ident: WOS:000245941000043
  article-title: Neural expression of G protein-coupled receptors GPR3, GPR6, and GPR12 up-regulates cyclic AMP levels and promotes neurite outgrowth
  publication-title: JOURNAL OF BIOLOGICAL CHEMISTRY
  doi: 10.1074/jbc.M700911200
  contributor:
    fullname: Tanaka, S
– ident: 10.1016/j.bmcl.2014.09.077_b0055
– volume: 54
  start-page: 3935
  year: 2011
  ident: 10.1016/j.bmcl.2014.09.077_b0060
  publication-title: J. Med. Chem.
  doi: 10.1021/jm200265b
  contributor:
    fullname: Gujjar
– volume: 104
  start-page: 2702
  year: 1971
  ident: 10.1016/j.bmcl.2014.09.077_b0070
  publication-title: Chem. Ber.
  doi: 10.1002/cber.19711040908
  contributor:
    fullname: Reimlinger
– volume: 349
  start-page: 437
  year: 2014
  ident: 10.1016/j.bmcl.2014.09.077_b0010
  publication-title: J. Pharmacol. Exp. Ther.
  doi: 10.1124/jpet.114.213082
  contributor:
    fullname: Ye
– volume: 4
  start-page: e4704
  year: 2009
  ident: 10.1016/j.bmcl.2014.09.077_b0045
  publication-title: PloS One
  doi: 10.1371/journal.pone.0004704
  contributor:
    fullname: Valverde
– volume: 282
  start-page: 10506
  year: 2007
  ident: 10.1016/j.bmcl.2014.09.077_b0015
  publication-title: J. Biol. Chem.
  doi: 10.1074/jbc.M700911200
  contributor:
    fullname: Tanaka
– volume: 61
  start-page: 43
  year: 2011
  ident: 10.1016/j.bmcl.2014.09.077_b0040
  publication-title: Neuropharmacology
  doi: 10.1016/j.neuropharm.2011.02.014
  contributor:
    fullname: Ruiz-Medina
– volume: 10
  start-page: 464
  year: 2005
  ident: 10.1016/j.bmcl.2014.09.077_b0095
  publication-title: Drug Discovery Today
  doi: 10.1016/S1359-6446(05)03386-6
  contributor:
    fullname: Abad-Zapatero
– volume: 167
  start-page: 892
  year: 2012
  ident: 10.1016/j.bmcl.2014.09.077_b0035
  publication-title: Br. J. Pharmacol.
  doi: 10.1111/j.1476-5381.2012.02043.x
  contributor:
    fullname: Tourino
– volume: 52
  start-page: 4429
  year: 2009
  ident: 10.1016/j.bmcl.2014.09.077_h0010
  publication-title: J. Med. Chem.
  doi: 10.1021/jm900319e
  contributor:
    fullname: Gloriam
– volume: 54
  start-page: 788
  year: 1999
  ident: 10.1016/j.bmcl.2014.09.077_b0065
  publication-title: Z. Naturforsch., B
  doi: 10.1515/znb-1999-0614
  contributor:
    fullname: Attaby
– volume: 19
  start-page: 43
  year: 2013
  ident: 10.1016/j.bmcl.2014.09.077_b0030
  publication-title: Nat. Med.
  doi: 10.1038/nm.3023
  contributor:
    fullname: Thathiah
– volume: 3
  start-page: 11
  year: 2002
  ident: 10.1016/j.bmcl.2014.09.077_h0005
  publication-title: Genome Biol.
  doi: 10.1186/gb-2002-3-11-research0063
  contributor:
    fullname: Joost
– volume: 14
  start-page: 941
  year: 2002
  ident: 10.1016/j.bmcl.2014.09.077_b0020
  publication-title: Cell. Signal.
  doi: 10.1016/S0898-6568(02)00041-4
  contributor:
    fullname: Uhlenbrock
– volume: 8
  start-page: e74680
  year: 2013
  ident: 10.1016/j.bmcl.2014.09.077_b0025
  publication-title: PloS One
  doi: 10.1371/journal.pone.0074680
  contributor:
    fullname: Nelson
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Snippet The identification of the novel and selective GPR3 inverse agonist AF64394, the first small molecule inhibitor of GPR3 receptor function, is described....
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SubjectTerms AF64394
Animals
Chemistry
Chemistry, Medicinal
Chemistry, Organic
Drug Inverse Agonism
G protein coupled receptor
GPR12
GPR3
GPR6
Inverse agonist
Life Sciences & Biomedicine
Mice
Orphan receptor
Pharmacology & Pharmacy
Physical Sciences
Pyrimidines - chemistry
Pyrimidines - pharmacology
Receptors, G-Protein-Coupled - antagonists & inhibitors
Receptors, G-Protein-Coupled - physiology
Science & Technology
Triazoles - chemistry
Triazoles - pharmacology
Title The identification of GPR3 inverse agonist AF64394; The first small molecule inhibitor of GPR3 receptor function
URI https://dx.doi.org/10.1016/j.bmcl.2014.09.077
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https://www.ncbi.nlm.nih.gov/pubmed/25442311
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https://search.proquest.com/docview/1635016147
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