Literature DB >> 18793851

Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4): Part I. Discovery of pyrazolo[3,4-d]pyrimidines as novel mGluR4 positive allosteric modulators.

Colleen M Niswender1, Evan P Lebois, Qingwei Luo, Kwangho Kim, Hubert Muchalski, Huiyong Yin, P Jeffrey Conn, Craig W Lindsley.   

Abstract

This letter describes the synthesis and SAR, developed through an iterative analogue library approach, of an mGluR4 positive allosteric modulator lead based on a pyrazolo[3,4-d]pyrimidine scaffold. Despite tremendous therapeutic potential, Compound 7, VU0080421, and related congeners represent only a handful of mGluR4 positive allosteric modulators ever described.

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Year:  2008        PMID： 18793851      PMCID： PMC3182458          DOI： 10.1016/j.bmcl.2008.08.087

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  19 in total

Review 1.  Targeting the metabotropic glutamate receptor mGluR4 for the treatment of diseases of the central nervous system.

Authors:  Michael J Marino; J Fred Hess; Nigel Liverton
Journal:  Curr Top Med Chem       Date:  2005       Impact factor: 3.295

Review 2.  Glutamate-based therapeutic approaches: allosteric modulators of metabotropic glutamate receptors.

Authors:  Michael J Marino; P Jeffrey Conn
Journal:  Curr Opin Pharmacol       Date:  2005-12-20       Impact factor: 5.547

3.  Pharmacological activation of mGlu4 metabotropic glutamate receptors inhibits the growth of medulloblastomas.

Authors:  Luisa Iacovelli; Antonietta Arcella; Giuseppe Battaglia; Simonetta Pazzaglia; Eleonora Aronica; Paola Spinsanti; Alessandra Caruso; Enrico De Smaele; Anna Saran; Alberto Gulino; Mara D'Onofrio; Felice Giangaspero; Ferdinando Nicoletti
Journal:  J Neurosci       Date:  2006-08-09       Impact factor: 6.167

4.  (R,S)-4-phosphonophenylglycine, a potent and selective group III metabotropic glutamate receptor agonist, is anticonvulsive and neuroprotective in vivo.

Authors:  F Gasparini; V Bruno; G Battaglia; S Lukic; T Leonhardt; W Inderbitzin; D Laurie; B Sommer; M A Varney; S D Hess; E C Johnson; R Kuhn; S Urwyler; D Sauer; C Portet; M Schmutz; F Nicoletti; P J Flor
Journal:  J Pharmacol Exp Ther       Date:  1999-06       Impact factor: 4.030

5.  Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.

Authors:  Craig W Lindsley; David D Wisnoski; William H Leister; Julie A O'brien; Wei Lemaire; David L Williams; Maryann Burno; Cyrille Sur; Gene G Kinney; Doug J Pettibone; Philip R Tiller; Sheri Smith; Mark E Duggan; George D Hartman; P Jeffrey Conn; Joel R Huff
Journal:  J Med Chem       Date:  2004-11-18       Impact factor: 7.446

6.  Combined administration of PHCCC, a positive allosteric modulator of mGlu4 receptors and ACPT-I, mGlu III receptor agonist evokes antidepressant-like effects in rats.

Authors:  K Kłak; A Pałucha; P Brański; M Sowa; A Pilc
Journal:  Amino Acids       Date:  2006-08-02       Impact factor: 3.520

7.  Allosteric modulation of group III metabotropic glutamate receptor 4: a potential approach to Parkinson's disease treatment.

Authors:  Michael J Marino; David L Williams; Julie A O'Brien; Ornella Valenti; Terrence P McDonald; Michelle K Clements; Ruiping Wang; Anthony G DiLella; J Fred Hess; Gene G Kinney; P Jeffrey Conn
Journal:  Proc Natl Acad Sci U S A       Date:  2003-10-30       Impact factor: 11.205

8.  Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4.

Authors:  Colleen M Niswender; Kari A Johnson; C David Weaver; Carrie K Jones; Zixiu Xiang; Qingwei Luo; Alice L Rodriguez; Joy E Marlo; Tomas de Paulis; Analisa D Thompson; Emily L Days; Tasha Nalywajko; Cheryl A Austin; Michael Baxter Williams; Jennifer E Ayala; Richard Williams; Craig W Lindsley; P Jeffrey Conn
Journal:  Mol Pharmacol       Date:  2008-07-29       Impact factor: 4.436

9.  Anxiolytic-like effects of PHCCC, an allosteric modulator of mGlu4 receptors, in rats.

Authors:  Katarzyna Stachowicz; Kinga Kłak; Aleksandra Kłodzińska; Ewa Chojnacka-Wojcik; Andrzej Pilc
Journal:  Eur J Pharmacol       Date:  2004-09-13       Impact factor: 4.432

10.  L-2-amino-4-phosphonobutyrate (L-AP4) is an agonist at the type IV metabotropic glutamate receptor which is negatively coupled to adenylate cyclase.

Authors:  C Thomsen; P Kristensen; E Mulvihill; B Haldeman; P D Suzdak
Journal:  Eur J Pharmacol       Date:  1992-11-02       Impact factor: 4.432
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  17 in total

1.  Allosteric modulation of the group III mGlu4 receptor provides functional neuroprotection in the 6-hydroxydopamine rat model of Parkinson's disease.

Authors:  Matthew J Betts; Michael J O'Neill; Susan Duty
Journal:  Br J Pharmacol       Date:  2012-08       Impact factor: 8.739

2.  Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu(4)) with oral efficacy in an antiparkinsonian animal model.

Authors:  Carrie K Jones; Darren W Engers; Analisa D Thompson; Julie R Field; Anna L Blobaum; Stacey R Lindsley; Ya Zhou; Rocco D Gogliotti; Satyawan Jadhav; Rocio Zamorano; Jim Bogenpohl; Yoland Smith; Ryan Morrison; J Scott Daniels; C David Weaver; P Jeffrey Conn; Craig W Lindsley; Colleen M Niswender; Corey R Hopkins
Journal:  J Med Chem       Date:  2011-10-19       Impact factor: 7.446

3.  Iterative experimental and virtual high-throughput screening identifies metabotropic glutamate receptor subtype 4 positive allosteric modulators.

Authors:  Ralf Mueller; Eric S Dawson; Colleen M Niswender; Mariusz Butkiewicz; Corey R Hopkins; C David Weaver; Craig W Lindsley; P Jeffrey Conn; Jens Meiler
Journal:  J Mol Model       Date:  2012-05-17       Impact factor: 1.810

Review 4.  Recent progress on the identification of metabotropic glutamate 4 receptor ligands and their potential utility as CNS therapeutics.

Authors:  Albert J Robichaud; Darren W Engers; Craig W Lindsley; Corey R Hopkins
Journal:  ACS Chem Neurosci       Date:  2011-06-14       Impact factor: 4.418

Review 5.  Progress toward advanced understanding of metabotropic glutamate receptors: structure, signaling and therapeutic indications.

Authors:  Shen Yin; Colleen M Niswender
Journal:  Cell Signal       Date:  2014-05-02       Impact factor: 4.315

6.  In Silico Studies Targeting G-protein Coupled Receptors for Drug Research Against Parkinson's Disease.

Authors:  Agostinho Lemos; Rita Melo; Antonio Jose Preto; Jose Guilherme Almeida; Irina Sousa Moreira; Maria Natalia Dias Soeiro Cordeiro
Journal:  Curr Neuropharmacol       Date:  2018       Impact factor: 7.363

Review 7.  Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review.

Authors:  Khalid Karrouchi; Smaail Radi; Youssef Ramli; Jamal Taoufik; Yahia N Mabkhot; Faiz A Al-Aizari; M'hammed Ansar
Journal:  Molecules       Date:  2018-01-12       Impact factor: 4.411

Review 8.  Metabotropic glutamate receptors: physiology, pharmacology, and disease.

Authors:  Colleen M Niswender; P Jeffrey Conn
Journal:  Annu Rev Pharmacol Toxicol       Date:  2010       Impact factor: 13.820

Review 9.  Therapeutic potential of targeting group III metabotropic glutamate receptors in the treatment of Parkinson's disease.

Authors:  Susan Duty
Journal:  Br J Pharmacol       Date:  2010-09       Impact factor: 8.739

10.  Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4). Part II: Challenges in hit-to-lead.

Authors:  Richard Williams; Colleen M Niswender; Qingwei Luo; Uyen Le; P Jeffrey Conn; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2008-12-25       Impact factor: 2.823
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