Literature DB >> 20582156

Re-exploration of the PHCCC Scaffold: Discovery of Improved Positive Allosteric Modulators of mGluR4.

Richard Williams1, Ya Zhou, Colleen M Niswender, Qingwei Luo, P Jeffrey Conn, Craig W Lindsley, Corey R Hopkins.   

Abstract

This Letter describes a detailed SAR analysis of the mGluR4 positive allosteric modulator, PHCCC. We have now developed compounds with improved potency and efficacy; in addition, compounds are presented that show selectivity for mGluR4 versus the other mGluR subtypes.

Entities:  

Year:  2010        PMID： 20582156      PMCID： PMC2889702          DOI： 10.1021/cn9000318

Source DB:  PubMed          Journal:  ACS Chem Neurosci        ISSN： 1948-7193            Impact factor:   4.418


  22 in total

1.  Development of a custom high-throughput preparative liquid chromatography/mass spectrometer platform for the preparative purification and analytical analysis of compound libraries.

Authors:  William Leister; Kimberly Strauss; David Wisnoski; Zhijian Zhao; Craig Lindsley
Journal:  J Comb Chem       Date:  2003 May-Jun

2.  Group III metabotropic glutamate receptor-mediated modulation of the striatopallidal synapse.

Authors:  Ornella Valenti; Michael J Marino; Marion Wittmann; Edward Lis; Anthony G DiLella; Gene G Kinney; P Jeffrey Conn
Journal:  J Neurosci       Date:  2003-08-06       Impact factor: 6.167

3.  Group III metabotropic glutamate-receptor-mediated modulation of excitatory transmission in rodent substantia nigra pars compacta dopamine neurons.

Authors:  Ornella Valenti; Guido Mannaioni; Guy R Seabrook; P Jeffrey Conn; Michael J Marino
Journal:  J Pharmacol Exp Ther       Date:  2005-03-10       Impact factor: 4.030

Review 4.  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 5.  Recent progress in the development of mGluR4 positive allosteric modulators for the treatment of Parkinson's disease.

Authors:  Craig W Lindsley; Colleen M Niswender; Darren W Engers; Corey R Hopkins
Journal:  Curr Top Med Chem       Date:  2009       Impact factor: 3.295

6.  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

Review 7.  Metabotropic glutamate receptor subtypes as targets for neuroprotective drugs.

Authors:  V Bruno; G Battaglia; A Copani; M D'Onofrio; P Di Iorio; A De Blasi; D Melchiorri; P J Flor; F Nicoletti
Journal:  J Cereb Blood Flow Metab       Date:  2001-09       Impact factor: 6.200

8.  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

9.  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

10.  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
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  18 in total

1.  Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery.

Authors:  Bruce J Melancon; Corey R Hopkins; Michael R Wood; Kyle A Emmitte; Colleen M Niswender; Arthur Christopoulos; P Jeffrey Conn; Craig W Lindsley
Journal:  J Med Chem       Date:  2012-01-06       Impact factor: 7.446

2.  Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type and Mutant mGlu1 Receptors Found in Schizophrenics.

Authors:  Pedro M Garcia-Barrantes; Hyekyung P Cho; Colleen M Niswender; Frank W Byers; Charles W Locuson; Anna L Blobaum; Zixiu Xiang; Jerri M Rook; P Jeffrey Conn; Craig W Lindsley
Journal:  J Med Chem       Date:  2015-10-08       Impact factor: 7.446

Review 3.  Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors.

Authors:  Craig W Lindsley; Kyle A Emmitte; Corey R Hopkins; Thomas M Bridges; Karen J Gregory; Colleen M Niswender; P Jeffrey Conn
Journal:  Chem Rev       Date:  2016-02-16       Impact factor: 60.622

4.  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 5.  Emerging paradigms in GPCR allostery: implications for drug discovery.

Authors:  Denise Wootten; Arthur Christopoulos; Patrick M Sexton
Journal:  Nat Rev Drug Discov       Date:  2013-08       Impact factor: 84.694

6.  The Discovery and Characterization of ML218: A Novel, Centrally Active T-Type Calcium Channel Inhibitor with Robust Effects in STN Neurons and in a Rodent Model of Parkinson's Disease.

Authors:  Zixiu Xiang; Analisa D Thompson; John T Brogan; Michael L Schulte; Bruce J Melancon; Debbie Mi; L Michelle Lewis; Bende Zou; Liya Yang; Ryan Morrison; Tammy Santomango; Frank Byers; Katrina Brewer; Jonathan S Aldrich; Haibo Yu; Eric S Dawson; Min Li; Owen McManus; Carrie K Jones; J Scott Daniels; Corey R Hopkins; Ximin Simon Xie; P Jeffrey Conn; C David Weaver; Craig W Lindsley
Journal:  ACS Chem Neurosci       Date:  2011-12-21       Impact factor: 4.418

7.  Special issue on the pharmacology and medicinal chemistry of allosteric modulators of metabotropic glutamate receptors (mGluRs).

Authors:  Craig W Lindsley
Journal:  ACS Chem Neurosci       Date:  2011-08-17       Impact factor: 4.418

Review 8.  "Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology.

Authors:  Michael R Wood; Corey R Hopkins; John T Brogan; P Jeffrey Conn; Craig W Lindsley
Journal:  Biochemistry       Date:  2011-03-04       Impact factor: 3.162

9.  Re-exploration of the mGlu₁ PAM Ro 07-11401 scaffold: Discovery of analogs with improved CNS penetration despite steep SAR.

Authors:  Pedro M Garcia-Barrantes; Hyekyung P Cho; Tahj M Starr; Anna L Blobaum; Colleen M Niswender; P Jeffrey Conn; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2016-03-14       Impact factor: 2.823

10.  Solution-phase parallel synthesis and SAR of homopiperazinyl analogs as positive allosteric modulators of mGlu₄.

Authors:  Yiu-Yin Cheung; Rocio Zamorano; Anna L Blobaum; C David Weaver; P Jeffrey Conn; Craig W Lindsley; Colleen M Niswender; Corey R Hopkins
Journal:  ACS Comb Sci       Date:  2011-02-21       Impact factor: 3.784
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