Literature DB >> 22148748

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

Bruce J Melancon1, Corey R Hopkins, Michael R Wood, Kyle A Emmitte, Colleen M Niswender, Arthur Christopoulos, P Jeffrey Conn, Craig W Lindsley.   

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Year:  2012        PMID： 22148748      PMCID： PMC3349997          DOI： 10.1021/jm201139r

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


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  210 in total

1.  An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission.

Authors:  Jana K Shirey; Zixiu Xiang; Darren Orton; Ashley E Brady; Kari A Johnson; Richard Williams; Jennifer E Ayala; Alice L Rodriguez; Jürgen Wess; David Weaver; Colleen M Niswender; P Jeffrey Conn
Journal:  Nat Chem Biol       Date:  2007-12-02       Impact factor: 15.040

Review 2.  Allosteric modulation of kinases and GPCRs: design principles and structural diversity.

Authors:  Jana A Lewis; Evan P Lebois; Craig W Lindsley
Journal:  Curr Opin Chem Biol       Date:  2008-04-18       Impact factor: 8.822

3.  The A, B, Cs of G-protein-coupled receptor pharmacology in assay development for HTS.

Authors:  Dj McLoughlin; F Bertelli; C Williams
Journal:  Expert Opin Drug Discov       Date:  2007-05       Impact factor: 6.098

4.  TAK-220, a novel small-molecule CCR5 antagonist, has favorable anti-human immunodeficiency virus interactions with other antiretrovirals in vitro.

Authors:  Cécile L Tremblay; Françoise Giguel; Yongbiao Guan; Ting-Chao Chou; Katsunori Takashima; Martin S Hirsch
Journal:  Antimicrob Agents Chemother       Date:  2005-08       Impact factor: 5.191

5.  Treatment of anxiety using fenobam (a nonbenzodiazepine) in a double-blind standard (diazepam) placebo-controlled study.

Authors:  J C Pecknold; D J McClure; L Appeltauer; L Wrzesinski; T Allan
Journal:  J Clin Psychopharmacol       Date:  1982-04       Impact factor: 3.153

6.  Novel 2- and 4-substituted 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric modulators of the A3 adenosine receptor.

Authors:  Yoonkyung Kim; Sonia de Castro; Zhan-Guo Gao; Adriaan P Ijzerman; Kenneth A Jacobson
Journal:  J Med Chem       Date:  2009-04-09       Impact factor: 7.446

7.  Different functional roles of T1R subunits in the heteromeric taste receptors.

Authors:  Hong Xu; Lena Staszewski; Huixian Tang; Elliot Adler; Mark Zoller; Xiaodong Li
Journal:  Proc Natl Acad Sci U S A       Date:  2004-09-07       Impact factor: 11.205

8.  Effect of the calcimimetic R-568 [3-(2-chlorophenyl)-N-((1R)-1-(3-methoxyphenyl)ethyl)-1-propanamine] on correcting inactivating mutations in the human calcium-sensing receptor.

Authors:  Jenny Ying Lin Lu; Yuhua Yang; Gilles Gnacadja; Arthur Christopoulos; Jeff D Reagan
Journal:  J Pharmacol Exp Ther       Date:  2009-09-16       Impact factor: 4.030

Review 9.  Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders.

Authors:  P Jeffrey Conn; Carrie K Jones; Craig W Lindsley
Journal:  Trends Pharmacol Sci       Date:  2009-02-07       Impact factor: 14.819

10.  Mutational analysis and molecular modeling of the allosteric binding site of a novel, selective, noncompetitive antagonist of the metabotropic glutamate 1 receptor.

Authors:  Pari Malherbe; Nicole Kratochwil; Frédéric Knoflach; Marie-Thérèse Zenner; James N C Kew; Claudia Kratzeisen; Hans P Maerki; Geo Adam; Vincent Mutel
Journal:  J Biol Chem       Date:  2002-12-30       Impact factor: 5.157
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  100 in total

1.  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 2.  Metabotropic glutamate receptor subtype 5: molecular pharmacology, allosteric modulation and stimulus bias.

Authors:  K Sengmany; K J Gregory
Journal:  Br J Pharmacol       Date:  2015-11-11       Impact factor: 8.739

3.  Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: Implications for optimizing preclinical neuroscience drug discovery.

Authors:  Kathy Sengmany; Junaid Singh; Gregory D Stewart; P Jeffrey Conn; Arthur Christopoulos; Karen J Gregory
Journal:  Neuropharmacology       Date:  2016-07-05       Impact factor: 5.250

Review 4.  The concept of allosteric interaction and its consequences for the chemistry of the brain.

Authors:  Jean-Pierre Changeux
Journal:  J Biol Chem       Date:  2013-07-22       Impact factor: 5.157

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 of VU0486846: steep SAR from a series of M1 PAMs based on a novel benzomorpholine core.

Authors:  Jeanette L Bertron; Hyekyung P Cho; Pedro M Garcia-Barrantes; Joseph D Panarese; James M Salovich; Kellie D Nance; Darren W Engers; Jerri M Rook; Anna L Blobaum; Colleen M Niswender; Shaun R Stauffer; P Jeffrey Conn; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2018-05-05       Impact factor: 2.823

7.  Synthesis and Preliminary Studies of a Novel Negative Allosteric Modulator, 7-((2,5-Dioxopyrrolidin-1-yl)methyl)-4-(2-fluoro-4-[11C]methoxyphenyl) quinoline-2-carboxamide, for Imaging of Metabotropic Glutamate Receptor 2.

Authors:  Xiaofei Zhang; Katsushi Kumata; Tomoteru Yamasaki; Ran Cheng; Akiko Hatori; Longle Ma; Yiding Zhang; Lin Xie; Lu Wang; Hye Jin Kang; Douglas J Sheffler; Nicholas D P Cosford; Ming-Rong Zhang; Steven H Liang
Journal:  ACS Chem Neurosci       Date:  2017-06-13       Impact factor: 4.418

8.  Integrated In Silico Fragment-Based Drug Design: Case Study with Allosteric Modulators on Metabotropic Glutamate Receptor 5.

Authors:  Yuemin Bian; Zhiwei Feng; Peng Yang; Xiang-Qun Xie
Journal:  AAPS J       Date:  2017-05-30       Impact factor: 4.009

9.  Chemical modification of the M(1) agonist VU0364572 reveals molecular switches in pharmacology and a bitopic binding mode.

Authors:  Gregory J Digby; Thomas J Utley; Atin Lamsal; Christian Sevel; Douglas J Sheffler; Evan P Lebois; Thomas M Bridges; Michael R Wood; Colleen M Niswender; Craig W Lindsley; P Jeffrey Conn
Journal:  ACS Chem Neurosci       Date:  2012-09-09       Impact factor: 4.418

Review 10.  Positive allosteric modulators of the μ-opioid receptor: a novel approach for future pain medications.

Authors:  N T Burford; J R Traynor; A Alt
Journal:  Br J Pharmacol       Date:  2014-07-01       Impact factor: 8.739
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