Recent advances in positive allosteric modulators of metabotropic glutamate receptors

被引:0
|
作者
Shipe, WD
Wolkenberg, SE
Williams, DL
Lindsley, CW
机构
[1] Merck Res Labs, Dept Med Chem, Technol Enabled Synth Grp, West Point, PA 19486 USA
[2] Imaging Res, West Point, PA 19486 USA
关键词
G protein-coupled receptor; metabotropic glutamate receptor; mGluR; positive allosteric modulator; potentiator;
D O I
暂无
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Positive allosteric modulators of metabotropic glutamate receptors (mGluRs) are the subject of intensive research due to their emerging therapeutic potential for a range of psychiatric and neurological disorders such as pain, anxiety, cognition, Parkinson's disease and schizophrenia. Positive allosteric modulators, which are small molecules capable of enhancing agonist-mediated receptor activity while possessing no intrinsic agonist activity, have recently been described for group I (mGluR1 and mGluR5), group II (mGluR2) and group III (mGluR4) mGluRs. Relative to classical mGluR agonists, these molecules offer improved selectivity versus other mGluRs and chemical tractability, and may reduce the liability of receptor desensitization.
引用
收藏
页码:449 / 457
页数:9
相关论文
共 50 条
  • [1] Screening for Positive Allosteric Modulators at Metabotropic Glutamate Receptors
    Langmead, Chris
    [J]. JOURNAL OF BIOMOLECULAR SCREENING, 2009, 14 (07) : 903 - 904
  • [2] Positive allosteric modulators of metabotropic glutamate 2 receptors in schizophrenia treatment
    Ellaithy, Amr
    Younkin, Jason
    Gonzalez-Maeso, Javier
    Logothetis, Diomedes E.
    [J]. TRENDS IN NEUROSCIENCES, 2015, 38 (08) : 506 - 516
  • [3] Photoswitchable allosteric modulators for metabotropic glutamate receptors
    Gomez-Santacana, Xavier
    Panarello, Silvia
    Rovira, Xavier
    Llebaria, Amadeu
    [J]. CURRENT OPINION IN PHARMACOLOGY, 2022, 66
  • [4] Asymmetric functioning of dimeric metabotropic glutamate receptors disclosed by positive allosteric modulators
    Goudet, C
    Kniazeff, J
    Hlavackova, V
    Malhaire, F
    Maurel, D
    Acher, F
    Blahos, J
    Prézeau, L
    Pin, JP
    [J]. JOURNAL OF BIOLOGICAL CHEMISTRY, 2005, 280 (26) : 24380 - 24385
  • [5] Metabotropic glutamate receptors: Agonists, antagonists and allosteric modulators
    Augelli-Szafran, CE
    Schwarz, RD
    [J]. ANNUAL REPORTS IN MEDICINAL CHEMISTRY, VOL 38, 2003, 38 : 21 - 30
  • [6] MODELLING THE FUNCTION OF METABOTROPIC GLUTAMATE RECEPTORS ALLOSTERIC MODULATORS
    Rovira, X.
    Roche, D.
    Serra, J.
    Pin, J. -P.
    Giraldo, J.
    [J]. METHODS AND FINDINGS IN EXPERIMENTAL AND CLINICAL PHARMACOLOGY, 2008, 30 : 78 - 78
  • [7] Glutamate-based therapeutic approaches: allosteric modulators of metabotropic glutamate receptors
    Marino, MJ
    Conn, PJ
    [J]. CURRENT OPINION IN PHARMACOLOGY, 2006, 6 (01) : 98 - 102
  • [8] Control of autoimmune inflammation using liposomes to deliver positive allosteric modulators of metabotropic glutamate receptors
    Gammon, Joshua M.
    Adapa, Arjun R.
    Jewell, Christopher M.
    [J]. JOURNAL OF BIOMEDICAL MATERIALS RESEARCH PART A, 2017, 105 (11) : 2977 - 2985
  • [9] Modeling of structure and binding site of allosteric modulators of metabotropic glutamate, receptors
    Yanamala, Naveena V. K.
    Tirupula, Kalyan C.
    Nadella, Kasturi
    Nagarajan, Vaidehi
    Klein-Seetharaman, Judith
    [J]. BIOPHYSICAL JOURNAL, 2007, : 5A - 5A
  • [10] Allosteric Modulators of Metabotropic Glutamate Receptors as Novel Therapeutics for Neuropsychiatric Disease
    Luessen, Deborah J.
    Conn, P. Jeffrey
    [J]. PHARMACOLOGICAL REVIEWS, 2022, 74 (03) : 630 - 661