Drug Design Strategies for GPCR Allosteric Modulators

被引:24
作者
Conn, P. Jeffrey [1 ]
Kuduk, Scott D. [2 ]
Doller, Dario [3 ,4 ]
机构
[1] Vanderbilt Univ, Dept Pharmacol, Vanderbilt Ctr Neurosci Drug Discovery, Nashville, TN 37203 USA
[2] Merck Res Labs, Dept Med Chem, West Point, PA USA
[3] Lundbeck Res USA, Neuroinflarnmat Dis Biol Unit, Paramus, NJ USA
[4] Lundbeck Res DK, Discovery Chem & DMPK, Valby, Denmark
来源
ANNUAL REPORTS IN MEDICINAL CHEMISTRY, VOL 47 | 2012年 / 47卷
关键词
PROTEIN-COUPLED RECEPTORS; LIGANDS; MECHANISM; DISCOVERY; AGONISTS; BINDING; MGLUR5; ASSAY;
D O I
10.1016/B978-0-12-396492-2.00028-X
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
引用
收藏
页码:441 / 457
页数:17
相关论文
共 44 条
[41]   The Best of Both Worlds? Bitopic Orthosteric/Allosteric Ligands of G Protein-Coupled Receptors [J].
Valant, Celine ;
Lane, J. Robert ;
Sexton, Patrick M. ;
Christopoulos, Arthur .
ANNUAL REVIEW OF PHARMACOLOGY AND TOXICOLOGY, VOL 52, 2012, 52 :153-178
[42]   Probe Dependence in the Allosteric Modulation of a G Protein-Coupled Receptor: Implications for Detection and Validation of Allosteric Ligand Effects [J].
Valant, Celine ;
Felder, Christian C. ;
Sexton, Patrick M. ;
Christopoulos, Arthur .
MOLECULAR PHARMACOLOGY, 2012, 81 (01) :41-52
[43]   Synthesis and SAR of centrally active mGlu5 positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold [J].
Williams, Richard ;
Manka, Jason T. ;
Rodriguez, Alice L. ;
Vinson, Paige N. ;
Niswender, Colleen M. ;
Weaver, C. David ;
Jones, Carrie K. ;
Conn, P. Jeffrey ;
Lindsley, Craig W. ;
Stauffer, Shaun R. .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2011, 21 (05) :1350-1353
[44]   "Molecular Switches" on mGluR Allosteric Ligands That Modulate Modes of Pharmacology [J].
Wood, Michael R. ;
Hopkins, Corey R. ;
Brogan, John T. ;
Conn, P. Jeffrey ;
Lindsley, Craig W. .
BIOCHEMISTRY, 2011, 50 (13) :2403-2410