Fluorescent GPCR Ligands as New Tools in Pharmacology

被引:40
作者
Kuder, Kamil [1 ]
Kiec-Kononowicz, Katarzyna [1 ]
机构
[1] Jagiellonian Univ, Fac Pharm, Dept Technol & Biotechnol Drugs, Coll Med, PL-30688 Krakow, Poland
关键词
Fluorescence; fluorescent ligands; fluorophores; GPCRs;
D O I
10.2174/092986708785747599
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
The expansion of fluorescent techniques for studying the ligand-receptor interaction resulted in a burst of the novel fluorescent ligands development. The discovery of the ligand, that is of high affinity to the receptor and whose localization could be easily visualized, even on the single cell level, gave the researchers a strong impulse to investigate that field of GPCR ligands. Moreover, paying attention to the "non pharmacological" advantages of these ligands, as well as the techniques to be used, fluorescent ligands are becoming treated more seriously, as the ligands themselves, and as novel, useful tools for studying GPCRs. Herein, we review results described in the literature, starting from the year 2000, in the field of the fluorescent GPCR small, non-peptide ligands according to the affinity to the selected receptors ( histamine, adenosine, adrenergic, cannabinoid, muscarinie, neuropeptide Y and serotonine) as well as the fluorophores that have been used to tag the molecules.
引用
收藏
页码:2132 / 2143
页数:12
相关论文
共 40 条
[1]  
Alexander SPH, 2004, BRIT J PHARMACOL, V141, pS1
[2]   Fluorescent non-imidazole histamine H3 receptor ligands with nanomolar affinities [J].
Amon, M ;
Ligneau, X ;
Schwartz, JC ;
Stark, H .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2006, 16 (07) :1938-1940
[3]   Highly potent fluorescence-tagged nonimidazole histamine H3 receptor ligands [J].
Amon, Michael ;
Ligneau, Xavier ;
Camelin, Jean-Claude ;
Berrebi-Bertrand, Isabelle ;
Schwartz, Jean-Charles ;
Stark, Holger .
CHEMMEDCHEM, 2007, 2 (05) :708-716
[4]   DIRECT MAPPING OF BETA-ADRENERGIC RECEPTORS IN RAT CENTRAL NERVOUS-SYSTEM BY A NOVEL FLUORESCENT BETA-BLOCKER [J].
ATLAS, D ;
MELAMED, E .
BRAIN RESEARCH, 1978, 150 (02) :377-385
[5]   SELECTIVE FLUORESCENT LIGANDS FOR PHARMACOLOGICAL RECEPTORS [J].
BAINDUR, N ;
TRIGGLE, DJ .
DRUG DEVELOPMENT RESEARCH, 1994, 33 (04) :373-398
[6]   CONCEPTS AND PROGRESS IN THE DEVELOPMENT AND UTILIZATION OF RECEPTOR-SPECIFIC FLUORESCENT LIGANDS [J].
BAINDUR, N ;
TRIGGLE, DJ .
MEDICINAL RESEARCH REVIEWS, 1994, 14 (06) :591-664
[7]   Pharmacology and direct visualisation of BODIPY-TMR-CGP:: a long-acting fluorescent β2-adrenoceptor agonist [J].
Baker, JG ;
Hall, IP ;
Hill, SJ .
BRITISH JOURNAL OF PHARMACOLOGY, 2003, 139 (02) :232-242
[8]   Pharmacological characterization of CGP 12177 at the human β2-adrenoceptor [J].
Baker, JG ;
Hall, IP ;
Hill, SJ .
BRITISH JOURNAL OF PHARMACOLOGY, 2002, 137 (03) :400-408
[9]   How photons start vision [J].
Baylor, D .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1996, 93 (02) :560-565
[10]   Synthesis and characterization of the first fluorescent antagonists for human 5-HT4 receptors [J].
Berque-Bestel, I ;
Soulier, JL ;
Giner, M ;
Rivail, L ;
Langlois, M ;
Sicsic, S .
JOURNAL OF MEDICINAL CHEMISTRY, 2003, 46 (13) :2606-2620