Ligand-binding modes in cationic biogenic amine receptors

Chembiochem : a European Journal of Chemical Biology
Masaji Ishiguro

Abstract

The binding site in G protein-coupled cationic biogenic amine receptors is formed in the cleft of the seven transmembrane segments. Upon binding the ligand, the receptors are activated or inactivated through the conformational changes of the transmembrane segments. G protein-coupled receptors bind four functionally distinct ligands; inverse agonists, antagonists, partial agonists, and full agonists. Hence, putative structural models for biogenic amine receptors corresponding to the ligand function (inverse agonist-, antagonist-, partial agonist-, and full agonist-bound receptor models) were built by using photointermediate models in the rhodopsin photocascade (M. Ishiguro et al. ChemBioChem. 2004, 5, 298-310). The ligand-receptor recognition of each was examined by modeling receptor-ligand complexes with functional ligands. The complex models suggested that each functional ligand binds the corresponding receptor structure and that ligand-specific interactions contribute to stabilization of the corresponding receptor structure.

References

Oct 1, 1992·Neuron·P R RobinsonD D Oprian
Jul 1, 1987·Proceedings of the National Academy of Sciences of the United States of America·C D StraderR A Dixon
Mar 1, 1995·Trends in Pharmacological Sciences·P Leff
Jan 1, 1994·Annual Review of Biochemistry·C D StraderR A Dixon
Sep 15, 1994·Biochemical and Biophysical Research Communications·K OhtaH Fukui
Aug 15, 1993·Proceedings of the National Academy of Sciences of the United States of America·S Arnis, K P Hofmann
Aug 20, 1996·Proceedings of the National Academy of Sciences of the United States of America·K WielandM J Lohse
Oct 11, 1996·The Journal of Biological Chemistry·S Acharya, S S Karnik
Jan 1, 1997·Journal of Receptor and Signal Transduction Research·A Scheer, S Cotecchia
Jan 15, 1998·Progress in Nucleic Acid Research and Molecular Biology·T P Sakmar
Oct 8, 1999·European Journal of Pharmacology·F HeitzC Guenet
Jun 24, 2000·Science·B BorhanK Nakanishi
Aug 5, 2000·Science·K PalczewskiM Miyano
Apr 25, 2002·Proceedings of the National Academy of Sciences of the United States of America·Tetsuji OkadaYoshinori Shichida
Oct 3, 2003·Journal of Medicinal Chemistry·Kristina E Furse, Terry P Lybrand
Feb 26, 2004·Proceedings of the National Academy of Sciences of the United States of America·Peter L FreddolinoWilliam A Goddard
Mar 5, 2004·Chembiochem : a European Journal of Chemical Biology·Masaji IshiguroTakahiro Hirano

❮ Previous
Next ❯

Citations

Sep 19, 2009·Bioorganic & Medicinal Chemistry Letters·Toshiyuki WakimotoYoshihide Suwa
Mar 26, 2005·Chembiochem : a European Journal of Chemical Biology·Thomas Klabunde, Andreas Evers
Aug 30, 2008·Journal of Peptide Science : an Official Publication of the European Peptide Society·Yoshinori SasakiRyoichi Katakai
Jul 22, 2008·Medicinal Research Reviews·Jing ZhangAo Zhang
Sep 15, 2005·Chemical Reviews·Francesca Fanelli, Pier G De Benedetti

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.