Specific binding of photoaffinity-labeling peptidomimetics of Pro-Leu-Gly-NH2 to the dopamine D2L receptor: evidence for the allosteric modulation of the dopamine receptor.

European Journal of Pharmacology
Amandeep MannR K Mishra

Abstract

The present study was undertaken to investigate the mechanistic role of l-prolyl-l-leucyl-glycinamide (PLG) in modulating agonist binding to the dopamine D(2L) receptor. Competition and displacement assays indicate that the photoaffinity-labeling peptidomimetics of PLG, 3(R)-[(4(S)-(4-azido-2-hydroxy-benzoyl) amino-2(S)-pyrrolidinylcarbonyl)amino]-2-oxo-1-pyrrolidineacetamide hydrochloride (1a) and 3(R)-[(4(S)-(4-azido-2-hydroxy-5-iodo-benzoyl)amino-2(S)-pyrrolidinylcarbonyl)amino]-2-oxo-1-pyrrolidineacetamide hydrochloride (1b) bind at the same site as PLG. Autoradiography was used to establish the covalent binding of [(125)I]-1b to an approximately 51kDa protein in bovine striatal membranes. Western blot analysis with a dopamine D(2L)-specific antibody, in combination with autoradiography, following a two-dimensional gel separation, suggested this approximately 51kDa protein to be the dopamine D(2L) receptor. Further evidence for binding of 1b to dopamine D(2L) was provided by samples immunoprecipitated with the D(2L) antibody. These samples were analyzed by western blotting in parallel with autoradiography of [(125)I]-1b labeled protein. Both methods revealed bands at approximately 51kDa. Furthermore, PLG is shown to compete...Continue Reading

References

Jan 1, 1976·Pharmacology, Biochemistry, and Behavior·A BarbeauA J Kastin
Jun 1, 1986·Pharmacology, Biochemistry, and Behavior·C Hara, A J Kastin
Oct 1, 1986·Pharmacology, Biochemistry, and Behavior·C Hara, A J Kastin
Jul 18, 1969·Science·A BarbeauJ Genest
Jan 1, 1983·Progress in Neuro-psychopharmacology & Biological Psychiatry·S ChiuR K Mishra
Sep 1, 1982·Journal of Biochemical and Biophysical Methods·B BjellqvistW Postel
Jan 1, 1994·Neuroscience and Biobehavioral Reviews·G W ReedR D Olson
Aug 1, 1994·Journal of Affective Disorders·R H EhrensingA H Mebane
Jan 1, 1993·Journal of Molecular Neuroscience : MN·G M RossR K Mishra
May 31, 2002·Pharmacological Reviews·Arthur Christopoulos, Terry Kenakin
Mar 5, 2004·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Anders A Jensen, Tracy A Spalding
Jul 29, 2004·Current Pharmaceutical Design·L T MayA Christopoulos
Oct 21, 2004·Biochemical Society Transactions·A ChristopoulosP M Sexton
Aug 30, 2005·The Journal of Pharmacology and Experimental Therapeutics·Vaneeta VermaRam K Mishra

❮ Previous
Next ❯

Citations

May 16, 2014·Medicinal Research Reviews·Shaoyong LuJian Zhang
Oct 29, 2015·Organic Letters·Ramesh Chingle, William D Lubell
Feb 13, 2013·Beilstein Journal of Organic Chemistry·Swapna BhagwanthRodney L Johnson
Sep 12, 2020·Pharmacological Reviews·C Sue CarterMarcy A Kingsbury
Aug 15, 2018·Journal of Medicinal Chemistry·Eric A WoldJia Zhou

❮ 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.