PMID: 3754598Jan 1, 1986Paper

Affinity-labeling steroids as biologically active probes of antiglucocorticoid hormone action

Journal of Steroid Biochemistry
S Stoney Simons, P A Miller

Abstract

The role of the glucocorticoid receptor in the expression of antiglucocorticoid action has been investigated with a chemically-reactive derivative of three glucocorticoid steroids with differing biological potencies, i.e. the C-21 mesylates of cortisol, dexamethasone and deacylcortivazol. Dexamethasone 21-mesylate (Dex-Mes) was the most useful derivative due to its favorable balance of high receptor affinity and predominantly irreversible antiglucocorticoid activity. A number of criteria have been used to conclude that [3H]Dex-Mes covalently labels glucocorticoid receptors in the steroid-binding cavity. The available data indicate that covalent Dex-Mes-labeled receptors (mol. wt approximately equal to 98,000) are responsible for the irreversible antiglucocorticoid activity while the partial agonist activity of Dex-Mes is due to non-covalent Dex-Mes-bound receptors. Further support for this hypothesis comes from the observations that deacylcortivazol 21-mesylate was a full glucocorticoid and did not affinity label receptors (and marginally labeled cytosol proteins) although it was capable of covalently-labeling bovine serum albumin. Several mechanisms for the expression of irreversible antiglucocorticoid activity by covalent Dex...Continue Reading

References

Feb 14, 1979·Biochemical and Biophysical Research Communications·S S SimonsD F Johnson
Apr 1, 1977·Molecular and Cellular Endocrinology·V C JordanG Prestwich
Oct 1, 1974·Proceedings of the National Academy of Sciences of the United States of America·K R YamamotoG M Tomkins
Aug 28, 1970·Journal of Molecular Biology·H H Samuels, G M Tomkins
Nov 15, 1984·The Biochemical Journal·G G Rousseau
Sep 1, 1980·Proceedings of the National Academy of Sciences of the United States of America·S S SimonsD F Johnson
May 1, 1984·Proceedings of the National Academy of Sciences of the United States of America·C Scheidereit, M Beato
Jan 1, 1984·Annual Review of Biochemistry·C T Walsh
Jun 1, 1981·Proceedings of the National Academy of Sciences of the United States of America·S S Simons, E B Thompson
Jan 1, 1982·Proceedings of the National Academy of Sciences of the United States of America·G AmitaiM Sokolovsky
Jan 1, 1980·Journal of Steroid Biochemistry·J P RaynaudJ P Mornon

❮ Previous
Next ❯

Citations

Sep 1, 1985·Journal of Steroid Biochemistry·M PonsS S Simons
Oct 1, 1988·Journal of Steroid Biochemistry·G G RousseauJ I Quivy
Feb 1, 1990·Journal of Steroid Biochemistry·K G PinneyJ A Katzenellenbogen
Jan 1, 1996·Pharmacology & Therapeutics·M K Agarwai
Mar 1, 1993·The Journal of Steroid Biochemistry and Molecular Biology·T BurollaudM Dautrevaux
Sep 1, 1993·The Journal of Steroid Biochemistry and Molecular Biology·Y MiyashitaS S Simons
Jan 12, 2000·Molecular and Cellular Endocrinology·Y Huang, S S Simons
Jun 28, 2008·Molecular and Cellular Endocrinology·Yunguang SunS Stoney Simons
Sep 11, 2016·Bioorganic & Medicinal Chemistry Letters·Oksana RyabtsovaHans De Winter
Jul 16, 2005·Stress : the International Journal on the Biology of Stress·B W M M PeetersG S F Ruigt

❮ 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.