PMID: 6965793Jan 1, 1980Paper

Specific binding of phorbol ester tumor promoters

Proceedings of the National Academy of Sciences of the United States of America
P E Driedger, P M Blumberg

Abstract

[20-(3)H]Phorbol 12,13-dibutyrate bound to particulate preparations from chicken embryo fibroblasts in a specific, saturable, reversible fashion. Equilibrium binding occurred with a K(d) of 25 nM; this value is very close to the 50% effective dose (ED(50)), 50 nM, previously determined for the biological response (induction of fibronectin loss) in growing chicken embryo fibroblasts. At saturation, 1.4 pmol of [20-(3)H]phorbol 12,13-dibutyrate was bound per mg of protein (approximately 7 x 10(4) molecules per cell). Binding was inhibited by phorbol 12-myristate 13-acetate (K(i) = 2 nM), mezerein (K(i) = 180 nM), phorbol 12,13-dibenzoate (K(i) = 180 nM), phorbol 12,13-diacetate (K(i) = 1.7 muM), phorbol 12,13,20-triacetate (K(i) = 39 muM), and phorbol 13-acetate (K(i) = 120 muM). The measured K(i) values are all within a factor of 3.5 of the ED(50) values of these derivatives for inducing loss of fibronectin in intact cells. Binding was not inhibited by the inactive compounds phorbol (10 mug/ml) and 4alpha-phorbol 12,13-didecanoate (10 mug/ml) or by the inflammatory but nonpromoting phorbol-related diterpene esters resiniferatoxin (100 ng/ml) and 12-deoxyphorbol 13-isobutyrate 20-acetate (100 ng/ml). These data suggest that biolo...Continue Reading

References

Feb 28, 1979·Biochemical and Biophysical Research Communications·K D BrownE Rozengurt
Feb 28, 1979·Biochemical and Biophysical Research Communications·P B FisherI B Weinstein
Jul 15, 1978·International Journal of Cancer. Journal International Du Cancer·P E Driedger, P M Blumberg
Nov 26, 1976·The Journal of Organic Chemistry·S M KupchanB R Sickles
Jan 1, 1975·Psychoneuroendocrinology·J R SmythiesR D Morin
Jan 1, 1974·CRC Critical Reviews in Toxicology·R K Boutwell

❮ Previous
Next ❯

Citations

Jan 1, 1983·Journal of Cancer Research and Clinical Oncology·R Keller
Jan 1, 1982·Journal of Cancer Research and Clinical Oncology·J MiwaH Yamasaki
Jan 1, 1989·Archives of Virology·M SimonB Bültmann
Feb 1, 1996·Pflügers Archiv : European journal of physiology·M L Calonge, A A Ilundáin
Feb 8, 1985·Biochimica Et Biophysica Acta·M C Cabot
Feb 17, 1984·European Journal of Pharmacology·S Heisler
Oct 24, 1994·European Journal of Pharmacology·A J WoodsP L Andrews
Jan 1, 1985·Pharmacology & Therapeutics·P B Fisher, S Grant
Jan 1, 1992·Pharmacology & Therapeutics·J DiGiovanni
Sep 1, 1993·Pharmacology & Therapeutics·A Basu
Jan 1, 1990·International Journal of Immunopharmacology·J FaveroJ W Parker
Jan 1, 1985·Biochimica Et Biophysica Acta·J M Vasiliev
Apr 1, 1991·Journal of Ethnopharmacology·F J Evans
May 1, 2004·Trends in Pharmacological Sciences·Alexandra C Newton
Sep 30, 1981·Biochemical and Biophysical Research Communications·N H Colburn, T D Gindhart
Jul 22, 1998·Progress in Neurobiology·H Majewski, L Iannazzo
Sep 1, 1980·Proceedings of the National Academy of Sciences of the United States of America·J CroopH Holtzer
Sep 1, 1980·Proceedings of the National Academy of Sciences of the United States of America·S H YuspaT Ben

❮ 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.