Antagonist of phorbol ester receptor-mediated chemotaxis in mouse peritoneal macrophages

Biologically active phorbol ester derivatives displace [3H]phorbol-12, 13-dibutyrate from thioglycollate-elicited mouse peritoneal macrophages in a time-, temperature-, and concentration-dependent manner. Scatchard analysis revealed an apparent Kd of 54.1 nM and 8.0 X 10(5) sites/cell, indicating th...

Full description

Saved in:
Bibliographic Details
Published in:Cancer research (Chicago, Ill.) Ill.), 1983-10, Vol.43 (10), p.4552-4556
Main Authors: STURM, R. J, SMITH, B. M, LANE, R. W, LASKIN, D. L, HARRIS, L. S, CARCHMAN, R. A
Format: Article
Language:English
Subjects:
Animals
Ascitic Fluid - cytology
Binding, Competitive
Biological and medical sciences
Caenorhabditis elegans Proteins
Carcinogenesis, carcinogens and anticarcinogens
Carrier Proteins
Chemical agents
chemotaxis
Chemotaxis - drug effects
Female
macrophages
Macrophages - drug effects
Medical sciences
Mice
Phorbol 12,13-Dibutyrate
Phorbol Esters - metabolism
phorbol myristate acetate
phorbol-12,13-diacetate
Protein Kinase C
receptors
Receptors, Cell Surface - metabolism
Receptors, Drug
Tetradecanoylphorbol Acetate - metabolism
Time Factors
Tumors
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Biologically active phorbol ester derivatives displace [3H]phorbol-12, 13-dibutyrate from thioglycollate-elicited mouse peritoneal macrophages in a time-, temperature-, and concentration-dependent manner. Scatchard analysis revealed an apparent Kd of 54.1 nM and 8.0 X 10(5) sites/cell, indicating that these macrophages possess saturable, high-affinity phorbol ester-binding sites. These derivatives also act as chemoattractants for the macrophage at equivalent concentrations. A notable exception to this pattern is phorbol-12,13-diacetate. Phorbol-12,13-diacetate inhibits specific binding of [3H]phorbol-12,13-dibutyrate (concentration required for a 50% inhibition of the maximum specific binding of [3H]phorbol-12,13-dibutyrate, 2.6 microM) and chemotaxis to phorbol-12-myristate, 13-acetate (concentration required for a 50% inhibition of the maximum chemotactic response, 0.39 microM) while exhibiting no activity as a chemoattractant at concentrations up to 10(-5) M. The data indicate that phorbol-12,13-diacetate may be an antagonist for receptor-mediated chemotaxis to phorbol-12-myristate, 13-acetate in the macrophage.
ISSN:0008-5472
1538-7445