PMID: 3757154Jan 1, 1986Paper

The antiproliferative properties of tamoxifen and phenothiazines may be mediated by a unique histamine receptor (?H3) distinct from the calmodulin-binding site

Cancer Chemotherapy and Pharmacology
L J BrandesR Bose

Abstract

N,N-diethyl-2-[(4-phenylmethyl)-phenoxy]-ethanamine HCl (DPPE), a novel histamine antagonist (?H3), which selectively binds with high affinity to the antiestrogen-binding site (AEBS/?H3), inhibits the activity of calmodulin-dependent myosin light chain kinase (MLCK) only at concentrations greater than 1 mM, as opposed to tamoxifen (TAM), which has an IC50 = 4 microM in the same assay. This suggests that the antiestrogen-binding site is distinct from the site on calmodulin which binds TAM and phenothiazines. However, at an in vitro concentration of 1 X 10(-6) M, the antiproliferative effects of DPPE and several phenothiazines, which also compete for binding to AEBS/?H3, are about equal; this suggests that affinity for AEBS/?H3 rather than that for the calmodulin-binding site may correlate with clinically relevant antigrowth effects of these compounds.

References

Jan 31, 1985·Biochemical and Biophysical Research Communications·L J BrandesR P Bogdanovic
Jan 1, 1985·Cancer Chemotherapy and Pharmacology·W N HaitE C Cadman
Jun 15, 1985·Biochemical Pharmacology·S D Lyman, V C Jordan
Sep 16, 1985·Biochemical and Biophysical Research Communications·E A Kroeger, L J Brandes
Jan 1, 1980·Annals of the New York Academy of Sciences·B WeissT L Wallace
Jan 13, 1984·Biochemical and Biophysical Research Communications·H Y Lam
Sep 17, 1984·Biochemical and Biophysical Research Communications·L J Brandes, M W Hermonat
Oct 15, 1984·Biochemical and Biophysical Research Communications·L J Brandes
Apr 16, 1984·Biochemical and Biophysical Research Communications·C K Watts, R L Sutherland

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Citations

Jan 1, 1997·European Journal of Cancer : Official Journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR)·K KudohI Nagata
Mar 1, 1989·Cancer Treatment Reviews·D J Stewart, W K Evans
Oct 15, 1990·Biochemical Pharmacology·L J BrandesJ M Gerrard
Mar 1, 1990·European Journal of Cancer : Official Journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR)·T TokoY Yamada
Aug 20, 2010·Systems Biology in Reproductive Medicine·Shyam Sundar Agrawal, Manonmani Alvin Jose
Jan 19, 2002·The Journal of Organic Chemistry·John F ValliantJames F Britten

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