Biochem Biophys Res Commun. 1990 Dec 14;173(2):534-40.

A mutation in the ligand binding domain of the androgen receptor of human LNCaP cells affects steroid binding characteristics and response to anti-androgens.

Veldscholte J, Ris-Stalpers C, Kuiper GG, Jenster G, Berrevoets C, Claassen E, van Rooij HC, Trapman J, Brinkmann AO, Mulder E.

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Department of Biochemistry II, Erasmus University Rotterdam, The Netherlands.

Abstract

LNCaP prostate tumor cells contain an abnormal androgen receptor system. Progestagens, estradiol and anti-androgens can compete with androgens for binding to the androgen receptor and can stimulate both cell growth and excretion of prostate specific acid phosphatase. We have discovered in the LNCaP androgen receptor a single point mutation changing the sense of codon 868 (Thr to Ala) in the ligand binding domain. Expression vectors containing the normal or mutated androgen receptor sequence were transfected into COS or Hela cells. Androgens, progestagens, estrogens and anti-androgens bind the mutated androgen receptor protein and activate the expression of an androgen-regulated reporter gene construct (GRE-tk-CAT). The mutation therefore influences both binding and the induction of gene expression by different steroids and antisteroids.

PMID:: 2260966; [PubMed - indexed for MEDLINE]

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Review The androgen receptor in LNCaP cells contains a mutation in the ligand binding domain which affects steroid binding characteristics and response to antiandrogens. [J Steroid Biochem Mol Biol. 1992]
Review The androgen receptor in LNCaP cells contains a mutation in the ligand binding domain which affects steroid binding characteristics and response to antiandrogens.
Veldscholte J, Berrevoets CA, Ris-Stalpers C, Kuiper GG, Jenster G, Trapman J, Brinkmann AO, Mulder E. J Steroid Biochem Mol Biol. 1992 Mar; 41(3-8):665-9.
Anti-androgens and the mutated androgen receptor of LNCaP cells: differential effects on binding affinity, heat-shock protein interaction, and transcription activation. [Biochemistry. 1992]
Anti-androgens and the mutated androgen receptor of LNCaP cells: differential effects on binding affinity, heat-shock protein interaction, and transcription activation.
Veldscholte J, Berrevoets CA, Brinkmann AO, Grootegoed JA, Mulder E. Biochemistry. 1992 Mar 3; 31(8):2393-9.
Unusual specificity of the androgen receptor in the human prostate tumor cell line LNCaP: high affinity for progestagenic and estrogenic steroids. [Biochim Biophys Acta. 1990]
Unusual specificity of the androgen receptor in the human prostate tumor cell line LNCaP: high affinity for progestagenic and estrogenic steroids.
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Montgomery BT, Young CY, Bilhartz DL, Andrews PE, Prescott JL, Thompson NF, Tindall DJ. Prostate. 1992; 21(1):63-73.
Review Regulation of growth of LNCaP human prostate tumor cells by growth factors and steroid hormones. [J Steroid Biochem Mol Biol. 1991]
Review Regulation of growth of LNCaP human prostate tumor cells by growth factors and steroid hormones.
Schuurmans AL, Bolt J, Veldscholte J, Mulder E. J Steroid Biochem Mol Biol. 1991; 40(1-3):193-7.

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