Protein Information

Name androgen receptor
Synonyms AIS; AR; Androgen receptor; DHTR; Dihydrotestosterone receptor; HUMARA; KD; NR3C4…

Compound Information

Name cycloheximide
CAS

Reference List

PubMed Abstract RScore(About this table)
19584240 Kim SH, Singh SV: D,L-Sulforaphane causes transcriptional repression of androgen receptor in human prostate cancer cells. Mol Cancer Ther. 2009 Jul;8(7):1946-54. Epub 2009 Jul 7.

The decrease in AR protein level resulting from SFN exposure was not reversed in the presence of the protein synthesis inhibitor cycloheximide.
2(0,0,0,2) Details
18008333 Chiu FL, Lin JK: Downregulation of androgen receptor expression by luteolin causes inhibition of cell proliferation and induction of apoptosis in human prostate cancer cells and xenografts. Prostate. 2008 Jan 1;68(1):61-71.

We determined the mechanism of AR downregulation with cycloheximide chase assays, proteasome inhibitor, and coimmunoprecipitation experiments.
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18202547 Harada N, Murata Y, Yamaji R, Miura T, Inui H, Nakano Y: Resveratrol down-regulates the androgen receptor at the post-translational level in prostate cancer cells. J Nutr Sci Vitaminol. 2007 Dec;53(6):556-60.

Furthermore, the half-life of AR protein was approximately 4 h in resveratrol-treated AR-positive prostate cancer LNCaP cells, compared to approximately 13 h in control cells, as determined by cycloheximide chase.
2(0,0,0,2) Details
17624924 Prescott J, Jariwala U, Jia L, Cogan JP, Barski A, Pregizer S, Shen HC, Arasheben A, Neilson JJ, Frenkel B, Coetzee GA: Androgen receptor-mediated repression of novel target genes. Prostate. 2007 Sep 15;67(13):1371-83.

Cycloheximide attenuated DHT-mediated repression of CHRM1, suggesting the requirement of new protein synthesis.
2(0,0,0,2) Details
18599551 Wu ZY, Chen K, Haendler B, McDonald TV, Bian JS: Stimulation of N-terminal truncated isoform of androgen receptor stabilizes human ether-a-go-go-related gene-encoded potassium channel protein via activation of extracellular signal regulated kinase 1/2. Endocrinology. 2008 Oct;149(10):5061-9. Epub 2008 Jul 3.

Consistently, the cycloheximide-based protein chase study showed that 5alpha-DHT prolonged HERG protein half-life. 5alpha-DHT/AR45 signaling induced phosphorylation of ERK1/2.
2(0,0,0,2) Details
16704988 Wang LG, Liu XM, Chiao JW: Repression of androgen receptor in prostate cancer cells by phenethyl isothiocyanate. Carcinogenesis. 2006 Oct;27(10):2124-32. Epub 2006 May 16.

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19366804 Steinkamp MP, O'Mahony OA, Brogley M, Rehman H, Lapensee EW, Dhanasekaran S, Hofer MD, Kuefer R, Chinnaiyan A, Rubin MA, Pienta KJ, Robins DM: Treatment-dependent androgen receptor mutations in prostate cancer exploit multiple mechanisms to evade therapy. Cancer Res. 2009 May 15;69(10):4434-42. Epub 2009 Apr 14.

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15805247 Cinar B, De Benedetti A, Freeman MR: Post-transcriptional regulation of the androgen receptor by Mammalian target of rapamycin. Cancer Res. 2005 Apr 1;65(7):2547-53.

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16467405 Kiyomiya K, Lee MS, Tseng IC, Zuo H, Barndt RJ, Johnson MD, Dickson RB, Lin CY: Matriptase activation and shedding with HAI-1 is induced by steroid sex hormones in human prostate cancer cells, but not in breast cancer cells. Am J Physiol Cell Physiol. 2006 Jul;291(1):C40-9. Epub 2006 Feb 8.

DHT-induced matriptase activation and shedding were significantly inhibited by the androgen antagonist bicalutamide, by the RNA transcription inhibitor actinomycin D, and by the protein synthesis inhibitor cycloheximide.
These results suggest that in LNCaP cells, androgen induces matriptase activation via the androgen receptor, and requires transcription and protein synthesis.
1(0,0,0,1) Details
17412801 Tai PJ, Huang YH, Shih CH, Chen RN, Chen CD, Chen WJ, Wang CS, Lin KH: Direct regulation of androgen receptor-associated protein 70 by thyroid hormone and its receptors. Endocrinology. 2007 Jul;148(7):3485-95. Epub 2007 Apr 5.

Cycloheximide treatment did not suppress induction of ARA70 transcription by T3, suggesting that this regulation is direct.
Androgen receptor (AR)-associated protein 70 (ARA70) was one gene found to be up-regulated by T3.
1(0,0,0,1) Details
19711044 Yum J, Jeong HM, Kim S, Seo JW, Han Y, Lee KY, Yeo CY: PKA-mediated stabilization of FoxH1 negatively regulates ERalpha activity. Mol Cells. 2009 Jul;28(1):67-71. Epub 2009 Jul 8.


FoxH1 represses the transcriptional activities of estrogen receptors and androgen receptors (AR).
1(0,0,0,1) Details
18974150 Chan CS, Song JS: CCCTC-binding factor confines the distal action of estrogen receptor. . Cancer Res. 2008 Nov 1;68(21):9041-9.

Distal enhancers have recently emerged as a common mode of gene regulation for several transcription factors, including estrogen and androgen receptors, the two key regulators of breast and prostate cancer major subtypes.
The proposed method combines a recent map of the insulator protein CCCTC-binding factor (CTCF) with previous ER location studies and expression profiling in the presence of the translation inhibitor cycloheximide, providing evidence that CTCF partitions the human genome into distinct ER-regulatory blocks.
1(0,0,0,1) Details
18935790 Huang YH, Tsai MM, Lin KH: Thyroid hormone dependent regulation of target genes and their physiological significance. Chang Gung Med J. 2008 Jul-Aug;31(4):325-34.

The data demonstrated that approximately 149 genes represented were positively regulated by T3, including fibrinogen, transferrin, fibronectin (FN), androgen receptor (AR)-associated protein (ARA70), and dehydroepiandrosterone sulfotransferase family 1A member 2 (SULT2A1).
The protein synthesis inhibitor, cycloheximide was used to determine whether the regulation was direct or indirect.
1(0,0,0,1) Details
17914092 Darby S, Stockley J, Khan MM, Robson CN, Leung HY, Gnanapragasam VJ: Expression of GnRH type II is regulated by the androgen receptor in prostate cancer. Endocr Relat Cancer. 2007 Sep;14(3):613-24.

In LNCaP cells, GnRH II induction by androgens was blocked by the AR inhibitor casodex, but not by cycloheximide treatment.
1(0,0,0,1) Details
15538745 Lou YR, Nazarova N, Talonpoika R, Tuohimaa P: 5alpha-dihydrotestosterone inhibits 1alpha,25-dihydroxyvitamin D3-induced expression of CYP24 in human prostate cancer cells. Prostate. 2005 May 15;63(3):222-30.


An androgen receptor (AR) antagonist, Casodex antagonized the DHT effect, whereas an AR agonist (due to the mutant AR in LNCaP cells) hydroxyflutamide did not.
1(0,0,0,1) Details
16728719 Sun YH, Gao X, Tang YJ, Xu CL, Wang LH: Androgens induce increases in intracellular calcium via a G protein-coupled receptor in LNCaP prostate cancer cells. J Androl. 2006 Sep-Oct;27(5):671-8. Epub 2006 May 25.


Neither an antagonist of intracellular androgen receptors (cyproterone acetate) nor a protein synthesis inhibitor (cycloheximide) affected this fast Ca2+ influx.
0(0,0,0,0) Details
18264125 Lafayette SS, Vladimirova I, Garcez-do-Carmo L, Monteforte PT, Caricati Neto A, Jurkiewicz A: Evidence for the participation of calcium in non-genomic relaxations induced by androgenic steroids in rat vas deferens. Br J Pharmacol. 2008 Mar;153(6):1242-50. Epub 2008 Feb 11.


The androgen-induced relaxation was also not blocked by the protein synthesis inhibitor cycloheximide (300 microM) or by the classical androgen receptor flutamide (up to 100 microM), corroborating that the effect is non-genomic.
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16548285 Castillo C, Castillo EF, Lopez J, Lopez RM: [Testosterone inhibits the contractile responses to phenylephrine associated with the release of intracellular calcium in rat aorta]. Gac Med Mex. 2006 Jan-Feb;142(1):1-8.


These changes were not affected by cycloheximide (10 (-5) M; a protein synthesis inhibitor of), flutamide (10 (-5) M; an androgenic receptor antagonist), or by adding aminoglutethimide (10 (-5) M; an aromatase inhibitor).
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17210686 Butcher NJ, Tetlow NL, Cheung C, Broadhurst GM, Minchin RF: Induction of human arylamine N-acetyltransferase type I by androgens in human prostate cancer cells. Cancer Res. 2007 Jan 1;67(1):85-92.


The increase in NAT1 mRNA was attenuated by concurrent cycloheximide treatment, suggesting that the effect of R1881 may not be by direct transcriptional activation of NAT1.
0(0,0,0,0) Details
19800357 Gonzalez-Montelongo MC, Marin R, Gomez T, Diaz M: Androgens are powerful non-genomic inducers of calcium sensitization in visceral smooth muscle. Steroids. 2009 Oct 1.

Androgen-induced potentiation was prevented by preincubation with androgen receptor (AR) antagonists but unaffected by cycloheximide plus actinomycin D, indicating that potentiation was mediated by ARs via a non-genomic mechanism.
32(0,1,1,2) Details
20207835 Gonzalez-Montelongo MC, Marin R, Gomez T, Marrero-Alonso J, Diaz M: Androgens Induce Nongenomic Stimulation of Colonic Contractile Activity through Induction of Calcium Sensitization and Phosphorylation of LC20 and CPI-17. Mol Endocrinol. 2010 Mar 5.

The results using flutamide, finasteride, cycloheximide, and actinomycin D indicate that androgen-induced potentiation is dependent on androgen receptors, requires reduction of testosterone to DHT, and occurs independently of transcriptional and translational events.
31(0,1,1,1) Details
17989348 Papineni S, Chintharlapalli S, Safe S: Methyl 2-cyano-3,11-dioxo-18 beta-olean-1,12-dien-30-oate is a peroxisome proliferator-activated receptor-gamma agonist that induces receptor-independent apoptosis in LNCaP prostate cancer cells. Mol Pharmacol. 2008 Feb;73(2):553-65. Epub 2007 Nov 7.

In contrast, beta-CDODA-Me also decreased androgen receptor (AR) and prostate-specific antigen (PSA) mRNA and protein levels through kinase-independent pathways. beta-CDODA-Me repressed AR mRNA transcription, whereas decreased PSA mRNA levels were dependent on protein synthesis and were reversed by cycloheximide.
31(0,1,1,1) Details