The Human Androgen Receptor Signaling Targets RT² Profiler PCR Array profiles the expression of 84 key genes mediating signal transduction in cells responsive to male sex steroid hormones. Androgen receptor (AR) present in the cytoplasm binds either one of the two androgenic hormones, testosterone or dihydrotestosterone produced by the testes. Ligand binding activates the receptor to translocate into the nucleus, homodimerize, and act as a transcription factor binding specific DNA response elements to mostly up-regulate gene expression. AR signaling is primarily responsible for normal prostate development, growth, and function as well as the development of primary and secondary male sexual characteristics. Dysregulated AR signaling has been implicated in prostate cancer pathophysiology, especially and importantly in cancers recurring after castration or antiandrogenic therapies where AR still promotes tumor growth due to its mutation, overexpression, or transactivation. Analyzing the expression of AR responsive genes can help better understand its normal functions and role in disease at the molecular level. Most of the targets of AR signaling included on this array have been discovered using genome-wide analysis of both gene expression and AR promoter binding sites via chromatin immuoprecipitation after treating LNCaP prostate cancer cells with the testosterone analog R1881. These AR targets regulate essential processes such as cell adhesion and structure, cell differentiation and proliferation, lipid metabolism, signal transduction, as well as trafficking and transport. Other transcription factors involved in these processes that also modulate the androgen response, particularly the Serum Response Factor (SRF), are also represented by the array. A set of controls present on each array enables data analysis using the ΔΔCT method of relative quantification and assessment of reverse transcription performance, genomic DNA contamination, and PCR performance. Using real-time PCR, research studies can easily and reliably analyze the expression of a focused panel of genes responsive to androgen receptor signaling with this array.
Androgen Receptor & Co-Transcription Factors: AR, ELK1, FOS, JUN, NFKB1, NFKB2, REL, RELA, SP1, SRF.
Up-Regulated by Androgen Receptor: ABHD2, ALDH1A3, APPBP2, CAMKK2, CENPN, CYP2U1, DBI, DHCR24, EAF2, ENDOD1, ERRFI1, FZD5, GUCY1A3, HERC3, HPGD, IGF1R, KLK2, KLK3, KLK4, KRT8, LIFR, LRIG1, LRRFIP2, NCAPD3, NFKBIA, NKX3-1, ORM1, PAK1IP1, PGC, PIAS1, PMEPA1, RAB4A, SEC22C, SGK1, SLC45A3, SMS, SNAI2, SPDEF, STEAP4, STK39, TIPARP, TPD52, TSC22D1, VAPA, ZBTB10, ZBTB16.
Down-Regulated by Androgen Receptor: IGFBP5, MT2A, MYC, PIK3R3, TRIB1, TSC22D3.
Regulated by Androgen Receptor: ABCC4, ACSL3, ADAMTS1, CITED2, CXCR7, ELL2, FAM105A, FKBP5, IRS2, MAF, MAP7D1, MME, NDRG1, ORM2, PPAP2A, RHOU, SLC26A2, SORD, TMPRSS2, VIPR1, WIPI1, ZNF189.
Cell Cycle: NCAPD3.
Metabolism: ACSL3, ALDH1A3, CYP2U1, DBI, DHCR24, HPGD, PPAP2A, SMS, SORD.
Proliferation & Differentiation & Apoptosis: ELL2, IGFBP5, LRIG1, MAF, NDRG1, STEAP4.
Proteases & Protease Inhibitors: ADAMTS1, KLK2, KLK3, KLK4, MME, PGC, TMPRSS2.
Signal Transduction: CAMKK2, CITED2, ERRFI1, FKBP5, FZD5, GUCY1A3, HERC3, IGF1R, IRS2, LIFR, NFKBIA, PAK1IP1, PIK3R3, PMEPA1, TPD52, VIPR1.
Stress Responses: LRRFIP2, ORM1, ORM2, SGK1, STK39.
Cell Adhesion & Motility: KRT8, MAP7D1, RHOU.
Transcriptional Regulation: CENPN, EAF2, MAF, MYC, NKX3-1, PIAS1, SNAI2, SPDEF, TRIB1, TSC22D1, TSC22D3, ZBTB10, ZBTB16, ZNF189.
Transporting & Trafficking: ABCC4, APPBP2, FKBP5, MT2A, RAB4A, SEC22C, SLC26A2, SLC45A3, VAPA, WIPI1.