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#34130051   2021/06/12 To Up

Clinicopathological characteristics of androgen receptor splicing variant 7 (AR-V7) expression in patients with castration resistant prostate cancer: A systematic review and meta-analysis.

 Studies have shown that AR-V7 may be correlated with the poor prognosis of castration resistant prostate cancer (CRPC), however, clinicopathological characteristics of AR-V7 have not been fully elucidated.
Qinchen Li, Zhize Wang, Jiahe Yi, Haixiang Shen, Zitong Yang, Libin Yan, Liping Xie

2311 related Products with: Clinicopathological characteristics of androgen receptor splicing variant 7 (AR-V7) expression in patients with castration resistant prostate cancer: A systematic review and meta-analysis.

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#34129879   2021/06/12 To Up

Kaempferol inhibits benign prostatic hyperplasia by resisting the action of androgen.

Kaempferol is a natural compound that inhibits tumor development in androgenic related prostate cancer. However, it is still not clear about its phyto-androgenic activity and whether it suppresses testosterone-induced benign prostatic hyperplasia (BPH) development. In this study, molecular docking, cellular immunofluorescence staining, chromatin immunoprecipitation and dual luciferase reporter assay were performed to investigate the androgenic activity of kaempferol. Dihydrotestosterone-induced gene expression and cell proliferation were further analyzed upon treatment with kaempferol. Testosterone-induced BPH was established in rats then the effect and mechanism of action of kaempferol on BPH development was then assessed. Docking data showed that kaempferol could bind to ASN705 and THR877 residues of androgen receptor which were also the binding sites of dihydrotestosterone. The nuclear translocation of androgen receptor was promoted directly more than 2 percent by kaempferol in androgen-dependent prostate cancer LNCaP cells. In addition, the in vivo interaction of androgen receptor with PSA promoter region and the transcriptional activity of androgen receptor were both significantly enhanced after kaempferol stimulation. However, kaempferol pretreatment suppressed dihydrotestosterone -induced effects including the transcriptional activity of androgen receptor, the expressions of PSA and AR genes and cell proliferation of LNCaP, BPH-1 and WPMY-1 cells. Consistently, kaempferol declined the prostate index almost 30 percent and improved the pathological properties in BPH rats, and the up-regulated T level in serum from BPH rats was highly decreased after kaempferol administration. Kaempferol exhibited its androgenic-like activity and served as a selective androgen receptor modulator that contributes to androgen-related BPH development.
Xueni Wang, Junjie Zhu, Huimin Yan, Mengyao Shi, Qiaoqi Zheng, Yu Wang, Yan Zhu, Lin Miao, Xiumei Gao

2726 related Products with: Kaempferol inhibits benign prostatic hyperplasia by resisting the action of androgen.

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#34129857   2021/06/12 To Up

Lipoproteins and cancer: The role of HDL-C, LDL-C, and cholesterol-lowering drugs.

Cholesterol is an amphipathic sterol molecule that is vital for maintaining normal physiological homeostasis. It is a relatively complicated molecule with 27 carbons whose synthesis starts with 2-carbon units. This in itself signifies the importance of this molecule. Cholesterol serves as a precursor for vitamin D, bile acids, and hormones, including estrogens, androgens, progestogens, and corticosteroids. Although essential, high cholesterol levels are associated with cardiovascular and kidney diseases and cancer initiation, progression, and metastasis. Although there are some contrary reports, current literature suggests a positive association between serum cholesterol levels and the risk and extent of cancer development. In this review, we first present a brief overview of cholesterol biosynthesis and its transport, then elucidate the role of cholesterol in the progression of some cancers. Suggested mechanisms for cholesterol-mediated cancer progression are plentiful and include the activation of oncogenic signaling pathways and the induction of oxidative stress, among others. The specific roles of the lipoprotein molecules, high-density lipoprotein (HDL) and low-density lipoprotein (LDL), in this pathogenesis, are also reviewed. Finally, we hone on the potential role of some cholesterol-lowering medications in cancer.
Kush Patel, Khosrow Kashfi

2772 related Products with: Lipoproteins and cancer: The role of HDL-C, LDL-C, and cholesterol-lowering drugs.

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#34129855   2021/06/12 To Up

Transcriptional profiling of primary prostate tumor in metastatic hormone-sensitive prostate cancer and association with clinical outcomes: correlative analysis of the E3805 CHAARTED study.

The phase III CHAARTED trial established upfront androgen deprivation therapy (ADT) plus docetaxel (D) as a standard for metastatic hormone-sensitive prostate cancer (mHSPC) based on meaningful improvement in overall survival (OS). Biological prognostic markers of outcomes and predictors of chemotherapy benefit are undefined.
A A Hamid, H-C Huang, V Wang, Y-H Chen, F Feng, R Den, G Attard, E M Van Allen, P T Tran, D E Spratt, R Dittamore, E Davicioni, G Liu, R DiPaola, M A Carducci, C J Sweeney

1141 related Products with: Transcriptional profiling of primary prostate tumor in metastatic hormone-sensitive prostate cancer and association with clinical outcomes: correlative analysis of the E3805 CHAARTED study.



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#34129460   // To Up

Using darolutamide in advanced prostate cancer: How I Do It.

Darolutamide is a nonsteroidal androgen inhibitor FDA approved for the treatment of castration-resistant non-metastatic prostate cancer (nmCRPC). After decades of offering androgen deprivation therapy (ADT) alone or first-generation androgen receptor blockers for patients whose PSA was rising despite castrate levels of testosterone, there are now three different treatment options to add to ADT. These include apalutamide approved in February 2018, enzalutamide FDA approved in June 2018, and darolutamide approved July 2019. Each of these androgen receptor pathway blockers, when added to ADT or surgical orchiectomy, prolongs metastasis-free-survival (MFS) and median survival (MS). This paper focuses on the use of the newest approved agent in this class, darololutmide.
Joelle Hamilton

1075 related Products with: Using darolutamide in advanced prostate cancer: How I Do It.



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#34128829   2021/06/01 To Up

Targeting androgen receptor signaling: a historical perspective.

The first case of prostate cancer was identified by histological examination by J. Adams, a surgeon at The London Hospital, in 1853. In his report, Adams noted that the condition was "a very rare disease". Now, over 150 years later, with increased life expectancy and screening, prostate cancer has become one of the most common cancers in men. In the United Sates alone, nearly 200,000 men are diagnosed with prostate cancer annually and about 33,000 succumb to their disease. Fifty years ago, men were typically diagnosed with prostate cancer in their seventies with disease that had metastasized to the bone and/or soft tissue. Diagnosis at such an advanced stage was a death sentence, with patients dying within two years. The pioneering work of Charles Huggins in the 1940s found that metastatic prostate cancer responds to androgen deprivation therapy (ADT), ushering in the rational use of hormone therapies that have irrevocably changed the course of prostate cancer disease management. Medical castration was the first effective systemic targeted therapy for any cancer and, to this day, androgen ablation remains the mainstay of prostate cancer therapy.
Alastair H Davies, Amina Zoubeidi

1267 related Products with: Targeting androgen receptor signaling: a historical perspective.

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#34128827   2021/06/01 To Up

Androgen receptor signalling inhibitors: post-chemotherapy, pre-chemotherapy and now in castration sensitive prostate cancer.

Based on pioneering work by Huggins, Hodges and others, hormonal therapies have been established as an effective approach for advanced prostate cancer (PC) for the past 8 decades. However, it quickly became evident that androgen deprivation therapy (ADT) via surgical or medical castration accomplishes inadequate inhibition of the androgen receptor (AR) axis, with clinical resistance inevitably emerging due to adrenal and intratumoral sources of androgens and other mechanisms. Early efforts to augment ADT by adding adrenal-targeting agents (aminoglutethimide, ketoconazole) or AR antagonists (flutamide, bicalutamide, nilutamide, cyproterone) failed to achieve overall survival (OS) benefits, although they did exhibit some evidence of limited clinical activity. More recently, four new Androgen Receptor Signalling Inhibitors (ARSIs) successfully entered clinical practice. Specifically, the CYP17 inhibitor abiraterone acetate and the 2nd generation AR antagonists (enzalutamide, apalutamide and darolutamide) achieved OS benefits for PC patients, confirmed the importance of reactivated AR signaling in castration-resistant PC and validated important concepts that had been proposed in the field several decades ago but had remained so far unproven, including adrenal-targeted therapy and combined androgen blockade. The past decade has seen steady advances towards more comprehensive AR axis targeting. Now the question is raised whether we have accomplished the maximum AR axis inhibition possible or there is still room for improvement. This review, marking the 80-year anniversary of ADT and 10-year anniversary of successful ARSIs, examines their current clinical use and discusses future directions, in particular combination regimens, to maximize their efficacy, delay emergence of resistance and improve patient outcomes.
Nicholas Mitsiades, Salma Kaochar

1464 related Products with: Androgen receptor signalling inhibitors: post-chemotherapy, pre-chemotherapy and now in castration sensitive prostate cancer.

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#34128479   // To Up

Selective androgen receptor modulators activate the canonical prostate cancer androgen receptor program and repress cancer growth.


Michael D Nyquist, Lisa S Ang, Alexandra Corella, Ilsa M Coleman, Michael P Meers, Anthony J Christiani, Cordell Pierce, Derek H Janssens, Hannah E Meade, Arnab Bose, Lauren Brady, Timothy Howard, Navonil De Sarkar, Sander B Frank, Ruth F Dumpit, James T Dalton, Eva Corey, Stephen R Plymate, Michael C Haffner, Elahe A Mostaghel, Peter S Nelson

2629 related Products with: Selective androgen receptor modulators activate the canonical prostate cancer androgen receptor program and repress cancer growth.

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#34128263   2021/06/14 To Up

Effect of androgen deprivation therapy on cognitive functioning in men with prostate cancer: A systematic review.

The objective of this study was to review publications assessing cognitive functioning in patients with prostate cancer treated with androgen deprivation therapy. We conducted a systematic review of the literature published in PubMed, Embase, Web of Science, Cochrane Library, and PsycINFO up to February 2020. A total of 31 studies were included. Half of the studies (n = 16) demonstrated that androgen deprivation therapy in patients with prostate carcinoma did not result in a negative effect on cognitive functioning, however, still a substantial proportion of the studies (n = 11) reported a negative effect on cognitive functioning. In four studies the results were inconclusive. In the three studies using additional functional magnetic resonance imaging, no significant effect on neuropsychological tests was found, but grey matter volume, brain activity, and brain connectivity were affected. Given the substantial number of studies showing a significant negative effect of androgen deprivation therapy on cognitive functioning, clinicians should be aware of this side effect. Furthermore, future research should focus on the further examination of brain characteristics using functional magnetic resonance imaging, since these techniques might be more sensitive in detecting brain abnormalities as a result of androgen deprivation therapy.
Cornelie D Andela, Rafil Matte, Ingrid M Jazet, Willemijn Cg Zonneveld, Jan W Schoones, A Edo Meinders

2676 related Products with: Effect of androgen deprivation therapy on cognitive functioning in men with prostate cancer: A systematic review.



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