The Fight Against Cancer
Nathan Keighley in Miraculous Medicines and the Chemistry of Drug Design, 2020
Some cancers are hormone-dependent. Hormones can serve as a signal for DNA replication, and derangements in this signalling process may lead to cancer. Steroid hormones bind to intracellular receptors to form complexes that act as nuclear transcription factors to control whether transcription takes place. Hormone antagonists can be used to block these receptors, thus impede cell proliferation. Oestrogen is commonly involved in these pathways. Oestrogen drugs are used in the treatment of prostate cancer because they inhibit the production of luteinising hormone and thereby decrease the synthesis of testosterone, which is linked with prostate cancer. In hormone-dependent breast cancer, oestrogen antagonists are used to block oestrogen receptors and prevent hormone binding.
Steroid Hormone Receptors Involved in Reproduction: Mechanism of Action
Robert E. Garfield, Thomas N. Tabb in Control of Uterine Contractility, 2019
Nonsteroidal antiestrogens were the first hormone antagonists in use. They belong to the triphenyl-ethylene series, and are structurally related to diethylstibestrol, although they bear a third phenolic ring (hence their designation), which is responsible for their antagonistic effects. They are characterized by two complex features: They are pure antagonists in birds, whereas they are strongly estrogenic in mice, the situation being intermediary in the human species;Their agonist properties are dissociated: they stimulate the synthesis of proteins in the liver, for example, the human plasma protein SBP (sex hormone binding protein, which binds estradiol and progesterone), or the uterine and mammary gland progesterone receptor, whereas they generally do not stimulate target cell growth and behave as pure estrogen antagonists in this respect, hence their therapeutic use in estrogen-dependent cancers.
Cancer treatment
Ian Peate in Nursing & Health Survival Guide, 2014
Hormone antagonists work with hormone-binding tumours of the breast, prostate and endometrium, blocking the hormone’s receptor site on the tumour, preventing it from receiving normal hormonal growth stimulation. These drugs do not cure, but cause regression of the tumour in approximately 40% of breast and endometrial tumours and in 80% of prostate tumours.
COVID-19 – compliant – IVF: reorganized clinical practice taking into account the pandemic
Published in Gynecological Endocrinology, 2022
Ermanno Greco, Valeria Donno, Pierfrancesco Greco, Cristina Arrivi, Katerina Litwicka, Maria Teresa Varricchio
Avoiding OHSS is mandatory: not only to avoid to the patient the hospitalization, but also because women with COVID-19 already experience hypovolemic and electrolyte imbalance, and OHSS could worsen them. The strategy that we are going to use is based on a single gonadotropin, namely follitropin delta (Rekovelle, Ferring), which dose is based on the patient’s body weight and AMH (Anti-Müllerian Hormone) value. Moreover, in order to reduce the number of visits to the patients, preference has been given to the ‘fixed’ GnRH (Gonadotropin-Releasing Hormone) antagonists protocol. The reason behind the choice of follitropin delta is that the Follitropin Delta strategy being based on an algorithm would permit the optimization of ovarian response minimizing the risk for excess, with increased safety for the patients treated [11,12]. Moreover the reduced need of adjusting the dose of Follicle-Stimulating Hormone (FSH) is expected to minimize the need of patient’s monitoring during stimulation [13].
Cancer epigenetics and the potential of epigenetic drugs for treating solid tumors
Published in Expert Review of Anticancer Therapy, 2019
Zhenghui Liu, Yingxue Gao, Xiong Li
The progression of many cancers depends on aberrant hormone metabolism or the mutation of hormone receptors, for example the mutation of estrogen/estrogen receptor in breast cancer and androgen/androgen receptor in prostate cancer. Hormone antagonists or inhibitors of hormone receptors have become the first-in-class therapeutics for these cancer types. However, cancer patients inevitably develop drug resistance after treatment and epigenetic changes have been identified as a key element for drug resistance. Epigenetic drugs may, therefore, overcome cancer resistance to hormonal drugs. Vorinostat and Bicalutamide, an androgen receptor antagonist, had a synergistic effect on cell proliferation and apoptosis induction in prostate cancer cell lines. In a phase II clinical trial, the combination of these two drugs followed by radical prostatectomy decreased the tumor size of primary prostate cancer [99,100]. A triple combination of TSA, Bicalutamide and Finasteride (a 5α-reductase inhibitor) targeting the androgen pathway had synergistic effects inducing prostate cancer cell apoptosis [101]. Azacytidine plus TSA and Diarylpropionitrile (DPN, a highly potent ERβ agonist) displayed strong anticancer effects, inducing apoptosis and decreasing proliferation in prostate cancer cells, along with downregulation of Cyclin D1 and VEGF [94].
Disruptions in the reproductive system of female rats after prenatal lipopolysaccharide-induced immunological stress: role of sex steroids
Published in Stress, 2019
V. M. Ignatiuk, M. S. Izvolskaya, V. S. Sharova, S. N. Voronova, L. A. Zakharova
We hypothesized that the development of disorders in the female reproductive system after prenatal LPS-induced immunological stress can be potentiated by sex hormones during the prepubertal period. The aim of this study was to investigate the role of sex steroids and actions of their antagonists in the development of the reproductive system disorders in female offspring prenatally exposed to LPS. Sex hormone antagonists (fulvestrant or flutamide) were injected during the time frames detected in our previous research when the level of sex hormones is elevated in prepubertal offspring after prenatal LPS treatment (Izvolskaia et al., 2016). Parameters of reproductive system function in postnatal females (body weight, time of vaginal opening (VO), quantitative ovary histology and sex steroid concentrations) were studied.
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