Abstract:
:The rationale underlying therapeutic strategies designed to inhibit the action of endogenous sex hormones in malignant breast cells is provided by the demonstration of their involvement in supporting the development and growth of breast carcinoma. The surgical removal of steroid-secreting glands, in order to reduce the level of oestrogens reaching their target tissues, has for years been substituted by the so-called endocrinotherapeutic approach, which is based on the counteraction of the steroid hormone activity by the hormonal receptor blockade with suitable antioestrogenic compounds. Over the past 25 years, the non-steroidal oestrogen antagonist tamoxifen has become the standard endocrine treatment for breast cancer. The triphenylethylene-derivative compound competes efficiently for binding to the oestrogen receptor, but the complex retains some transcriptional activity. Consequently, tamoxifen exhibits, both ' in vitro and in vivo ', a range of biological activity from full oestrogen antagonism to partial agonism. There is also evidence suggesting that the agonist activity of this compound may ultimately stimulate breast tumour growth, thus causing some treatment failures. Moreover, the use of tamoxifen is limited by the possible onset of drug-resistance in many patients. Nevertheless, widely tested tamoxifen has proved to be very helpful for the development of new compounds to be used as long-term adjuvant therapy or as preventive agents. These novel oestrogen antagonists belong to two major classes: tamoxifen analogs and new pure steroidal-like antioestrogens. The search for and development of compounds devoid of tamoxifen cross-resistance, with a safer toxicity profile as well as the lack of oestrogenic effects, provide the bases to improve the current therapeutic applications of antioestrogens.
journal_name
Pharmacol Resjournal_title
Pharmacological researchauthors
de Cupis A,Schettini G,Favoni REdoi
10.1006/phrs.1998.0437keywords:
subject
Has Abstractpub_date
1999-05-01 00:00:00pages
335-44issue
5eissn
1043-6618issn
1096-1186pii
S1043661898904376journal_volume
39pub_type
杂志文章,评审abstract::The mitochondrial citrate carrier (CIC) is a nuclear-encoded protein located in the inner mitochondrial membrane. By mediating efflux of citrate from the mitochondria to the cytosol, CIC links mitochondrial central carbon metabolism and cytosolic lipogenesis together. Abnormal activity or expression of CIC was found i...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2020.105132
更新日期:2020-11-01 00:00:00
abstract::Disruption of the circadian clock is associated with a variety of human pathologies, including cancer. Rather than being a mere consequence of a global changes associated with the cancer cell transcriptome, the aberrant clock gene expression observed in many tumors may serve for cancer cell survival. This scenario sug...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2015.08.008
更新日期:2015-10-01 00:00:00
abstract::Antioxidants have a great potential as adjuvant therapeutics in patients with Duchenne muscular dystrophy, although systematic comparisons at pre-clinical level are limited. The present study is a head-to-head assessment, in the exercised mdx mouse model of DMD, of natural compounds, resveratrol and apocynin, and of t...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2016.02.016
更新日期:2016-04-01 00:00:00
abstract::T lymphocytes produced by the thymus are essential mediators of immunity. Accelerated thymic atrophy appears in the patients with administration of glucocorticoids (GCs) which are commonly-used drugs to treat autoimmune and infectious diseases, leading to dysregulation of immunity with manifestation of progressive dim...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2018.09.011
更新日期:2018-11-01 00:00:00
abstract::Because many Ca2+ channel blocking agents are known to cause adverse systemic effects, in this study we tested the haemodynamic side effects of nimodipine with and without a mild hypoxic-ischaemic (HI) insult in a newborn piglet model. Fifteen min after completing a brief period of asphyxia we gave i.v. nimodipine as ...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1996.0002
更新日期:1996-01-01 00:00:00
abstract::Despite the evolving advances in clinical approaches to obesity and its inherent comorbidities, the therapeutic challenge persists. Among several pharmacological tools already investigated, recent studies suggest that melatonin supplementation could be an efficient therapeutic approach in the context of obesity. In th...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2020.105254
更新日期:2021-01-01 00:00:00
abstract::Exposure to ionizing radiation causes damage to living tissues; however, only a small number of agents have been approved for use in radiation injuries. Radioprotector is the primary countermeasure to radiation injury and none radioprotector has indeed reached the drug development stage. Repurposing the long list of a...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2016.09.024
更新日期:2016-11-01 00:00:00
abstract::Perinatal encounter of a hormone and its developing target receptor sets the receptor-hormone-signal transduction complex for life (hormonal imprinting). In this critical period excess of the appropriate hormone or foreign molecules able to bind the receptor can cause faulty imprinting with life-long consequences. At ...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/s1043-6618(03)00217-2
更新日期:2003-11-01 00:00:00
abstract::Bombycis corpus(BC) or Bombyx Batryticatus, a batryticated silkworm and white-stiff silkworm, is a drug consisting of the dried larva of silkworm, Mobyz mori L., dead and stiffened due to the infection of Beauveria (Bals.) Vuill. In the present study, we have examined the protective effect of the water extracts agains...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.2000.0746
更新日期:2001-01-01 00:00:00
abstract::Effect of moclobemide, a selective monoamine oxidase-type A enzyme inhibitor, was investigated on the body temperature of male mice. Moclobemide (15-30 mg kg(-1), i.p.) produced significant reductions of body temperature in both normal and yeast-induced hyperthermic male mice. The hypothermic effect of moclobemide was...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/s1043-6618(03)00108-7
更新日期:2003-09-01 00:00:00
abstract::Metastatic and primary bone cancers are usually accompanied by severe pain that is difficult to manage. In light of the adverse side effects of opioids, manipulation of the endocannabinoid system may provide an effective alternative for the treatment of cancer pain. The present study determined that a local, periphera...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2011.03.007
更新日期:2011-07-01 00:00:00
abstract::The mechanism for the pathological increase in cell death in various disease states e.g. HIV immunodefficiency or even ageing or Alzheimer's disease, occurs by complex and as yet undefined mechanism(s) related to immunological, virological or biochemical disturbances (i.e. energy depletion, oxidative stress, increased...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/s1043-6618(05)80044-1
更新日期:1995-12-01 00:00:00
abstract::The aim of this study was to investigate effect of antiemetics on G6PD and antioxidant enzymes. Antiemetics are currently being used to reduce or prevent nausea and vomiting in patients. This is the first study to show effect of antiemetics on glucose-6-phosphate dehydrogenase (G6PD) and antioxidant enzyme activities....
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2004.05.007
更新日期:2004-11-01 00:00:00
abstract::Regulatory T cells (Tregs) modulate ongoing immune responses to prevent autoimmunity in healthy bodies and inhibit effective anti-tumor immunity responses in tumor patients, leading to tumor progression. The function of Tregs in tumor immunity suggests that elimination of Tregs in the host may enhance the anti-tumor i...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2020.104659
更新日期:2020-03-01 00:00:00
abstract::Male weanling Wistar rats were fed a 4% cholestyramine diet and used as a model to demonstrate that a reduction in serum low density lipoproteins stimulates de novo cholesterogenesis leading to DNA synthesis and cell proliferation. Feeding this diet resulted in a decrease in serum very low density lipoproteins and low...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/1043-6618(89)90195-3
更新日期:1989-09-01 00:00:00
abstract::Alcohol abuse and addiction are serious global health problems. Tackling these disorders requires an understanding of how ethanol produces its effects. Early cell culture studies implicated the protein kinase C (PKC) family of serine-threonine kinases in mediating both acute and chronic responses to ethanol exposure. ...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2007.04.008
更新日期:2007-06-01 00:00:00
abstract::Mesial temporal lobe epilepsy (MTLE) is frequently associated with hippocampal sclerosis (Hs), possibly caused by a primary brain injury that occurs a long time before the appearance of neurological symptoms. MTLE-Hs is, however, a heterogeneous condition that evolves with time, involving both environmental and geneti...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2016.09.019
更新日期:2016-11-01 00:00:00
abstract::Posttranslational modifications of proteins are important regulatory processes endowing the proteins functional complexity. Over the last decade, numerous studies have shed light on the roles of palmitoylation, one of the most common lipid modifications, in various aspects of neuronal functions. Major players regulati...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2016.06.008
更新日期:2016-09-01 00:00:00
abstract::The aqueous extract from aerial parts of Artemisia copa Phil. (Compositae), was evaluated for antinociceptive activity using writhing, formalin, and hot-plate tests in mice. A dose-related antinociceptive response was obtained in the writhing test at doses of 500 and 1000 mg/kg p.o. (percentage of inhibition 23.3 and ...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2003.12.016
更新日期:2004-07-01 00:00:00
abstract::The present study was aimed at investigating the role of endogenous nitric oxide (NO) in regulating Na,K-ATPase activity in the kidney. The expression of alpha-1 and beta-1 subunits; and the enzymatic activity of Na,K-ATPase were determined in the kidney of rats treated with an NO synthase inhibitor, N(G)-nitro-L-argi...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1999.0570
更新日期:2000-01-01 00:00:00
abstract::Anti-hypertensive agents may differently stimulate compensatory neuro-hormonal mechanisms and induce different effects on the cardiovascular remodeling and function. The combination of low doses of the two synergistic drugs may lead to a lesser activation of counter regulatory mechanisms and could provide optimal ther...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2004.10.010
更新日期:2005-04-01 00:00:00
abstract:OBJECTIVES:There is still a need to develop new effective medications for the treatment of ulcerative colitis, particularly for patients who are intolerant or resistant to first line therapies. This article compared the efficacy and safety of etrolizumab and infliximab in moderate to severe ulcerative colitis. METHODS...
journal_title:Pharmacological research
pub_type: 杂志文章,meta分析
doi:10.1016/j.phrs.2018.11.003
更新日期:2019-01-01 00:00:00
abstract::Changes in vascular responsiveness are the basis for some of the cardiovascular complications in cholestasis. Since the duration of cholestasis is important in determining the degree of the complications, we investigated the time-course dependent evolution of vascular relaxation responsiveness in the aortic rings of c...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.2001.0892
更新日期:2001-12-01 00:00:00
abstract::Rapid technological advances in genetics have created conceptual chaos regarding the genetics of drug response. Terms for differing concepts are used interchangeably: pharmacogenetics with pharmacogenomics, personalized medicine with personalized prescription. Biomarker has many definitions. The author prefers the con...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2008.10.002
更新日期:2009-02-01 00:00:00
abstract::Osteopontin (OPN) is known as an active player in the progression of vascular remodeling diseases, however, the precise role in the proliferation of vascular smooth muscle cells (VSMC) is unclear. Thus, this study investigated the role of OPN in VSMC proliferation induced by 4-hydroxynonenal (HNE), and identified the ...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2016.03.041
更新日期:2016-06-01 00:00:00
abstract:PURPOSE OF THE REVIEW:This review article discusses recent advances in the mechanism of dipeptidyl peptidase-4 (DPP-4) actions in renal diseases, especially diabetic kidney fibrosis, and summarizes anti-fibrotic functions of various DPP-4 inhibitors in diabetic nephropathy (DN). RECENT FINDINGS:DN is a common complica...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2019.104391
更新日期:2019-09-01 00:00:00
abstract::Prader-Willi syndrome (PWS), the leading genetic cause of obesity, is characterized by a striking hyperphagic behavior that can lead to obesity, type-2 diabetes, cardiovascular disease and death. The molecular mechanism underlying impaired satiety in PWS is unknown. Oleoylethanolamide (OEA) is a lipid mediator involve...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2016.12.024
更新日期:2017-03-01 00:00:00
abstract::An interaction of drug with food, herbs, and dietary supplements is usually the consequence of a physical, chemical or physiologic relationship between a drug and a product consumed as food, nutritional supplement or over-the-counter medicinal plant. The current educational review aims at reminding to the prescribing ...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2016.09.038
更新日期:2017-04-01 00:00:00
abstract::Some antihistamines (mainly terfenadine and astemizole) have been demonstrated to cause QT interval prolongation and, in some cases, torsade-de-pointes. We investigated the cardiac electrophysiological effects of brompheniramine, a conventional antihistamine. Brompheniramine was reported to prolong QT interval in isol...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2006.08.004
更新日期:2006-12-01 00:00:00
abstract::Combination antiretroviral therapy reduces morbidity and mortality in HIV infected patients. However, the cure of HIV infection is hindered by the persistence of the latent HIV reservoir. Latency reversing agents (LRAs) are developed to target the HIV latently infected cells for HIV reactivation. In addition to revers...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2018.10.023
更新日期:2019-01-01 00:00:00