Raloxifene.

Abstract:

:Efforts to interfere with the initiation and promotion of breast and other cancers by endocrine manipulation are not new. It is of obvious benefit to cancer patients to administer substances that combine minimal general toxicity with maximal oestrogen inhibition. Raloxifene is a relatively recent addition to a group of compounds loosely designated as antioestrogens, which implies their ability to antagonize oestrogen effects via competitive binding to the various receptors. This is a reductionist simplification, since their effect varies and ranges from interaction with lipid transduction cascades, covalent binding to proteins and DNA, regulation of growth factors, erbB2, mdr1 and probably p53 expression, complexing with E-cadherin/catenin to active induction of apoptosis and many other effects on the genome. Also, the action of most antioestrogens is not solely antagonistic and different compounds do exert some agonistic effects in various tissues. Apart from some "pure" antioestrogens, the benzothiophene derivative Raloxifene has been found to combine a high degree of selective oestrogen suppression with several other desirable characteristics, such as reduction of bone demineralisation and antiatherogenic effects without endometrial stimulation. It is well tolerated, has been successfully tested as a chemopreventive agent for breast cancer in certain groups of the population and does not prevent ovulation in women with normal menstrual cycles. Certainly, Raloxifene is only another forerunner of upcoming "designer" oestrogen modulators, but it represents a welcome addition to the therapeutic choices available for the control of some menopausal problems as well as for the prevention and treatment of breast cancer, as outlined in the following brief review.

journal_name

Curr Drug Targets

journal_title

Current drug targets

authors

Kellen JA

doi

10.2174/1389450013348263

keywords:

subject

Has Abstract

pub_date

2001-12-01 00:00:00

pages

423-5

issue

4

eissn

1389-4501

issn

1873-5592

journal_volume

2

pub_type

杂志文章,评审
  • Gene therapy for arthritis.

    abstract::Recent progress in molecular biology has provided application of gene transfer methods in arthritis. Two clinical trails using ex vivo retrovirus mediated delivery of interleukin -1 receptor antagonist gene for rheumatoid arthritis has begun in USA and Germany. However, there are still many issues to be elucidated; on...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/1389450033490777

    authors: Tomita T,Hashimoto H,Yoshikawa H

    更新日期:2003-11-01 00:00:00

  • Targeted Thromboelastographic (TEG) Blood Component and Pharmacologic Hemostatic Therapy in Traumatic and Acquired Coagulopathy.

    abstract::Trauma-induced coagulopathy (TIC) is a recently described condition which traditionally has been diagnosed by the common coagulation tests (CCTs) such as prothrombin time/international normalized ratio (PT/INR), activated partial thromboplastin time (aPTT), platelet count, and fibrinogen levels. The varying sensitivit...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/1389450117666160310153211

    authors: Walsh M,Fritz S,Hake D,Son M,Greve S,Jbara M,Chitta S,Fritz B,Miller A,Bader MK,McCollester J,Binz S,Liew-Spilger A,Thomas S,Crepinsek A,Shariff F,Ploplis V,Castellino FJ

    更新日期:2016-01-01 00:00:00

  • The Role of Type 2 Fibroblast Growth Factor in Periodontal Therapy.

    abstract::The prevalence of periodontitis is around 20-50% of global population. If not treated, it can cause of tooth loss. Periodontal treatment aims at preserving the patient's teeth from various methods, including infection control and restoring lost periodontal tissue. The periodontium has great biological regenerative pot...

    journal_title:Current drug targets

    pub_type: 杂志文章

    doi:10.2174/1389450121999201105152639

    authors: Mohammadipour HS,Forouzanfar F,Forouzanfar A

    更新日期:2020-11-05 00:00:00

  • Curcumin Sensitizes Cancers Towards TRAIL-induced Apoptosis via Extrinsic and Intrinsic Apoptotic Pathways.

    abstract::Tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) is a natural protein expressed in a wide range of tissues in our body. It is a promising anti-cancer agent due to its selective killing of cancer cells, rendering normal cells unharmed. However, resistance occurs either intrinsically or develops ove...

    journal_title:Current drug targets

    pub_type: 杂志文章

    doi:10.2174/1389450121666200302124426

    authors: Ngai SC

    更新日期:2020-01-01 00:00:00

  • Pharmacogenomics in the Americas: the impact of genetic admixture.

    abstract::In this review we focus on the impact of genetic admixture on pharmacogenomics in the American continent, where five centuries of intermarriage between Amerindians, European and Africans, resulted in the extensive population heterogeneity observed nowadays. We compare two alternative views of human genomic variation, ...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/138945006779025392

    authors: Suarez-Kurtz G,Pena SD

    更新日期:2006-12-01 00:00:00

  • Endothelium as a therapeutic target in sepsis.

    abstract::The endothelium plays an important role in health and disease. Endothelial dysfunction contributes to sepsis pathophysiology. An important goal is to develop novel therapies that reverse endothelial dysfunction in sepsis. This review will consider the role of the endothelium in sepsis and will highlight its untapped t...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/138945007780362782

    authors: Aird WC

    更新日期:2007-04-01 00:00:00

  • Animal models of carcinogenesis in inflamed colorectum: potential use in chemoprevention study.

    abstract::Inflammation is a risk factor for cancer development in several tissues. In the colorectum, inflammatory bowel disease (ulcerative colitis and Crohn's disease) is a longstanding inflammatory disease with increased risk for colorectal cancer (CRC). Several molecular events involving in chronic inflammatory process cont...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/138945012804545452

    authors: Tanaka T

    更新日期:2012-12-01 00:00:00

  • Targeting transcription: a new concept of anti-inflammatory therapy of airway diseases.

    abstract::Most pathological conditions that result in human diseases are associated with altered gene expression. With the advent of new technologies that might control gene expression and a broader knowledge of transcription factors and pathways, new strategies have emerged that offer promising first results for therapeutical ...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/138945006777435326

    authors: Quarcoo D,Hamelmann E

    更新日期:2006-06-01 00:00:00

  • Biomarkers, critical disease pathways, drug targets, and alternative medicine in male breast cancer.

    abstract::While breast cancer (BC) is commonest malignancy among female with highest death rate, male breast cancer (MBC) is very rare but exhibits highest cancer specific death in men and the incidences of MBCs are rising rapidly. Due to rarity of the disease, no detail information about biomarkers and drug targets available a...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/138945009787122842

    authors: Barh D

    更新日期:2009-01-01 00:00:00

  • Prospectives of Antihypertensive Nano-ceuticals as Alternative Therapeutics.

    abstract:BACKGROUND:Global death rate due to cardiovascular diseases (CVDs) is highest as compared to other ailments. Principal risk factor associated with CVDs is hypertension. Major classes of current antihypertensive (AHT) therapies include angiotensin converting enzyme inhibitors (ACEI), angiotensin receptor blockers (ARBs)...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/1389450117666160711163119

    authors: Niaz T,Hafeez Z,Imran M

    更新日期:2017-01-01 00:00:00

  • Antioxidants as a Potential Preventive and Therapeutic Strategy for Cadmium.

    abstract::Epidemiological studies provide a growing number of evidences that chronic exposure to relatively low levels of cadmium (Cd), nowadays taking place in industrialized countries, may cause health hazard. Thus, growing interest has been focused on effective ways of protection from adverse effects of exposure to this heav...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/1389450116666150506114336

    authors: Brzóska MM,Borowska S,Tomczyk M

    更新日期:2016-01-01 00:00:00

  • Fetal determinants of type 2 diabetes.

    abstract::Type 2 diabetes, which has dramatically increased during the last decade normally results from a combination of pancreatic beta cell dysfunction and insulin resistance. One of the most recent risk factors identified for type 2 diabetes is a sub-optimal fetal and neonatal environment. Numerous human epidemiological stu...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/138945007781386866

    authors: Reusens B,Ozanne SE,Remacle C

    更新日期:2007-08-01 00:00:00

  • Mucosal healing and anti TNFs in IBD.

    abstract::Mucosal healing has been incorporated in the assessment of treatment efficacy in ulcerative colitis, but in Crohn's disease this concept has only emerged after biological therapies have been evaluated in clinical trials. Systemic steroids don't induce mucosal healing in Crohn's disease, but purine analogues and anti T...

    journal_title:Current drug targets

    pub_type: 杂志文章

    doi:10.2174/138945010790309902

    authors: van Assche G,Vermeire S,Rutgeerts P

    更新日期:2010-02-01 00:00:00

  • Zoledronic Acid: Pleiotropic Anti-Tumor Mechanism and Therapeutic Outlook for Osteosarcoma.

    abstract:BACKGROUND:Osteosarcoma is considered the most frequent primary bone malignancy. Lung metastasis is the leading cause of death and the most consistent factor for predicting negative patient outcome in osteosarcoma. Third-generation nitrogen-containing bisphosphonates, such as zoledronic acid, have been shown to reduce ...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/1573399811666150615145409

    authors: Ouyang Z,Li H,Zhai Z,Xu J,Dass CR,Qin A,Dai K

    更新日期:2018-01-01 00:00:00

  • Possible Effects of Dietary Anthocyanins on Diabetes and Insulin Resistance.

    abstract::Diabetes is reaching epidemic proportions worldwide. Many dietary compounds have been found to exert health beneficial effects against different pathologies including diabetes. Most bioactive compounds have been identified in fruits and vegetables and their mechanisms of action explored both in vitro and in vivo. In p...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/1389450116666151001105230

    authors: Turrini E,Ferruzzi L,Fimognari C

    更新日期:2017-01-01 00:00:00

  • The complex biology of FOXO.

    abstract::FOXO transcription factors control proliferation, apoptosis, differentiation and metabolic processes. Loss of FOXO function has been identified in several human cancers, and results in increased cellular survival and a predisposition to neoplasia, especially in epithelial cancer. FOXO factors are therefore bona fide t...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/138945011796150307

    authors: Monsalve M,Olmos Y

    更新日期:2011-08-01 00:00:00

  • The deficit in low molecular weight thiols as a target for antiageing therapy.

    abstract::The popular use of antioxidative vitamins illustrates the growing awareness of oxidative stress as an important hazard to our health and as an important factor in the ageing process. Superoxide radicals and superoxide-derived reactive oxygen species (ROS) are constantly formed in most cells and tissues. To ensure that...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/1389450110607011505

    authors: Dröge W,Kinscherf R,Hildebrandt W,Schmitt T

    更新日期:2006-11-01 00:00:00

  • Clinical aspects of natural anti-angiogenic drugs.

    abstract::Natural products represent a rich resource for drug delivery and are currently being exploited to target tumour angiogenesis. A vast array of products of natural origin have been shown to have anti-angiogenic potential in preclinical models, including purified endogenous inhibitors, and exogenous compounds derived fro...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/138945006776054951

    authors: Neal CP,Berry DP,Doucas H,Manson MM,Steward W,Garcea G

    更新日期:2006-03-01 00:00:00

  • TGF-Beta signaling manipulation as potential therapy for IBD.

    abstract::Crohn's disease (CD) and ulcerative colitis (UC), two chronic and relapsing inflammatory bowel diseases (IBD), are supposed to develop in genetically-predisposed individuals as a result of an excessive immune mucosal response directed against normal components of the gut microbiota. There is also evidence that defects...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/13894501113149990157

    authors: Marafini I,Zorzi F,Codazza S,Pallone F,Monteleone G

    更新日期:2013-11-01 00:00:00

  • Central oxytocinergic neurotransmission: a drug target for the therapy of psychogenic erectile dysfunction.

    abstract::A group of oxytocinergic neurons originating in the paraventricular nucleus of the hypothalamus and projecting to extrahypothalamic brain areas (e.g. hippocampus, medulla oblongata and spinal cord) control penile erection. Activation of these neurons by dopamine and dopamine agonists, excitatory amino acids (N-methyl-...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/1389450033347190

    authors: Melis MR,Argiolas A

    更新日期:2003-01-01 00:00:00

  • Targeting PPAR isoforms following CNS injury.

    abstract::A major focus has developed for the discovery of proregenerative and neuroprotective therapeutic agents to help the millions of Americans who receive a CNS injury annually. Tribulations have been encountered along the way due to the complicated set of pathways that are initiated post-injury. To target this complicated...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/1389450111314070003

    authors: Yonutas HM,Sullivan PG

    更新日期:2013-06-01 00:00:00

  • The Therapeutic Potential of Quercetin in Parkinson's Disease: Insights into its Molecular and Cellular Regulation.

    abstract::Parkinson's disease (PD) is a chronic and progressive neurodegenerative disorder characterized by the progressive death of dopaminergic neurons in the substantia nigra pars compacta (SNc). PD is a multifactorial disorder, with several different factors being suggested to play a synergistic pathophysiological role, inc...

    journal_title:Current drug targets

    pub_type: 杂志文章

    doi:10.2174/1389450120666191112155654

    authors: Tamtaji OR,Hadinezhad T,Fallah M,Shahmirzadi AR,Taghizadeh M,Behnam M,Asemi Z

    更新日期:2020-01-01 00:00:00

  • Proline Oxidase (POX) as A Target for Cancer Therapy.

    abstract::Proline dehydrogenase/proline oxidase (PRODH/POX) is an enzyme catalyzing the first step of proline degradation, during which ROS and/or ATP is generated. POX is widely distributed in living organisms and is responsible for a number of regulatory processes such as redox homeostasis, osmotic adaptation, cell signaling ...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/138945011613151031150637

    authors: Kononczuk J,Czyzewska U,Moczydlowska J,Surażyński A,Palka J,Miltyk W

    更新日期:2015-01-01 00:00:00

  • Colloidal carrier systems for transcutaneous immunization.

    abstract::Recently, the skin has emerged as a potential alternative route for non-invasive delivery of vaccine. It has been recognized as a highly immune-reactive tissue containing an abundance of antigen presenting cells, especially within the epidermis. Transcutaneous immunization, introduction of antigen through topical appl...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/138945011794751492

    authors: Gupta PN,Vyas SP

    更新日期:2011-04-01 00:00:00

  • Recent Advances in Protein-Protein Docking.

    abstract::Protein-protein interactions (PPIs) play important roles in a variety of biological processes, and many PPIs have been regarded as biologically compelling targets for drug discovery. Extensive efforts have been made to develop feasible proteinprotein docking approaches to study PPIs in silico. Most of these approaches...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/1389450117666160112112640

    authors: Zhang Q,Feng T,Xu L,Sun H,Pan P,Li Y,Li D,Hou T

    更新日期:2016-01-01 00:00:00

  • MicroRNAs in arterial remodelling, inflammation and atherosclerosis.

    abstract::Atherosclerosis is now widely appreciated to represent a chronic inflammatory reaction of the vascular wall in response to dyslipidemia and endothelial distress involving the inflammatory recruitment of leukocytes and the activation of resident vascular cells. The proliferative response of smooth muscle cells critical...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/138945010791591377

    authors: Weber C,Schober A,Zernecke A

    更新日期:2010-08-01 00:00:00

  • Regulation of thrombospondin1 by extracellular proteases.

    abstract::The contribution of proteases to developmental, physiological and pathological processes has been well accepted. Cleavage of matrix proteins is a key requirement for cell migration and remodeling of the extracellular environment. The constant process of matrix turnover is dependent on the delicate balance between degr...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/138945008785909365

    authors: Iruela-Arispe ML

    更新日期:2008-10-01 00:00:00

  • Prediction of Late Recurrence and Distant Metastasis in Early-stage Breast Cancer: Overview of Current and Emerging Biomarkers.

    abstract::Recently, a significant number of breast cancer (BC) patients have been diagnosed at an early stage. It is therefore critical to accurately predict the risk of recurrence and distant metastasis for better management of BC in this setting. Clinicopathologic patterns, particularly lymph node status, tumor size, and horm...

    journal_title:Current drug targets

    pub_type: 杂志文章

    doi:10.2174/1389450121666200312105908

    authors: Gouri A,Benarba B,Dekaken A,Aoures H,Benharkat S

    更新日期:2020-01-01 00:00:00

  • Prevention of ischemic stroke: surgery.

    abstract::The last 15 years have witnessed a resurgence of the role of surgical options for prevention of ischemic stroke. The landmark randomized trials including NASCET and ECST were published and explored the role of carotid endarterectomy in this regard. Patients with high grade stenosis of the internal carotid artery (> or...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/138945007781077391

    authors: Rajamani K,Chaturvedi S

    更新日期:2007-07-01 00:00:00

  • Targeting glycogen synthase kinase-3 in the CNS: implications for the development of new treatments for mood disorders.

    abstract::There exists an immediate need to develop novel medications for the treatment of mood disorders such as bipolar disorder and depression. Initial interest in glycogen synthase kinase-3 (GSK-3) as a target for the treatment of mood disorders arose from the finding that the mood stabilizing drug lithium directly inhibite...

    journal_title:Current drug targets

    pub_type: 杂志文章,评审

    doi:10.2174/1389450110607011399

    authors: Gould TD,Picchini AM,Einat H,Manji HK

    更新日期:2006-11-01 00:00:00