Therapeutic potential of S179D prolactin--from prostate cancer to angioproliferative disorders: the first selective prolactin receptor modulator.

Abstract:

:Increasing evidence suggests an important role for autocrine/paracrine prolactin in breast and prostate cancers and other disease states. Prolactin production in these extrapituitary sites is not governed by dopamine agonists, a finding that has spurred the production of prolactin receptor antagonists. This review focuses on one such antagonist, S179D prolactin, which was produced by mimicking a natural antagonist, phosphorylated prolactin. S179D prolactin is a very effective growth antagonist, partly because it inhibits signalling from unmodified prolactin and partly because it produces its own intracellular signal. This signal results in cell differentiation, cell-cycle arrest or apoptosis depending on dose, duration of treatment and cellular context. S179D prolactin is also a potent antiangiogenic and initial studies have shown it to be a potent anti-inflammatory agent. In light of these additional modes of action, it is suggested that S179D prolactin should now be more aptly referred to as a selective prolactin receptor modulator.

authors

Walker AM

doi

10.1517/13543784.15.10.1257

subject

Has Abstract

pub_date

2006-10-01 00:00:00

pages

1257-67

issue

10

eissn

1354-3784

issn

1744-7658

journal_volume

15

pub_type

杂志文章,评审
  • Contraceptives with novel benefits.

    abstract:INTRODUCTION:Progesterone receptor (PR) agonists (progestins) and antagonists are developed for female contraceptives. However, non-contraceptive applications of newer progestins and PR modulators are being given more attention. AREAS COVERED:The newer PR agonists including drospirenone, nomegestrol, trimegestone, die...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.2012.642368

    authors: Su Y,Lian QQ,Ge RS

    更新日期:2012-01-01 00:00:00

  • Investigational PD-1 inhibitors in HL and NHL and biomarkers for predictors of response and outcome.

    abstract:INTRODUCTION:Inhibitors against the PD-1/PD-L1 pathway are revolutionizing the treatment and management of malignancies. AREAS COVERED:We summarize our current understanding of the function of PD-1, its role in immune evasion, the clinical data available that support the use of PD-1 antagonist in Hodgkin and non-Hodgk...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1080/13543784.2018.1416091

    authors: Chang A,Schlafer D,Flowers CR,Allen PB

    更新日期:2018-01-01 00:00:00

  • Developments in the treatment of chronic hepatitis C.

    abstract::Hepatitis C virus is the most common chronic, blood-bourne infection, affecting 170 million people worldwide, approximately 3% of the global population. Of those infected with hepatitis C virus, 50 - 85% will develop chronic hepatitis C. Although hepatitis C is primarily a disease of the liver, a diagnosis is currentl...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.11.4.515

    authors: Pockros PJ

    更新日期:2002-04-01 00:00:00

  • Platelet P2Y12 receptor inhibition by thienopyridines: status and future.

    abstract::Thienopyridines have a well-established role in the treatment of coronary artery disease, especially in the setting of acute coronary syndromes and percutaneous coronary interventions. Ticlopidine, the first FDA-approved thienopyridine, was shown to be effective in reducing coronary events in high risk patients, but t...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543780903176415

    authors: Porto I,Giubilato S,De Maria GL,Biasucci LM,Crea F

    更新日期:2009-09-01 00:00:00

  • Small-molecule EGFR tyrosine kinase inhibitors for the treatment of cancer.

    abstract:INTRODUCTION:EGFR has been implicated in various malignancies such as NSCLC, breast, head and neck, and pancreatic cancer. Numerous drugs have been developed in order to target the tyrosine domain of EGFR as an approach in cancer treatment. AREAS COVERED:This article focuses on the different generations of EGFR tyrosi...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.2014.928283

    authors: Lee CC,Shiao HY,Wang WC,Hsieh HP

    更新日期:2014-10-01 00:00:00

  • Experimental therapies targeting apolipoprotein C-III for the treatment of hyperlipidemia - spotlight on volanesorsen.

    abstract:INTRODUCTION:Despite the substantial reduction in cardiovascular morbidity and mortality after the management of dyslipidemia with statins, residual risk remains even after achieving low-density lipoprotein cholesterol targets. This residual risk appears to be partly attributed to low levels of high-density lipoprotein...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1080/13543784.2019.1582028

    authors: Milonas D,Tziomalos K

    更新日期:2019-04-01 00:00:00

  • PTI-821: sustained-release oxycodone using gel-cap technology.

    abstract::PTI-821 is a long-acting formulation of oxycodone that is intended to deter abuse through its gel-cap technology. Produced by Pain Therapeutics in alliance with King Pharmaceuticals, PTI-821 is designed to provide strong pain relief with the intent of offering greater safety than is presently available from convention...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.16.3.359

    authors: Webster LR

    更新日期:2007-03-01 00:00:00

  • Immunoadsorption, current status and future developments.

    abstract::The association of abnormalities in the cellular and humoral immune system with various autoimmune diseases provides the rationale for apheresis technologies. While plasmapheresis or plasma exchange is limited by its non-selective removal of all plasma components, modern apheresis techniques aim to provide more specif...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.9.9.2017

    authors: Braun N,Bosch T

    更新日期:2000-09-01 00:00:00

  • Insulin sensitizers in 2013: new insights for the development of novel therapeutic agents to treat metabolic diseases.

    abstract::Insulin-sensitizing thiazolidinediones (TZDs) correct a root cause of type 2 diabetes and potentially other diseases of metabolic dysfunction, including conditions ranging from oncologic, inflammatory, and neurodegenerative diseases. Importantly, compounds with this mode of action can modify disease progression, as op...

    journal_title:Expert opinion on investigational drugs

    pub_type: 社论,评审

    doi:10.1517/13543784.2013.839659

    authors: Colca JR,Tanis SP,McDonald WG,Kletzien RF

    更新日期:2014-01-01 00:00:00

  • Polidocanol for endovenous microfoam sclerosant therapy.

    abstract:BACKGROUND:Polidocanol is a liquid surfactant having endothelial cell lytic properties. In the form of a controlled, dispensed microfoam it is administered endovenously as a sclerosing agent in the treatment of varicose veins. OBJECTIVE:This review summarizes efficacy of polidocanol endovenous microfoam sclerotherapy ...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543780903376163

    authors: Eckmann DM

    更新日期:2009-12-01 00:00:00

  • Therapeutic targets and early stage clinical trials for pulmonary fibrosis.

    abstract:INTRODUCTION:Idiopathic pulmonary fibrosis (IPF) is an age-associated, progressive, and irreversible fatal interstitial lung disease. Although many drugs have failed in clinical trials, these failures improved the understanding of the pathogenesis of IPF. Currently, there are two drugs approved for IPF that slow the pr...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1080/13543784.2019.1554054

    authors: Sato S,Yanagihara T,Kolb MRJ

    更新日期:2019-01-01 00:00:00

  • Investigational non-JAK inhibitors for chronic phase myelofibrosis.

    abstract:INTRODUCTION:Patients with myelofibrosis (MF) have no effective treatment option after the failure of approved JAK inhibitor (JAKi) therapy. Non-JAK inhibitors (non-JAKi) that target non-canonical molecular pathways are undergoing clinical evaluations to optimize efficacy and/or to reduce hematological toxicity of JAKi...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1080/13543784.2020.1751121

    authors: Bankar A,Gupta V

    更新日期:2020-05-01 00:00:00

  • The Annual European Congress of Rheumatology: recent advances in the treatment of rheumatic diseases. Lisbon, Portugal, June 18-21, 2003.

    abstract::The topics discussed at this conference covered many aspects of the pathogenesis, epidemiology, diagnosis and treatment of rheumatic diseases, from the search of new therapeutic targets and evaluation of new diagnostic techniques to preclinical and clinical development of novel therapies. This contribution focuses pri...

    journal_title:Expert opinion on investigational drugs

    pub_type:

    doi:10.1517/13543784.12.10.1713

    authors: Hellmich B,Gross WL

    更新日期:2003-10-01 00:00:00

  • Recent advances in the management of adult myositis.

    abstract::Standard drug therapy of adult polymyositis, dermatomyositis and inclusion body myositis includes high-dose corticosteroids and cytotoxic drugs (methotrexate, azathioprine (AZA) and cyclophosphamide). Recent data are in favour of the early introduction of a cytotoxic or immunomodulating drug in addition to corticoster...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.10.7.1265

    authors: Fam AG

    更新日期:2001-07-01 00:00:00

  • Academy for Eating Disorders International Conference on Eating Disorders. Denver, CO, USA, May 29-31, 2003.

    abstract::The focus of this meeting was the interface between eating disorders and obesity. A symposium at this meeting dealt with advances in treatment for bulimia nervosa (BN) and binge eating disorder. There were two presentations in this symposium that addressed pharmacological treatments. One reviewed drug treatments for B...

    journal_title:Expert opinion on investigational drugs

    pub_type:

    doi:10.1517/13543784.12.8.1441

    authors: Kaplan AS

    更新日期:2003-08-01 00:00:00

  • Lorecivivint, an intra-articular potential disease-modifying osteoarthritis drug.

    abstract::Introduction: Osteoarthritis (OA) is the most common form of arthritis. Knee OA is associated with joint pain, activity limitation, physical disability, reduced health-related quality of life, and increased mortality. To date, all pharmacologic treatments for OA are directed toward pain management. Lorecivivint (LOR) ...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章

    doi:10.1080/13543784.2020.1842357

    authors: Sabha M,Siaton BC,Hochberg MC

    更新日期:2020-12-01 00:00:00

  • Ganetespib for small cell lung cancer.

    abstract:INTRODUCTION:Heat shock proteins (Hsps) are part of a complex network of chaperone proteins that are critically involved in the conformational maturation of intracellular proteins and regulate their degradation via the proteasome system Hsps (especially Hsp70 and Hsp90) are upregulated in many cancers and are potential...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1080/13543784.2017.1268599

    authors: Subramaniam DS,Warner EA,Giaccone G

    更新日期:2017-01-01 00:00:00

  • Retaspimycin hydrochloride (IPI-504): a novel heat shock protein inhibitor as an anticancer agent.

    abstract::Heat shock proteins are vital to cell survival under conditions of stress. They bind client proteins to assist in protein stabilization, translocation of polypeptides across cell membranes and recovery of proteins from aggregates. Heat shock protein inhibitors are a diverse group of novel agents that have been demonst...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543780903158934

    authors: Hanson BE,Vesole DH

    更新日期:2009-09-01 00:00:00

  • Discontinued drugs in 2006: pulmonary-allergy, dermatological, gastrointestinal and arthritis drugs.

    abstract::This perspective is the second in a series discussing drugs dropped from development in 2006, with a focus on pulmonary-allergy, dermatological, gastrointestinal and arthritis drugs. A survey of discontinued drugs from 2006 is provided, based on data from the Pharmaprojects database, along with an analysis of biology,...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.16.9.1327

    authors: Ozdemir C,Akdis CA

    更新日期:2007-09-01 00:00:00

  • Emerging therapeutic strategies for minimal change disease and focal and segmental glomerulosclerosis.

    abstract:INTRODUCTION:Minimal change disease (MCD) and Focal and segmental glomerulosclerosis (FSGS) are two of the major causes of nephrotic syndrome (NS) in children and adults. According to KDIGO (Kidney Disease: Improving Global Outcomes) guidelines, the treatment of adult primary MCD and FSGS should be based on immunosuppr...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1080/13543784.2018.1540587

    authors: Siligato R,Cernaro V,Nardi C,De Gregorio F,Gembillo G,Costantino G,Conti G,Buemi M,Santoro D

    更新日期:2018-11-01 00:00:00

  • An array of immunotherapeutic strategies for B-cell lymphomas.

    abstract::With FDA approval of monoclonal antibodies (mAb) against the B-cell-specific cell surface molecule CD20, immunotherapy in B-cell non-Hodgkin's-lymphomas (NHL) has gained momentum. Since the first description of the CD20 mAb and its use in a single patient, it has taken more than 20 years to implement this in current t...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章

    doi:10.1517/13543784.8.12.2059

    authors: Schultze JL

    更新日期:1999-12-01 00:00:00

  • A novel CXCR4 antagonist for hematopoietic stem cell mobilization.

    abstract:BACKGROUND:Hematopoietic stem cell (HSC) transplantation is a treatment option for hematological malignancies. Current mobilization regimes frequently result in inadequate numbers of HSC for transplant therefore alternative methods of mobilization are required. OBJECTIVE:The chemokine receptor CXCR4 and ligand SDF-1 a...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.17.11.1749

    authors: Fricker SP

    更新日期:2008-11-01 00:00:00

  • The therapeutic potential of cationic peptides.

    abstract::Novel classes of antibiotics that are useful against resistant bacteria are a major need in human medicine. Cationic antimicrobial peptides are utilised as nature's antibiotics, being produced constitutively or in response to infection in virtually every type of organism from plants and insects to man. Thus, these pep...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章

    doi:10.1517/13543784.7.2.167

    authors: Hancock RE

    更新日期:1998-02-01 00:00:00

  • Abatacept for the treatment of systemic lupus erythematosus.

    abstract:INTRODUCTION:Due to improvements in our understanding of the pathogenesis of systemic lupus erythematosus (SLE), several target drugs have been and are being developed. One of the possible targets in SLE is co-stimulation between antigen-presenting cells and T cells. Abatacept is a co-stimulation moderator approved for...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.2016.1154943

    authors: Pimentel-Quiroz VR,Ugarte-Gil MF,Alarcón GS

    更新日期:2016-01-01 00:00:00

  • Tetomilast: new promise for phosphodiesterase-4 inhibitors?

    abstract:INTRODUCTION:Tetomilast is a novel thiazole phosphodiesterase-4 (PDE-4) inhibitor, which may prove useful in both the treatment of inflammatory bowel disease (IBD) and chronic obstructive pulmonary disease (COPD). Here, the authors review the pharmacology of the drug, and offer critical review of the available data for...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.2012.732065

    authors: Bickston SJ,Snider KR,Kappus MR

    更新日期:2012-12-01 00:00:00

  • The therapeutic potential of testosterone patches.

    abstract::In the last decade, transdermal delivery of testosterone (T) has been shown to be a safe and effective means of treating male hypogonadism. Transdermal T patches can provide for physiologic androgen replacement in over 90% of men with hypogonadism. In addition, T patches have been shown to be equivalent to im. T ester...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章

    doi:10.1517/13543784.7.12.1977

    authors: Amory JK,Matsumoto AM

    更新日期:1998-12-01 00:00:00

  • Therapies in development for the treatment of migraine.

    abstract::While oral formulations of agonists at the serotonin (5-HT) receptor subdivisions 5-HT(1B/1D)--the "triptan" class of drugs--dominate the market for migraine therapy and while still more triptans are under development, recent research efforts have also explored other pharmacological avenues, which are mostly based on ...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.11.12.1813

    authors: Mucke H

    更新日期:2002-12-01 00:00:00

  • Immunotherapy in atopic dermatitis.

    abstract::Atopic dermatitis (AD) is a common inflammatory disease involving the skin and often other organs and systems, mainly respiratory. A definitive general consensus on the AD pathogenesis has not yet been established, however several lines of evidence suggest that T-cells play a crucial role in priming AD early-stage les...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.10.1.49

    authors: Mastrandrea F

    更新日期:2001-01-01 00:00:00

  • New therapeutic perspectives with clevidipine: an ultra-short-acting intravenous Ca2+ channel blocker.

    abstract::Intravenous antihypertensive agents are used in clinical situations in which the immediate, precise control of blood pressure is a clinical necessity. Clevidipine is a new, vascular-selective, dihyrdopyridine Ca(2+) channel blocker, which exerts its hemodynamic effects through selective arterial vasodilation without e...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.16.9.1449

    authors: Gradman AH,Vivas Y

    更新日期:2007-09-01 00:00:00

  • Risperidone (Risperdal): clinical experience with a new antipsychosis drug.

    abstract::Risperidone (Risperdal) is a benzisoxazole derivative with a high affinity for serotonin 5-HT2 and dopamine D2 receptors, and some affinity for alpha- adrenergic, histamine H1 and dopamine D1 receptors. It has no anticholinergic effects. Early studies demonstrated risperidone to be an effective medication for psychoti...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章

    doi:10.1517/13543784.8.4.443

    authors: Keks NA,Culhane C

    更新日期:1999-04-01 00:00:00