Abstract:
INTRODUCTION:Aberrant regulation of platelet-derived growth factors (PDGFs) and their receptors (PDGFR) has been shown to be involved in many solid tumors, including breast cancer. PDGFR-α and PDGFR-β expressions were documented in breast cancer and are correlated with tumor aggressiveness and metastasis. Preclinical evidence further suggests tumor stimulatory roles of PDGFRs expressed by tumor stroma cells and indicates a deleterious effect of stromal PDGFRs on intratumoral drug uptake. AREAS COVERED:This review summarizes the present understanding of PDGF signaling in breast cancer based on experimental studies and available clinical trials. It also provides a critical discussion of selected ongoing clinical trials in patients with breast cancer involving PDGFR inhibition with tyrosine kinase inhibitors, specifically in endocrine responsive breast cancer. EXPERT OPINION:An increased molecular understanding of response and resistance mechanisms to endocrine therapy will be essential for therapeutic advances in PDGFR-directed cancer therapy. Future developments in the field will rely on clinical studies where prospective analyses of target expression in breast cancer cells and in the tumor stroma are included. More selective PDGFR inhibitors with reduced side effects will be crucial for combinatorial therapies. Development of sensitive diagnostics is of critical importance for patient selection and monitoring of therapeutic effects.
journal_name
Expert Opin Investig Drugsjournal_title
Expert opinion on investigational drugsauthors
Criscitiello C,Gelao L,Viale G,Esposito A,Curigliano Gdoi
10.1517/13543784.2014.895323subject
Has Abstractpub_date
2014-05-01 00:00:00pages
599-610issue
5eissn
1354-3784issn
1744-7658journal_volume
23pub_type
杂志文章,评审abstract:BACKGROUND:Acute decompensated heart failure (ADHF) is associated with increased hospitalization rates and high in-hospital mortality, and has emerged as a major public health problem over the past decade. In recent years, several new drugs and therapeutic approaches have failed to reduce short- and long-term morbidity...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543780902922660
更新日期:2009-06-01 00:00:00
abstract::The deposition of a platelet rich thrombus on an atherosclerotic plaque is a critical step in the development of unstable coronary syndromes. Currently available therapeutic agents such as aspirin and ticlopidine are relatively weak inhibitors of platelet aggregation. Recently, antagonists to platelet glycoprotein IIb...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1517/13543784.6.9.1257
更新日期:1997-09-01 00:00:00
abstract:INTRODUCTION:Because of the central role of the mammalian target of rapamycin (mTOR) pathway in the control and distribution of signals essential for mRNA translation of mitogenic genes and generation of oncogenic proteins, effective targeting of mTOR remains a major goal in medical oncology. AREAS COVERED:This articl...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.2013.787066
更新日期:2013-06-01 00:00:00
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
更新日期:2017-01-01 00:00:00
abstract:IMPORTANCE OF THE FIELD:Treatments of pulmonary arterial hypertension (PAH) that have so far proven efficacious are all based on the restoration of endothelium control of pulmonary vascular tone and structure, by administration of prostacyclins, endothelin receptor antagonists and phosphodiesterase-5 inhibitors. Howeve...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543781003727099
更新日期:2010-04-01 00:00:00
abstract::In spite of tremendous efforts to control cancer, the mortality associated with this disease has been increasing in developed countries in the recent decades. Inadequate efficiency of existing therapeutic regimens and the rise of multi-drug resistant cancer cells are the main factors which require a broadening of inve...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.9.6.1243
更新日期:2000-06-01 00:00:00
abstract::Tuberculosis (TB), which kills more people than any other infectious disease, was declared a global emergency by the World Health Organization in 1993. The emergence of new Mycobacterium tuberculosis strains that are resistant to some or all current antitubercular drugs seriously hampers the control of the disease. Up...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.11.8.1033
更新日期:2002-08-01 00:00:00
abstract:INTRODUCTION:IL-6 is a key cytokine in the pathogenesis of rheumatoid arthritis (RA). The clinical efficacy of tocilizumab (TCZ), a humanized anti-IL6-receptor mAb, confirmed the value of IL-6 blockade in this disease. A number of new anti-IL-6 biologics are currently in Phase I - III of clinical development for RA. A...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.2014.912276
更新日期:2014-07-01 00:00:00
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
更新日期:2007-09-01 00:00:00
abstract::In addition to a variety of other novel agents, interest in histone deacetylase inhibitors (HDACIs) as antineoplastic drugs has recently accelerated and increasing numbers of these compounds have entered clinical trials in humans. HDACIs represent a prototype of molecularly targeted agents that perturb signal transduc...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.13.1.21
更新日期:2004-01-01 00:00:00
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
更新日期:2012-01-01 00:00:00
abstract::Telomerase is a holoenzyme responsible for the maintenance of telomeres, the protein-nucleic acid complexes at the ends of eukaryotic chromosomes that serve to maintain chromosomal stability and integrity. Telomerase activity is essential for the sustained proliferation of most immortal cells, including cancer cells. ...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.10.12.2141
更新日期:2001-12-01 00:00:00
abstract::Zolmitriptan is a new oral acute treatment for migraine. It is a selective and potent agonist at the serotonin (5-HT)(1B/1D) receptor and was developed to improve on the oral bioavailability, tissue selectivity and CNS penetration of earlier compounds. Animal studies confirmed that these objectives had been attained. ...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1517/13543784.7.4.633
更新日期:1998-04-01 00:00:00
abstract::Control of the immune system is of indispensable importance for graft acceptance and function. Immunological changes in the graft before and after organ harvesting, the transplantation procedure itself and the organ recipients clinical state contribute to the immune response. Leukocyte trafficking [1] into a graft is ...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.9.4.789
更新日期:2000-04-01 00:00:00
abstract::The annual meeting of the American Diabetes Association was held in Boston, MA. There were over 6500 participants, one-third from overseas, and 1103 papers were presented. Abstracts from the meeting have been published, from which abstract numbers are given below, e.g., (A141). Considerable progress has been made in u...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1517/13543784.6.8.1113
更新日期:1997-08-01 00:00:00
abstract::In the last three years, most efforts of virologists and immunologists involved in the field of HIV have been focussed on strategies aimed at eradicating the infection. So far, however, all attempts have been unsuccessful. Indeed, even if the currently available potent antiretroviral regimens are able to induce a prof...
journal_title:Expert opinion on investigational drugs
pub_type: 社论
doi:10.1517/13543784.9.2.193
更新日期:2000-02-01 00:00:00
abstract:IMPORTANCE OF THE FIELD:Curcumin has been investigated in preclinical and translational stroke models because of its pleiotropic 'neuroprotective' activities. Since curcumin has poor blood-brain barrier (BBB) penetration following acute administration, creative medicinal chemistry has been used to modify the parent cur...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.2011.542410
更新日期:2011-01-01 00:00:00
abstract::Presentations at the William Harvey Research Conference on PDE Inhibitors described the molecular biology, biochemical regulation. pharmacology, and therapeutic utility of inhibitors of cyclic nucleotide phosphodiesterases (PDEs). Most of the talks focused on PDE4 and PDE5. two members of the 11-member PDE family that...
journal_title:Expert opinion on investigational drugs
pub_type:
doi:10.1517/13543784.9.3.621
更新日期:2000-03-01 00:00:00
abstract::Complement is part of the innate immune system, acting to protect the host from microorganisms such as bacteria, and other foreign and abnormal cells. Although primarily protective, complement activation can also cause damage to the host. In a number of inflammatory diseases, including rheumatoid arthritis and dermati...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.14.7.807
更新日期:2005-07-01 00:00:00
abstract:INTRODUCTION:Obinutuzumab is a novel humanized type II glycoengineered anti-CD20 antibody approved for first-line treatment of chronic lymphocytic leukemia (CLL) in combination with chlorambucil and for treatment of rituximab-refractory follicular lymphoma (FL). Areas covered: We describe current preclinical and clinic...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1080/13543784.2017.1373087
更新日期:2017-10-01 00:00:00
abstract::A major session at this annual gathering of the cancer researchers from around the globe dealt with the current state of immunotherapy for cancer. Immunotherapy is a form of cancer treatment that enhances its scientific promise and legitimacy with each passing year. As a result, this topic has become one of the most h...
journal_title:Expert opinion on investigational drugs
pub_type:
doi:10.1517/13543784.9.6.1413
更新日期:2000-06-01 00:00:00
abstract::ATP-gated P2X7 receptors (P2X7) make a unique family of extracellular ATP-activated plasma membrane ion channels expressed in haematopoietic and epithelial cells. They have been extensively studied in immune cells where their activation leads to the rapid release of pro-inflammatory cytokines and the initiation of the...
journal_title:Expert opinion on investigational drugs
pub_type: 社论
doi:10.1517/13543784.2011.583918
更新日期:2011-07-01 00:00:00
abstract:INTRODUCTION:Erectile function is an important aspect in the quality of life of many men. For men with erectile dysfunction (ED), a spectrum of treatment options exists. Novel therapies for ED are currently being developed in order to delay surgical placement of a penile prosthesis - the final step in the management of...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1080/13543784.2017.1324570
更新日期:2017-06-01 00:00:00
abstract:IMPORTANCE OF THE FIELD:Antibacterial drug discovery and development has slowed considerably in recent years, with novel classes discovered decades ago and regulatory approvals tougher to get. Traditional approaches and the newer genomic mining approaches have not yielded novel classes of antibacterial compounds. Inste...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543780903505092
更新日期:2010-02-01 00:00:00
abstract:INTRODUCTION:Heat shock protein 90 (HSP90) serves as a critical facilitator for oncogene addiction. There has been augmenting enthusiasm in pursuing HSP90 as an anticancer strategy. In fact, since the initial serendipitous discovery that geldanamycin (GM) inhibits HSP90, the field has rapidly moved from proof-of-concep...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.2014.902442
更新日期:2014-05-01 00:00:00
abstract:INTRODUCTION:The purpose of this article is to highlight novel therapies that are being used in scleroderma (SSc). Therapeutic interventions in SSc generally target at least one of three ongoing biological processes characteristic of the disease: vasculopathy, autoimmunity and tissue fibrosis. Treatment decisions in SS...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.2014.848852
更新日期:2014-02-01 00:00:00
abstract::Background: We aimed to estimate population-based trends in the prevalence of coexisting type 2 diabetes (T2D) and suspected nonalcoholic fatty liver disease (NAFLD) and pioglitazone use among U.S. adults.Research design and methods: We conducted a cross-sectional analysis of the National Health and Nutrition Examinat...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1080/13543784.2020.1704731
更新日期:2020-02-01 00:00:00
abstract:INTRODUCTION:Epithelial ovarian cancer (EOC) is the fourth commonest cause of female cancer death in the developed world. Although progress in treatment has improved survival, ∼ 80% of patients with advanced EOC will experience a recurrence and eventually will become resistant to chemotherapy. The aim of treatment for ...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.2015.1072168
更新日期:2015-01-01 00:00:00
abstract::Ovarian stimulation during infertility treatment is used either alone or in conjunction with intrauterine insemination and assisted reproductive technologies. At the present time, the two main medications used for ovarian stimulation include an oral antioestrogen, clomiphene citrate and injectable gonadotrophins. In s...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.12.3.353
更新日期:2003-03-01 00:00:00
abstract::The discovery of peroxisome proliferator-activated receptor gamma (PPARgamma) as the molecular target for antidiabetic thiazolidinediones has heralded a new era in the approach to understanding the pathophysiology of insulin resistance and its relationship to cardiovascular disease. However, the subsequent discovery o...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1517/13543784.8.11.1859
更新日期:1999-11-01 00:00:00