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. Since the discovery that telomerase activity is detected in 85-90% of all human tumours and tumour-derived cell lines but not in most normal somatic cells, telomerase has become the focus of much attention as a novel and potentially highly-specific target for the development of new anticancer chemotherapeutics. Herein we review the current perspective for the development of telomerase inhibitors as cancer chemotherapeutics. These include antisense strategies, reverse transcriptase inhibitors and compounds capable of interacting with high-order telomeric DNA tetraplex ("G-quadruplex") structures, so as to prevent enzyme access to the necessary linear telomere substrate. Critical appraisal of each individual approach is provided together with highlighted areas of likely future development.
journal_name
Expert Opin Investig Drugsjournal_title
Expert opinion on investigational drugsauthors
Perry PJ,Arnold JR,Jenkins TCdoi
10.1517/13543784.10.12.2141subject
Has Abstractpub_date
2001-12-01 00:00:00pages
2141-56issue
12eissn
1354-3784issn
1744-7658journal_volume
10pub_type
杂志文章,评审abstract:INTRODUCTION:Lupus nephritis (LN) is a significant contributor to morbidity and mortality in systemic lupus erythematosus (SLE). Current therapies for LN are limited by significant toxicities and high rates of relapse. A clear and present need exists for the development of effective, targeted and well-tolerated treatme...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.2014.950837
更新日期:2014-10-01 00:00:00
abstract:INTRODUCTION:In the last decade, concerns have been raised around the use of erythropoiesis-stimulating agents (ESAs) and intravenous iron in chronic kidney disease (CKD) patients, especially when given at high doses. Moreover, treatment with ESA is expensive. AREAS COVERED:We searched PubMed for original articles, re...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1080/13543784.2018.1493455
更新日期:2018-07-01 00:00:00
abstract::Major depressive disorder (MDD) affects journal_title:Expert opinion on investigational drugs pub_type: 杂志文章,评审 doi:10.1517/13543780903286396 更新日期:2009-11-01 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::Human cytomegalovirus (HCMV) is the most common viral opportunistic infection in patients suffering with acquired immunodeficiency virus (AIDS). HCMV is a systemic infection that may infect several sites in the body, including the retina, gastrointestinal tract, lungs, liver, and central nervous system. Retinitis is t...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1517/13543784.6.9.1157
更新日期:1997-09-01 00:00:00
abstract::Introduction: Therapeutic oligonucleotides have emerged as a promising new class of drug that could silence undruggable targets; they can potentially treat metabolic liver diseases such as nonalcoholic fatty liver disease (NAFLD), hereditary hemochromatosis and alpha 1 antitrypsin deficiency. Areas covered: This artic...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1080/13543784.2021.1879792
更新日期:2021-01-29 00:00:00
abstract:INTRODUCTION:Thermo transient receptor potential (thermoTRP) channels are some of the most intensely pursued therapeutic targets of the past decade. They are considered promising targets of numerous diseases including chronic pain and cancer. Modulators of these proteins, in particular TRPV1-4, TRPM8 and TRPA1, have re...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1080/13543784.2020.1825680
更新日期:2020-11-01 00:00:00
abstract::Atherothrombosis, or thrombus formation, at the site of a disrupted atherosclerotic plaque is the common pathophysiology related to myocardial infarction, ischaemic stroke and peripheral arterial disease. A growing body of evidence demonstrates an important role for vascular inflammation in the pathophysiology of athe...
journal_title:Expert opinion on investigational drugs
pub_type: 社论
doi:10.1517/13543784.13.5.457
更新日期:2004-05-01 00:00:00
abstract::Preclinical and clinical evidence support the effectiveness of neurotrophins in Alzheimer's disease (AD) and neurodegenerative diseases. Delivery of neurotrophins to target sites in the brain remains a major obstacle for their use in humans. Development of orally active agents that mimic the effects of nerve growth fa...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1517/13543784.6.10.1413
更新日期:1997-10-01 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
abstract:INTRODUCTION:Aurora kinases are key regulators of mitosis and inhibition of Aurora kinase activity is a rational therapeutic strategy in the treatment of solid tumors and hematological malignancies. AREAS COVERED:This paper will provide an updated summary of preclinical and clinical experience with ENMD-2076 in hemato...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.2012.668882
更新日期:2012-05-01 00:00:00
abstract:INTRODUCTION:Dasatinib is a novel tyrosine kinase inhibitor with activity against the Src family kinases. The Src pathway is active in breast cancer and has been shown to promote cell proliferation, invasiveness, and metastases. Preclinical data support the use of dasatinib to inhibit breast cancer cell growth, modulat...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1517/13543784.2013.793308
更新日期:2013-06-01 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:BACKGROUND:Treatment of advanced renal cell carcinoma (RCC) has undergone significant changes over the past 3 years after a long period of relative stagnation. A better understanding of the biology of the tumor led to the discovery of molecular targeted therapies resulting in significant improvement in outcome for this...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.17.10.1501
更新日期:2008-10-01 00:00:00
abstract::Overactive bladder (OAB) is a chronic distressing condition characterised by urinary urgency with or without urge incontinence, usually with frequency (voiding at least eight times daily) and nocturia. It affects millions of people worldwide independent of age, sex and race. The prevalence increases with age and is re...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.15.9.1017
更新日期:2006-09-01 00:00:00
abstract::Helicobacter pylori infection causes peptic ulcer disease and must be regarded as a serious infectious disease. Over the past two decades treatment of the infection has been a controversial issue. Treatment is purely empirical and based on combinations of two, three or four existing drugs. Antimicrobial resistance is ...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.10.8.1559
更新日期:2001-08-01 00:00:00
abstract:BACKGROUND:Dexamethasone cipecilate is a corticosteroid nasal spray whose local efficacy durability has been improved by introduction of a liposoluble functional group to its chemical structure. This study was conducted to evaluate the efficacy of once-daily treatment with this drug in patients with perennial allergic ...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,随机对照试验
doi:10.1517/13543784.2010.531258
更新日期:2010-12-01 00:00:00
abstract:INTRODUCTION:Cardiovascular disease is the leading cause of death worldwide, accounting for 30% of all deaths, with elevated blood pressure probably the most important modifiable risk factor. Worldwide, elevated blood pressure is estimated to cause 7.5 million deaths, about 12.8% of the total of all annual deaths. New ...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.2013.797962
更新日期:2013-07-01 00:00:00
abstract::Background: To compare the pharmacokinetic (PK) profile, safety, and immunogenicity between golimumab and the biosimilar BAT2506 in healthy Chinese male subjects. Research design and methods: A total of 180 healthy male subjects were recruited for this randomized, double-blinded, single-dose, parallel study. They rece...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1080/13543784.2021.1851364
更新日期:2021-01-01 00:00:00
abstract::Gene transfer technology is under exploration to find therapies for the treatment of Parkinson's disease (PD) and other neurodegenerative disorders. The technology of genetic transfer can also be used as a neurobiological tool to understand the role of various genes in animal models of neurodegeneration. We describe t...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1517/13543784.8.10.1551
更新日期:1999-10-01 00:00:00
abstract::It is now widely accepted that the renin-angiotensin system (RAS) not only contributes to pathological mechanisms involved, e.g. in hypertension or hypertensive and diabetic end-organ damage, but also harbors a "protective arm" represented mainly by two receptors, the AT2 (angiotensin type 2) receptor and the Mas rece...
journal_title:Expert opinion on investigational drugs
pub_type: 评论,杂志文章
doi:10.1517/13543784.2012.681046
更新日期:2012-06-01 00:00:00
abstract:INTRODUCTION:The ubiquitin-proteasome system (UPS) is responsible for the degradation of misfolded or damaged proteins, regulating inflammatory processes and cell cycle progression. The aim of this article is to summarize the currently available data regarding the possible utility of proteasome inhibitors (PIs) in the ...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.2013.840287
更新日期:2014-01-01 00:00:00
abstract:IMPORTANCE OF THE FIELD:The use of traditional medicines of natural origin is being encouraged for the treatment of chronic disorders, as synthetic drugs in such cases may cause unpredictable adverse effects. Berberine, a traditional plant alkaloid, is used in Ayurvedic and Chinese medicine for its antimicrobial and an...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.2010.517745
更新日期:2010-10-01 00:00:00
abstract::Disruption of a vulnerable atherosclerotic plaque is well-recognised as the primary cause of stroke, non-fatal myocardial infarction and sudden cardiac death. Novel therapeutic agents are being developed to stabilise such plaques. The initial evaluation of these drugs would be facilitated by the use of non-invasive im...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.11.5.693
更新日期:2002-05-01 00:00:00
abstract::There is still considerable interest in cephem antibacterial agents. In fact, there are a significant number of patents submitted for this antibacterial class. All the new cephem derivatives, independent of which group they belong to (III to V), possess a 2-amino-5-thiazolyl or a 5-amino-2-thiadiazolyl ring with an ox...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1517/13543784.6.3.305
更新日期:1997-03-01 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:INTRODUCTION:In the treatment of advanced/metastatic head and neck cancer (HNC), resistance to chemotherapy and to anti-EGFR agents remains a major issue, and new molecular drugs are eagerly awaited. Over the last decade, knowledge of the genetic landscape of HNC has rapidly grown. However, no tailored therapeutic inte...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1080/13543784.2016.1175435
更新日期:2016-07-01 00:00:00
abstract::In order to improve therapy and increase the quality of life for diabetic patients, it has been of significant interest to develop rapid-acting insulin preparations that mimic the physiological meal-time profile of insulin more closely than soluble human insulin. Insulin aspart (B28Asp human insulin) is a novel rapid-...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1517/13543784.8.9.1431
更新日期:1999-09-01 00:00:00
abstract::Female hormonal contraceptive methods have undergone slow change over the past four decades. Due to social, political and legal reasons, as well as medical complications, several new methods have been removed from the contraceptive armamentarium almost as quickly as they have been added. With worldwide unintended preg...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.14.4.449
更新日期:2005-04-01 00:00:00
abstract::The eating disorders anorexia nervosa, bulimia nervosa and binge eating disorder are common, significant public health problems which are treated with nutritional, psychotherapeutic and pharmacological interventions. A number of drugs (mostly antidepressant drugs) are currently used in their treatment to some benefit,...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.12.3.491
更新日期:2003-03-01 00:00:00