A consideration of PPAR-gamma ligands with respect to lipophilicity: current trends and perspectives.

abstract：:Considerable advances have been made on compounds that are active as inhibitors of HIV entry and fusion. The discovery of chemokines a few years ago focused the attention on coreceptor inhibitors in addition to fusion and attachment blockers. During the last 5 years, there has been an intense research activity from bo...

journal_title：Expert opinion on investigational drugs

authors： Citterio P,Rusconi S

更新日期：2007-01-01 00:00:00

abstract：:After thousands of years of interest the last few decades have seen a huge increase in our knowledge of the cannabinoids and their mode of action. Their potential as medical therapeutics has long been known. However, very real concerns over their safety and efficacy have lead to caution and suspicion when applying the...

journal_title：Expert opinion on investigational drugs

authors： Grundy RI

更新日期：2002-10-01 00:00:00

abstract：:Numerous studies over the last few years have suggested that modulating the glutamatergic system may be an efficient method to achieve an antidepressant effect. Data suggest that metabotropic glutamate receptors (mGlu receptors), related to long-term, modulatory effects on glutamatergic neurotransmission, may be a goo...

journal_title：Expert opinion on investigational drugs

authors： Palucha A

更新日期：2006-12-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:Aspirin, an irreversible inhibitor of thromboxane A(2) production, in combination with clopidogrel, an inhibitor of PY(12) ADP platelet receptors, represents the current standard-of-care of antiplatelet therapy for patients with acute coronary syndrome and those undergoing percutaneous coronary ...

journal_title：Expert opinion on investigational drugs

authors： Tomasello SD,Angiolillo DJ,Goto S

更新日期：2010-12-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:Molecules isolated from animals, insects, plants or microorganisms can provide prototypes for design of biopharmaceutical products. Some venom toxins and their derivatives are used in medicine, while others provide templates for development of new drugs. AREAS COVERED IN THIS REVIEW:The mild to...

journal_title：Expert opinion on investigational drugs

authors： Kerkis I,Silva Fde S,Pereira A,Kerkis A,Rádis-Baptista G

更新日期：2010-12-01 00:00:00

abstract：INTRODUCTION:the search for effective inhibitors to multiple infectious agents including influenza, smallpox and hemorrhagic fever viruses is an area of active research as many of these agents pose dramatic health and economic challenges to the human population. Many of these infectious agents are not only endemic thre...

journal_title：Expert opinion on investigational drugs

authors： Narayanan A,Bailey C,Kashanchi F,Kehn-Hall K

更新日期：2011-02-01 00:00:00

abstract：:Atrial natriuretic peptide (ANP) and B-type natriuretic peptide (BNP) are secreted by the heart and play important roles in the compensation of congestive heart failure with their vasodilating, natriuretic, antiproliferative, lusitropic and neurohumoral-modulating properties. Based on these beneficial properties, exog...

journal_title：Expert opinion on investigational drugs

authors： Boerrigter G,Burnett JC Jr

更新日期：2004-06-01 00:00:00

abstract：:Targeting cellular proliferation persists as a mainstay of cancer therapeutic strategy. Although microtubule-targeting drugs (such as taxanes and vinca alkaloids) have been used successfully in the clinic to treat a variety of cancers, they carry substantial liabilities that have spurred drug companies to aggressively...

journal_title：Expert opinion on investigational drugs

authors： Miglarese MR,Carlson RO

更新日期：2006-11-01 00:00:00

abstract：BACKGROUND:Age-related macular degeneration (AMD) affects > 14 million individuals worldwide. Although 90% of patients with AMD have the dry form, neovascular AMD accounts for the vast majority of patients who develop legal blindness. Until recently, few treatment options existed for treatment of neovascular AMD. The a...

journal_title：Expert opinion on investigational drugs

authors： Dixon JA,Oliver SC,Olson JL,Mandava N

更新日期：2009-10-01 00:00:00

abstract：:Type 2 diabetes is a chronic metabolic disease that adversely affects both the quality and longevity of life. The disease is characterised by elevated blood glucose (hyperglycaemia) that is associated with microvascular complications and increased macrovascular risk. Existing oral agents, either alone or in combinatio...

journal_title：Expert opinion on investigational drugs

authors： Coghlan M,Leighton B

更新日期：2008-02-01 00:00:00

abstract：INTRODUCTION:Noise-induced hearing loss (NIHL) due to industrial, military, and recreational noise exposure is a major, but also potentially preventable cause of acquired hearing loss. For the United States it is estimated that 26 million people (15% of the population) between the ages of 20 and 69 have a high-frequenc...

journal_title：Expert opinion on investigational drugs

authors： Sha SH,Schacht J

更新日期：2017-01-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:The evolution of targeted therapies is dependent upon identification of cellular moieties that can be pharmacologically modulated. As one such example, the serine-threonine kinase Akt was identified nearly two decades ago. Since then, its role in mediating multiple signaling cascades (ultimately...

journal_title：Expert opinion on investigational drugs

authors： Pal SK,Reckamp K,Yu H,Figlin RA

更新日期：2010-11-01 00:00:00

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 foc...

journal_title：Expert opinion on investigational drugs

authors： Walker AM

更新日期：2006-10-01 00:00:00

abstract：:COPD is a chronic disease of the lung that is characterised by decreased air flow and associated abnormal inflammatory responses of the lungs. A total of 80% of COPD incidences are observed in patients with history of smoking tobacco. The chronic condition of COPD is characterised by airway remodelling, which leads to...

journal_title：Expert opinion on investigational drugs

authors： Srivastava PK,Dastidar SG,Ray A

更新日期：2007-07-01 00:00:00

abstract：:Sitagliptin is a once-daily, orally active, competitive and fully reversible inhibitor of dipeptidyl peptidase 4, the enzyme that is responsible for the rapid degradation of the incretin hormone glucagon-like peptide-1. It is the first in this new class of antihyperglycaemic agents to gain regulatory approval for the ...

journal_title：Expert opinion on investigational drugs

authors： Deacon CF

更新日期：2007-04-01 00:00:00

abstract：BACKGROUND:Age-related macular degeneration is the leading cause of blindness among elderly individuals in industrialized countries. New drugs and advanced concepts for the treatment of dry AMD (dAMD) are needed. A new approach is the application of intravenous infusions of prostaglandin E1. OBJECTIVE:The aim of this ...

journal_title：Expert opinion on investigational drugs

authors： Augustin AJ,Diehm C,Grieger F,Bentz J

更新日期：2013-07-01 00:00:00

abstract：INTRODUCTION:Available drugs partially attenuate the hyperglycemia characteristic of diabetes. However, successful approaches to treat the root cause or to cure or prevent diabetes remain elusive. Drug discovery and development programs continue to focus on mechanisms that impact specific symptoms of diabetes. In 2014,...

journal_title：Expert opinion on investigational drugs

authors： Colca JR

更新日期：2015-01-01 00:00:00

abstract：:The beneficial effect of beta-hydroxy-beta-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors (statins) in primary prevention of coronary artery disease in those with hypercholesterolaemia and in secondary prevention in those with established coronary vascular disease are now well known. A growing body of eviden...

journal_title：Expert opinion on investigational drugs

authors： Delanty N,Vaughan CJ,Sheehy N

更新日期：2001-10-01 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

authors： McMahan ZH,Wigley FM

更新日期：2014-02-01 00:00:00

abstract：INTRODUCTION:GLP-1 receptor agonists have been shown to be effective in the treatment of type 2 diabetes mellitus (T2DM). Although the first GLP-1 receptor agonist, exenatide, was approved in the mid-2000s, other agents with longer durations of action (that do not require twice-daily dosing) are now being developed. In...

journal_title：Expert opinion on investigational drugs

authors： Garber AJ

更新日期：2012-01-01 00:00:00

abstract：:Asthma is a serious world health problem characterised by a chronic inflammatory disorder of the airways. Asthma attacks, or exacerbations, are episodic but airway inflammation is chronically present. Thus, this disorder requires long-term management. The goals of asthma management include prevention steps for long-te...

journal_title：Expert opinion on investigational drugs

authors： Centanni S,Santus P

更新日期：2002-01-01 00:00:00

abstract：INTRODUCTION:Despite the heterogeneity of prostate cancer (PCa), androgen stimulation is fundamental to its development, growth, and lethality. Therefore, the blockade of androgen receptor (AR) signaling is critical to controlling the disease, even after progression with castrate levels of androgens. AREAS COVERED:We ...

journal_title：Expert opinion on investigational drugs

authors： Isaacsson Velho P,Carducci MA

更新日期：2018-10-01 00:00:00

abstract：:Growth hormone-insensitivity syndrome (GHIS) is usually caused by mutations in the growth hormone receptor. Recombinant IGF-I has been used to treat GHIS either alone (mecasermin) or in combination with IGF-binding protein (IGFBP)-3 (mecasermin rinfabate). IGF-I increases the growth velocity of children with IGF defic...

journal_title：Expert opinion on investigational drugs

authors： Kemp SF,Thrailkill KM

更新日期：2006-04-01 00:00:00

abstract：INTRODUCTION:Currently, there is no cure available for the hereditary neurodegenerative disease proximal spinal muscular atrophy (SMA), which is the number one genetic killer in early childhood. However, growing knowledge of SMA pathophysiology has opened new avenues for potential therapeutic interventions. AREAS COVE...

journal_title：Expert opinion on investigational drugs

authors： Kaczmarek A,Schneider S,Wirth B,Riessland M

更新日期：2015-01-01 00:00:00

abstract：INTRODUCTION:Posttraumatic stress disorder (PTSD) is a prevalent, chronic and disabling anxiety disorder that may develop following exposure to a traumatic event. There is currently no effective pharmacotherapy for PTSD and therefore the discovery of novel, evidence-based treatments is particularly important. This revi...

journal_title：Expert opinion on investigational drugs

authors： Ragen BJ,Seidel J,Chollak C,Pietrzak RH,Neumeister A

更新日期：2015-05-01 00:00:00

abstract：:Introduction: Cyclin-dependent kinase 7 (CDK7) is a part of the CDK-activating kinase family (CAK) which has a key role in the cell cycle and transcriptional regulation. Several lines of evidence suggest that CDK7 is a promising therapeutic target for cancer. CDK7 selective inhibitors such as SY-5609 and CT7001 are in...

journal_title：Expert opinion on investigational drugs

authors： Liang H,Du J,Elhassan RM,Hou X,Fang H

更新日期：2021-01-01 00:00:00

abstract：INTRODUCTION:Type 2 diabetes is a chronic metabolic disease characterized by persistent hyperglycemia resulting from progressive deficient of insulin in patients with a background of insulin resistance. Current treatment algorithms recommended by American Diabetes Association/The European Association for the Study of D...

journal_title：Expert opinion on investigational drugs

authors： Tan X,Cao X,Zhou M,Zou P,Hu J

更新日期：2017-09-01 00:00:00

abstract：INTRODUCTION:The progression of the mammalian cell cycle is driven by the transient activation of complexes consisting of cyclins and cyclin-dependent kinases (CDKs). Loss of control over the cell cycle results in accelerated cell division and malignant transformation and can be caused by the upregulation of cyclins, t...

journal_title：Expert opinion on investigational drugs

authors： Węsierska-Gądek J,Kramer MP

更新日期：2011-12-01 00:00:00

abstract：:Parkinson's disease (PD) is a neurodegenerative disorder associated with the loss of dopaminergic neurons in the substantia nigra. The decline of dopamine leads to motor dysfunctions manifested as tremor, rigidity and bradykinesia. The pharmacological treatment of choice for the past 30 years has primarily been the do...

journal_title：Expert opinion on investigational drugs

authors： Tuite P,Riss J

更新日期：2003-08-01 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

authors： How J,Yee K

更新日期：2012-05-01 00:00:00