Cannabinoid receptor ligands: clinical and neuropharmacological considerations, relevant to future drug discovery and development.

abstract：INTRODUCTION:We carried out a screen for small molecule selective inhibitors of eukaryotic DNA polymerases (pols). Dehydroaltenusin, isolated from a fungus (Alternaria tenuis), was found to be a specific inhibitor of pol α. AREAS COVERED:We succeeded in chemically synthesizing dehydroaltenusin along with five analogs....

journal_title：Expert opinion on investigational drugs

authors： Mizushina Y,Maeda N,Kuriyama I,Yoshida H

更新日期：2011-11-01 00:00:00

abstract：INTRODUCTION:The addition of monoclonal antibody (mAb) epidermal growth factor receptor (EGFR) inhibitors to classic chemotherapy doublet backbones has improved survival of metastatic colorectal cancer (mCRC). However, the role of triple-drug chemotherapy regimens in combination with an anti-EGFR mAb inhibitor is not y...

journal_title：Expert opinion on investigational drugs

authors： Matos I,Noguerido A,Ros J,Mulet N,Argilés G,Elez É,Tabernero J

更新日期：2019-05-01 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：:Cyclooxygenase-2 (COX-2) is constitutively expressed in the central nervous system, and is thought to have an important functional role therein. COX-2 interacts with neurotransmitters such as acetylcholine, 5-hydroxytryptamine and glutamate but is also involved in the regulation of the central nervous system immune sy...

journal_title：Expert opinion on investigational drugs

authors： Müller N,Strassnig M,Schwarz MJ,Ulmschneider M,Riedel M

更新日期：2004-08-01 00:00:00

abstract：INTRODUCTION:Angiogenesis inhibition represents a rational therapeutic strategy in the management of solid tumors. Brivanib is a dual tyrosine kinase inhibitor with selectivity against VEFGR-2 and FGFR. AREAS COVERED:This review provides an updated summary of preclinical and clinical experience with brivanib in cancer...

journal_title：Expert opinion on investigational drugs

authors： Diaz-Padilla I,Siu LL

更新日期：2011-04-01 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

authors： Smith-Harrison L,Starke NR,Smith RP,Kovac JR

更新日期：2017-06-01 00:00:00

abstract：:Despite the use of the statins to lower low-density lipoprotein-cholesterol, leading to major reductions in the mortality and morbidity that is associated with coronary artery disease, considerable mortality and morbidity remains. Increasing high-density lipoprotein (HDL)-cholesterol levels has been associated with re...

journal_title：Expert opinion on investigational drugs

authors： Doggrell SA

更新日期：2006-02-01 00:00:00

abstract：:Carvedilol is a beta-blocker with ancillary properties. Pilot clinical studies with carvedilol, added to the standard therapy of digoxin, diuretics and ACE inhibitors, showed beneficial effects in mild, moderate and severe heart failure. Patients consistently showed improvement in LV ejection fraction and NYHA functio...

journal_title：Expert opinion on investigational drugs

authors： Doggrell SA

更新日期：2001-05-01 00:00:00

abstract：:Introduction: A compound that simultaneously inhibits PDE3 and PDE4 should increase airway caliber by relaxing the smooth muscle and, simultaneously, suppress airway inflammatory responses. Ensifentrine (RPL554) is considered a PDE3/4 inhibitor, although its affinity for PDE3 is 3,440 times higher than that for PDE4, ...

journal_title：Expert opinion on investigational drugs

authors： Cazzola M,Calzetta L,Rogliani P,Matera MG

更新日期：2019-10-01 00:00:00

abstract：INTRODUCTION:About 185,000,000 people worldwide are chronically infected with hepatitis C virus (HCV). Currently, the most successful HCV infection antiviral therapies reduce the chance of progression towards the advanced phases of the hepatopathy (liver cirrhosis, hepatocellular carcinoma and death). Recently, however...

journal_title：Expert opinion on investigational drugs

authors： Gentile I,Zappulo E,Buonomo AR,Maraolo AE,Borgia G

更新日期：2015-01-01 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：: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：:Poly (ADP-ribose) polymerase (PARP) plays a key role in DNA repair mechanisms by detecting and initiating repair after DNA strand breaks. Inhibition of PARP in DNA repair-defective tumors (like those with BRCA1 or BRCA2 mutations) can lead to gross genomic instability and cell death. Likewise, combining PARP inhibitio...

journal_title：Expert opinion on investigational drugs

authors： Rodon J,Iniesta MD,Papadopoulos K

更新日期：2009-01-01 00:00:00

abstract：:Ovarian cancer leads to more fatalities than any other form of gynaecological cancer in North America and Europe. Over the last 30 years survival figures have improved somewhat due to improvements in diagnosis, surgery and chemotherapy. Despite these advances, the majority of patients will die from their disease, with...

journal_title：Expert opinion on investigational drugs

authors： Harries M,Kaye SB

更新日期：2001-09-01 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

authors： Fernández-Carvajal A,González-Muñiz R,Fernández-Ballester G,Ferrer-Montiel A

更新日期：2020-11-01 00:00:00

abstract：INTRODUCTION:Asthma is a common respiratory disease characterized by airway inflammation, bronchoconstriction and airway hyperresponsiveness and symptoms such as coughing, wheezing, shortness of breath and chest tightness. Allergic rhinitis is a common comorbidity in asthma and glucocorticoids are the key stone in the ...

journal_title：Expert opinion on investigational drugs

authors： Meteran H,Backer V

更新日期：2016-08-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:The sodium/hydrogen exchanger-1 (NHE-1/SLC9A1) is a ubiquitous plasma membrane protein whose main role is maintenance of intracellular pH and volume. NHE-1 plays a role in atherogenesis; however, its clinical relevance has not yet been established. AREAS COVERED IN THIS REVIEW:We herein review ...

journal_title：Expert opinion on investigational drugs

authors： Sarigianni M,Tsapas A,Mikhailidis DP,Kaloyianni M,Koliakos G,Fliegel L,Paletas K

更新日期：2010-12-01 00:00:00

abstract：:Binding of microbial cell surface adhesins to host receptor molecules is a critical early step in microbial infection and pathogenesis. Anti-adhesive strategies aimed at blocking this interaction offer an attractive means of preventing infection at an early stage. The strategy should reduce the likelihood of resistant...

journal_title：Expert opinion on investigational drugs

authors： Kelly CG,Younson JS

更新日期：2000-08-01 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

authors： Marchetti C,Ledermann JA,Benedetti Panici P

更新日期：2015-01-01 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

authors： Kumar A,Herrmann HC

更新日期：1997-09-01 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

authors： Economidis MA,Mishell DR Jr

更新日期：2005-04-01 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

authors： Steckelings UM,Unger T

更新日期：2012-06-01 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：: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：:This paper reviews the clinical pharmacology, efficacy and safety of the novel antipsychotic drug aripiprazole. All published citations regarding aripiprazole were reviewed using a Medline((R)) search (completed for citations through mid-year, 2002). In addition, abstracts from recent scientific meetings presenting da...

journal_title：Expert opinion on investigational drugs

authors： Keck PE Jr,McElroy SL

更新日期：2003-04-01 00:00:00

abstract：INTRODUCTION:The salivary gland (SG) in primary Sjögren's syndrome (pSS) is characterized by its lack of function (hyposalivation) and lymphocytic invasion. Small-molecule inhibitors (SMIs) are a new class of drugs, whose diminutive size permits diffusion into cells. SMIs targeting components of the immune system are e...

journal_title：Expert opinion on investigational drugs

authors： Pringle S,Wang X,Bootsma H,Spijkervet FKL,Vissink A,Kroese FGM

更新日期：2019-07-01 00:00:00

abstract：:There are several reasons to believe that agents that augment cAMP-mediated signalling in cardiac myocytes should have beneficial effects in patients with heart failure. However, clinical trials of first-generation cyclic nucleotide phosphodiesterase (PDE3) inhibitors, which raise cAMP content by blocking its hydrolys...

journal_title：Expert opinion on investigational drugs

authors： Movsesian MA

更新日期：2000-05-01 00:00:00

abstract：:Introduction: Neuropathic pain is a chronic condition that significantly affects the quality of life of millions of people globally. Most of the pharmacologic treatments currently in use demonstrate modest efficacy and over half of all patients do not respond to medical management. Hence, there is a need for new, effi...

journal_title：Expert opinion on investigational drugs

authors： Kushnarev M,Pirvulescu IP,Candido KD,Knezevic NN

更新日期：2020-03-01 00:00:00

abstract：:Anorexia nervosa (AN), bulimia nervosa (BN) and binge eating disorder (BED) each occur in about 0.5-1.5% of the population in westernised countries, and primarily affect women. At present, a variety of pharmacological treatments are used in addition to psychotherapy, with antidepressants being most the common. Current...

journal_title：Expert opinion on investigational drugs

authors： Crow S

更新日期：1997-04-01 00:00:00

abstract：:The increasing frequency of fungal infections in immunocompromised patients together with the emergence of strains resistant to currently used antifungal drugs point to an increased need for a new class of antimycotics. Antimicrobial peptides are promising candidates for the treatment of fungal infections since they h...

journal_title：Expert opinion on investigational drugs

authors： Lupetti A,Danesi R,van 't Wout JW,van Dissel JT,Senesi S,Nibbering PH

更新日期：2002-02-01 00:00:00