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Drug Evaluation, Preclinical (0):
Recent article
Drug Evaluation, Preclinical
Abstract
A series of 1,2,4-trisubstituted-1H- imidazole derivatives (4a-o) was synthesized by reacting 2,4-disubstituted-1H-imidazoles (3a-o) with chlorobenzene in the presence of triethylamine. Phenylglyoxal (2) was reacted with different aromatic aldehydes in the presence of ammonium acetate and glacial ace...
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PMID: 21928710
PDF is available here.
PDF is available here.
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Abstract
We attempt to investigate the interaction of metformin, PR and IGF-II expression, and identify whether metformin can enhance the antitumor effect of medroxyprogesterone acetate (MPA) using Ishikawa and HEC-1B EC cell lines. We found that both IGF-I and IGF-II inhibit PR A/B mRNA and protein expressi...
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PMID: 21168492
PDF is available here.
PDF is available here.
Abstract
Abstract
We have discovered and optimized a series of benzoxaborole-6-carboxamides to provide trypanocidal compounds that are orally active in murine models of human African trypanosomiasis. A key feature of this series is the presence of a boron atom in the heterocyclic core structure, which is essential to...
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PMID: 21859301
PDF is available here.
PDF is available here.
Abstract
The present study aimed to evaluate the protective and curative effects of the 15 KD protein isolated from the seeds of Peganum harmala L. against carbon tetrachloride (CCl4) induced oxidative stress in rats.
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PMID: 21845799
PDF is available here.
PDF is available here.
Abstract
Mepolizumab (Bosatria(®), GlaxoSmithKline) is a biologic agent developed to treat asthma. It represents a humanized monoclonal antibody of IgG1 κ type, which targets human IL-5 and thus prevents its interaction with the α-chain of the IL-5 receptor. To date, it has not been approv...
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PMID: 21790283
PDF is available here.
PDF is available here.
Abstract
Attempt has been made to evaluate free radical scavenging activity of ethanolic extract of Piper trioicum Roxb. and Physalis minima L. individually. In this study goat liver has been used as lipid source. This in vitro evaluation was done by measuring the malondialdehyde (MDA) of tissue homogenates....
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PMID: 21715277
PDF is available here.
PDF is available here.
Abstract
In the current study, the applicability and scope of descriptor based QSAR models to complement virtual screening using molecular docking approach have been applied to identify potential virtual screening hits targeting DNA gyrase A from Mycobacterium tuberculosis, an effective and v...
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PMID: 20953648
PDF is available here.
PDF is available here.
Abstract
These results indicate catechol as an important bioactive metabolite from salicortin....
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PMID: 21305449
PDF is available here.
PDF is available here.
Abstract
We tested the safety and efficacy of WST11, a novel water soluble vascular occluding agent, for vascular targeted photodynamic therapy of the dog prostate and compared it to WST09 vascular targeted photodynamic therapy....
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PMID: 21600602
PDF is available here.
PDF is available here.
Abstract
Non-steroidal anti-inflammatory drug (NSAID) intake is associated with high prevalence of gastrointestinal or cardiovascular adverse effects. All efforts to develop NSAIDs that spare the gastrointestinal tract and the cardiovasculature are still far from achieving a breakthrough. In...
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PMID: 21553931
PDF is available here.
PDF is available here.
Abstract
In vitro embryo production (IVP) suffers from excessive developmental failure. Its inefficiency is linked, in part, to reactive oxygen species (ROS) brought on by high ex vivo oxygen (O(2)) tensions. To further delineate the effects of ROS on IVP, the intracellular ROS levels of early bovine embryos...
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PMID: 21557923
PDF is available here.
PDF is available here.
Abstract
We investigated whether paracrine signalling between the bovine oocyte and cumulus cells is altered during the course of in vitro maturation (IVM). Bovine COCs were cocultured with denuded oocytes or treated with specific oocyte-secreted factors, namely recombinant bone morphogenetic protein (BMP)-15...
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PMID: 21557924
PDF is available here.
PDF is available here.
Clinical Cancer Research (17)9 2011
Abstract
Our findings warrant further investigation of the combination of farnesyltransferase and Akt inhibitors. Clin Cancer Res; 17(9); 2852-62. ©2011 AACR....
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PMID: 21536547
PDF is available here.
PDF is available here.
médecine/sciences (27)5 2011
Abstract
Sepsis is defined as a systemic response to infection, characterized by an intense inflammatory response linked to coagulation activation and fibrinolysis inhibition, two processes which are intimately associated. In a field where mortality remains very high, administration of activated protein C, a...
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PMID: 21609671
PDF is available here.
PDF is available here.
Xenobiotica (41)5 2011
Abstract
We describe the adaptation of a modified replicon system for a high-throughput screening (HTS) in anti-HCV drug discovery. In this system, the antiviral activity and cytotoxicity of any experimental compound are measured from a single well. This duplex measurement greatly increases the efficiency of...
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PMID: 19009266
PDF is available here.
PDF is available here.
Xenobiotica (41)5 2011
Abstract
We have adapted the HCVpp infection assay with HCVpp harboring a luciferase reporter to a 96-well format and screened a small-molecule compound library to identify inhibitors of HCV entry. Such active viral entry inhibitors have the potential to be first-in-class antiviral drugs that can be incorpor...
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PMID: 19009270
PDF is available here.
PDF is available here.
Abstract
Abstract
A class of compounds with a common thiazolo[3,2-a]pyrimidinone motif has been developed as general inhibitors of Bcl-2 family proteins. The lead compound was originally identified in a random screening of a small compound library using a fluorescence polarization-based competitive bi...
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PMID: 21520420
PDF is available here.
PDF is available here.
Abstract
We examined pharmacological activities of these compounds in vitro (binding studies) and in vivo (MES test). Pharmacological evaluations revealed one of the compounds, 5a, to be a good lead, exhibiting moderate binding at NMDA receptors (IC(50) = 7.86 μM; K(i) = 5.28 μM), MES neuroprotection activ...
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PMID: 21496213
PDF is available here.
PDF is available here.
AANA Journal (79)2 2011
Abstract
Our data suggest that myristicin does not decrease anxiety by modulation of the GABA(A) receptor but may promote anxiogenesis. When myristicin was combined with midazolam, an antagonist-like effect similar to the flumazenil and myristicin combination was exhibited by a decrease in anxiolysis compare...
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PMID: 21560973
PDF is available here.
PDF is available here.
Annales d'Endocrinologie (72)2 2011
Abstract
We developed a small molecule ligand that is a full agonist at TSHR. Importantly for its clinical potential, this agonist elevated serum thyroxine and stimulated thyroidal radioiodide uptake in mice after its absorption from the gastrointestinal tract following oral administration. Graves' disease (...
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PMID: 21511239
PDF is available here.
PDF is available here.
Abstract
We review the genes required for M. tuberculosis persistence and propose a regulatory network for the action of these genes using text mining. This should provide fresh insights into the persistence mechanisms of M. tuberculosis and suggest candidates for new drug targets and immune intervention....
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PMID: 21267668
PDF is available here.
PDF is available here.
Abstract
Abstract
To develop safe and cheap thrombolytic agents, a fibrinolytic enzyme productive strain of LSSE-62 was isolated from Chinese soybean paste. This strain was identified as Bacillus amyloliquefaciens by 16S rDNA sequence analysis. Nucleotide and amino acid sequence analysis showed that this fibrinolytic...
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PMID: 21391672
PDF is available here.
PDF is available here.
Abstract
Further pediatric development of PG11047 will require better defining a target population and identifying combinations for which there is a tumor-selective cytotoxic effect. The regression observed for an ependymoma xenograft and the exquisite sensitivity of some Ewing sarcoma cell lines to the anti...
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PMID: 21360650
PDF is available here.
PDF is available here.
Abstract
Heat shock protein 90 (Hsp90) is a significant target in the development of rational cancer therapy, due to its role at the crossroads of multiple signaling pathways associated with cell proliferation and viability. Here, a novel series of Hsp90 inhibitors containing a quinolein-2-...
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PMID: 21374821
PDF is available here.
PDF is available here.
Abstract
Tumors with mutations in the gene encoding the serine-threonine protein kinase BRAF are dependent on the MAPK signaling pathway for their growth, what offers an opportunity to test oncogene-targeted therapy. Mutations at the position V600 of BRAF were described in approximately 8% of...
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PMID: 21426297
PDF is available here.
PDF is available here.
Investigacion clinica (52)1 2011
Abstract
We studied the effect of montelukast on the cellular inflammatory infiltrate in a model of murine arthritis induced by sodium monourate crystals (SMU), using a subcutaneous air cavity (air pouch) in BALB/c mice. Seven groups of BALB/c mice (n = 4) were distributed into five experimental groups and t...
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PMID: 21612136
PDF is available here.
PDF is available here.
Abstract
Therapeutic angiogenesis is a novel treatment for ischemic stroke, and vascular endothelial growth factor (VEGF) is a key angiogenic and neuroprotective pharmacological candidate for therapy. However, the greatest challenge of preclinical studies is demonstrating that VEGF-based ther...
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PMID: 20874695
PDF is available here.
PDF is available here.
Abstract
The proteasome has emerged as an important clinically relevant target for the treatment of hematologic malignancies. Since the Food and Drug Administration approved the first-in-class proteasome inhibitor bortezomib (Velcade) for the treatment of relapsed/refractory multiple myeloma...
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PMID: 21247382
PDF is available here.
PDF is available here.
Abstract
We present pharmacological studies on Ca(v)3.1 T-type channels using automated patch-clamp. The IC(50) values obtained from automated patch-clamp and conventional one showed a good correlation (correlation coefficient of 0.82), suggesting that the automated patch-clamp is an efficient and reliable m...
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PMID: 21460418
PDF is available here.
PDF is available here.
Abstract
Our results point out the antiprotozoal potential of the Amaryllidaceae species against T. vaginalis. This parasite causes trichomonosis, the most prevalent nonviral sexually transmitted diseases (STD) worldwide and a public health problem that requires new therapeutic alternatives as well bioactive...
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PMID: 21308614
PDF is available here.
PDF is available here.
Abstract
The chemical investigation of the twigs of Morus mesozygia resulted in the isolation of three new prenylated 2-arylbenzofurans, named moracin KM, LM, and SC (1-3), nine known 2-arylbenzofurans (4-12), and two known flavonoids (13-14). The structures of the new compounds were established as [2'',3'':6...
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PMID: 21308616
PDF is available here.
PDF is available here.
Abstract
We screened extracts of a propolis sample from Algeria with the aim to isolate compounds able to selectively inhibit this enzyme. A butanolic extract (B (3)) of the investigated propolis sample was found to potently inhibit MMP-3 activity (IC (50) = 0.15 ± 0.03 µg/mL), with no or only weak activit...
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PMID: 21305446
PDF is available here.
PDF is available here.
Abstract
We studied the interaction of [6]-gingerol, [8]-gingerol, [10]-gingerol (racemates), and [6]-shogaol with guinea pig M (3) receptors, guinea pig 5-HT (3) receptors, and rat 5-HT (4) receptors. In whole segments of guinea pig ileum (bioassay for contractile M (3) receptors), [6]-gingerol, [8]-gingero...
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PMID: 21305447
PDF is available here.
PDF is available here.
Abstract
These results suggest that TCE is a potential agent for alleviating diabetic complications....
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PMID: 21308613
PDF is available here.
PDF is available here.
Abstract
Mouse models for Huntington's Disease (HD) and HD patients demonstrate motor and behavioral dysfunctions, such as progressive loss of coordination and memory, and share similar transcriptional profiles and striatal neuron atrophy. Clear differences between the mouse and human disease...
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PMID: 21315254
PDF is available here.
PDF is available here.
Abstract
We describe the development and optimisation of a novel series of PTR1 inhibitors, based on benzo[d]imidazol-2-amine derivatives. Data are reported on 33 compounds. This series was initially discovered by a virtual screening campaign (J. Med. Chem., 2009, 52, 4454). The inhibitors adopted an alterna...
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PMID: 21275054
PDF is available here.
PDF is available here.
Abstract
We demonstrate that 3-bromoacivicin is a CTP synthetase inhibitor three times as potent as its 3-chloro analogue, the natural antibiotic acivicin. Because CTP synthetase was suggested to be a potential drug target in African trypanosomes, the in vitro/in vivo antitrypanosomal activity of 3-bromo...
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PMID: 21275056
PDF is available here.
PDF is available here.
Abstract
We evaluated their ability to inhibit both microbial growth and sortase A, an enzyme that plays a key role in cell wall protein anchoring and virulence in Staphylococcus aureus. Most prenylated flavonoids (7-13) displayed potent inhibitory activity against gram-positive and gram-negative bacteria ex...
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PMID: 21380804
PDF is available here.
PDF is available here.
Abstract
We partially purified the neutral sphingomyelinase2 (nSMase2) and identified the inhibitors, D-lyxophytosphingosine and D-arabino-phytosphingosine, which have an inhibitory effect on nSMase2 in a concentration-dependent manner. A Dixon plot of each phytosphingosines revealed their probable inhibitor...
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PMID: 21380806
PDF is available here.
PDF is available here.
Abstract
A high-performance liquid chromatographic method was developed and validated to determine liquiritin, hesperidin, and glycyrrhizin levels in a traditional Korean medicine, Pyungwi-san (PWS). Reverse-phase chromatography using a C18 column operating at 40oC, and photodiode array detection at 254 nm an...
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PMID: 21380802
PDF is available here.
PDF is available here.
Abstract
A flavanol glycoside, glucodistylin (1) and three polyphenol derivatives, gallate (2), (+)-catechin (3) and (+)-gallocatechin (4) were isolated from an aqueous acetone extract of the bark of Quercus acutissima. Of these compounds, glucodistylin exhibited uncompetitive inhibitory activity against reco...
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PMID: 21380803
PDF is available here.
PDF is available here.
Abstract
We focused our strategy on the allosteric inhibitors capable of targeting the NS2B-NS3pro interface rather than the NS3pro active site. Using virtual ligand screening of the diverse, ∼275,000-compound library and the catalytic domain of the two-component West Nile virus (WNV) NS2B-NS3pro as a rece...
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PMID: 21050032
PDF is available here.
PDF is available here.
Abstract
Fraxinus rhynchophylla showed significant inhibitory activity on adipocyte differentiation in the 3T3-L1 preadipocyte cell line as assessed by measuring fat accumulation using Oil Red O staining. Further fractionation led to the isolation of two secoiridoids, oleuropein and hydroxyframoside B. Hydrox...
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PMID: 21294077
PDF is available here.
PDF is available here.
Biochimica et Biophysica Acta (1810)2 2011
Abstract
Defects of the CLN3 gene on chromosome 16p12.1 lead to the juvenile form of neuronal ceroid-lipofuscinosis (JNCL, Batten Disease), the most common recessive inherited neurodegenerative disorder in children. Dysregulation of intracellular calcium homeostasis in the absence of a functional CLN3 protein...
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PMID: 20933060
PDF is available here.
PDF is available here.
Clinical Cancer Research (17)10 2011
Abstract
To evaluate 2-deoxy-2-[(18)F]fluoro-d-glucose positron emission tomography imaging ((18)FDG-PET) as a predictive, noninvasive, pharmacodynamic (PD) biomarker of response following administration of a small-molecule insulin-like growth factor-1 receptor and insulin receptor (IGF-1R/IR) inhibitor, OSI-...
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PMID: 21257723
PDF is available here.
PDF is available here.
Abstract
We also analyzed its effect on cell proliferation IN VITRO, cytotoxicity, and skin irritation. Different extracts obtained from the aerial parts of A. pichinchensis, topically administrated, were evaluated in a healing model by scalpel-blade incision on the rat. The extracts, at 10 % concentrations,...
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PMID: 21267810
PDF is available here.
PDF is available here.
Abstract
As a continuation of our previous work, which resulted in the identification of a new hit compound as an HIV-1 integrase inhibitor, three novel series of salicylic acid derivatives were synthesized using three versatile and practical synthetic strategies and were assayed for their ca...
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PMID: 21246739
PDF is available here.
PDF is available here.
Clinical Cancer Research (17)2 2011
Abstract
Pancreatic cancer is the fourth leading cause of cancer-related deaths, in which the 5-year survival rate is less than 5%. Current standard of care therapies offer little selectivity and high toxicity. Novel, tumor-selective approaches are desperately needed. Although prior work suggested that β-lap...
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PMID: 21224367
PDF is available here.
PDF is available here.
Abstract
The protein kinase CK2 sustains multiple pro-survival functions in cellular DNA damage response and its level is tightly regulated in normal cells but elevated in cancers. Because CK2 is thus considered as potential therapeutic target, DNA double-strand break (DSB) formation and rejoining, apoptosis...
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PMID: 21310046
PDF is available here.
PDF is available here.
Abstract
We addressed this issue by examining liver response to BBR in diabetic rats, in which hyperglycemia was induced in Sprague-Dawley rats by high fat diet. We observed that BBR decreased fasting glucose significantly. Gluconeogenic genes, Phosphoenolpyruvate carboxykinase (PEPCK) and Glucose-6-phosphat...
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PMID: 21304897
PDF is available here.
PDF is available here.
Abstract
Calcitonin gene-related peptide (CGRP), substance P and nerve growth factor play an important role in inflammatory pain in various somatic pain models but their role in chronic pancreatitis has not been well studied.
The aim of this study was to investigate the effect...
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PMID: 21737902
PDF is available here.
PDF is available here.
Clinical Science (120)2 2011
Abstract
The aim of the present study was to test the effect of sitagliptin and exendin-4 upon metabolic alterations, β-cell mass decrease and hepatic steatosis induced by F (fructose) in rats. Normal adult male Wistar rats received a standard commercial diet without (C) or with 10% (w/v) F in the drinking...
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PMID: 20795946
PDF is available here.
PDF is available here.
Kardiologiia (51)1 2011
Abstract
The aim of the study was to evaluate the efficacy and safety of administered intravenously niferidil in doses 10, 20 and 30 mkg per kg in patients with persistent atrial fibrillation (AF) and flutter (AFL) for pharmacological cardioversion. The study included 30 patients (22 male) with persistent AF...
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PMID: 21626804
PDF is available here.
PDF is available here.
Abstract
Structure-based library design employs both structure-based drug design (SBDD) and combinatorial library design. Combinatorial library design concepts have evolved over the past decade, and this chapter covers several novel aspects of structure-based library design together with successful case stud...
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PMID: 20981524
PDF is available here.
PDF is available here.
Abstract
We present several examples of successful applications of both approaches for virtual screening to illustrate their utility. We suggest that the expert use of both QSAR and pharmacophore models, either independently or in combination, enables users to achieve targeted libraries enriched with experim...
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PMID: 20981521
PDF is available here.
PDF is available here.
Abstract
We present our efforts to implement a multi-objective optimization method, MEGALib, custom-designed to the library design problem. The method exploits existing knowledge, e.g. from previous biological screening experiments, to identify and profile molecular fragments used subsequently to design comp...
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PMID: 20981518
PDF is available here.
PDF is available here.