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FLAAS

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Douglas S Williamson et al.
Journal of medicinal chemistry, 52(6), 1510-1513 (2009-03-05)
The design and synthesis of novel adenosine-derived inhibitors of HSP70, guided by modeling and X-ray crystallographic structures of these compounds in complex with HSC70/BAG-1, is described. Examples exhibited submicromolar affinity for HSP70, were highly selective over HSP90, and some displayed...
James G Douglass et al.
Journal of medicinal chemistry, 51(4), 1007-1025 (2008-02-01)
Platelet P2Y12 receptors play a central role in the regulation of platelet function and inhibition of this receptor by treatment with drugs such as clopidogrel results in a reduction of atherothrombotic events. We discovered that modification of natural and synthetic...
Nicolas Desroy et al.
Bioorganic & medicinal chemistry, 17(3), 1276-1289 (2009-01-07)
Gram-negative bacteria lacking heptoses in their lipopolysaccharide (LPS) display attenuated virulence and increased sensitivity to human serum and to some antibiotics. Thus inhibition of bacterial heptose synthesis represents an attractive target for the development of new antibacterial agents. HldE is...
Alessio Ciulli et al.
Journal of medicinal chemistry, 49(16), 4992-5000 (2006-08-04)
Mapping interactions at protein-ligand binding sites is an important aspect of understanding many biological reactions and a key part of drug design. In this paper, we have used a fragment-based approach to probe "hot spots" at the cofactor-binding site of...
ATPases as drug targets: insights from heat shock proteins 70 and 90.
Andrew J Massey
Journal of medicinal chemistry, 53(20), 7280-7286 (2010-07-09)
Katia Mellal et al.
Scientific reports, 9(1), 12903-12903 (2019-09-11)
In subretinal inflammation, activated mononuclear phagocytes (MP) play a key role in the progression of retinopathies. Little is known about the mechanism involved in the loss of photoreceptors leading to vision impairment. Studying retinal damage induced by photo-oxidative stress, we...
Rui Xiong et al.
Toxicology and applied pharmacology, 280(2), 285-295 (2014-08-26)
Para-quinones such as 1,4-Benzoquinone (BQ) and menadione (MD) and ortho-quinones including the oxidation products of catecholamines, are derived from xenobiotics as well as endogenous molecules. The effects of quinones on major protein handling systems in cells; the 20/26S proteasome, the...
Leilei Zhang et al.
Journal of medicinal chemistry, 52(14), 4419-4428 (2009-06-18)
In this paper, a peptide substrate (Pep8) of TSSK1 is identified. Using Pep8 as a substrate, two homogeneous and efficient assays for TSSK1 inhibitors screening have been developed, including luminescent kinase assay and LC-MS-based high-throughput assay. Two classes of compounds...
Francisco J Adrián et al.
Nature chemical biology, 2(2), 95-102 (2006-01-18)
Chronic myelogenous leukemia (CML) is a myeloproliferative disorder characterized at the molecular level by the expression of Bcr-abl, a 210-kDa fusion protein with deregulated tyrosine kinase activity. Encouraged by the clinical validation of Bcr-abl as the target for the treatment...
Xi-Lan Tang et al.
Inflammation, 38(1), 94-101 (2014-09-06)
Inflammatory response is an important mechanism in the pathogenesis of cardiovascular diseases. Cardiac fibroblasts play a crucial role in cardiac inflammation and might become a potential therapeutic target in cardiovascular diseases. Kaempferol, a flavonoid commonly existing in many edible fruits...
Lizhen Qiao et al.
Journal of chromatography. A, 1360, 240-247 (2014-08-19)
Glucaminium-based ionic liquids are a new class of recently developed ionic liquids and prepared by functionalizing the amine group of N-methyl-d-glucamine, which renders them good hydrophilicity due to the presence of the glucose structure and charged quaternary ammonium group. In...
Yanhui Yang et al.
Bioorganic & medicinal chemistry letters, 21(13), 3943-3946 (2011-06-07)
Mycobacterium tuberculosis pantothenate synthetase is a potential anti-tuberculosis target, and a high-throughput screening system was previously developed to identify its inhibitors. Using a similar system, we screened a small library of compounds and identified actinomycin D (ActD) as a weak...
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Rui Xiong et al.
Molecular pharmacology, 88(6), 1045-1054 (2015-09-26)
A potential cause of neurodegenerative diseases, including Parkinson's disease (PD), is protein misfolding and aggregation that in turn leads to neurotoxicity. Targeting Hsp90 is an attractive strategy to halt neurodegenerative diseases, and benzoquinone ansamycin (BQA) Hsp90 inhibitors such as geldanamycin...
Shay Eliahu et al.
Journal of medicinal chemistry, 53(6), 2472-2481 (2010-02-24)
Dinucleoside polyphosphates exert their physiological effects via P2 receptors (P2Rs). They are attractive drug candidates, as they offer better stability and specificity compared to nucleotides, the most common P2 receptor ligands. The activation of pancreatic P2Y receptors by nucleotides increases...
Els L R Swennen et al.
European journal of immunology, 35(3), 852-858 (2005-02-19)
In vitro studies suggest that extracellular nucleotides and nucleosides may be important regulators of inflammatory and immune responses. Most studies with adenosine 5'-triphosphate (ATP) have been performed in cell lines, which are remote from the human situation. The purpose of...
Weerachat Sompong et al.
PloS one, 10(6), e0129495-e0129495 (2015-06-09)
Ferulic acid (FA) is the ubiquitous phytochemical phenolic derivative of cinnamic acid. Experimental studies in diabetic models demonstrate that FA possesses multiple mechanisms of action associated with anti-hyperglycemic activity. The mechanism by which FA prevents diabetes-associated vascular damages remains unknown....
Shay E Eliahu et al.
European journal of medicinal chemistry, 44(4), 1525-1536 (2008-09-02)
P2Y nucleotide receptors (P2YRs) are attractive pharmaceutical targets. Most P2YR agonists proposed as drugs consist of a nucleotide scaffold, but their use is limited due to their chemical and enzymatic instabilities. To identify drug candidates, we developed non-hydrolyzable P2YR agonists....
A Hari Kishore et al.
Journal of medicinal chemistry, 51(4), 792-797 (2008-01-25)
Aurora kinases are essential for chromosomal segregation and cell division and thereby important for maintaining the proper genomic integrity. There are three classes of aurora kinases in humans: A, B, and C. Aurora kinase A is frequently overexpressed in various...
Ronald W Sarver et al.
Journal of AOAC International, 104(1), 39-48 (2020-11-30)
Many food recalls are related to the presence of undeclared allergens and microorganisms in food products. To reduce these occurrences, portable diagnostic assay kits are available to quantitate mycotoxins, to detect allergens and gluten in foods and on environmental surfaces...
Takashi Yoshida et al.
Nature chemical biology, 2(11), 596-607 (2006-09-26)
Transient receptor potential (TRP) proteins form plasma-membrane cation channels that act as sensors for diverse cellular stimuli. Here, we report a novel activation mechanism mediated by cysteine S-nitrosylation in TRP channels. Recombinant TRPC1, TRPC4, TRPC5, TRPV1, TRPV3 and TRPV4 of...
Nora Grahl et al.
PLoS pathogens, 11(8), e1005133-e1005133 (2015-09-01)
Candida albicans is both a major fungal pathogen and a member of the commensal human microflora. The morphological switch from yeast to hyphal growth is associated with disease and many environmental factors are known to influence the yeast-to-hyphae switch. The...
Hoseok Choi et al.
Biosensors & bioelectronics, 73, 93-99 (2015-06-09)
We report a simple method for analyzing sequential phosphorylation by protein kinases using fluorescent peptide substrates and microfluidic isoelectric focusing (μIEF) electrophoresis. When a dye-labeled peptide substrate was sequentially phosphorylated by two consecutive protein kinases (mitogen-activated protein kinase (MAPK) and...
Kei Moriyama et al.
Journal of medicinal chemistry, 51(1), 159-166 (2007-12-11)
One of the possible mechanisms of antiviral action of ribavirin (1-beta- d-ribofuranosyl-1,2,4-triazole-3-carboxamide, 1) is the accumulation of mutations in viral genomic RNA. The ambiguous incorporation of 5'-triphosphate of ribavirin (RTP, 8) by a viral RNA-dependent RNA polymerase (RdRp) is a...
Antonia Efstathiou et al.
Bio-protocol, 10(2), e3493-e3493 (2020-01-20)
The identification of small molecules possessing inhibitory activity in vitro, against a given target kinase, is the first step in the drug discovery process. Herein, we describe a non radioactive protocol using luciferase-based ATP assay for the identification of inhibitors...
Maria A Argiriadi et al.
Bioorganic & medicinal chemistry letters, 20(1), 330-333 (2009-11-19)
MK2 is a Ser/Thr kinase of significant interest as an anti-inflammatory drug discovery target. Here we describe the development of in vitro tools for the identification and characterization of MK2 inhibitors, including validation of inhibitor interactions with the crystallography construct...
Randomized clinical trial of adenosine 5?-triphosphate in patients with advanced non-small-cell lung cancer
Agteresch HJ, et al.
Journal of the National Cancer Institute, 92(4), 321-328 (2000)
Denis Fourches et al.
Chemical research in toxicology, 23(1), 171-183 (2009-12-18)
Drug-induced liver injury is one of the main causes of drug attrition. The ability to predict the liver effects of drug candidates from their chemical structures is critical to help guide experimental drug discovery projects toward safer medicines. In this...
Ziyi Yin et al.
Autophagy, 15(7), 1234-1257 (2019-02-20)
Macroautophagy/autophagy is critical for normal appressorium formation and pathogenicity of the rice blast fungus Magnaporthe oryzae, but the molecular base of autophagy linked to pathogenicity remains elusive in this or other pathogenic fungi. We found that MoHat1, a histone acetyltransferase...
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