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Nir London et al.
Nature chemical biology, 10(12), 1066-1072 (2014-10-27)
Chemical probes that form a covalent bond with a protein target often show enhanced selectivity, potency and utility for biological studies. Despite these advantages, protein-reactive compounds are usually avoided in high-throughput screening campaigns. Here we describe a general method (DOCKovalent)
Nicholas Kwiatkowski et al.
Nature, 511(7511), 616-620 (2014-07-22)
Tumour oncogenes include transcription factors that co-opt the general transcriptional machinery to sustain the oncogenic state, but direct pharmacological inhibition of transcription factors has so far proven difficult. However, the transcriptional machinery contains various enzymatic cofactors that can be targeted
Voin Petrović et al.
Journal of inorganic biochemistry, 140, 228-235 (2014-09-01)
Na(+)/K(+)-ATPase is in charge of maintaining the ionic and osmotic intracellular balance by using ATP as an energy source to drive excess Na(+) ions out of the cell in exchange for K(+) ions. We explored whether three representative cytotoxic gold(III)
S Martín et al.
International journal for parasitology, 45(13), 831-840 (2015-08-05)
The limitations associated with the use of anthelmintic drugs in the control of gastrotintestinal nematodosis, such as the emergence of anthelmintic resistance, have stimulated the study of the immunological control of many parasites. In the case of Haemonchus contortus, several
Zrinka Karačić et al.
Biological chemistry, 393(12), 1523-1532 (2013-05-15)
Human dipeptidyl peptidase III (DPP III) is a member of the metallopeptidase family M49, involved in protein metabolism and oxidative stress response. DPPIII crystal structure shows the two lobe-like domains separated by a wide cleft. The human enzyme has a
Guangshuo Zhu et al.
Hypertension (Dallas, Tex. : 1979), 65(2), 385-392 (2014-12-03)
Nitroxyl (HNO), the reduced and protonated form of nitric oxide (NO·), confers unique physiological effects including vasorelaxation and enhanced cardiac contractility. These features have spawned current pharmaceutical development of HNO donors as heart failure therapeutics. HNO interacts with selective redox
Yipin Wu et al.
American journal of physiology. Regulatory, integrative and comparative physiology, 309(7), R747-R756 (2015-08-01)
Inwardly rectifying potassium channels play essential roles in renal physiology across phyla. Barium-sensitive K(+) conductances are found on the basolateral membrane of a variety of insect Malpighian (renal) tubules, including Drosophila melanogaster. We found that barium decreases the lumen-positive transepithelial
S Peter et al.
Journal of physiology and pharmacology : an official journal of the Polish Physiological Society, 66(3), 449-462 (2015-06-19)
After parturition, uterine bacterial infections lead to inflammatory processes such as subclinical/clinical endometritis with high prevalence in dairy cows. Endometrial epithelial cells participate in this immune response with the production of pro-inflammatory factors. The objective of the present study was
Peng Ye et al.
Molecular and cellular biology, 34(18), 3421-3434 (2014-07-09)
The ubiquitin-proteasome pathway degrades ubiquitinated proteins to remove damaged or misfolded protein and thus plays an important role in the maintenance of many important cellular processes. Because the pathway is also crucial for tumor cell growth and survival, proteasome inhibition
Jie Li et al.
Toxicological sciences : an official journal of the Society of Toxicology, 143(1), 196-208 (2014-10-22)
Excess accumulation of endogenous all-trans-retinal (atRAL) contributes to degeneration of the retinal pigment epithelium (RPE) and photoreceptor cells, and plays a role in the etiologies of age-related macular degeneration (AMD) and Stargardt's disease. In this study, we reveal that human
Kolsoom Parvaneh et al.
BioMed research international, 2015, 897639-897639 (2015-09-15)
Probiotics are live microorganisms that exert beneficial effects on the host, when administered in adequate amounts. Mostly, probiotics affect the gastrointestinal (GI) tract of the host and alter the composition of gut microbiota. Nowadays, the incidence of hip fractures due
R Janáky et al.
Neurochemical research, 25(9-10), 1397-1405 (2000-11-04)
We review here the possible mechanisms of neuronal degeneration caused by L-cysteine, an odd excitotoxin. L-Cysteine lacks the omega carboxyl group required for excitotoxic actions via excitatory amino acid receptors, yet it evokes N-methyl-D-aspartate (NMDA) -like excitotoxic neuronal death and
Mathieu Taveau et al.
Molecular and cellular biology, 23(24), 9127-9135 (2003-12-04)
Calpain 3 (Capn3) is known as the skeletal muscle-specific member of the calpains, a family of intracellular nonlysosomal cysteine proteases. This enigmatic protease has many unique features among the calpain family and, importantly, mutations in Capn3 have been shown to
Melissa A Badding et al.
PloS one, 9(6), e101310-e101310 (2014-07-01)
Welding processes that generate fumes containing toxic metals, such as hexavalent chromium (Cr(VI)), manganese (Mn), and nickel (Ni), have been implicated in lung injury, inflammation, and lung tumor promotion in animal models. While federal regulations have reduced permissible worker exposure
Mahesh Kumar Verma et al.
SpringerPlus, 3, 251-251 (2014-06-18)
Apart from elevated glucose, triglyceride and cholesterol, elevated levels of serum free-fatty acid (FFA) are observed in diabetic patients. Increased FFA load can cause multiple dysregulation which are collectively known as lipotoxicity. Impacts of FFA induced lipotoxicity were evaluated on
Alok Pandey et al.
The Journal of biological chemistry, 288(52), 36773-36786 (2013-11-13)
For iron-sulfur (Fe-S) cluster synthesis in mitochondria, the sulfur is derived from the amino acid cysteine by the cysteine desulfurase activity of Nfs1. The enzyme binds the substrate cysteine in the pyridoxal phosphate-containing site, and a persulfide is formed on
S Sofia M Rodrigues et al.
Chemphyschem : a European journal of chemical physics and physical chemistry, 16(9), 1880-1888 (2015-04-25)
Immobilization of quantum dots (QDs) onto solid supports could improve their applicability in the development of sensing platforms and solid-phase reactors by allowing the implementation of reusable surfaces and the execution of repetitive procedures. As the reactivity of QDs relies
Joanna Czarnecka et al.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, 822(1-2), 85-90 (2005-07-05)
New method of qualitative and quantitative analysis of nucleotides in human cerebrospinal fluid (CSF), based on the combination of extraction of purines and pyrimidines to the solid phase (SPE) and high-performance liquid chromatography (HPLC), was proposed. Use of SPE and
Annelies Geirnaert et al.
FEMS microbiology ecology, 91(6) (2015-05-23)
Butyrate-producing bacteria are promising probiotic candidates to target microbial dysbiosis in gastrointestinal disorders like inflammatory bowel diseases. Butyricicoccus pullicaecorum 25-3(T), a butyrate-producing clostridial cluster IV strain, is such a candidate. Little is known about its abundance in the colon microbiota
Anouk A J Hamers et al.
PloS one, 10(8), e0133598-e0133598 (2015-08-05)
Nuclear receptor Nur77, also referred to as NR4A1 or TR3, plays an important role in innate and adaptive immunity. Nur77 is crucial in regulating the T helper 1/regulatory T-cell balance, is expressed in macrophages and drives M2 macrophage polarization. In
Nazmin Bithi et al.
Nature communications, 12(1), 1745-1745 (2021-03-21)
Hydrogen sulfide (H2S) is a cytoprotective redox-active metabolite that signals through protein persulfidation (R-SSnH). Despite the known importance of persulfidation, tissue-specific persulfidome profiles and their associated functions are not well characterized, specifically under conditions and interventions known to modulate H2S
Charles Ansong et al.
Proceedings of the National Academy of Sciences of the United States of America, 110(25), 10153-10158 (2013-05-31)
Characterization of the mature protein complement in cells is crucial for a better understanding of cellular processes on a systems-wide scale. Toward this end, we used single-dimension ultra-high-pressure liquid chromatography mass spectrometry to investigate the comprehensive "intact" proteome of the
Valery Kh Akparov et al.
The FEBS journal, 282(7), 1214-1224 (2015-01-27)
The crystal structures of carboxypeptidase T (CpT) complexes with phenylalanine and arginine substrate analogs - benzylsuccinic acid and (2-guanidinoethylmercapto)succinic acid - were determined by the molecular replacement method at resolutions of 1.57 Å and 1.62 Å to clarify the broad
Yoshio Takeuchi et al.
Bioorganic & medicinal chemistry letters, 18(23), 6202-6205 (2008-10-28)
In order to investigate crystallographically the mechanism of inhibition of cysteine protease by alpha-methyl-gamma,gamma-diphenylallenecarboxylic acid ethyl ester 3, a cysteine protease inhibitor having in vivo stability, we synthesized N-(alpha-methyl-gamma,gamma-diphenylallenecarbonyl)-L-phenylalanine ethyl ester 4. Reaction of 4 with thiophenol, the SH group
Hans F N Kvitvang et al.
Analytical chemistry, 83(7), 2705-2711 (2011-03-11)
Metabolite profiling methods are important tools for measurement of metabolite pools in biological systems. While most metabolite profiling methods report relative intensities or depend on a few internal standards representing all metabolites, the ultimate requirement for a quantitative description of
Tanzila Mukhtar et al.
Scientific reports, 10(1), 4625-4625 (2020-03-15)
Neural stem cells (NSCs) generate neurons of the cerebral cortex with distinct morphologies and functions. How specific neuron production, differentiation and migration are orchestrated is unclear. Hippo signaling regulates gene expression through Tead transcription factors (TFs). We show that Hippo
Roomina Jahroomishirazi et al.
Cells, tissues, organs, 200(2), 141-152 (2015-05-23)
Mesenchymal stem cells (MSCs) have great promise in the field of regenerative medicine due to their differentiation potential into several lineages. Besides the bone marrow, MSCs can be obtained from the dermis, which represents a large stem cell reservoir in
Zhi-Zhun Mo et al.
BMC complementary and alternative medicine, 15, 238-238 (2015-07-17)
The inhibitory effect of andrographolide sodium bisulphite (ASB) on jack bean urease (JBU) and Helicobacter pylori urease (HPU) was performed to elucidate the inhibitory potency, kinetics and mechanism of inhibition in 20 mM phosphate buffer, pH 7.0, 2 mM EDTA
Tiago Sousa et al.
Journal of pharmaceutical sciences, 103(10), 3171-3175 (2014-08-06)
Azo-bonded prodrugs of 5-aminosalicylic acid (mesalazine)-sulfasalazine, balsalazide, and olsalazine, which are used in the treatment of ulcerative colitis, rely on colonic bacteria to cleave the azo bond and liberate the active drug in the large intestine. The aim of this
Assuero F Garcia et al.
Biochimica et biophysica acta, 1844(6), 1094-1103 (2014-03-19)
In eukaryotes, there are still steps of the vitamin B1 biosynthetic pathway not completely understood. In Arabidopsis thaliana, THI1 protein has been associated with the synthesis of the thiazole ring, a finding supported by the identification of a thiamine pyrophosphate
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