The endothelium-derived relaxing factor (EDRF), now known to be nitric oxide (NO) is generated in the vascular endothelium by nitric oxide synthase (NOS). (justia.com)
Once expressed this inducible nitric oxide synthase (hereinafter "iNOS") generates NO continuously for long periods. (justia.com)
This study establishes the biochemical function of LACC1 in humans/mice and its role in bridging inducible nitric oxide synthase and polyamine metabolism in inflammatory macrophages. (yale.edu)
oxidoreductase acting on paired donors, incorporating 1 atom of oxygen, with NADH or NADPH as one donor) inhibitor that interferes with the action of nitric oxide synthase (EC 1.14.13.39). (ebi.ac.uk)
Enzyme6
This enzyme belongs to the family of ligases, specifically those forming carbon-nitrogen bonds as acid-D-ammonia (or amine) ligases (amide synthases). (wikipedia.org)
So far a relatively unexplored target is the cell wall enzyme β-ketoacyl-ACP-synthase "KasA", which plays a crucial role in maintaining the membrane impermeability and hence the cell ability to resist to With 9.6 million new cases and 1.5 million deaths in 2014, tuberculosis (TB) is alongside with AIDS the most deadly infection. (uni-wuerzburg.de)
So far a relatively unexplored target is the cell wall enzyme β-ketoacyl-ACP-synthase "KasA", which plays a crucial role in maintaining the membrane impermeability and hence the cell ability to resist to the immune response and drug therapy. (uni-wuerzburg.de)
KasA is a key enzyme in the fatty acid synthase "FAS-II" elongation cycle, responsible for the extension of the growing acyl chain within the biosynthesis of precursors for the most hydrophobic constituents of the cell wall - mycolic acids. (uni-wuerzburg.de)
The identification of EDRF as NO has coincided with the discovery of a biochemical pathway by which NO is synthesized from the amino acid L-arginine by the enzyme NO synthase. (justia.com)
Imidazolinones, pyrimidinylthiobenzoates, sulfonylaminocarbonyltriazolinones, sulfonylureas, and triazolopyrimidines are herbicides that inhibit acetolactate synthase (ALS), also called acetohydroxyacid synthase (AHAS), a key enzyme in the biosynthesis of the branched-chain amino acids isoleucine, leucine, and valine (LaRossa and Schloss 1984). (weedscience.com)
Inhibitor2
Design of the novel KasA inhibitors, performed in the research group of Prof. Sotriffer by C. Topf and B. Schaefer, was based on the recently published crystal structure of KasA in complex with its known inhibitor thiolactomycin (TLM). (uni-wuerzburg.de)
Use of such a non-selective NO synthase inhibitor requires that great care be taken in order to avoid the potentially serious consequences of over-inhibition of the constitutive NO-synthase including hypertension and possible thrombosis and tissue damage. (justia.com)
Polyketide synthase2
Indanomycin is biosynthesized by a hybrid nonribosomal peptide synthase/polyketide synthase (NRPS/PKS) followed by a number of `tailoring' steps to form the two ring systems that are present in the mature product. (iucr.org)
Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. (inra.fr)
Inhibitors2
A novel series of nNOS inhibitors with an amidinothiophene-hydroxypiperidine scaffold was designed based on X-ray structures and in - silico models. (rsc.org)
Thus, while non-selective NO synthase inhibitors have therapeutic utility provided that appropriate precautions are taken, NO synthase inhibitors which are selective in the sense that they inhibit the inducible NO synthase to a considerably greater extent than the constitutive isoforms of NO synthase would be of even greater therapeutic benefit and easier to use (S. Moncada and E. Higgs, FASEB J., 9, 1319-1330, 1995). (justia.com)
Synthetase1
4-methyleneglutamine synthetase: a new amide synthetase present in germinating peanuts" (PDF). (wikipedia.org)
EPSP2
Glycines (glyphosate) are herbicides that inhibit 5-enolpyruvylshikimate-3-phosphate (EPSP) synthase (Amrhein 1980) which produces EPSP from shikimate-3-phosphate and phosphoenolpyruvate in the shikimic acid pathway. (weedscience.com)
Although plant death apparently results from events occurring in response to EPSP synthase inhibition, the actual sequence of phytotoxic processes is unclear. (weedscience.com)
Amine1
Compounds with a linear aliphatic amine linker demonstrated a superior property over those with a sulfonamide or an amide -like linker. (rsc.org)
Inhibition1
Catalyst decomposition can be observed by NMR methods, but RPKA methods reveal that product inhibition is operative, where tertiary amides are more inhibitory than secondary amides. (imperial.ac.uk)
Metabolism1
Drosophila melanogaster as a model system to study long chain fatty acid amide metabolism. (bu.edu)
Hydrolysis2
Catalysis of the ligation of an acid to ammonia (NH3) or an amide via a carbon-nitrogen bond, with the concomitant hydrolysis of the diphosphate bond in ATP or a similar triphosphate. (cathdb.info)
The degradation of OTA to non-toxic or less toxic OTα via the hydrolysis of the amide bond is the most important OTA biodegradation mechanism. (frontiersin.org)
Fatty1
after reuptake, AEA is hydrolyzed by fatty acid amide hydrolase (FAAH), and 2-AG by monoacylglycerol lipase (MAGL). (irjournal.org)
Therapeutic1
A longstanding effort to do so is by exploiting protein structures to predict new reagents and therapeutic leads (structure-based ligand discovery). (ucsf.edu)
Biosynthesis1
Impairment of thymidylate (dTMP) biosynthesis severely diminishes the viability of parasitic protozoa and the absence of enzymatic activities specifically involved in the formation of dTMP (e.g. dUTPase, thymidylate synthase, dihydrofolate reductase or thymidine kinase) results in decreased deoxythymidine triphosphate (dTTP) levels and the so-called thymineless death. (eurekaselect.com)
Enzymes2
As of late 2007, two structures have been solved for this class of enzymes, with PDB accession codes 11AS and 12AS. (wikipedia.org)
Natural products classed as polyketides, nonribosomal peptides and hybrids of both are often biosynthesized by giant, complex enzymes known as polyketide synthases (PKS) and nonribosomal peptide synthetases (NRPS). (iucr.org)
Compounds3
Regarding the biological results of the chromone-based compounds, similar structure-activity correlations could be drawn from the binding assay and the whole cell activity testing on M. tuberculosis. (uni-wuerzburg.de)
Virtual screening approaches can roughly be divided into target structure-based screening (often referred to as docking) and screening using active compounds as templates (ligand-based virtual screening). (benthamscience.com)
A class of organic compounds containing a ring structure made up of more than one kind of atom, usually carbon plus another atom. (lookformedical.com)
Mechanism1
Tóth, J. Keeping uracil out of DNA: physiological role, structure and catalytic mechanism of dUTPases. (eurekaselect.com)
Regulation1
Our lab focuses on investigating the structure, function, and regulation of proteins involved in cell signaling, epigenetics, and gene regulation. (bu.edu)
Derivatives1
Precise structural data have been obtained from the solved crystal structures of three chromone derivatives: the screening hit GS-71 (3b), its trimethylammonium salt (18) and 6-nitro-substituted N-benzyl-N-methyl-chromone-2-carboxamide (9i). (uni-wuerzburg.de)
Activity2
The relationship between the chemical structure of a compound and its biological or pharmacological activity. (lookformedical.com)
In stationary phase, cardiolipin synthase activity has been observed to increase approximately 10-fold in the Gram-negative model organism Escherichia coli , suggesting CL is an essential membrane component to cope with starvation 4 . (nature.com)
Complex2
Ureas and amides are herbicides that inhibit photosynthesis by binding to the Q B -binding niche on the D1 protein of the photosystem II complex in chloroplast thylakoid membranes. (weedscience.com)
As an example of one of the complex transformations on this pathway, the figure below shows the structure of the pyrimidine synthase catalyzing the complex rearrangement of aminoimidazole ribotide (left) to the thiamin pyrimidine (right). (tamu.edu)
Glycan3
Based on the ganglio GSL series, gangliosides are synthesized, where sialic acids are linked to the glycan structure to produce negatively charged GSLs. (springer.com)
Of note, with these extraction procedures, GSLs are categorized by their glycan structure, whereas the lipid tails are not determined (Fahy et al. (springer.com)
Glycan preparation The majority of CMP-sialic acid synthase (NmCSS) and 2,3-sialyltransferase 1 mutant E271F/R313Y from (PmST1m) or 2,6-sialyltransferase from (Pd2,6ST). (neighborhoodhousecharterschool.org)
Amino2
Since the most of the products possessed a very low solubility in the aqueous buffer medium used in biological assays, polar groups (nitro, succinamidyl and trimethyl-amino substituent in position 6 of the chromone ring or hydroxyl group on the benzene ring in the amide part have been inserted to the molecule. (uni-wuerzburg.de)
A class of amino acids characterized by a closed ring structure. (lookformedical.com)
Ligands2
Developing computational methods to relate receptors by the similarity of their ligands, rather than by protein sequence or structure. (ucsf.edu)
Zinc binding to the peptide replica and analogs to residues 93-115 of horse liver alcohol dehydrogenase (ADH) was examined by competition of the peptides and the chromophoric chelator 4-(2- pyridylazo)resorcinol for zinc and X-ray absorption fine structure analysis of the zinc ligands. (researchgate.net)
Chemical1
The chemical structure of 90% of mammalian GSLs is based on glucosyl ceramide, whereas galactosyl ceramide serves as a precursor for the remainder. (springer.com)
The current Natural Products Library (NPL) at Scripps Research's Natural Product Discovery Center consists of: (i) purified natural products with fully assigned structures, (b) MPLC (on C-18 semipreparative column) fractions, and (c) crude extracts. (ufl.edu)
Molecular1
This truncated variant allows consistent and easy crystallization, but importantly the structure was used as a search model in molecular replacement, allowing the full-length IdmH structure to be determined to 2.7 Å resolution. (iucr.org)
Cell2
This paper identifies new N-acyl-amide metabolites encoded by Neisseria meningitidis and by mammals and evaluates their human cell immunological responses and sphingosine receptor signaling. (yale.edu)
These cell types were first described as huge brick-like structures occupying much of the inner nuclear layer in the fish retina (27, 28). (org.es)
Crystal2
Here, the crystal structure of a selenomethionine-labelled truncated form of IdmH (IdmH- Δ 99-107) was solved using single-wavelength anomalous dispersion (SAD) phasing. (iucr.org)
Tests the new methods in well-controlled systems, determining x-ray crystal structures and measuring binding thermodynamics. (ucsf.edu)
Flexible1
In both cases, the introduction of a nitro group to position 6 of the chromone ring and the presence of a flexible substituent in the amide part showed a positive effect. (uni-wuerzburg.de)
Procedures1
Two simple workup procedures that provide the pure amide product without the need for further purification have been developed. (imperial.ac.uk)
Model1
Due to autofluorescence, detected in most of the products, this model structure was not further varied. (uni-wuerzburg.de)
Systems1
Both systems consist of a range of domains which incorporate a number of starter and extender units to build a linear structure. (iucr.org)
Analysis1
Product-containing fractions were pooled and lyophilized for mass spectrum (MS) and NMR analysis to confirm structures. (neighborhoodhousecharterschool.org)
Learn1
You will learn how to structure your curriculum and build an engaging classroom. (nyas.org)
Virtual2
First, a virtual screening hit, chromone-2-carboxamide derivative GS-71, was modified in the amide part. (uni-wuerzburg.de)
The latter virtual screening hit, a pyrimidinone derivative VS-8 was synthesized and the structure was modified by substitution in positions 2, 4, 5 and 6 of the pyrimidine ring. (uni-wuerzburg.de)