Fatty Acid Synthesis Inhibitors
Fatty Acid Synthases
Fatty Acid Synthase, Type I
Ribosome Inactivating Proteins, Type 2
Structure of the complex between the antibiotic cerulenin and its target, beta-ketoacyl-acyl carrier protein synthase. (1/220)In the biosynthesis of fatty acids, the beta-ketoacyl-acyl carrier protein (ACP) synthases catalyze chain elongation by the addition of two-carbon units derived from malonyl-ACP to an acyl group bound to either ACP or CoA. The enzyme is a possible drug target for treatment of certain cancers and for tuberculosis. The crystal structure of the complex of the enzyme from Escherichia coli, and the fungal mycotoxin cerulenin reveals that the inhibitor is bound in a hydrophobic pocket formed at the dimer interface. Cerulenin is covalently attached to the active site cysteine through its C2 carbon atom. The fit of the inhibitor to the active site is not optimal, and there is thus room for improvement through structure based design. (+info)
Monounsaturated but not polyunsaturated fatty acids are required for growth of the deep-sea bacterium Photobacterium profundum SS9 at high pressure and low temperature. (2/220)There is considerable evidence correlating the production of increased proportions of membrane unsaturated fatty acids (UFAs) with bacterial growth at low temperatures or high pressures. In order to assess the importance of UFAs to microbial growth under these conditions, the effects of conditions altering UFA levels in the psychrotolerant piezophilic deep-sea bacterium Photobacterium profundum SS9 were investigated. The fatty acids produced by P. profundum SS9 grown at various temperatures and pressures were characterized, and differences in fatty acid composition as a function of phase growth, and between inner and outer membranes, were noted. P. profundum SS9 was found to exhibit enhanced proportions of both monounsaturated (MUFAs) and polyunsaturated (PUFAs) fatty acids when grown at a decreased temperature or elevated pressure. Treatment of cells with cerulenin inhibited MUFA but not PUFA synthesis and led to a decreased growth rate and yield at low temperature and high pressure. In addition, oleic acid-auxotrophic mutants were isolated. One of these mutants, strain EA3, was deficient in the production of MUFAs and was both low-temperature sensitive and high-pressure sensitive in the absence of exogenous 18:1 fatty acid. Another mutant, strain EA2, produced little MUFA but elevated levels of the PUFA species eicosapentaenoic acid (EPA; 20:5n-3). This mutant grew slowly but was not low-temperature sensitive or high-pressure sensitive. Finally, reverse genetics was employed to construct a mutant unable to produce EPA. This mutant, strain EA10, was also not low-temperature sensitive or high-pressure sensitive. The significance of these results to the understanding of the role of UFAs in growth under low-temperature or high-pressure conditions is discussed. (+info)
Acylation stabilizes a protease-resistant conformation of protoporphyrinogen oxidase, the molecular target of diphenyl ether-type herbicides. (3/220)Protein acylation is an important way in which a number of proteins with a variety of functions are modified. The physiological role of the acylation of cellular proteins is still poorly understood. Covalent binding of fatty acids to nonintegral membrane proteins is thought to produce transient or permanent enhancement of the association of the polypeptide chains with biological membranes. In this paper, we investigate the functional role for the palmitoylation of an atypical membrane-bound protein, yeast protoporphyrinogen oxidase, which is the molecular target of diphenyl ether-type herbicides. Palmitoylation stabilizes an active heat- and protease-resistant conformation of the protein. Palmitoylation of protoporphyrinogen oxidase has been demonstrated to occur in vivo both in yeast cells and in a heterologous bacterial expression system, where it may be inhibited by cerulenin leading to the accumulation of degradation products of the protein. The thiol ester linking palmitoleic acid to the polypeptide chain was shown to be sensitive to hydrolysis by hydroxylamine and also by the widely used serine-protease inhibitor phenylmethylsulfonyl fluoride. (+info)
Biosynthesis and elongation of short- and medium-chain-length fatty acids. (4/220)Short- and medium-chain-length fatty acids (FAs) are important constituents of a wide array of natural products. Branched and straight short-chain-length FAs originate from branched chain amino acid metabolism, and serve as primers for elongation in FA synthase-like reactions. However, a recent model proposes that the one-carbon extension reactions that utilize 2-oxo-3-methylbutyric acid in leucine biosynthesis also catalyze a repetitive one-carbon elongation of short-chain primers to medium-chain-length FAs. The existence of such a mechanism would require a novel form of regulation to control carbon flux between amino acid and FA biosynthesis. A critical re-analysis of the data used to support this pathway fails to support the hypothesis for FA elongation by one-carbon extension cycles of alpha-ketoacids. Therefore, we tested the hypothesis experimentally using criteria that distinguish between one- and two-carbon elongation mechanisms: (a) isotopomer patterns in terminal carbon atom pairs of branched and straight FAs resulting from differential labeling with [(13)C]acetate; (b)(13)C]threonine labeling patterns in odd- and even chain length FAs; and (c) differential sensitivity of elongation reactions to inhibition by cerulenin. All three criteria indicated that biosynthesis of medium-chain length FAs is mediated primarily by FA synthase-like reactions. (+info)
Activity of the phosphatidylcholine biosynthetic pathway modulates the distribution of fatty acids into glycerolipids in proliferating cells. (5/220)PtdCho accumulation is a periodic, S phase-specific event that is modulated in part by cell cycle-dependent fluctuations in CTP:phosphocholine cytidylyltransferase (CCT) activity. A supply of fatty acids is essential to generate the diacylglycerol (DG) precursors for phosphatidylcholine (PtdCho) biosynthesis but it is not known whether the DG supply is also coupled to the cell cycle. Although the rate of fatty acid synthesis in a macrophage cell line was dramatically stimulated in response to the growth factor, CSF-1, it was not regulated by the cell cycle. Increased fatty acid synthesis correlated with elevated acetyl-CoA carboxylase (ACC) and fatty acid synthase (FAS) steady-state mRNA levels. Cellular fatty acid synthesis was essential for membrane PL synthesis. Cerulenin inhibition of endogenous fatty acid synthesis also inhibited PtdCho synthesis, which was not relieved by exogenous fatty acids. Inhibition of CCT activity by the addition of lysophosphatidylcholine (lysoPtdCho) or temperature-shift of a conditionally defective CCT diverted newly synthesized DG to the TG pool where it accumulated. Enforced expression of CCT stimulated PtdCho biosynthesis and reduced TG synthesis. Thus, the cellular DG supply did not regulate PtdCho biosynthesis and CCT activity governs the partitioning of DG into either the PL or TG pools, thereby controlling both PtdCho and TG biosynthesis. (+info)
Malonyl-coenzyme-A is a potential mediator of cytotoxicity induced by fatty-acid synthase inhibition in human breast cancer cells and xenografts. (6/220)A biologically aggressive subset of human breast cancers and other malignancies is characterized by elevated fatty-acid synthase (FAS) enzyme expression, elevated fatty acid (FA) synthesis, and selective sensitivity to pharmacological inhibition of FAS activity by cerulenin or the novel compound C75. In this study, inhibition of FA synthesis at the physiologically regulated step of carboxylation of acetyl-CoA to malonyl-CoA by 5-(tetradecyloxy)-2-furoic acid (TOFA) was not cytotoxic to breast cancer cells in clonogenic assays. FAS inhibitors induced a rapid increase in intracellular malonyl-CoA to several fold above control levels, whereas TOFA reduced intracellular malonyl-CoA by 60%. Simultaneous exposure of breast cancer cells to TOFA and an FAS inhibitor resulted in significantly reduced cytotoxicity and apoptosis. Subcutaneous xenografts of MCF7 breast cancer cells in nude mice treated with C75 showed FA synthesis inhibition, apoptosis, and inhibition of tumor growth to less than 1/8 of control volumes, without comparable toxicity in normal tissues. The data suggest that differences in intermediary metabolism render tumor cells susceptible to toxic fluxes in malonyl-CoA, both in vitro and in vivo. (+info)
Specialized fatty acid synthesis in African trypanosomes: myristate for GPI anchors. (7/220)African trypanosomes, the cause of sleeping sickness, need massive amounts of myristate to remodel glycosyl phosphatidylinositol (GPI) anchors on their surface glycoproteins. However, it has been believed that the parasite is unable to synthesize any fatty acids, and myristate is not abundant in the hosts' bloodstreams. Thus, it has been unclear how trypanosomes meet their myristate requirement. Here we found that they could indeed synthesize fatty acids. The synthetic pathway was unique in that the major product, myristate, was preferentially incorporated into GPIs and not into other lipids. The antibiotic thiolactomycin inhibited myristate synthesis and killed the parasite, making this pathway a potential chemotherapeutic target. (+info)
Structural modeling and site-directed mutagenesis of the actinorhodin beta-ketoacyl-acyl carrier protein synthase. (8/220)A three-dimensional model of the Streptomyces coelicolor actinorhodin beta-ketoacyl synthase (Act KS) was constructed based on the X-ray crystal structure of the related Escherichia coli fatty acid synthase condensing enzyme beta-ketoacyl synthase II, revealing a similar catalytic active site organization in these two enzymes. The model was assessed by site-directed mutagenesis of five conserved amino acid residues in Act KS that are in close proximity to the Cys169 active site. Three substitutions completely abrogated polyketide biosynthesis, while two replacements resulted in significant reduction in polyketide production. (3)H-cerulenin labeling of the various Act KS mutant proteins demonstrated that none of the amino acid replacements affected the formation of the active site nucleophile. (+info)
OPUS Würzburg | Development of synthesis pathways and characterization of cerulenin analogues as inhibitors of the fatty acid...
The work deals with the synthesis and characterization of cerulenin analogues as inhibitors of efflux pump mediated resistance of Candida albicans isolates and as inhibitors of the fatty acid synthesis enzyme KasA of Mycobacterium tuberculosis. Cerulenin was chosen as the lead structure, being a substrate of the efflux pumps in Candida albicans on one hand and therefore variations on the structure could lead to a blocking of the efflux pumps as in the case of tetracycline and inhibitor 13-CPTC of the TetB efflux pump. On the other hand, cerulenin is a known inhibitor of the FAS system but inhibition is unselective in type I and II FAS. Therefore, analogues could result in increased selectivity towards the type II FAS system in M. tuberculosis. The first cerulenin derivatives were prepared by coupling 2,3-dihydrofuran to the before synthesized 1-octaniodide, followed by ring opening and oxidation in one step by chromic acid and transfer of the resulting 4-keto acid to amides to give analogues 4a-d, 4e
Cerulenin is a potent inhibitor of antigen processing by antigen-presenting cells. | The Journal of Immunology
Cerulenin is an antibiotic that inhibits eukaryotic lipid and sterol synthesis and blocks lipid modification of proteins. The effect of cerulenin on the ability of accessory cells to present antigen to T cells was investigated. This antibiotic strongly inhibits the ability of accessory cells to present antigen to murine T-T hybrids. This effect is observed for multiple distinct antigens including L-glutamic acid60-L-alanine30-L-tyrosine10, bovine insulin, L-glutamic acid56-L-lysine35-L-phenylalanine9, and ovalbumen. Presentation by both macrophage and B lymphoblastoid cell lines is inhibited. The ability to effectively pulse these cells with antigen is inhibited but not the ability of these same cells to present antigen that they have previously processed. Furthermore, this inhibition is selective as it can occur without significant inhibition of the antigen-presenting cell protein or DNA synthesis. Cerulenin does not inhibit antigen uptake or catabolism as assessed with labeled antigen. By ...
5620 Fatty acid synthase (FAS) is a 250-270 kd cytosolic multifunctional polypeptide required for the conversion of dietary carbohydrates to fatty acids. While high levels of FAS expression compared to normal tissue have been observed in several cancers, including breast, prostate, colon and lung carcinoma, there is little information regarding gliomas. For the first time, we show high levels of FAS expression associated with glioma cell lines. Western blotting revealed higher FAS expression (4-20 fold increase) in U251, U138, NSB-19, and U373 human glioma cell lines and in C6 rat glioma cells compared to normal rat astrocytes. Cerulenin-mediated inhibition of lipid synthesis was determined using 14C labeled acetic acid. After labeling, total lipids were extracted and counted for 14C by scintillation counting. Endogenous fatty acid synthesis in cerulenin-treated glioma cells decreased by 49%, 49.7% and 51.1% at 2 hours in NSB-19, U251, and C6 cells, respectively. Cell cycle analysis, using flow ...
Acetic Acid, Sodium Salt, [2-14C]-, Specific Activity: 45-60mCi (1.66-2.22GBq)/mmol, 1mCi (37MBq) | PerkinElmer
1 mCi quantities of [2-14C]-Acetic Acid, Sodium Salt, Specific Activity: 45-60mCi (1.66-2.22GBq)/mmol are available for your research. Application of [14C]Acetic Acid can be found in: migration in paddy soil-to-rice plant system after breakdown by microorganisms below the plow layer in geological disposal research, effects of cerulenin on the endogenous fatty acid synthetic activity in oral squamous cell carcinoma (OSCC), in vivo incorporation into goldfish liver lipids during ?-hexachlorocyclohexane exposure in aquatic toxicology, etc.. ...
Acetic Acid, Sodium Salt, [1,2-14C]-, 1mCi (37MBq) | PerkinElmer
1 mCi quantities of [1,2-14C]-Acetic Acid, Sodium Salt are available for your research. Application of [14C]Acetic Acid can be found in: migration in paddy soil-to-rice plant system after breakdown by microorganisms below the plow layer in geological disposal research, effects of cerulenin on the endogenous fatty acid synthetic activity in oral squamous cell carcinoma (OSCC), in vivo incorporation into goldfish liver lipids during ?-hexachlorocyclohexane exposure in aquatic toxicology, etc. ...
Proderma Lapte Praf Nan 3 Comfortis x 800gr | Proderma.ro
Proderma.ro, proderma Lapte Praf Nan 3 Comfortis x 800gr|O combinatie unica de ingrediente ce raspunde nevoilor nutritionale speciale pentru dezvoltarea normala a copilului tau.
RCSB PDB - 1OX0: The crystal structure of beta-ketoacyl-[acyl carrier protein] synthase II from Streptococcus...
1OX0: The 1.3-Angstrom-Resolution Crystal Structure of beta-Ketoacyl-Acyl Carrier Protein Synthase II from Streptococcus pneumoniae.
Fatty Acid Synthesis Inhibitors -Pipeline Insights, 2015 | Global Market Research Reports
Fatty Acid Synthesis Inhibitors- Pipeline Insights, 2015, provides the in-depth analysis of the pipeline assets across the Fatty Acid Synthesis Inhibitors. The main objective of this report to track competitor pipeline molecules, related research activities, technology, collaborations, in-licensing and out-licensing deals.
Widespread and enzyme-independent Nε-acetylation and Nε-succinylation of proteins in the chemical conditions of the...
TY - JOUR. T1 - Widespread and enzyme-independent Nε-acetylation and Nε-succinylation of proteins in the chemical conditions of the mitochondrial matrix. AU - Wagner, Gregory R.. AU - Payne, R. Mark. PY - 2013/10/4. Y1 - 2013/10/4. N2 - Background:The mechanisms initiating protein acylation in mitochondria are unknown. Results:The pH and acyl-CoA concentrations of the mitochondrial matrix are sufficient to cause protein lysine acetylation and succinylation. Conclusion:Protein acylation in mitochondria may be a nonenzymatic event facilitated by the alkaline pH and high acyl-CoA concentrations. Significance:The mitochondrial deacylases SIRT3 and SIRT5 may have evolved to regulate nonenzymatic protein acylation.. AB - Background:The mechanisms initiating protein acylation in mitochondria are unknown. Results:The pH and acyl-CoA concentrations of the mitochondrial matrix are sufficient to cause protein lysine acetylation and succinylation. Conclusion:Protein acylation in mitochondria may be a ...
Acylation - Wikipedia
Protein acylation is the post-translational modification of proteins via the attachment of functional groups through acyl linkages. Protein acylation has been observed as a mechanism controlling biological signaling. One prominent type is fatty acylation, the addition of fatty acids to particular amino acids (e.g. myristoylation, palmitoylation or palmitoleoylation). Different types of fatty acids engage in global protein acylation. Palmitoleoylation is an acylation type where the monounsaturated fatty acid palmitoleic acid is covalently attached to serine or threonine residues of proteins. Palmitoleoylation appears to play a significant role in trafficking and targeting and function of Wnt proteins.. ...
METHODS FOR ALTERING LIPIDS IN ALGAE AND YEAST - Patent application
TABLE-US-00001 TABLE 1 Compound Chemical Name/Structure Compound Class Abscisic acid (2Z,4E)-5-[(1S)-1-hydroxy-2,6,6-trimethyl-4- Plant Growth oxocyclohex-2-en-1-yl]-3-methylpenta-2,4-dienoic acid Hormone BPDQ 4-[(3-bromophenyl)amino]-6,7-diamino-quinazoline Kinase Inhibitor Arctigenin (3R,4R)-4-[(3,4-dimethoxyphenyl)methyl]-3-[(4- Plant Lignan, hydroxy-3-methoxyphenyl)methyl]-2-tetrahydrofuranone Antiviral, Antitumor Baicalein 5,6,7-Trihydroxy-2-phenyl-chromen-4-one Lipoxygenase Inhibitor CDC25 Phosphatase 6-Chloro-7-(2-morpholin-4-yl-ethylamino)-quinoline- Phosphatase Inhibitor Inhibiror I 5,8-dione Cerulenin (2R,3S)-3-[(4E,7E)-Nona-4,7-dienoyl]oxirane-2- Antifungal, Fatty carboxamide Acid Synthesis Inhibitor Eicosapentaenoic (5Z,8Z,11Z,14Z,17Z)-eicosa-5,8,11,14,17-pentenoic acid Cyclooxygenase acid Inhibitor Ethyl 4-[(hydroxyamino)-ethylamino]cyclohexa- Phosphatase Inhibitor 3,4-dephostatin 3,5-diene-1,2-dione Forskolin (3R,4aR,5S,6S,6aS,10S,10aR,10bS)-6,10,10b- MAP Kinase ...
Humana 1 GOS 600g lapte praf de la nastere la 40.81 lei | Mattca
Cumpara Humana 1 GOS 600g lapte praf de la nastere la pretul de 40.81 lei ✅ Comanda confidentiala, produse verificate de farmacisti reali, impachetare sigura.
RCSB PDB for 3TZK
3TZK: Dissecting the Structural Elements for the Activation of beta-Ketoacyl-(Acyl Carrier Protein) Reductase from Vibrio cholerae.
GTPase - Fatty Acid Synthase Inhibitors Induce Apoptosis
Background Lipid oxidation of membrane phospholipids is accompanied by the formation of oxidation-specific epitopes (OSE). antibodies as a result of Siglec-G deficiency inhibits diet-induced hepatic inflammation and atherosclerosis in mice . However, the relationship between plasma antibody levels targeting OSE and hepatic inflammation during NAFLD has not been investigated Lurasidone in humans so far. Here, we aimed to determine an association between plasma antibodies targeting OSE and NAFLD in humans. For this purpose, IgM and IgG antibody titers against different model epitopes of oxidized lipids were measured in the plasma of patients with NAFLD and compared to those in control subjects. Liver biopsies from patients with biopsy-proven NASH were examined for the presence of MDA epitopes by immunohistochemistry. Additionally, to test the specificity of our findings for NAFLD, antibody levels were determined in two cohorts consisting of patients with hepatitis C and inflammatory bowel ...
We describe novel imaging protocols that allow detection of small cancer - Fatty Acid Synthase Inhibitors Induce Apoptosis
We describe novel imaging protocols that allow detection of small cancer cell colonies deep inside tissue phantoms with high sensitivity and specificity. to deeper tumors. We show that under these conditions Syryl-9M can detect as few as 10 cells in a biologically relevant phantom. This outstanding characteristic should bode very well for development of new highly efficient near-IR clinical imaging agents. 2. Methods 2.1. Cells and cell culture For our collagen gel phantom experiments, we required cell lines that we knew from experience would not be adversely affected by culturing in three dimensional collagen type I gels. This was true of all the cell lines used in this work. Three of the lines, normal mammary, +SA and 4T1, were also derived from the same BALB/c inbred mouse strain. The MDA-MB-231 and NIHOVCAR3 cells were chosen to represent malignant human cell lines. Passage Ambrisentan two, normal mouse mammary epithelial cells were propagated from cells obtained from Dr. H. L. Hosick in ...
Widok | FH-Prof. Dr. Julian Weghuber
R. Wagner, G. Stübiger, D. Veigel, M. Wuczkowski, P. Lanzerstorfer, J. Weghuber, E. Karteris, K. Nowikovsky, N. Wilfinger, C. Singer, R. Colomer, B. Benhamu, M. Lopez-Rodrguez, P. Valent, T. Grunt - Multi-level suppression of receptor-PI3K-mTORC1 by fatty acid synthase inhibitors is crucial for their efficacy against ovarian cancer cells - Oncotarget, Vol. 8, No. 7, ...
detergent praf | Kimicar Romania
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Clove extract functions as a natural fatty acid synthesis inhibitor and prevents obesity in a mouse model
Numerous medicinal plants have been reported to prevent various chronic diseases. In this study, we screened a new FASN inhibitor-alcohol extract of clove (AEC) using a fast microplate method developed in our laboratory. The major components of AEC were: eugenol (42.27%), acetyl eugenol (29.12%), ca …
PLOS Pathogens: De novo Fatty Acid Biosynthesis Contributes Significantly to Establishment of a Bioenergetically Favorable...
Author Summary Vaccinia virus, the prototypic poxvirus, is closely related to variola virus, the etiological agent of smallpox. A full understanding of the poxviral life cycle is imperative for the development of novel antiviral therapies, the design of new vaccines, and the effective and safe use of these viruses as oncolytic agents. Metabolomic studies have shed light on the novel mechanisms used by viruses to replicate efficiently within their hosts. de novo fatty acid biosynthesis has been shown to be of relevance for numerous viral infections as well as for the development of cancer. Here we describe an important role for de novo fatty acid biosynthesis during vaccinia infection. Ongoing synthesis of palmitate is needed to fuel the production of energy within mitochondria. The biochemical events of viral DNA replication and protein synthesis are minimally affected by inhibition of this pathway, but viral assembly is disrupted more dramatically. Further exploration of this pathway will provide
PLOS ONE: Inhibition of Fatty Acid Metabolism Reduces Human Myeloma Cells Proliferation
Multiple myeloma is a haematological malignancy characterized by the clonal proliferation of plasma cells. It has been proposed that targeting cancer cell metabolism would provide a new selective anticancer therapeutic strategy. In this work, we tested the hypothesis that inhibition of β-oxidation and de novo fatty acid synthesis would reduce cell proliferation in human myeloma cells. We evaluated the effect of etomoxir and orlistat on fatty acid metabolism, glucose metabolism, cell cycle distribution, proliferation, cell death and expression of G1/S phase regulatory proteins in myeloma cells. Etomoxir and orlistat inhibited β-oxidation and de novo fatty acid synthesis respectively in myeloma cells, without altering significantly glucose metabolism. These effects were associated with reduced cell viability and cell cycle arrest in G0/G1. Specifically, etomoxir and orlistat reduced by 40-70% myeloma cells proliferation. The combination of etomoxir and orlistat resulted in an additive inhibitory effect
Directed tagging of the Arabidopsis FATTY ACID ELONGATION1 (FAE1) gene with the maize transposon activator. | Plant Cell
The FATTY ACID ELONGATION1 (FAE1) gene of Arabidopsis is required for the synthesis of very long chain fatty acids in the seed. The product of the FAE1 gene is presumed to be a condensing enzyme that extends the chain length of fatty acids from C18 to C20 and C22. We report here the cloning of FAE1 by directed transposon tagging with the maize element Activator (Ac). An unstable fae1 mutant was isolated in a line carrying Ac linked to the FAE1 locus on chromosome 4. Cosegregation and reversion analyses established that the new mutant was tagged by Ac. A DNA fragment flanking Ac was cloned by inverse polymerase chain reaction and used to isolate FAE1 genomic clones and a cDNA clone from a library made from immature siliques. The predicted amino acid sequence of the FAE1 protein shares homology with those of other condensing enzymes (chalcone synthase, stilbene synthases, and beta-ketoacyl-acyl carrier protein synthase III), supporting the notion that FAE1 is the structural gene for a synthase or ...
PRAF2 stimulates cell proliferation and migration and predicts poor prognosis in neuroblastoma
Prenylated Rab acceptor 1 domain family, member 2 (PRAF2) is a novel 19-kDa protein with four transmembrane-spanning domains that belongs to the PRAF protein family. Neuroblastoma (NB) is the most common malignant extracranial solid tumor of childhood that originates in primitive cells of the developing sympathetic nervous system. We investigated the correlation of PRAF2 mRNA expression to NB clinical and genetic parameters using Affymetrix expression analysis of a series of 88 NB tumors and examined the functional role of PRAF2 in an NB cell line using RNA interference. We found that high PRAF2 expression is significantly correlated to several unfavorable NB characteristics: MYCN amplification, high age at diagnosis, poor outcome and high INSS stage. The shRNA-mediated PRAF2 downregulation in the SK-N-SH NB cell line resulted in decreased cellular proliferation, migration and matrix-attachment. These findings were confirmed in NB patient tumor samples, where high PRAF2 expression is ...
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DETERGENT PENTRU APARATE DE AER CONDITIONAT CLIMANET - Laborexromania.ro
Detergent spumogen concentrat pentru curatarea radiatoarelor lamelare ale aparatelor de aer conditionat montate in unitatile interioare sau exterioare. Elimina eficient depunerile de praf si mizeria chiar si de natura organica (musculite, etc). Mod de utilizare: Diluati produsul in solutii apoase cu concentratia de 1-5%. Folositi un pulverizator pentru a-l aplica direct pe zona de curatat. Lasati spuma sa actioneze cateva minute dupa care clatiti cu apa. Ambalare bidon 1 kg (cod: CLINET1000), cutie 12 bidoane (cod:CLINET12000)
SURLARİÇİ/LEFKOŞA - Onbeş Kasım Kıbrıs Üniversitesi
Onbeş Kasım Kıbrıs Üniversitesi kendisini mevcut yükseköğretim kuruluşlarından farklılaştıracak olanakların bilincinde olduğu için kurulmuştur.
Why do mitochondria synthesize fatty acids? Evidence for involvement in lipoic acid production | PNAS
The function of fatty acid biosynthesis in mitochondria has remained an enigma. In eukaryotic plants, synthesis of fatty acids occurs primarily in plastids such as chloroplasts, and products of this pathway supply acyl precursors for mitochondrial and other extraplastidial membranes. The discovery of ACP in plant mitochondria (4, 5) has raised the possibility that these organelles also participate in de novo fatty acid synthesis. However, ACP has been considered to have several other functions in metabolism, and, in mitochondria, ACP is reported to be one component of the respiratory electron transport chain (14). Thus, whether ACP participates in fatty acid synthesis in plant mitochondria and what function this pathway might have in any eukaryotic organism has been unclear. In this study, we have demonstrated that the de novo synthesis of fatty acids does occur in pea mitochondria, indicating that these organelles possess the complete set of enzymes needed to assemble fatty acids. The analysis ...
PRAF3 induces apoptosis and inhibits migration and invasion in human esophageal squamous cell carcinoma | BMC Cancer | Full Text
Members of the Prenylated Rab acceptor domain family (PRAF) are essential for the regulation of many cellular processes [22, 23]. Here we have demonstrated that PRAF3 could induce apoptosis and inhibit migration and invasion of ESCC cells and hence may serve as a tumor suppressor in ESCC.. Although the role of PRAF3 has been studied in several other tumors using tumor cell lines [7, 9, 10, 24], there is a lack of investigation into the relationship between PRAF3 expression and the clinical features of ESCCs. In the present study, we found that the expression level of PRAF3 mRNA and protein in ESCC tissues was significantly lower than that in the matched normal tissues. In addition, we found that down-regulation of PRAF3 expression was significantly correlated with poorly differentiated grading, advanced tumor stage and lymph node metastasis of ESCC. These results would imply that PRAF3 may play an important role in regulating the progression and metastasis of ESCCs, although further in vivo ...
LB-237 Many human cancers including breast cancer exhibit increased de novo fatty acid synthesis with overexpression of fatty acid synthase (FAS). Unlike normal cells and tissues that preferentially utilize circulating fatty acids derived from the diet, cancers synthesize fatty acids endogenously for membrane biosynthesis to sustain cell proliferation. The transcription factor Sp1 is highly expressed in a variety of cancers. Sp1 regulates gene expression by interacting with GC-rich promoter sequences. Genes that regulate cell cycle progression often contain such promoter sequences, and Sp1 is critical for their expression. The promoter region of FAS also has Sp1 binding sites, and Sp1 together with sterol regulatory element-binding protein-1 (SREBP-1) has been shown to regulate FAS expression in hepatocytes. Here, we hypothesize that Sp1 coordinately regulates FAS and cell cycle progression in estrogen-responsive MCF-7 breast cancer cells. Based on previous studies, to up-regulate Sp1 activity ...
The Importance of the de novo Group in Your Fatty Acid Profile - Valacta
There are three groups of fatty acids, so what makes the de novo group so important? The data from Quebec clearly demonstrates that herds with more de novo fatty acids also have higher fat and protein levels in their milk. This relationship has also been demonstrated elsewhere in the world.
D-aminolevulinic acid synthase: Definition with D-aminolevulinic acid synthase Pictures and Photos
Definition of D-aminolevulinic acid synthase with photos and pictures, translations, sample usage, and additional links for more information.
Oocist de giardia, Helminti și epilepsii
Semne si simptome Giardioza poate evolua in mai multe moduri; unii bolnavi pot fi purtatori ai parazitului si sa fie asimptomatici, dar sa Singele si mucusul nu sunt caracteristice. Etanșări de etanșare și. Viermi la copii: simptome fiabile și tratament adecvat jucăriile cu săpun, ștergeți suprafețele de mobilier de la praf, covoare de vid etc.
Totul despre alergii | Laboratoarele Sfanta Maria
Simptomele sunt : stranut, prurit nazal, rinoree apoasa si/sau obstructie nazala. Aceste simptome apar ca urmare a unor reactii imunologice excesive in prezenta unor substante straine denumite alergeni.. Gradul de sensibilizare al persoanei si cantitatea de alergeni influenteaza in mod decisiv aparitia si agravarea simptomatologiei.. Alergenii pot fi: praf - acarienii existenti in acesta, polen, mucegai, puf, pene, par, scuame. Cand acesti alergeni intra in contact cu ochii sau cu mucoasele cailor respiratorii ale persoanelor potential alergice, sistemul imunitar declanseaza o reactie inflamatorie care antreneaza dilatarea vaselor sangvine si cresterea secretiilor legate de simptomatologia rinitelor alergice.. Rinita alergica este deseori asociata cu o conjunctivita, precum si cu alte patologii, ca sinuzita, astmul bronsic, deviatia de sept nazal, polipoza nazala.. Exista, in principal, trei tipuri de rinita alergica :. Rinita alergica sezoniera - febra fanulului, apare indeosebi primavara si ...
Helminti izkārnījumos 1 mm, Kas ir helminti
Discutarea simptomelor, a testelor de laborator, a recomandărilor pentru tratament și profilaxie. Induktivno kuplovana plazma - ICP 3. Uzturvielu lentes helminti absorbē visu ķermeņa virsmu.
Fatty Acid Uptake and Lipid Storage Induced by HIF-1α Contribute to Cell Growth and Survival after Hypoxia-Reoxygenation
An in vivo model of antiangiogenic therapy allowed us to identify genes upregulated by bevacizumab treatment, including Fatty Acid Binding Protein 3 (FABP3) and FABP7, both of which are involved in fatty acid uptake. In vitro, both were induced by hypoxia in a hypoxia-inducible factor-1α (HIF-1α)-dependent manner. There was a significant lipid droplet (LD) accumulation in hypoxia that was time and O[subscript 2] concentration dependent. Knockdown of endogenous expression of FABP3, FABP7, or Adipophilin (an essential LD structural component) significantly impaired LD formation under hypoxia. We showed that LD accumulation is due to FABP3/7-dependent fatty acid uptake while de novo fatty acid synthesis is repressed in hypoxia. We also showed that ATP production occurs via β-oxidation or glycogen degradation in a cell-type-dependent manner in hypoxia-reoxygenation. Finally, inhibition of lipid storage reduced protection against reactive oxygen species toxicity, decreased the survival of cells ...
MreB filaments align along greatest principal membrane curvature to orient cell wall synthesis | eLife
Protein acylation is critical for many cellular functions across all domains of life. In bacteria, lipoproteins have important roles in virulence and are targets for the development of antimicrobials and vaccines. Bacterial lipoproteins are secreted from the cytosol via the Sec pathway and acylated on an N-terminal cysteine residue through the action of three enzymes. In Gram-negative bacteria, the Lol pathway transports lipoproteins to the outer membrane. Here, we demonstrate that the Aat secretion system is a composite system sharing similarity with elements of a type I secretion systems and the Lol pathway. During secretion, the AatD subunit acylates the substrate CexE on a highly conserved N-terminal glycine residue. Mutations disrupting glycine acylation interfere with membrane incorporation and trafficking. Our data reveal CexE as the first member of a new class of glycine-acylated lipoprotein, while Aat represents a new secretion system that displays the substrate lipoprotein on the cell ...
Fatty Acid Synthesis: Activation, Steps and Control
Fatty acid synthesis occurs similarly to Beta-oxidation - acetyl groups are added to a growing chain. This notes explains the fatty acid synthesis process..
Detergent ecologic praf pt. masina de spalat vase Sonett 3kg
Detergent ecologic praf pt. masina de spalat vase, Sonett, 3kg Varianta vrac economica Un detergent bio sub forma de pudra destinat spalarii automate a vaselor in masina de spalat vase. Chiar daca nu...
Açık Eriş[email protected]: Kuadriseps femoris kası rehabilitasyonunda izometrik egzersiz ve elektriksel kas uyarılmasının klinik sonuçları
Diz eklemine ait yumuşak doku travması ve effüzyon ile başvuran hastalarda maksimal istemli izometrik egzersiz, elektrik sel kas uyarılması ve her 2 sinin birlikte uygulanmasının kuadriseps femoris kası güçlenmesi üzerine olan etkilerini ve birbirlerine karşı üstünlüklerini araştırmak amacı ile bu çalışmayı planladık. Uludağ üniversitesi Tıp Fakültesi Fiziksel Tıp ve Rehabilitasyon Kliniği-Polikliniğine başvuran 16 olgu klinik muayene, laboratuar incelemesi ve radyolojik görünümlerine dayanarak diz ekleminde akut yumuşak doku travması tanısı ile tedaviye alındı. Kuadriseps femoris kasına olguların 5 inde elektriksel kas uyarılması, 5 inde elektriksel kas uyarılması ile birlikte maksimal istemli izometrik egzersiz, 6 sında maksimal istemli isometrik egzersiz programı uygulandı.Tüm hastalar klinik olarak kuadriseps femoris kası maksimal istemli izometrik kontraksiyon gücü, 10 maksimum ağırlık kaldırma kapasitesi, uyluk ortası çevre ...
BioChem: Lipid Biosynthesis Flashcards - Cram.com
Study Flashcards On BioChem: Lipid Biosynthesis at Cram.com. Quickly memorize the terms, phrases and much more. Cram.com makes it easy to get the grade you want!
Dezastru provocat de un șofer fără carnet și praf de beat - Ziarul Mesagerul de Sibiu
În municipiul Mediaș, un localnic în vârstă de 22 de ani a condus, sâmbătă în zori,un autoturism pe strada Avram Iancu. Pe fondul neatenției în conducere, a intrat în coliziune cu un autoturism staționat, pe care l-a proiectat în alt autoturism parcat în fața acestuia.. Evenimentul s-a soldat cu pagube materiale, iar în urma verificărilor efectuate de către polițiști s-a constatat că medieșeanul nu are dreptul de a conduce autovehicule pe drumurile publice.. De asemenea, testarea sa alcoolscopică a indicat o valoare de 0,48 mg/l alcool pur în aerul expirat, șoferul fiind însoțit la o unitate medicală unde i s-au recoltat probe biologice în vederea stabilirii alcoolemiei în sânge.. În cauză s-au întocmit actele premergătoare efectuării de cercetări penale sub aspectul săvârșirii infracțiunilor de conducere fără permis, respectiv conducere sub influența alcoolului.. ...
BeautyBarometer, cine, ce, cum, CONCURS - BeautyBarometer
Premiul va rasplati descrierea care ma va convinge si pe mine ca imi cunosti blogul. Atentie nu trebuie nici sa ma lauzi, nici sa ma faci praf, eu nu sunt fana a extremelor, adica daca imi citesti blogul te-ai cam lamurit despre ce scriu si cum scriu. Imi doresc sa imi spui simplu si in termeni normali ce reprezinta blogul meu pentru tine si cum i-ai spune tu rapid cuiva ceva despre blogul meu. Lasa-mi textul acesta in comentariu la acest articol. ...
17. Ulusal Çocuk Cerrahisi Hemşireliği Kongresi. 30 Ekim - 2 Kasım October - 2 November 2013 Eskişehir - PDF
17. Ulusal Çocuk Cerrahisi Hemşireliği Kongresi 30 Ekim - 2 Kasım October - 2 November 2013 Eskişehir Ulusal Çocuk Cerrahisi Hemşireliği Kongresi Kurulları KONGRE ONURSAL ÜYELERİ Prof.
Lithuanians in Canada
Lietuviu Kanadoje grupe. Naujai prisijunge nepamirskite prisistatyti kas jus sieja su Kanada, kuo uzsiimate, kokios temos domina.
Lithuanians in Canada
Lietuviu Kanadoje grupe. Naujai prisijunge nepamirskite prisistatyti kas jus sieja su Kanada, kuo uzsiimate, kokios temos domina.
IDEALS @ Illinois: Lipid Metabolism in Corn Tissue Culture and Molecular Biology of Soybean Seed Maturation
Lipid metabolism of corn (Zea mays) tissue culture was studied using seven strains or inbred lines. The lipid content from the embryogenic callus derived from these lines followed the same trend as the lipid content found in the seeds, however there was no consistent lipid pattern observed for the leaf or root callus from these same lines relative to the tissue that it originated from. Therefore corn embryogenic callus provides an ideal tissue to study lipid metabolism. Embryogenic calli were also used to select cell lines resistant to cerulenin, an inhibitor of fatty acid synthesis. While it was hypothesized that the cerulenin-resistant calli might be an overproducing-oil line, the selected resistant calli did not exhibit an increase in lipid content relative to the control calli ...
Volume 3.21 | Jun 9 - Intestinal Cell News
Oroxylin A Suppresses the Development and Growth of Colorectal Cancer through Reprogram of HIF1α-Modulated Fatty Acid Metabolism Researchers investigated the metabolism-modulating effects of oroxylin A on the fatty acid metabolism in colon cancer cells under hypoxia. They found that HIF1α upregulated adipophilin, fatty acid synthase and sterol regulatory element-binding protein 1, and downregulated carnitine palmitoyltransferase 1, resulting in the promoted lipid uptake and transport, increased de novo fatty acid synthesis and suppressed fatty acid oxidation. [Cell Death Dis] Full Article Aldose Reductase Inhibitor Increases Doxorubicin-Sensitivity of Colon Cancer Cells and Decreases Cardiotoxicity Scientists showed that treatment of colorectal cancer cells with fidarestat increases the efficacy of doxorubicin (DOX)-induced death in HT-29 and SW480 cells and in nude mice xenografts. Aldose reductase inhibition resulted in higher intracellular accumulation of DOX and decreased the expression of ...
Starvation-induced collective behavior in C. elegans by Alexander B. Artyukhin, Virginia Commonwealth University J. Yim et al.
We describe a new type of collective behavior in C. elegans nematodes, aggregation of starved L1 larvae. Shortly after hatching in the absence of food, L1 larvae arrest their development and disperse in search for food. In contrast, after two or more days without food, the worms change their behavior-they start to aggregate. The aggregation requires a small amount of ethanol or acetate in the environment. In the case of ethanol, it has to be metabolized, which requires functional alcohol dehydrogenase sodh-1. The resulting acetate is used in de novo fatty acid synthesis, and some of the newly made fatty acids are then derivatized to glycerophosphoethanolamides and released into the surrounding medium. We examined several other Caenorhabditis species and found an apparent correlation between propensity of starved L1s to aggregate and density dependence of their survival in starvation. Aggregation locally concentrates worms and may help the larvae to survive long starvation. This work demonstrates how
Intracellular citrate accumulation by oxidized ATM-mediated metabolism reprogramming via PFKP and CS enhances hypoxic breast...
Citrate, a substance being related to de novo fatty acid synthesis and tricarboxylic acid (TCA) cycle, has a pivotal role in cell survival. However, the molecular mechanisms that regulate intracellular citrate in triple-negative breast cancer (TNBC), especially under hypoxic condition, remain poorly understood. Here we find that hypoxia (1% O2) induces DNA damage-independent ATM activation (oxidized ATM) and suppression of oxidized ATM reduces intracellular citrate via decreasing the levels of phosphofructokinase (PFKP) and citrate synthase (CS), two key glucose metabolism-associated enzymes. Mechanistically, PFKP is regulated by HIF1A at the translational level, whereas CS is of posttranscriptional regulation by UBR5-mediated ubiquitination. Interestingly, accumulation of citrate in cytoplasm or exogenous citrate significantly enhances cell migration, invasion, and metastasis of hypoxic TNBC cells in vitro and in mice xenografts. The underlying mechanism mainly involves citrate-stimulated activation of
44106a Q8 - reactants and products and the name of the enzyme 3(6 pts A and B represent intermediates in fatty acid synthesis...
View Notes - 44106a_Q8 from BICH 441 at Texas A&M. reactants and products and the name of the enzyme. 3. (6 pts). A and B represent intermediates in fatty acid synthesis catalyzed by fatty acid
WikiGenes - FASN - fatty acid synthase
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Phospholipid synthesis by organotypic cell cultures of fetal human lung | Biochemical Society Transactions
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SACOL RS06355 - AureoWiki
MetabolismFatty acid and phospholipid metabolismBiosynthesisfatty acid/phospholipid synthesis protein PlsX (TIGR00182; HMM-score: 408.3) ...
Rasedustest - Meravita - Kas olen rase? - Rasedus - Rasestumine
Selle testiga on võimalik kodustes tingimustes kiiresti ja lihtsalt tuvastada rasedust juba selle varajases staadiumis. Tulemused 3 minutiga. Tutvu tootega
In sterol synthesis, cerulenin inhibits HMG-CoA synthetase activity. It was also reported that cerulenin specifically inhibited ... But in general conclusion, cerulenin has inhibitory effects on sterol synthesis. Cerulenin causes a dose- ... Cerulenin is an antifungal antibiotic that inhibits fatty acid and steroid biosynthesis. It was the first natural product ... Huang P, Zhu S, Lu S, Dai Z, Jin Y (April 2000). "[An experimental study on cerulenin induced apoptosis of human colonic cancer ...
Cerulenin, Andrastin A, Herbimycin, and Neoxaline Koji Nakanishi Tohru Fukuyama Kitasato Shibasaburō List of Japanese Nobel ... a fatty acid biosynthesis inhibitor named cerulenin; Furthermore, compounds having a unique structure and biological activity ...
"Inhibition of beta-ketoacyl-acyl carrier protein synthases by thiolactomycin and cerulenin. Structure and mechanism". J. Biol. ...
Beta-ketoacyl-ACP synthase III
At least two of the existing drugs for tuberculosis were originally derived from microbes; cerulenin from the fungus ...
Cerulenin, a molecule that appears to inhibit by mimicking the "condensation transition state" can only inhibit B or F, but not ... "Inhibition of β-Ketoacyl-Acyl Carrier Protein Synthases by Thiolactomycin and Cerulenin STRUCTURE AND MECHANISM". Journal of ...
Cerulenin is known to inhibit synthase I in Carthamus tinctorius, Spinacia oleracea, Brassica napus, Allium ampeloprasu, ... For example, cerulenin inhibits synthase II in Spinacia oleracea, Allium ampelprasum, Escherichia coli, and Streptoccoccus ... A number of inhibitors include cerulenin in Sinapis alba, Daucus carota, and Phaseolus vulgaris, apigenin in Secale cereale and ...
In axenic culture, S. oryzae produces 0.3-0.627 micrograms of helvolic acid and 0.9-4.8 micrograms of cerulenin per milliliter ... For forty years prior to 2005, the industrial strain used to manufacture the antibiotic cerulenin was known under the invalidly ... Bills GF; Platas G; Gams W (November 2004). "Conspecificity of the cerulenin and helvolic acid producing 'Cephalosporium ...
Subsequent discoveries included alamethicin, aphidicolin, brefeldin A, cephalosporin, cerulenin, citromycin, eupenifeldin, ...
Cerulenin, Aphidicolin Experimental drugs and drug precursors: Parthenolide, Puromycin, Rapamycin, Anisomycin, Thapsigargin, ...
The molecular formula C12H17NO3 may refer to: Anhalidine Anhalinine Anhalonidine Bucetin Bufexamac Cerulenin Etamivan MEDA ...
List of biomolecules
... x Cerulenin Cetrimonium bromide (Cetrimide) - C19H42BrN Chelerythrine Chromomycin A3 Chaparonin Chitin α-Chloralose Chlorophyll ...
OPUS Würzburg | Development of synthesis pathways and characterization of cerulenin analogues as inhibitors of the fatty acid...
... cerulenin analogues 15a-b. A fourth class of cerulenin analogues was synthesized with the aromatic analogues 17a-e. This ... Cerulenin was chosen as the lead structure, being a substrate of the efflux pumps in Candida albicans on one hand and therefore ... On the other hand, cerulenin is a known inhibitor of the FAS system but inhibition is unselective in type I and II FAS. ... The first cerulenin derivatives were prepared by coupling 2,3-dihydrofuran to the before synthesized 1-octaniodide, followed by ...
An Essential Role for the Tumor-Suppressor Merlin in Regulating Fatty Acid Synthesis | Cancer Research | American Association...
3B), together with cerulenin treatment. Knockdown of Acaca led to a striking reduction in cerulenin- and GSK2194069-induced ... Interestingly, Nf2−/− and control MEFs react differently to cerulenin treatment (Supplementary Table S3). Although cerulenin ... caused an increase in cerulenin toxicity in Nf2f/fcells, but had little effect on cerulenin toxicity in Nf2−/−cells (Fig. 3F). ... in cerulenin-treated Nf2−/− cells, but not in cerulenin-treated Nf2f/f cells. ...
Frontiers | Protein Lipidation by Palmitoylation and Myristoylation in Cancer
PRAF2 PRA1 domain family member 2 [Homo sapiens (human)] - Gene - NCBI
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IMSEAR at SEARO: Inhibition of fatty acid synthase supresses osteosarcoma cell invasion and migration.
At least two of the isolates of S. oryzae produced titres of cerulenin and helvolic acid similar to those of KF-140. This ... Conspecificity of the cerulenin and helvolic acid producing Cephalosporium caerulens, and the hypocrealean fungus Sarocladium ... Fermentation processes for the biochemical reagents cerulenin and helvolic acid employ Cephalosporium caerulens, an invalidly ... another Acremonium-like fungus which also produces cerulenin and helvolic acid. Morphological comparisons, rDNA sequence data, ...
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Cerulenin increased the apoptosis rates and enhanced the cleavage of PARP caused by bestatin. Furthermore, cerulenin, orlistat ... METHODS: Cerulenin, orlistat and siRNAs was applied to inhibit FASN. The cell viability and apoptosis were assessed with MTT ( ... Indeed, cerulenin induced the up-regulation of PEPT1 mRNA expression rather than affecting the protein level after the cells ... RESULTS: In the current study, we found that inhibiting FASN by cerulenin and orlistat both augmented the effects of bestatin ...
Nonvesicular sterol movement from plasma membrane to ER requires oxysterol-binding protein-related proteins and...
Lactams | Harvard Catalyst Profiles | Harvard Catalyst
DeCS 2017 - December 21, 2017 version
Atividade de enzimas associadas ao estado de indução em mudas de cacaueiro expostas a dois actinomicetos residentes de...
... of the isolates produced cerulenin at detectable levels. Both BRM 6461 (296.0 µg mL-1) and BRM 6493 (undetectable cerulenin) ... Thus, the variability of 28 Sarocladium oryzae isolates was evaluated for the cerulenin production, as well as its potential ... basically constituted by cerulenin, reduced the severity of rice leaf blast and possibly activated the defense mechanisms of ...
Download Against All Odds: My Story 2006
Strategies to enhance the production of pinoresinol and its glucosides by endophytic fungus (Phomopsis sp. XP-8) isolated from...
condition mean min max
antibacterial - Drug Discovery Opinion
... cerulenin and triclosan, if supplied with exogenous fatty acids at levels that would be present in human serum. Using ... cerulenin, which are believed to act primarily by inhibiting steps in the FASII pathway. The natural products, platensimycin ... were able to overcome the inhibitory effect of cerulenin treatment. ...
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Mycobacterium bovis (BCG kas(B)) | The Antimicrobial Index Knowledgebase - TOKU-E
Centers for Disease Control and Prevention. 2020. DSR-052-02: Preparation of viral transport medium.. ClinicalTrials.gov [Internet]. Bethesda (MD): National Library of Medicine (US). 2000 Feb 29 . Identifier NCT04322682, Colchicine Coronavirus SARS-CoV2 Trial (COLCORONA) (COVID-19); 2020 March 26 [cited 2021 Jan 26][~ 6 pages]. Available from: https://clinicaltrials.gov/ct2/show/NCT04322682. Gao J, Tian Z, Yang X (2020) Breakthrough: Chloroquine phosphate has shown apparent efficacy in treatment of COVID-19 associated pneumonia in clinical studies. Biosci. Trends doi 10.5582. ePub PMID 32074550. Hoffmann M (2020) SARS-CoV-2 Cell entry depends on ACE2 and TMPRSS2 and Is blocked by a clinically proven protease inhibitor. Cell. Doi 10.1016. in press.. Letko M et al (2020) Functional assessment of cell entry and receptor usage for SARS-CoV-2 and other lineage B betacoronaviruses. Nat. Microbiol. 5:562-569. Li G et al (2021) Safety and efficacy of Artemisinin-Piperaquine for treatment of COVID-19: An ...
DeCS 2016 - June 12, 2016 version
DeCS 2017 - December 21, 2017 version
- Cerulenin was chosen as the lead structure, being a substrate of the efflux pumps in Candida albicans on one hand and therefore variations on the structure could lead to a blocking of the efflux pumps as in the case of tetracycline and inhibitor 13-CPTC of the TetB efflux pump. (uni-wuerzburg.de)
- On the other hand, cerulenin is a known inhibitor of the FAS system but inhibition is unselective in type I and II FAS. (uni-wuerzburg.de)
- We performed the cerulenin, an inhibitor of FASN, to inhibit FASN expression in U2-OS cells. (who.int)
- To obtain analogues with all structural features of cerulenin including two double bonds and the epoxide function, a third pathway was chosen. (uni-wuerzburg.de)
- Expression of prenylated Rab acceptor 1 domain family, member 2 (PRAF2) in neuroblastoma: correlation with clinical features, cellular localization, and cerulenin-mediated apoptosis regulation. (nih.gov)
Analogues as inhibitors1
- The work deals with the synthesis and characterization of cerulenin analogues as inhibitors of efflux pump mediated resistance of Candida albicans isolates and as inhibitors of the fatty acid synthesis enzyme KasA of Mycobacterium tuberculosis. (uni-wuerzburg.de)
- Fas inhibitors cerulenin or C75 inhibited 2-ME-induced caspase activation, PARP cleavage, apoptosis and reversed mitochondrial membrane hyperpolarization, thereby recapitulating the increased expression of MTS-hOGG1. (nih.gov)
- These results show that cerulenin efficiently inhibits lipid biosynthesis in Chlamydomonas . (plantae.org)
- The fungal products cerulenin and thiolactomycin target the condensing enzymes of fatty acid biosynthesis . (virology2016.com)
- 7. Cerulenin suppresses ErbB2-overexpressing breast cancer by targeting ErbB2/PKM2 pathway. (nih.gov)
- To obtain analogues with all structural features of cerulenin including two double bonds and the epoxide function, a third pathway was chosen. (uni-wuerzburg.de)
- Improvement of ( 2S )-pinocembrin titres was then achieved by optimization of gene organizations, using of codon-optimized pathway enzymes and addition of cerulenin for increasing intracellular malonyl CoA pools. (biomedcentral.com)
- 173, 353-359] mediated a cerulenin-sensitive, de novo fatty acid synthesis independent of the fatty acid synthetase complex present in the cytoplasm. (liverpool.ac.uk)
- Treatment of wild type cells with cerulenin results in. (iecnc.org)
- Results Overview of the study We compiled a YM201636 set of 31 chemically and functionally varied small molecules associated with inhibition of biological processes involving a wide range of cellular compartments: the cell membrane (cerulenin, is definitely supported by numerous levels of evidence extracted from literature sources and the BRENDA enzyme database . (og-l002.com)
- Cerulenin and C75, which target the keto-acyl synthase domain of FAS, were the first small molecules to be described as inhibitors of FAS activity in human tumor cells. (aacrjournals.org)