Farnesyl pyrophosphate (FPP), also known as farnesyl diphosphate (FDP), is an intermediate in both the mevalonate and non-mevalonate pathways used by organisms in the biosynthesis of terpenes, terpenoids, and sterols. It is used in the synthesis of CoQ (part of the electron transport chain), as well as being the immediate precursor of squalene (via the enzyme squalene synthase), dehydrodolichol diphosphate (a precursor of dolichol, which transports proteins to the ER lumen for N-glycosylation), and geranylgeranyl pyrophosphate (GGPP). Farnesyl pyrophosphate synthase (a prenyl transferase) catalyzes sequential condensation reactions of dimethylallyl pyrophosphate with 2 units of 3-isopentenyl pyrophosphate to form farnesyl pyrophosphate, as is shown in the following two steps: Dimethylallyl pyrophosphate reacts with 3-isopentenyl pyrophosphate to form geranyl pyrophosphate: Geranyl pyrophosphate then reacts with another molecule of 3-isopentenyl pyrophosphate to form farnesyl pyrophosphate The ...
Catalyzes the biosynthesis of presqualene diphosphate (PSPP). Works in combination with SSL-2 or SSL-3 to produce respectively squalene or botryococcene. In most other species, farnesyl diphosphate (FPP) is converted into squalene in a two-step reaction by a single enzyme.
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Phospho-N-acetylmuramoyl-pentapeptide-transferaseUDP-Mur2Ac(oyl-L-Ala-gamma-D-Glu-L-Lys-D-Ala-D-Ala) + undecaprenyl phosphate = UMP + Mur2Ac(oyl-L-Ala-gamma-D-Glu-L-Lys-D-Ala-D-Ala)-diphosphoundecaprenol ...
Isoprenoids represent the largest class of metabolites with amazing diversities in structure and function. They are involved in protecting plants against pathogens or herbivores or involved in attracting pollinators. Isoprenoids are derived from geranyl diphosphate (GPP; C10), farnesyl diphosphate (FPP; C15), geranylgeranyl diphosphate (GGPP; C20), and geranylfarnesyl diphosphate (GFPP; C25) that are in turn formed by sequential condensations of isopentenyl diphosphate (IPP; C5) with an allylic acceptor such as dimethylallyl diphosphate (DMAPP; C5), GPP, FPP, or GGPP in a reaction catalyzed by isoprenyl diphosphate synthases (IDSs). IDS enzyme assay for determination of prenyl diphosphate products is generally performed using radiolabelled substrates, and the products formed are identified by employing expensive instruments such as phosphor imager, radio-GC, or radioHPLC. Though a non-radioactive assay for measuring IDS activity in crude plant extract has been reported, it requires a complex methodology
Catalyzes the dephosphorylation of diacylglycerol diphosphate (DGPP) to phosphatidate (PA) and the subsequent dephosphorylation of PA to diacylglycerol (DAG). Also has undecaprenyl pyrophosphate phosphatase activity, required for the biosynthesis of the lipid carrier undecaprenyl phosphate. Can also use lysophosphatidic acid (LPA) and phosphatidylglycerophosphate as substrates. The pattern of activities varies according to subcellular location, PGP phosphatase activity is higher in the cytoplasmic membrane, whereas PA and LPA phosphatase activities are higher in the outer membrane. Activity is independent of a divalent cation ion and insensitive to inhibition by N-ethylmaleimide (By similarity).
p,Polymyxins are antibiotics used in the last line of defense to combat multidrug-resistant infections by Gram-negative bacteria. Polymyxin resistance arises through charge modification of the bacterial outer membrane with the attachment of the cationic sugar 4-amino-4-deoxy-l-arabinose to lipid A, a reaction catalyzed by the integral membrane lipid-to-lipid glycosyltransferase 4-amino-4-deoxy-L-arabinose transferase (ArnT). Here, we report crystal structures of ArnT from Cupriavidus metallidurans, alone and in complex with the lipid carrier undecaprenyl phosphate, at 2.8 and 3.2 angstrom resolution, respectively. The structures show cavities for both lipidic substrates, which converge at the active site. A structural rearrangement occurs on undecaprenyl phosphate binding, which stabilizes the active site and likely allows lipid A binding. Functional mutagenesis experiments based on these structures suggest a mechanistic model for ArnT family enzymes.,/p,. ...
Isoprenoids make up a large group of essential molecules involved in diverse cellular processes including energy metabolism [10-14]. In all metazoan organisms, isoprenoids are produced via the mevalonate pathway. Thus, in the present study, we assessed the effects of various mevalonate metabolites on PPARγ activity, which plays an important role in adipocyte differentiation. We have reported that one of the mevalonate metabolites, FPP, which is the precursor of almost all isoprenoids and is positioned at branch points leading to the synthesis of other longer-chain isoprenoids [35], enhances the expression levels of adipogenic genes, such as aP2, LPL, adiponectin and GLUT4, suggesting that the addition of FPP promoted adipocyte differentiation.. FPP plays an important role as the substrate of protein farnesylation reactions catalysed by FPTase [36]. Members of the Ras GTPase family are major substrates of post-translational modification by farnesylation, a process essential for their proper ...
Todenhoefer, Tilman; Hennenlotter, Joerg; Kuehs, Ursula; Gerber, Valentina; Gakis, Georgios; Vogel, Ulrich; Aufderklamm, Stefan; Merseburger, Axel; Knapp, Judith; Stenzl, Arnulf; Schwentner, Christian ...
Terpenoids, also known as isoprenoids, are a large class of natural products consisting of isoprene (C5) units. There are two biosynthetic pathways, the mevalonate pathway [MD:M00095] and the non-mevalonate pathway or the MEP/DOXP pathway [MD:M00096], for the terpenoid building blocks: isopentenyl diphosphate (IPP) and dimethylallyl diphosphate (DMAPP). The action of prenyltransferases then generates higher-order building blocks: geranyl diphosphate (GPP), farsenyl diphosphate (FPP), and geranylgeranyl diphosphate (GGPP), which are the precursors of monoterpenoids (C10), sesquiterpenoids (C15), and diterpenoids (C20), respectively. Condensation of these building blocks gives rise to the precursors of sterols (C30) and carotenoids (C40). The MEP/DOXP pathway is absent in higher animals and fungi, but in green plants the MEP/DOXP and mevalonate pathways co-exist in separate cellular compartments. The MEP/DOXP pathway, operating in the plastids, is responsible for the formation of essential oil ...
Terpenoids, also known as isoprenoids, are a large class of natural products consisting of isoprene (C5) units. There are two biosynthetic pathways, the mevalonate pathway [MD:M00095] and the non-mevalonate pathway or the MEP/DOXP pathway [MD:M00096], for the terpenoid building blocks: isopentenyl diphosphate (IPP) and dimethylallyl diphosphate (DMAPP). The action of prenyltransferases then generates higher-order building blocks: geranyl diphosphate (GPP), farsenyl diphosphate (FPP), and geranylgeranyl diphosphate (GGPP), which are the precursors of monoterpenoids (C10), sesquiterpenoids (C15), and diterpenoids (C20), respectively. Condensation of these building blocks gives rise to the precursors of sterols (C30) and carotenoids (C40). The MEP/DOXP pathway is absent in higher animals and fungi, but in green plants the MEP/DOXP and mevalonate pathways co-exist in separate cellular compartments. The MEP/DOXP pathway, operating in the plastids, is responsible for the formation of essential oil ...
Frick, S., Nagel, R., Schmidt, A., Bodemann, R., Rahfeld, P., Pauls, G., Brandt, W., Gershenzon, J., Boland, W., Burse, A. (2013). Metal ions control product specificity of isoprenyl diphosphate synthases in the insect terpenoid pathway. Proceedings of the National Academy of Sciences of the United States of America, 110(11), 4194-4199. doi:10.1073/pnas.1221489110. [BOL553] ...
Definition of farnesyl pyrophosphate. Provided by Stedmans medical dictionary and Drugs.com. Includes medical terms and definitions.
Our Bio-dosimeter must have some sort of visible output to alert users to radioactivity (detected as DNA damage). In a previous iGEM project, colrcoli, we attempted to use E.coli as a paint tool. To that end, we examined biosynthesis of carotenoid pigments as a way of producing color. Here, we attempted to use biosynthesis of the carotenoid lycopene as a reporter for DNA damage.. Carotenoid is a family of natural pigments. Many plants such as fruits and vegetables contain these pigments. For example, tomato has lycopene(red), carrot has carotene(orange). Xanthophyll(yellow) is found in almost all plants.. Biosynthesis of carotenoid pigments starts from FPP(FARNESYL DIPHOSPHATE). FPP is formed from isopentenylpyrophosphate(IPP) and dimethylallylpyrophosphate(DMAPP), which can be biologically produced by two distinct pathways, the mevalonate and non-mevalonate pathways. In E.coli, FPP is formed through the non-mevalonate pathway. By the introduction of heterologous enzymatic genes colorless FPP ...
The speed that bacterial pathogens gain resistance to antibiotics is alarming. Designing new antibacterial agents is urgent, but it requires understanding their bacterial targets at the molecular level to achieve high specificity and potency. In this thesis, I discuss the structural and biochemical investigations of three potential protein targets for antibiotics. The first is a UDP-Glc/GlcNAc 4-epimerase, called Gne, from the human pathogen Campylobacter jejuni. This enzyme is the sole source of N-acetylgalactosamine (GalNAc) in C. jejuni, which is a common component in three major glycoconjugates decorating the cell surface and is critical for pathogenesis. The second target protein is an integral membrane protein, called MraY, which catalyzes the transfer of phospho-N-acetylmuramyl (MurNAc) pentapeptide to a lipid carrier, undecaprenyl phosphate (C55-P), producing Lipid I in the peptidoglycan biosynthesis pathway. In the following step, a peripheral protein called MurG catalyzes transferring ...
Researchers at the Institute for Molecular Bioscience (IMB) at The University of Queensland (UQ) have initiated a research program to resurrect the antibiotic fruilimicin B that displays broad spectrum activity against a variety of gram positive bacteria. Unlike daptomycin, friulimicin B maintains activity in the presence of pulmonary lung surfactant, which opens the possibility for use in treatment of Gram-positive lung infections. Friulimicin B represents a new MoA for human antibiotics that involves the complexation of undecaprenyl phosphate (C55-P), which interferes with both peptidoglycan and teichoic acid biosynthesis.. ...
article{76337ac6-36e6-4fff-b6e8-dfb8093c0fd5, abstract = {A clone encoding farnesyl diphosphate synthase (FPPS) was obtained by PCR from a cDNA library made from young leaves of Artemisia annua. A cDNA clone encoding the tobacco epi-aristolochene synthase (eAS) was kindly supplied by J. Chappell (University of Kentucky, Lexington, KY, USA). Two fusions were constructed, i.e. FPPS/eAS and eAS/FPPS. The stop codon of the N-terminal enzyme was removed and replaced by a short peptide (Gly-Ser-Gly) to introduce a linker between the two ORFs. These two fusions and the two single cDNA clones were separately introduced into a bacterial expression vector (pET32). Escherichia coli was transformed with the expression vectors and enzymatically active soluble proteins were obtained after induction with isopropyl thio-beta-d-thiogalactoside. The recombinant enzymes were purified using immobilized metal affinity chromatography on Co2+ columns. The fusion enzymes produced epi-aristolochene from isopentenyl ...
en] Isoprenoids form an extensive group of natural products involved in a number of important biological processes. Their biosynthesis proceeds through sequential 1-4 condensations of isopentenyl diphosphate (C(5)) with an allylic acceptor, the first of which is dimethylallyl diphosphate (C(5)). The reactions leading to the production of geranyl diphosphate (C(10)), farnesyl diphosphate (C(15)) and geranylgeranyl diphosphate (C(20)), which are the precursors of mono-, sesqui- and diterpenes, respectively, are catalyzed by a group of highly conserved enzymes known as short-chain isoprenyl diphosphate synthases, or prenyltransferases. In recent years, the sequences of many new prenyltransferases have become available, including those of several plant and animal geranyl diphosphate synthases, revealing novel mechanisms of product chain-length selectivity and an intricate evolutionary path from a putative common ancestor. Finally, there is considerable interest in designing inhibitors specific to ...
Looking for online definition of dolichyl phosphate glucosyltransferase in the Medical Dictionary? dolichyl phosphate glucosyltransferase explanation free. What is dolichyl phosphate glucosyltransferase? Meaning of dolichyl phosphate glucosyltransferase medical term. What does dolichyl phosphate glucosyltransferase mean?
The majority of circulating human γδ T cells expresses a TCR comprising the variable segments Vγ9 and Vδ2 (Vγ9Vδ2 TCR). These cells massively expand in various infectious diseases, exhibit MHC-unrestricted cytolysis, and, in the presence of IL-2, produce Th1-type cytokines such as IFN-γ and TNF-α (1, 2). In addition, there is increasing evidence for an important role in host defense (3, 4) and tumor surveillance (5, 6). A hallmark of Vγ9Vδ2 T cells is their unique Ag reactivity. Several types of Vγ9Vδ2 T cell activators are known. At first the three types of phosphoantigens which comprise (E)-4-hydroxy-3-methyl-but-enyl pyrophosphate (HMB-PP),6 isopentenyl pyrophosphate (IPP), and bromohydrin pyrophosphate or Phosphostim (BrHPP). HMB-PP is the immediate precursor of IPP in the 1-deoxy-d-xylulose-5-phosphate pathway of isoprenoid synthesis, which is common to plants, many bacteria, and apicomplexan protozoa but absent in mammals (1, 7). IPP is found in all organisms. Its Vγ9Vδ2 T ...
Accepted name: fructose-bisphosphatase. Reaction: D-fructose 1,6-bisphosphate + H2O = D-fructose 6-phosphate + phosphate. For diagram of reaction click here, alternative click here.. Other name(s): hexose diphosphatase; FBPase; fructose 1,6-diphosphatase; fructose 1,6-diphosphate phosphatase; D-fructose 1,6-diphosphatase; fructose 1,6-bisphosphatase; fructose diphosphatase; fructose diphosphate phosphatase; fructose bisphosphate phosphatase; fructose 1,6-bisphosphate 1-phosphatase; fructose 1,6-bisphosphate phosphatase; hexose bisphosphatase; D-fructose-1,6-bisphosphate phosphatase. Systematic name: D-fructose-1,6-bisphosphate 1-phosphohydrolase. Comments: The animal enzyme also acts on sedoheptulose 1,7-bisphosphate.. Links to other databases: BRENDA, EXPASY, GTD, KEGG, Metacyc, PDB, CAS registry number: 9001-52-9. References:. 1. El-Badry, A.M. Hexosediphosphatase from spinach chloroplasts. Purification, crystallization and some properties. Biochim. Biophys. Acta 333 (1974) 366-377.. 2. ...
The biosynthesis of bacterial cell wall peptidoglycan is a complex process involving many different steps taking place in the cytoplasm (synthesis of the nucleotide precursors) and on the inner and outer sides of the cytoplasmic membrane (assembly and polymerization of the disaccharide-peptide monomer unit, respectively). This review summarizes the current knowledge on the membrane steps leading to the formation of the lipid II intermediate, i.e. the substrate of the polymerization reactions. It makes the point on past and recent data that have significantly contributed to the understanding of the biosynthesis of undecaprenyl phosphate, the carrier lipid required for the anchoring of the peptidoglycan hydrophilic units in the membrane, and to the characterization of the MraY and MurG enzymes which catalyze the successive transfers of the N-acetylmuramoyl-peptide and N-acetylglucosamine moieties onto the carrier lipid, respectively. Enzyme inhibitors and antibacterial compounds interfering with ...
Geranylgeranyl diphosphate is a twenty-carbon isoprenoid phospholipid whose lipid moiety could be post-translationally incorporated into protein to market membrane association. dependence on planning cytoplasmic and membrane fractions for Traditional western blot evaluation. Rap1 is consistently used being a biomarker for mobile geranylgeranylation, and is particularly helpful for in tissues studies where tissues for analysis is bound, precluding evaluation by subcellular fractionation. For instance, Rap1 geranylgeranylation was discovered to become impaired by GGDPS inhibitors at metastatic sites in the adrenal gland and mesenteric metastatic sites, although it was not modified in non-tumorous adrenal glands. Related using the inhibition of Rap1 prenylation, mice treated using the GGDPS inhibitor also display decreased tumor burden (Reilly et al., 2015a). A significant benefit of GGDPS inhibition may be the capability to impair geranylgeranylation of proteins that are altered by both ...
Currently, statins are the only drugs acting on the mammalian isoprenoid pathway. The mammalian genes in this pathway are not easily amenable to genetic manipulation. Thus, it is difficult to study the effects of the inhibition of various enzymes on the intermediate and final products in the isoprenoid pathway. In fission yeast, antifungal compounds such as azoles and terbinafine are available as inhibitors of the pathway in addition to statins, and various isoprenoid pathway mutants are also available. Here in these mutants, treated with statins or antifungals, we quantified the final and intermediate products of the fission yeast isoprenoid pathway using liquid chromatography-mass spectrometry/mass spectrometry. In hmg1-1, a mutant of the gene encoding 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGR), ergosterol (a final sterol product), and squalene (an intermediate pathway product), were decreased to approximately 80% and 10%, respectively, compared with that of wild-type cells. Consistently
Geranylgeranyl pyrophosphate synthase 2; Heterodimeric geranyl(geranyl)-diphosphate (GPP) synthase large subunit. In vitro, the large subunit catalyzes mainly the trans-addition of the three molecules of IPP onto DMAPP to form geranylgeranyl pyrophosphate while the small subunit alone is inactive. Upon association of the two subunits, the product profile is not changed (376 aa ...
Vγ9/Vδ2 T cells are unique to humans and primates and represent a minor and unconventional constituent of the leukocyte population in peripheral blood (0.5-5%); yet they are assumed to play an early and essential role in sensing danger by invading pathogens as they expand dramatically in many acute infections and may exceed all other lymphocytes within a few days, e.g. in tuberculosis, salmonellosis, ehrlichiosis, brucellosis, tularemia, listeriosis, toxoplasmosis, and malaria. Of note, all Vγ9/Vδ2 T cells recognize the same small microbial compound (E)-4-hydroxy-3-methyl-but-2-enyl pyrophosphate (HMB-PP), a natural intermediate of the non-mevalonate pathway of isopentenyl pyrophosphate (IPP) biosynthesis.[5] HMB-PP is an essential metabolite in most pathogenic bacteria including Mycobacterium tuberculosis and malaria parasites, but is absent from the human host. Bacterial species that lack the non-mevalonate pathway and synthesize IPP via the classical mevalonate pathway instead, such as ...
Farnesyl pyrophosphate synthase (FPPS) may be the main molecular focus on of nitrogen-containing bisphosphonates (N-BPs), used clinically seeing that bone tissue resorption inhibitors. RIS using the phenyl band of Tyr204 demonstrated needed for the maintenance of the isomerized enzyme-inhibitor complicated. Research with conformationally limited analogues of RIS reaffirmed the need for Thr201 in the forming of hydrogen bonds with N-BPs. To conclude we have discovered new top features of FPPS inhibition by N-BPs and uncovered unknown roles from the energetic site residues in catalysis and substrate binding. FPPS computations from the stabilization aftereffect of Thr201 in the carbocation types (1.5?Kcal/mol) suggest a far more substantial role from the Thr201 residue in catalysis compared to the a single reported right here [35]. Compensation with the various other energetic site residues forecasted to stabilize the carbocation intermediate, such as for example Gln240 as well as the carbonyl of ...
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The IUPHAR/BPS Guide to Pharmacology. farnesyl diphosphate ligand page. Quantitative data and detailed annnotation of the targets of licensed and experimental drugs.
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A comprehensive book on isoprenoids does not exist. Isoprenoid Synthesis in Plants and Microorganisms: New Concepts and Experimental Approaches fills this gap by presenting the latest and the most applicable information on isoprenoids. The most recent TERPNET conference serves as the backdrop and provides much of the inspiration for the topics covered in the book.
Schistosomiasis affects over 200 million people worldwide, with over 200,000 deaths annually. Currently, praziquantel is the only drug available against schistosomiasis. We report here that Schistosoma mansoni farnesyl diphosphate synthase (SmFPPS) and geranylgeranyl diphosphate synthase (SmGGPPS) a …
TY - JOUR. T1 - α-Methylation enhances the potency of isoprenoid triazole bisphosphonates as geranylgeranyl diphosphate synthase inhibitors. AU - Matthiesen, Robert A.. AU - Varney, Michelle L.. AU - Xu, Pauline C.. AU - Rier, Alex S.. AU - Wiemer, David F.. AU - Holstein, Sarah A. PY - 2018/1/15. Y1 - 2018/1/15. N2 - Disruption of protein geranylgeranylation via inhibition of geranylgeranyl diphosphate synthase (GGDPS) represents a novel therapeutic strategy for a variety of malignancies, especially those characterized by excessive protein secretion such as multiple myeloma. Our work has demonstrated that some isoprenoid triazole bisphosphonates are potent and selective inhibitors of GGDPS. Here we present the synthesis and biological evaluation of a new series of isoprenoid triazoles modified by incorporation of a methyl group at the α-carbon. These studies reveal that incorporation of an α-methyl substituent enhances the potency of these compounds as GGDPS inhibitors, and, in the case of ...
Information for linalyl benzoate 126-64-7 including linalyl benzoate CAS NO 126-64-7, linalyl benzoate Suppliers, linalyl benzoate Manufacturers, related products of linalyl benzoate.
STATIN INHIBITION OF MACROPHAGE INTEGRIN-INDUCED RAC2-MYOSIN IIA INTERACTION: AN ANTI-INFLAMMATORY EFFECT. Kenneth E. Ike, Alan Morrison, and Jeffrey R. Bender. Section of Cardiovascular Medicine, Department of Internal Medicine, Yale University, School of Medicine, New Haven, CT. HMG-CoA reductase inhibitors (statins) are pharmaceuticals that are utilized for the treatment of lipid disorders along with the primary and secondary prevention of coronary heart disease. HMG-CoA reductase is the rate-limiting enzyme in cholesterol synthesis, converting HMG-CoA to mevalonate. The isoprenoid products, farnesyl pyrophosphate (FPP) and geranylgeranyl pyrophosphate (GGPP), are derived from the mevalonate pathway and serve as substrates in the prenylation of 2% of cellular proteins including the Rho family of low molecular weight G-proteins which mediate multiple cellular signals. Prenylation is an important post-translational modification of proteins that plays a role in the subcellular localization of proteins
Farnesol (FOH) is an isoprenoid alcohol that may be endogenously generated within the cells by enzymatic dephosphorylation of farnesyl pyrophosphate (FPP), an intermediate of the metabolic pathway yielding sterols and other isoprenoid compounds from mevalonate (4). In addition to geranylgeranyl pyrophosphate, FPP also plays an important role as a precursor of protein prenylation such as in the posttranslational modification of oncogenic RAS proteins and other GTP-binding proteins (11). When exogenously added to the medium, FOH is subjected to either phosphorylation, yielding FPP, or oxidation, to give farnesal, farnesoic acid, and prenyldicarboxylic acid in mammalian cells (4). Recently, FOH has attracted much attention since it causes apoptotic cell death of human acute leukemia CEM-C1 cells (15, 20) and HL-60 cells (23). Interference with a phosphatidylinositol type of signaling has been proposed to be a cause of apoptosis in FOH-treated mammalian cells. In our previous study, FOH was found to ...
Sesquiterpenes are a class of terpenes that consist of three isoprene units and have the molecular formula C15H24. Like monoterpenes, sesquiterpenes may be acyclic or contain rings, including many unique combinations. Biochemical modifications such as oxidation or rearrangement produce the related sesquiterpenoids. Sesquiterpenes are found naturally in plants and insects, as semiochemicals, e.g. defensive agents or pheromones. The reaction of geranyl pyrophosphate with isopentenyl pyrophosphate results in the 15-carbon farnesyl pyrophosphate which is an intermediate in the biosynthesis of sesquiterpenes such as farnesene. Oxidation of farnesene then provides sesquiterpenoids such as farnesol. There are more cyclic sesquiterpenes than cyclic monoterpenes because of the increased chain length and additional double bond. In addition to common six-membered ring systems such as is found in zingiberene (a constituent of the oil from ginger), cyclization of one end of the chain to the other end can ...
C100 Introduction: Zoledronic acid (ZOL), a nitrogen-containing bisphosphonate, is a potent inhibitor of the activity of farnesyl-pyrophosphate synthase leading to a blockade of the mevalonate pathway and interfering with protein modifications critical for cell signaling and growth. However, cell permeability to ZOL is poor, and therefore cytotoxic activity is minimal except when internalized by fluid-phase endocytosis into osteoclasts. The purpose of this study was to deliver ZOL to the intracellular compartment of tumor cells via encapsulation in liposomes targeted to the folate receptor (FR), which is over-expressed in a broad spectrum of tumors. Methods: ZOL was entrapped passively in the water phase of liposomes of various compositions.with or without a lipophilic folate ligand inserted in the lipid bilayer. The formulations tested had a ZOL:phospholipid molar ratio of ~0.1, a folate:phospholipid molar ratio of 0.005, and a mean vesicle diameter of ~100 nm. A spike of C14-radiolabeled ZOL ...
Indicated groups were compared using Wilcoxon matched\pairs signed rank test (****DH10b (Invitrogen) were transformed with 3?L of the reaction product via heat shock at 42C for 45?s and plated onto 100?g/mL ampicillin containing LB Broth with agar (Sigma) plates. 3, = 115258C6762C7645C60T follicular helper, LNsCD4+CD44+CD62Llow CXCR5+PD\1+ 3, = 345658C6762C7645C60T regulatory, Continue Reading. ...
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Daudi cells (5 × 108) were lysed according to reference 14. Cell lysates were concentrated four times using Biomax-10K filters (Millipore) and 125 μl aliquots were incubated for 60 min at 37°C under conditions described (14) in a total volume of 500 μl. The reaction was stopped by addition of an equal volume of methanol and cooling on ice. The sample was clarified by centrifugation at 9,000 rpm and stored at −20°C until HPLC separation or phosphatase treatment. HPLC separation was performed as reported (14) with some modifications. Briefly, a Spherisorb SAX 5μ HPLC column (4.6 mm × 25 cm; VDS Optilab) was used together with the buffers described in reference 14. The gradient was 0-2 min 0% B, 2-13.5 min 57% B, 13.5-14.5 min 99% B, 14.5-35 min 99% B. Radioactivity was detected online with a β scintillation detector (Packard Instrument Co.) using Ultima Flo M (Packard Instrument Co.) as scintillant. UV monitoring (254 nm) was also applied. Separate HPLC runs under identical conditions ...
A novel double labelling experiment involving (15S,17 E)-[15-3H1,17-2H1] CPP gave [16-3H1,16-2H1] abietadiene where the stereochemistry of the methyl was established as R by degradation and enzymatic analysis of the generated chiral methyl acetic acid. This indicated a surprising syn facial relationship of the intramolecular proton transfer and methyl migration on the si face of the terminal olefin affected by rAS ...
The goals of the present study were to elucidate the structural basis of bisphosphonates interaction with hGGPPS and to determine the accurate metal-ligand interaction network underlying GGPPS-bisphosphonate binding. In addition, given that mevalonate pathway enzymes, and specifically GGPPS, were highlighted in recent years as potential drug targets (Andela et al., 2003; Jiang et al., 2014; Gruenbacher and Thurnher, 2015), we sought to provide a reliable model for future drug design and screening. Importantly, preclinical studies have established the potential use of GGPPS inhibitors in the treatment of solid and hematologic malignancies, such as lung alveolar carcinoma (Andela et al., 2003), breast cancer (Ginestier et al., 2012), multiple myeloma (Lacbay et al., 2018), metastatic prostate cancer (Reilly et al., 2015, 2017), and KRAS-mutant lung cancer (Xia et al., 2014). Moreover, GGPPS enzymes from parasites leading to human diseases such as malaria, Chagas disease, leishmaniasis, and ...
2.A.66.2 The Polysaccharide Transport (PST) Family. The protein members of the PST family are generally of 400-500 amino acyl residues in size and traverse the membrane as putative α-helical spanners twelve times. Analyses conducted in 1997 showed that they formed two major clusters. One is concerned with lipopolysaccharide O-antigen (undecaprenol pyrophosphate-linked O-antigen repeat unit) export (flipping from the cytoplasmic side to the periplasmic side of the inner membranes) in Gram-negative bacteria. On the periplasmic side, polymerization occurs catalyzed by Wzy. The other is concerned with exopolysaccharide or capsular polysaccharide export in both Gram-negative and Gram-positive bacteria. However, arachaeal and eukaryotic homologues are now recognized. The mechanism of energy coupling is not established, but homology with the MATE family suggests that they are secondary carriers. A review of Wzx undecaprenyl pyrophosphate (UndPP)-linked polysaccharide repeat units occurs by a ...
Farnesyltransferase (FTase) is a zinc enzyme that has been the subject of particular attention in anti-cancer research. This enzyme promotes the addition of a farnesyl group from farnesyl diphosphate (FPP) to a cysteine residue of a protein substrate containing a typical -CAAX motif at the carboxyl …
60037-55-0 - IVLBHBFTRNVIAP-MEGGAXOGSA-N - Solanesyl pyrophosphate - Similar structures search, synonyms, formulas, resource links, and other chemical information.
Complete information for FDPSP8 gene (Pseudogene), Farnesyl Diphosphate Synthase Pseudogene 8, including: function, proteins, disorders, pathways, orthologs, and expression. GeneCards - The Human Gene Compendium
ethyl linalyl acetate 1 | C13H24O2 | CID 526765 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
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Song, L. (2006). „A soluble form of phosphatase in Saccharomyces cerevisiae capable of converting farnesyl diphosphate into E,E-farnesol. Appl. Biochem. Biotechnol. 128: 149-158. PMID 16484724 ...
Gene target information for Fdps - farnesyl diphosphate synthetase (house mouse). Find diseases associated with this biological target and compounds tested against it in bioassay experiments.
This page includes the following topics and synonyms: Conenzyme Q10, Ubiquinone, CoQ, Vitamin Q10, 2,3 Dimethoxy-5-Methyl-6-Decaprenyl Benzoquinone.
Plasmid mIFP12-Farnesyl-5 from Dr. Michael Davidsons lab contains the insert Farnesyl and is published in Nat Methods. 2015 Aug;12(8):763-765. doi: 10.1038/nmeth.3447. Epub 2015 Jun 22. This plasmid is available through Addgene.