Rare monosaccharides and biologically active iminosugars from carbohydrate chirons by Best, D

“…Access to hexosaminidase inhibiting acetamido- substituted piperidines is presented, including 2-acetamido-1,5-imino-1,2,5-trideoxy-D- galactitol, which has been found to be one of the few known potent and specific inhibitors of α- N-acetyl-galactosaminidase. This inhibitory profile may allow the compound’s use for further investigation of a strategy for cancer treatment.…”

Kinetic analysis of matrix metalloproteinase activity using fluorogenic triple-helical substrates. by Lauer-Fields, J, Broder, T, Sritharan, T, Chung, L, Nagase, H, Fields, G

“…The substrates were designed to incorporate the fluorophore/quencher pair of (7-methoxycoumarin-4-yl)acetyl (Mca) and N-2,4-dinitrophenyl (Dnp) in the P(5) and P(5)' positions, respectively. …”

Integrated modelling of whole-plant metabolism and growth by Konuntakiet, T

“…Relaxing model constraints for metabolite flow between organs revealed optimal patterns of resource partitioning and utilisation for improved growth, including leaf-based nitrate assimilation, increased amino acid transport in the phloem, threonine catabolism as a carbon-efficient route for acetyl-CoA production, and branch-chain amino acids as a respiratory substrate. …”

Epigenetic pathway inhibitors represent potential drugs for treating pancreatic and bronchial neuroendocrine tumors by Lines, K, Stevenson, M, Filippakopoulos, P, Müller, S, Lockstone, H, Wright, B, Grozinsky-Glasberg, S, Grossman, A, Knapp, S, Buck, D, Bountra, C, Thakker, R

“…Two inhibitors, referred to as (+)-JQ1 (JQ1) and PFI-1, targeting the bromo and extra terminal (BET) protein family which bind acetylated histone residues, were most effective in decreasing proliferation (by 40-85%, P<0.001) and increasing apoptosis (by 2-3.6 fold, P<0.001) in all 3 NET cell lines. …”

Effect of nitric oxide on the differentiation of fibroblasts into myofibroblasts in the Peyronie's fibrotic plaque and in its rat model. by Vernet, D, Ferrini, MG, Valente, E, Magee, T, Bou-Gharios, G, Rajfer, J, Gonzalez-Cadavid, N

“…Induction of iNOS in PD and TA cultures with a cytokine cocktail and a NO donor, S-nitroso-N-acetyl penicillamine (SNAP), was detected by immunohistochemistry. …”

Integrative approaches in fragment-based drug discovery by Grosjean, H

“…Chapter 3 reports a crystallographic fragment screening against PHIP(2), resolving 47 fragments at the acetylated-lysine binding site, and evaluates the abilities of crowdsourced computational methods to replicate fragment binding and crystallographic poses. …”

N-ethyl-N-Nitrosourea (ENU) induced mutations within the klotho gene lead to ectopic calcification and reduced lifespan in mouse models by Esapa, C, Hannan, F, Babinsky, V, Potter, P, Thomas, G, Croucher, P, Brown, M, Brown, S, Cox, R, Thakker, R

“…For example, studies of tumoural calcinosis, a disorder characterised by hyperphosphataemia and progressive EC, have revealed mutations of fibroblast growth factor 23 (<em>FGF23</em>), polypeptide N-acetyl galactosaminyltransferase 3 (<em>GALNT3</em>) and klotho (KL), which are all part of a phosphate-regulating pathway. …”

Proteomic and metabolomic changes driven by elevating myocardial creatine suggest novel metabolic feedback mechanisms. by Zervou, S, Yin, X, A Nabeebaccus, A, O'Brien, B, L Cross, R, McAndrew, D, Atkinson, R, Eykyn, T, Mayr, M, Neubauer, S, Lygate, C

“…For example, positive correlations with α-glucose (r² = 0.45; P = 0.002), acetyl-carnitine (r² = 0.50; P = 0.001), glutamine (r² = 0.59; P = 0.0002); and negative correlations with taurine (r² = 0.74; P &lt; 0.0001), fumarate (r² = 0.45; P = 0.003), aspartate (r² = 0.59; P = 0.0002), alanine (r² = 0.66; P &lt; 0.0001) and phosphocholine (r² = 0.60; P = 0.0002). …”

Interplay between chromatin conformation and transcription in eukaryotes by Bhardwaj, S

“…Cohesive cohesin ensures stable cohesion because it is acetylated by the Eso1 acetyltransferase, which preferentially interacts with Mis4. …”

Solution structure and characterisation of the human pyruvate dehydrogenase complex core assembly. by Vijayakrishnan, S, Kelly, S, Gilbert, R, Callow, P, Bhella, D, Forsyth, T, Lindsay, J, Byron, O

“…Mammalian pyruvate dehydrogenase complex (PDC) is a key multi-enzyme assembly that is responsible for glucose homeostasis maintenance and conversion of pyruvate into acetyl-CoA. It comprises a central pentagonal dodecahedral core consisting of two subunit types (E2 and E3BP) to which peripheral enzymes (E1 and E3) bind tightly but non-covalently. …”

Mutate & conjugate: a method for rapid in-cell validation of epigenetic targets by Thomas, AM

“…Bromodomains are epigenetic ‘reader’ modules that recognise and bind to acetylated lysines on histone tails, and signal for the recruitment of protein complexes responsible for gene regulation. …”

Melatonin augments hypothermic neuroprotection in a perinatal asphyxia model. by Robertson, N, Faulkner, S, Fleiss, B, Bainbridge, A, Andorka, C, Price, D, Powell, E, Lecky-Thompson, L, Thei, L, Chandrasekaran, M, Hristova, M, Cady, E, Gressens, P, Golay, X, Raivich, G

“…Melatonin-augmented hypothermia significantly reduced the hypoxic-ischaemic-induced increase in the area under the curve for proton magnetic resonance spectroscopy lactate/N-acetyl aspartate and lactate/total creatine ratios in the deep grey matter. …”

Effects of C-1-substituted glucose analogue on the activation states of glycogen synthase and glycogen phosphorylase in rat hepatocytes. by Board, M, Bollen, M, Stalmans, W, Kim, Y, Fleet, G, Johnson, L

“…The aim is to produce a compound that may exert more effective control over glycogen metabolism than the parent glucose molecule and which could alleviate hyperglycaemia in Type-II diabetes. N-Acetyl-beta-D-glucopyranosylamine (1-GlcNAc) has a Ki for muscle GPb in crude extracts of 30 microM, 367-fold lower than that of beta-D-glucose [Board, Hadwen and Johnson (1995) Eur. …”

Metabolic profiling of angiopoietin-like protein 3 and 4 inhibition: a drug-target Mendelian randomization analysis by Wang, Q, Oliver-Williams, C, Raitakari, OT, Viikari, J, Lehtimäki, T, Kähönen, M, Järvelin, M-R, Salomaa, V, Perola, M, Danesh, J, Kettunen, J, Butterworth, AS, Holmes, MV, Ala-Korpela, M

“…All three genotypes associated with lower concentrations of an inflammatory biomarker glycoprotein acetyls and genetic mimicry of ANGPTL3 inhibition and LPL enhancement were also associated with lower C-reactive protein. …”

Interferon-gamma and nitric oxide synthase 2 mediate the aggregation of resident adherent peritoneal exudate cells: implications for the host response to pathogens by Chandrasekar, BS, Yadav, S, Victor, ES, Majumdar, S, Deobagkar-Lele, M, Wadhwa, N, Podder, S, Das, M, Nandi, D

“…Studies with NG-methyl-L-arginine (LNMA), an inhibitor of Nitric oxide synthase (Nos), NO donors, e.g., S-nitroso-N-acetyl-DL-penicillamine (SNAP) or Diethylenetriamine/nitric oxide adduct (DETA/NO), and <em>Nos2</em>^-/- mice identified Nitric oxide (NO) induced by Ifnγ as a key regulator of aggregation of APECs. …”

Metabolic signatures of genetically elevated vitamin D among Chinese: observational and Mendelian randomization study by Zhuang, Z, Yu, C, Guo, Y, Bian, Z, Yang, L, Millwood, IY, Walters, RG, Chen, Y, Xu, Q, Zou, M, Chen, J, Chen, Z, Lv, J, Huang, T, Li, L

“…For amino acids, fatty acids, ketone bodies, glycoprotein acetyls, fatty acids, and other traits, we did not observe any significant causal association. …”

OPENING OF CARBOHYDRATE 5,6-EPOXIDES WITH CHIRAL ACETATE AND PROPIONATE ENOLATE EQUIVALENTS ATTACHED TO THE IRON CHIRAL AUXILIARY [C5H5)FE(CO)(PPH(3))] by Davies, S, Kellie, H, Polywka, R

“…The lithium enolate derived from the chiral iron acetyl complex (RS)-[(C5H5)Fe(CO)(PPh3)COCH3] (RS)-1 opens, in the presence of boron trifluoride etherate, the carbohydrate 5,6-epoxides, 5,6-anhydro-3-O-benzyl-1,2-O-isopropylidene-α-D-allofuranose 3, 5,6-anhydro-3-O-benzyl-1,2-O-isopropylidene-β-L-talonofuranose 4, 5,6-anhydro-3-O-benzyl-1,2-O-isopropylidene-α-D-glucofuranose 5, and 5,6-anhydro-3-O-benzyl-1,2-O-isopropylidene-β-L-idofluranose 6 to generate after decomplexation the doubly homologated γ-lactones 3-O-benzyl-6,7-dideoxy-1,2-O-isopropylidene-α-D-allo-octafuranurono-5,8-lactone 15, 3-O-benzyl-6,7-dideoxy-1,2-O-isopropylidene-β-L-talono-octafuranurono-5,8-lactone 16, 3-O-benzyl-6,7-dideoxy-1,2-O-isopropylidene-α-D-gluco-octafuranurono-5,8-lactone 17, and 3-O-benzyl-6,7-dideoxy-1,2-O-isopropylidene-β-L-ido-octafuranurono-5,8-lactone 18 respectively. …”

Identification and characterization of a novel interaction between pulmonary surfactant protein D and decorin. by Nadesalingam, J, Bernal, A, Dodds, A, Willis, A, Mahoney, D, Day, A, Reid, K, Palaniyar, N

“…First, the direct binding and competition experiments show that the carbohydrate recognition domain (CRD) of SP-D binds in a calcium dependent-manner to the sulfated N-acetyl galactosamine moiety of the glycosaminoglycan chain. …”

Novel approaches to predictive developmental and reproductive toxicology by Verslype, A

“…By using both model organisms, I was able to detect developmental disruptions and changes in fatty acid accumulation caused by a selection of Acetyl-CoA Carboxylase (ACCase) inhibitors known to be teratogenic in mammals. …”

Propofol-based anaesthesia versus sevoflurane-based anaesthesia for living donor kidney transplantation: results of the VAPOR-1 randomized controlled trial by Nieuwenhuijs-Moeke, GJ, Nieuwenhuijs, VB, Seelen, MAJ, Berger, SP, Van Den Heuvel, MC, Burgerhof, JGM, Ottens, PJ, Ploeg, RJ, Leuvenink, HGD, Struys, MMRF

“…Concentrations of kidney injury molecule-1 (KIM-1), N-acetyl-β-d-glucosaminidase (NAG), and heart-type fatty acid binding protein (H-FABP) in the first urine upon reperfusion showed no differences. …”