Search Results - "Whitehead, Roger C."

Synthesis and Biological Evaluation of Coumarin-Based Inhibitors of NAD(P)H: Quinone Oxidoreductase-1 (NQO1) by Nolan, Karen A, Doncaster, Jeremy R, Dunstan, Mark S, Scott, Katherine A, Frenkel, A. David, Siegel, David, Ross, David, Barnes, John, Levy, Colin, Leys, David, Whitehead, Roger C, Stratford, Ian J, Bryce, Richard A

“…The synthesis is reported here of two novel series of inhibitors of human NAD(P)H quinone oxidoreductase-1 (NQO1), an enzyme overexpressed in several types of…”
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Deubiquitinases Regulate the Activity of Caspase-1 and Interleukin-1β Secretion via Assembly of the Inflammasome by Lopez-Castejon, Gloria, Luheshi, Nadia M., Compan, Vincent, High, Stephen, Whitehead, Roger C., Flitsch, Sabine, Kirov, Aleksandr, Prudovsky, Igor, Swanton, Eileithyia, Brough, David

“…IL-1β is a potent pro-inflammatory cytokine produced in response to infection or injury. It is synthesized as an inactive precursor that is activated by the…”
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Synthesis of Stereoenriched Piperidines via Chemo-Enzymatic Dearomatization of Activated Pyridines by Harawa, Vanessa, Thorpe, Thomas W., Marshall, James R., Sangster, Jack J., Gilio, Amelia K., Pirvu, Lucian, Heath, Rachel S., Angelastro, Antonio, Finnigan, James D., Charnock, Simon J., Nafie, Jordan W., Grogan, Gideon, Whitehead, Roger C., Turner, Nicholas J.

“…The development of efficient and sustainable methods for the synthesis of nitrogen heterocycles is an important goal for the chemical industry. In particular,…”
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Eeyarestatin 24 impairs SecYEG‐dependent protein trafficking and inhibits growth of clinically relevant pathogens by Steenhuis, Maurice, Koningstein, Gregory M., Oswald, Julia, Pick, Tillman, O’Keefe, Sarah, Koch, Hans‐Georg, Cavalié, Adolfo, Whitehead, Roger C., Swanton, Eileithyia, High, Stephen, Luirink, Joen

“…Eeyarestatin 1 (ES1) is an inhibitor of endoplasmic reticulum (ER) associated protein degradation, Sec61‐dependent Ca2+ homeostasis and protein translocation…”
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Negative Cooperativity in NAD(P)H Quinone Oxidoreductase 1 (NQO1) by Megarity, Clare F., Abdel‐Aal Bettley, Hoda, Caraher, M. Clare, Scott, Katherine A., Whitehead, Roger C., Jowitt, Thomas A., Gutierrez, Aldo, Bryce, Richard A., Nolan, Karen A., Stratford, Ian J., Timson, David J.

“…NAD(P)H quinone oxidoreductase‐1 (NQO1) is a homodimeric protein that acts as a detoxifying enzyme or as a chaperone protein. Dicourmarol interacts with NQO1…”
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Structural determination of oleanane-28,13β-olide and taraxerane-28,14β-olide fluoro-lactonization products from the reaction of oleanolic acid with SelectfluorTM by Eadsforth, Megan A, Kong, Linghan, Whitehead, George, Vitórica-Yrezábal, Iñigo J, O'Keefe, Raymond T, Bryce, Richard A, Whitehead, Roger C

“…The X-ray crystal structure data of 12-α-fluoro-3β-hy-droxy-olean-28,13β-olide methanol hemisolvate, 2C30H47FO3·CH3OH, (1), and…”
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Dual Action of Eeyarestatin 24 on Sec-Dependent Protein Secretion and Bacterial DNA by Schäfer, Ann-Britt, Steenhuis, Maurice, Jim, Kin Ki, Neef, Jolanda, O’Keefe, Sarah, Whitehead, Roger C., Swanton, Eileithyia, Wang, Biwen, Halbedel, Sven, High, Stephen, van Dijl, Jan Maarten, Luirink, Joen, Wenzel, Michaela

“…Eeyarestatin 24 (ES24) is a promising new antibiotic with broad-spectrum activity. It shares structural similarity with nitrofurantoin (NFT), yet appears to…”
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Predisposition in synthesis: efficient routes to (±)-untenone A and (±)-manzamenones A, C and F by Al-Busafi, Saleh, Whitehead, Roger C

“…Short syntheses of (±)-untenone A, (±)-manzamenones A, C and F from 2-furanacetonitrile are described using an approach modelled on a likely biogenetic pathway…”
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Effective Separation of Am(III) from Cm(III) Using Modified BTPhen Ligands by M. Harwood, Laurence, Afsar, Ashfaq, C. Edwards, Alyn, Geist, Andreas, J. Hudson, Michael, Westwood, James, C. Whitehead, Roger

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Inhibition of protein translocation at the endoplasmic reticulum promotes activation of the unfolded protein response by McKibbin, Craig, Mares, Alina, Piacenti, Michela, Williams, Helen, Roboti, Peristera, Puumalainen, Marjo, Callan, Anna C, Lesiak-Mieczkowska, Karolina, Linder, Stig, Harant, Hanna, High, Stephen, Flitsch, Sabine L, Whitehead, Roger C, Swanton, Eileithyia

“…Selective small-molecule inhibitors represent powerful tools for the dissection of complex biological processes. ES(I) (eeyarestatin I) is a novel modulator of…”
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Novel Inhibitors of NRH:Quinone Oxidoreductase 2 (NQO2): Crystal Structures, Biochemical Activity, and Intracellular Effects of Imidazoacridin-6-ones by Dunstan, Mark S, Barnes, John, Humphries, Matthew, Whitehead, Roger C, Bryce, Richard A, Leys, David, Stratford, Ian J, Nolan, Karen A

“…Imidazoacridin-6-ones are shown to be potent nanomolar inhibitors of the enzyme NQO2. By use of computational molecular modeling, a reliable QSAR was…”
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A synthetic approach to novel carvotacetone and antheminone analogues with anti-tumour activity by Christou, Stephania, Ozturk, Emel, Pritchard, Robin G., Quayle, Peter, Stratford, Ian J., Whitehead, Roger C., Williams, Katharine F.

“…A synthetic approach to analogues of the terpenoid natural product antheminone A is described which employs (−)-quinic acid as starting material. A key…”
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Draft Genome Sequences of Pseudomonas putida UV4 and UV4/95, Toluene Dioxygenase-Expressing Producers of cis -1,2-Dihydrodiols by Skvortsov, Timofey, Hoering, Patrick, Arkhipova, Ksenia, Whitehead, Roger C, Boyd, Derek R, Allen, Christopher C R

“…Here, we present draft genome sequences of strains UV4 and UV4/95, which demonstrate an ability to conduct a wide range of industrially important…”
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The synthesis of 2-oxyalkyl-cyclohex-2-enones, related to the bioactive natural products COTC and antheminone A, which possess anti-tumour properties by Arthurs, Claire L., Morris, Gareth A., Piacenti, Michela, Pritchard, Robin G., Stratford, Ian J., Tatic, Tanja, Whitehead, Roger C., Williams, Katharine F., Wind, Natasha S.

“…The syntheses of five novel 2-oxyalkyl-cyclohex-2-enones, structurally related to the natural products COTC and antheminone A, are described. The target…”
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Triazoloacridin-6-ones as novel inhibitors of the quinone oxidoreductases NQO1 and NQO2 by Nolan, Karen A., Humphries, Matthew P., Barnes, John, Doncaster, Jeremy R., Caraher, Mary C., Tirelli, Nicola, Bryce, Richard A., Whitehead, Roger C., Stratford, Ian J.

“…A series of 5-, 8-substituted triazoloacridin-6-ones have been synthesized and biologically evaluated as novel inhibitors of the quinone oxidoreductases, NQO1…”
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Chemical predisposition in synthesis: application to the preparation of the pyrrolidine natural products, plakoridines A and B by Etchells, Laura L., Helliwell, Madeleine, Kershaw, Neil M., Sardarian, Ali, Whitehead, Roger C.

“…The pyrrolidine natural products, plakoridines A and B, as well as an array of unnatural analogues, have been prepared using a five-step synthetic sequence…”
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(−)-Quinic acid: a versatile precursor for the synthesis of analogues of 2-crotonyloxymethyl-(4 R,5 R,6 R)-4,5,6-trihydroxycyclohex-2-enone (COTC) which possess anti-tumour properties by Arthurs, Claire L., Lingley, Katharine F., Piacenti, Michela, Stratford, Ian J., Tatic, Tanja, Whitehead, Roger C., Wind, Natasha S.

“…Syntheses of three novel analogues of the Streptomyces metabolite COTC are described, using the versatile chiral pool starting material, (−)-quinic acid. The…”
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Analogues of 2-crotonyloxymethyl-(4 R,5 R,6 R)-4,5,6-trihydroxycyclohex-2-enone (COTC) with anti-tumor properties by Arthurs, Claire L., Wind, Natasha S., Whitehead, Roger C., Stratford, Ian J.

“…The syntheses of three novel analogues of the naturally occurring cytotoxic agent COTC are described and the results of bioassays of the target compounds…”
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Arene cis-dihydrodiols: Useful precursors for the preparation of analogues of the anti-tumour agent, 2-crotonyloxymethyl-(4 R,5 R,6 R)-4,5,6-trihydroxycyclohex-2-enone (COTC) by Arthurs, Claire L., Raftery, James, Whitby, Helen L., Whitehead, Roger C., Wind, Natasha S., Stratford, Ian J.

“…The synthesis of 6- epi-COTC, a diastereoisomer of Streptomyces metabolite 2-crotonyloxymethyl-(4 R,5 R,6 R)-4,5,6-trihydroxycyclohex-2-enone (COTC), is…”
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Arene cis-dihydrodiols—useful precursors for the preparation of antimetabolites of the shikimic acid pathway: application to the synthesis of 6,6-difluoroshikimic acid and (6 S)-6-fluoroshikimic acid by Humphreys, Jane L., Lowes, David J., Wesson, Karen A., Whitehead, Roger C.

“…The synthesis of 6,6-difluoroshikimic acid ( 11) has been achieved in ten steps from the enantiopure diol 16, which is derived from enzymatic…”
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