Search Results - "Mellor, Geoffrey W."

Temperature-dependences of the kinetics of reactions of papain and actinidin with a series of reactivity probes differing in key molecular recognition features by Gul, Sheraz, Mellor, Geoffrey W, Thomas, Emrys W, Brocklehurst, Keith

“…The temperature-dependences of the second-order rate constants (k) of the reactions of the catalytic site thiol groups of two cysteine peptidases papain (EC…”
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Rational design of 4-amino-5,6-diaryl-furo[2,3- d]pyrimidines as potent glycogen synthase kinase-3 inhibitors by Miyazaki, Yasushi, Maeda, Yutaka, Sato, Hideyuki, Nakano, Masato, Mellor, Geoffrey W.

“…4-Amino-5,6-diaryl-furo[2,3- d]pyrimidines have been identified as inhibitors of glycogen synthase kinase-3β (GSK-3β). One representative derivative,…”
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Discovery of 6-Aryl-7-alkoxyisoquinoline Inhibitors of IκB Kinase-β (IKK-β) by Christopher, John A, Bamborough, Paul, Alder, Catherine, Campbell, Amanda, Cutler, Geoffrey J, Down, Kenneth, Hamadi, Ahmed M, Jolly, Adrian M, Kerns, Jeffrey K, Lucas, Fiona S, Mellor, Geoffrey W, Miller, David D, Morse, Mary A, Pancholi, Kiritkant D, Rumsey, William, Solanke, Yemisi E, Williamson, Rick

“…The identification and progression of a potent and selective series of isoquinoline inhibitors of IκB kinase-β (IKK-β) are described. Hit-generation chemistry…”
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The discovery of 2-amino-3,5-diarylbenzamide inhibitors of IKK-α and IKK-β kinases by Christopher, John A., Avitabile, Barbara G., Bamborough, Paul, Champigny, Aurelie C., Cutler, Geoffrey J., Dyos, Susan L., Grace, Ken G., Kerns, Jeffrey K., Kitson, Jeremy D., Mellor, Geoffrey W., Morey, James V., Morse, Mary A., O’Malley, Carolyn F., Patel, Champa B., Probst, Nicholas, Rumsey, William, Smith, Clive A., Wilson, Michael J.

“…A potent and selective series of 2-amino-3,5-diarylbenzamide inhibitors of IKK-α and IKK-β is described. The most potent compounds are 8h, 8r and 8v, with…”
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3,5-Disubstituted-indole-7-carboxamides: The discovery of a novel series of potent, selective inhibitors of IKK-β by Miller, David D., Bamborough, Paul, Christopher, John A., Baldwin, Ian R., Champigny, Aurelie C., Cutler, Geoffrey J., Kerns, Jeffrey K., Longstaff, Timothy, Mellor, Geoffrey W., Morey, James V., Morse, Mary A., Nie, Hong, Rumsey, William L., Taggart, John J.

“…The discovery and hit-to-lead exploration of a novel series of selective IKK-β kinase inhibitors is described. The initial lead fragment 3 was identified by…”
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5-(1 H-Benzimidazol-1-yl)-3-alkoxy-2-thiophenecarbonitriles as potent, selective, inhibitors of IKK-ε kinase by Bamborough, Paul, Christopher, John A., Cutler, Geoffrey J., Dickson, Marion C., Mellor, Geoffrey W., Morey, James V., Patel, Champa B., Shewchuk, Lisa M.

“…The identification and hit-to-lead exploration of a novel, potent, and selective series of substituted benzimidazole-thiophene carbonitrile inhibitors of IKK-…”
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Development and validation of a fluoroimmunoassay for urinary normetanephrine by Gallacher, G, Mellor, G W, Landon, J, Sjostrom, L

“…The development of a separation fluoroimmunoassay for urinary normetanephrine is described. Antiserum specific to normetanephrine was coupled, using cyanogen…”
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3,5-Disubstituted-indole-7-carboxamides: The discovery of a novel series of potent, selective inhibitors of IIK-β by MILLER, David D, BAMBOROUGH, Paul, MORSE, Mary A, HONG NIE, RUMSEY, William L, TAGGART, John J, CHRISTOPHER, John A, BALDWIN, Ian R, CHAMPIGNY, Aurelie C, CUTLER, Geoffrey J, KERNS, Jeffrey K, LONGSTAFF, Timothy, MELLOR, Geoffrey W, MOREY, James V

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Discovery of 6-Aryl-7-alkoxyisoquinoline Inhibitors of IKB Kinase-β (IKK-β) by CHRISTOPHER, John A, BAMBOROUGH, Paul, MELLOR, Geoffrey W, MILLER, David D, MORSE, Mary A, PANCHOLI, Kiritkant D, RUMSEY, William, SOLANKE, Yemisi E, WILLIAMSON, Rick, ALDER, Catherine, CAMPBELL, Amanda, CUTLER, Geoffrey J, DOWN, Kenneth, HAMADI, Ahmed M, JOLLY, Adrian M, KERNS, Jeffrey K, LUCAS, Fiona S

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Discovery of 6-aryl-7-alkoxyisoquinoline inhibitors of IkappaB kinase-beta (IKK-beta) by Christopher, John A, Bamborough, Paul, Alder, Catherine, Campbell, Amanda, Cutler, Geoffrey J, Down, Kenneth, Hamadi, Ahmed M, Jolly, Adrian M, Kerns, Jeffrey K, Lucas, Fiona S, Mellor, Geoffrey W, Miller, David D, Morse, Mary A, Pancholi, Kiritkant D, Rumsey, William, Solanke, Yemisi E, Williamson, Rick

“…The identification and progression of a potent and selective series of isoquinoline inhibitors of IkappaB kinase-beta (IKK-beta) are described. Hit-generation…”
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Characterization of the Electrostatic Perturbation of a Catalytic Site (Cys)-S –/(His)-Im +H Ion-pair in One Type of Serine Proteinase Architecture by Kinetic and Computational Studies on Chemically Mutated Subtilisin Variants by Plou, Francisco J., Kowlessur, Devanand, Malthouse, Paul G.J., Mellor, Geoffrey W., Hartshorn, Michael J., Pinitglang, Surapong, Patel, Hasu, Topham, Christopher M., Thomas, Emrys W., Verma, Chandra, Brocklehurst, Keith

“…We have used two structurally well-characterized serine proteinase variants, subtilisins Carlsberg and BPN′, to produce (Cys)-S −/(His)-Im +H ion-pairs by…”
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Fluorescence polarization immunoassay of urinary vanillylmandelic acid by Mellor, G W, Gallacher, G

“…This rapid fluorescence polarization immunoassay for urinary vanillylmandelic acid (VMA) involves use of our previously described antiserum and label and the…”
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The kinetically influential ionizations of chymopapain M by Thomas, M P, Mellor, G W, Brocklehurst, K

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Evidence from activation parameters for enzyme active centre desolvation promoted by specific binding interactions by Mellor, G W, Thomas, M P, Gul, S, Noble, M A, Thomas, E W, Brocklehurst, K

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Ficin: a cysteine proteinase with binding site-catalytic site signalling characteristics intermediate between those of papain and actinidin by Patel, M, Thomas, M P, Kayani, I S, Mellor, G W, Thomas, E W, Brocklehurst, K

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New substrate-derived thiol-specific time-dependent inhibitors for the characterisation of the coupling of binding site interactions with catalytic site chemistry in the cysteine proteinases by Mellor, G W, Patel, M, Thomas, M P, Kowlessur, D, Sreedharan, S K, Thomas, E W, Brocklehurst, K

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Catalytic antibody activity elicited by active immunisation : evidence for natural variation involving preferential stabilization of the transition state by GALLACHER, G, JACKON, C. S, SEARCEY, M, GOEL, R, MELLOR, G. W, SMITH, C. Z, BROCKLEHURST, K

“…1. The hydrolytic activity of IgG purified from (a) 13 samples of ovine antiserum collected from three animals during a two-year immunisation programme using a…”
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Comparison of three different activation methods for coupling antibodies to magnetisable cellulose particles by al-Abdulla, I H, Mellor, G W, Childerstone, M S, Sidki, A M, Smith, D S

“…The periodate and 1,1'-carbonyldiimidazole activation methods were compared with the cyanogen bromide procedure for coupling antibodies to magnetisable…”
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Catalytic antibody activity elicited by active immunisation by GALLACHER, Gerard, JACKSON, Caroline S., SEARCEY, Mark, GOEL, Rajiv, MELLOR, Geoffrey W., SMITH, Carmen Z., BROCKLEHURST, Keith

“…1 The hydrolytic activity of IgG purified from (a) 13 samples of ovine antiserum collected from three animals during a two‐year immunisation programme using a…”
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