Search Results - "Grimley, Rachel L"

Mechanistic enzymology in drug discovery: a fresh perspective by Holdgate, Geoffrey A., Meek, Thomas D., Grimley, Rachel L.

“…Key Points The application of detailed mechanistic enzyme kinetics is vital for the characterization of enzyme targets; furthermore, it is crucial to aid in…”
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(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells by Barsyte-Lovejoy, Dalia, Li, Fengling, Oudhoff, Menno J., Tatlock, John H., Dong, Aiping, Zeng, Hong, Wu, Hong, Freeman, Spencer A., Schapira, Matthieu, Senisterra, Guillermo A., Kuznetsova, Ekaterina, Marcellus, Richard, Allali-Hassani, Abdellah, Kennedy, Steven, Lambert, Jean-Philippe, Couzens, Amber L., Aman, Ahmed, Gingras, Anne-Claude, Al-Awar, Rima, Fish, Paul V., Gerstenberger, Brian S., Roberts, Lee, Benn, Caroline L., Grimley, Rachel L., Braam, Mitchell J. S., Rossi, Fabio M. V., Sudol, Marius, Brown, Peter J., Bunnage, Mark E., Owen, Dafydd R., Zaph, Colby, Vedadi, Masoud, Arrowsmith, Cheryl H.

“…SET domain containing (lysine methyltransferase) 7 (SETD7) is implicated in multiple signaling and disease related pathways with a broad diversity of reported…”
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Discovery and Characterization of Small Molecule Inhibitors of the BET Family Bromodomains by Chung, Chun-wa, Coste, Hervé, White, Julia H, Mirguet, Olivier, Wilde, Jonathan, Gosmini, Romain L, Delves, Chris, Magny, Sylvie M, Woodward, Robert, Hughes, Stephen A, Boursier, Eric V, Flynn, Helen, Bouillot, Anne M, Bamborough, Paul, Brusq, Jean-Marie G, Gellibert, Françoise J, Jones, Emma J, Riou, Alizon M, Homes, Paul, Martin, Sandrine L, Uings, Iain J, Toum, Jérôme, Clément, Catherine A, Boullay, Anne-Bénédicte, Grimley, Rachel L, Blandel, Florence M, Prinjha, Rab K, Lee, Kevin, Kirilovsky, Jorge, Nicodeme, Edwige

“…Epigenetic mechanisms of gene regulation have a profound role in normal development and disease processes. An integral part of this mechanism occurs through…”
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Mechanistic enzymology in drug discovery: a fresh perspective by Holdgate, Geoffrey A, Meek, Thomas D, Grimley, Rachel L

“…This corrects the article DOI: 10.1038/nrd.2017.219…”
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Identification of Histone Peptide Binding Specificity and Small-Molecule Ligands for the TRIM33α and TRIM33β Bromodomains by Sekirnik, Angelina R., Reynolds, Jessica K., See, Larissa, Bluck, Joseph P., Scorah, Amy R., Tallant, Cynthia, Lee, Bernadette, Leszczynska, Katarzyna B., Grimley, Rachel L., Storer, R. Ian, Malattia, Marta, Crespillo, Sara, Caria, Sofia, Duclos, Stephanie, Hammond, Ester M., Knapp, Stefan, Morris, Garrett M., Duarte, Fernanda, Biggin, Philip C., Conway, Stuart J.

“…TRIM33 is a member of the tripartite motif (TRIM) family of proteins, some of which possess E3 ligase activity and are involved in the ubiquitin-dependent…”
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Design and development of histone deacetylase (HDAC) chemical probes for cell-based profiling by Albrow, Victoria E, Grimley, Rachel L, Clulow, James, Rose, Colin R, Sun, Jianmin, Warmus, Joseph S, Tate, Edward W, Jones, Lyn H, Storer, R Ian

“…Histone deacetylases (HDACs) contribute to regulation of gene expression by mediating higher-order chromatin structures. They assemble into large multiprotein…”
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Bridging the gap between in silico and cell‐based analysis of the nuclear factor‐κB signaling pathway by in vitro studies of IKK2 by Ihekwaba, Adaoha E. C, Wilkinson, Stephen J, Waithe, Dominic, Broomhead, David S, Li, Peter, Grimley, Rachel L, Benson, Neil

“…Previously, we have shown by sensitivity analysis, that the oscillatory behavior of nuclear factor (NF‐κB) is coupled to free IkappaB kinase‐2 (IKK2) and…”
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Erratum: Mechanistic enzymology in drug discovery: a fresh perspective by Holdgate, Geoffrey A., Meek, Thomas D., Grimley, Rachel L.

“…Nature Reviews Drug Discovery, 10.1038/nrd.2017.219 (2017) In the affiliations of this article, the address provided for Discovery Sciences, IMED Biotech Unit,…”
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Evidence That the Transfer of Hydride Ion Equivalents between Nucleotides by Proton-translocating Transhydrogenase Is Direct by Venning, Jamie D., Grimley, Rachel L., Bizouarn, Tania, Cotton, Nick P.J., Jackson, J. Baz

“…The molecular masses of the purified, recombinant nucleotide-binding domains (domains I and III) of transhydrogenase from Rhodospirillum rubrum were determined…”
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Interaction of Nucleotides with the NAD(H)-binding Domain of the Proton-translocating Transhydrogenase of Rhodospirillum rubrum by Bizouarn, T, Diggle, C, Quirk, P G, Grimley, R L, Cotton, N P, Thomas, C M, Jackson, J B

“…Transhydrogenase catalyzes the reduction of NADP by NADH coupled to the translocation of protons across a membrane. The polypeptide composition of the enzyme…”
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Role of Methionine-239, an Amino Acid Residue in the Mobile-Loop Region of the NADH-Binding Domain (Domain I) of Proton-Translocating Transhydrogenase by Grimley, Rachel L, Quirk, Philip G, Bizouarn, Tania, Thomas, Christopher M, Jackson, J. Baz

“…Transhydrogenase couples the transfer of hydride equivalents between NAD(H) and NADP(H) to proton translocation across a membrane. The one-dimensional proton…”
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Mutation of Tyr in the NAD(H)-binding Subunit of the Proton-translocating Nicotinamide Nucleotide Transhydrogenase of Rhodospirillum rubrum Affects the Conformational Dynamics of a Mobile Loop and Lowers the Catalytic Activity of the Enzyme by Christine Diggle, Philip G. Quirk, Tania Bizouarn, Rachel L. Grimley, Nick P. J. Cotton, Christopher M. Thomas, J. Baz Jackson

“…The Tyr residue in the mobile loop region of the soluble, domain I polypeptide (called Th s ) of the proton-translocating transhydrogenase from Rhodospirillum…”
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Bridging the gap between in silico and cell-based analysis of the nuclear factor-kappaB signaling pathway by in vitro studies of IKK2 by Ihekwaba, Adaoha E C, Wilkinson, Stephen J, Waithe, Dominic, Broomhead, David S, Li, Peter, Grimley, Rachel L, Benson, Neil

“…Previously, we have shown by sensitivity analysis, that the oscillatory behavior of nuclear factor (NF-kappaB) is coupled to free IkappaB kinase-2 (IKK2) and…”
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Bridging the gap between in silico and cell-based analysis of the nuclear factor-[kappa]B signaling pathway by in vitro studies of IKK2 by Adaoha E. C. Ihekwaba, Wilkinson, Stephen J, Waithe, Dominic, Broomhead, David S, Li, Peter, Grimley, Rachel L, Benson, Neil

“…Previously, we have shown by sensitivity analysis, that the oscillatory behavior of nuclear factor (NF-kappaB) is coupled to free IkappaB kinase-2 (IKK2) and…”
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The involvement of NADP(H) binding and release in energy transduction by proton-translocating nicotinamide nucleotide transhydrogenase from Escherichia coli by Bizouarn, Tania, Grimley, Rachel L., Cotton, Nick P.J., Stilwell, Shaun N., Hutton, Mike, Jackson, J.Baz

“…Proton-translocating transhydrogenase was solubilised and purified from membranes of Escherichia coli. Consistent with recent evidence [Hutton, M., Day, J.,…”
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Mutation of amino acid residues in the mobile loop region of the NAD(H)-binding domain of proton-translocating transhydrogenase by Gupta, Susmita, Quirk, Philip G., Venning, Jamie D., Slade, James, Bizouarn, Tania, Grimley, Rachel L., Cotton, Nick P.J., Jackson, J.Baz

“…The effects of single amino acid substitutions in the mobile loop region of the recombinant NAD(H)-binding domain (dI) of transhydrogenase have been examined…”
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Mutation of Tyr235 in the NAD(H)-binding subunit of the proton-translocating nicotinamide nucleotide transhydrogenase of Rhodospirillum rubrum affects the conformational dynamics of a mobile loop and lowers the catalytic activity of the enzyme by Diggle, C, Quirk, P G, Bizouarn, T, Grimley, R I, Cotton, N P, Thomas, C M, Jackson, J B

“…The Tyr residue in the mobile loop region of the soluble, domain I polypeptide (called Ths) of the proton-translocating transhydrogenase from Rhodospirillum…”
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Conformational Dynamics of a Mobile Loop in the NAD(H)‐Binding Subunit of Proton‐Translocating Transhydrogenases from Rhodospirillum Rubrum and Escherichia Coli by Diggle, Christine, Cotton, Nick P. J., Grimley, Rachel L., Quirk, Philip G., Thomas, Christopher M., Jackson, J. Baz

“…Transhydrogenase catalyses the reversible transfer of reducing equivalents between NAD(H) and NADP(H) to the translocation of protons across a membrane…”
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Crystallization of the dI component of transhydrogenase, a proton-translocating membrane protein by Sedelnikova, Sveta E., Burke, Jackie, Buckley, Patrick A., Rice, David W., Jackson, J. Baz, Cotton, Nick P. J., Grimley, Rachel L., Baker, Patrick J.

“…Nicotinamide nucleotide transhydrogenase couples the exchange of a hydride‐ion equivalent between NAD(H) and NADP(H) to the translocation of protons across an…”
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