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Targeting low-druggability bromodomains fragment based screening and inhibitor design against the BAZ2B bromodomain

Fleur M. Ferguson Oleg Fedorov; Apirat Chaikuad; Martin Philpott; João Renato Carvalho Muniz; Ildiko Felletar; Frank von Delft; Tom Heightman; Stefan Knapp; Chris Abell; Alessio Ciulli

Journal of Medicinal Chemistry Washington, DC : American Chemical Society - ACS v. 56, n. 24, p. 10183-10187, Dec. 2013

Washington, DC American Chemical Society - ACS 2013

Localização: IFSC - Inst. Física de São Carlos    (PROD021601 )(Acessar)

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Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl3,4-apyrrolo3,4-ccarbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models

Hudkins, Robert L ; Diebold, James L ; Tao, Ming ; Josef, Kurt A ; Park, Chung Ho ; Angeles, Thelma S ; Aimone, Lisa D ; Husten, Jean ; Ator, Mark A ; Meyer, Sheryl L ; Holskin, Beverly P ; Durkin, John T ; Fedorov, Alexander A ; Fedorov, Elena V ; Almo, Steven C ; Mathiasen, Joanne R ; Bozyczko-Coyne, Donna ; Saporito, Michael S ; Scott, Richard W ; Mallamo, John P

Journal of medicinal chemistry, 25 September 2008, Vol.51(18), pp.5680-9 [Periódico revisado por pares]

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3
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Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors

Popp, Tobias A ; Tallant, Cynthia ; Rogers, Catherine ; Fedorov, Oleg ; Brennan, Paul E ; Müller, Susanne ; Knapp, Stefan ; Bracher, Franz

Journal of medicinal chemistry, 13 October 2016, Vol.59(19), pp.8889-8912 [Periódico revisado por pares]

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4
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Discovery of (2S,3R)-N-2-(pyridin-3-ylmethyl)-1-azabicyclo2.2.2oct-3-ylbenzobfuran-2-carboxamide (TC-5619), a selective α7 nicotinic acetylcholine receptor agonist, for the treatment of cognitive disorders

Mazurov, Anatoly A ; Kombo, David C ; Hauser, Terry A ; Miao, Lan ; Dull, Gary ; Genus, John F ; Fedorov, Nikolai B ; Benson, Lisa ; Sidach, Serguei ; Xiao, Yunde ; Hammond, Philip S ; James, John W ; Miller, Craig H ; Yohannes, Daniel

Journal of medicinal chemistry, 26 November 2012, Vol.55(22), pp.9793-809 [Periódico revisado por pares]

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Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF

Bennett, James ; Fedorov, Oleg ; Tallant, Cynthia ; Monteiro, Octovia ; Meier, Julia ; Gamble, Vicky ; Savitsky, Pavel ; Nunez-Alonso, Graciela A ; Haendler, Bernard ; Rogers, Catherine ; Brennan, Paul E ; Müller, Susanne ; Knapp, Stefan

Journal of medicinal chemistry, 25 February 2016, Vol.59(4), pp.1642-7 [Periódico revisado por pares]

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6
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Structure-activity studies of 7-heteroaryl-3-azabicyclo3.3.1non-6-enes: a novel class of highly potent nicotinic receptor ligands

Breining, Scott R ; Melvin, Matt ; Bhatti, Balwinder S ; Byrd, Gary D ; Kiser, Melanie N ; Hepler, Christopher D ; Hooker, Dawn N ; Zhang, Jenny ; Reynolds, Leslie A ; Benson, Lisa R ; Fedorov, Nikolai B ; Sidach, Serguei S ; Mitchener, J Pike ; Lucero, Linda M ; Lukas, Ronald J ; Whiteaker, Paul ; Yohannes, Daniel

Journal of medicinal chemistry, 26 November 2012, Vol.55(22), pp.9929-45 [Periódico revisado por pares]

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Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit

Gerstenberger, Brian S ; Trzupek, John D ; Tallant, Cynthia ; Fedorov, Oleg ; Filippakopoulos, Panagis ; Brennan, Paul E ; Fedele, Vita ; Martin, Sarah ; Picaud, Sarah ; Rogers, Catherine ; Parikh, Mihir ; Taylor, Alexandria ; Samas, Brian ; O'Mahony, Alison ; Berg, Ellen ; Pallares, Gabriel ; Torrey, Adam D ; Treiber, Daniel K ; Samardjiev, Ivan J ; Nasipak, Brian T ; Padilla-Benavides, Teresita ; Wu, Qiong ; Imbalzano, Anthony N ; Nickerson, Jeffrey A ; Bunnage, Mark E ; Müller, Susanne ; Knapp, Stefan ; Owen, Dafydd R

Journal of medicinal chemistry, 26 May 2016, Vol.59(10), pp.4800-11 [Periódico revisado por pares]

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8
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8-Substituted Pyrido3,4-dpyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors

Bavetsias, Vassilios ; Lanigan, Rachel M ; Ruda, Gian Filippo ; Atrash, Butrus ; Mclaughlin, Mark G ; Tumber, Anthony ; Mok, N Yi ; Le Bihan, Yann-Vaï ; Dempster, Sally ; Boxall, Katherine J ; Jeganathan, Fiona ; Hatch, Stephanie B ; Savitsky, Pavel ; Velupillai, Srikannathasan ; Krojer, Tobias ; England, Katherine S ; Sejberg, Jimmy ; Thai, Ching ; Donovan, Adam ; Pal, Akos ; Scozzafava, Giuseppe ; Bennett, James M ; Kawamura, Akane ; Johansson, Catrine ; Szykowska, Aleksandra ; Gileadi, Carina ; Burgess-Brown, Nicola A ; Von Delft, Frank ; Oppermann, Udo ; Walters, Zoe ; Shipley, Janet ; Raynaud, Florence I ; Westaway, Susan M ; Prinjha, Rab K ; Fedorov, Oleg ; Burke, Rosemary ; Schofield, Christopher J ; Westwood, Isaac M ; Bountra, Chas ; Müller, Susanne ; Van Montfort, Rob L M ; Brennan, Paul E ; Blagg, Julian

Journal of medicinal chemistry, 25 February 2016, Vol.59(4), pp.1388-409 [Periódico revisado por pares]

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Structure-Based Identification of Inhibitory Fragments Targeting the p300/CBP-Associated Factor Bromodomain

Chaikuad, A. ; Lang, S. ; Brennan, P.E. ; Temperini, C. ; Fedorov, O. ; Hollander, J. ; Nachane, R. ; Abell, C. ; Muller, S. ; Siegal, G.D.

Journal of medicinal chemistry

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Design of a chemical probe for the Bromodomain and Plant Homeodomain Finger-containing (BRPF) family of proteins

Igoe, N ; Bayle, Ed ; Tallant, C ; Fedorov, O ; Meier, Jc ; Savitsky, P ; Rogers, C ; Morias, Y ; Scholze, S ; Boyd, H ; Cunoosamy, D ; Andrews, Dm ; Cheasty, A ; Brennan, Pe ; Müller, S ; Knapp, S ; Fish, Pv

Journal of Medicinal Chemistry , 60 (16) pp. 6998-7011. (2017)

2017

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