The Role of Protein Structural Analysis in the Next Generation Sequencing Era

Por Yue, Wyatt W., Froese, D. Sean, Brennan, Paul E.
Publicado no Chemical Diagnostics (2012)

Targeting the Small GTPase Superfamily through Their Regulatory Proteins

Por Gray, Janine L., von Delft, Frank, Brennan, Paul E.
Publicado no Angew Chem Int Ed Engl (2020)

TargetDB: A target information aggregation tool and tractability predictor

Por De Cesco, Stephane, Davis, John B., Brennan, Paul E.
Publicado no PLoS One (2020)

RHO to the DOCK for GDP disembarking: Structural insights into the DOCK GTPase nucleotide exchange factors

Por Thompson, Andrew P., Bitsina, Christina, Gray, Janine L., von Delft, Frank, Brennan, Paul E.
Publicado no J Biol Chem (2021)

Chemical probes and inhibitors of bromodomains outside the BET family

Por Moustakim, Moses, Clark, Peter G. K., Hay, Duncan A., Dixon, Darren J., Brennan, Paul E.
Publicado no Medchemcomm (2016)

Identifying Small‐Molecule Binding Sites for Epigenetic Proteins at Domain–Domain Interfaces

Por Bowkett, David, Talon, Romain, Tallant, Cynthia, Schofield, Chris, von Delft, Frank, Knapp, Stefan, Bruton, Gordon, Brennan, Paul E.
Publicado no ChemMedChem (2018)

Structural Insights into Interaction Mechanisms of Alternative Piperazine-urea YEATS Domain Binders in MLLT1

Por Ni, Xiaomin, Heidenreich, David, Christott, Thomas, Bennett, James, Moustakim, Moses, Brennan, Paul E., Fedorov, Oleg, Knapp, Stefan, Chaikuad, Apirat
Publicado no ACS Med Chem Lett (2019)

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

Por Chaikuad, Apirat, Lang, Steffen, Brennan, Paul E., Temperini, Claudia, Fedorov, Oleg, Hollander, Johan, Nachane, Ruta, Abell, Chris, Müller, Susanne, Siegal, Gregg, Knapp, Stefan
Publicado no J Med Chem (2016)

BRD3 and BRD4 BET Bromodomain Proteins Differentially Regulate Skeletal Myogenesis

Por Roberts, Thomas C., Etxaniz, Usue, Dall’Agnese, Alessandra, Wu, Shwu-Yuan, Chiang, Cheng-Ming, Brennan, Paul E., Wood, Matthew J. A., Puri, Pier Lorenzo
Publicado no Sci Rep (2017)

A phenotypic high-content, high-throughput screen identifies inhibitors of NLRP3 inflammasome activation

Por Nizami, Sohaib, Millar, Val, Arunasalam, Kanisa, Zarganes-Tzitzikas, Tryfon, Brough, David, Tresadern, Gary, Brennan, Paul E., Davis, John B., Ebner, Daniel, Di Daniel, Elena
Publicado no Sci Rep (2021)

The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains

Por Hay, Duncan, Fedorov, Oleg, Filippakopoulos, Panagis, Martin, Sarah, Philpott, Martin, Picaud, Sarah, Hewings, David S., Uttakar, Sagar, Heightman, Tom D., Conway, Stuart J., Knapp, Stefan, Brennan, Paul E.
Publicado no Medchemcomm (2013)

A poised fragment library enables rapid synthetic expansion yielding the first reported inhibitors of PHIP(2), an atypical bromodomain

Por Cox, Oakley B., Krojer, Tobias, Collins, Patrick, Monteiro, Octovia, Talon, Romain, Bradley, Anthony, Fedorov, Oleg, Amin, Jahangir, Marsden, Brian D., Spencer, John, von Delft, Frank, Brennan, Paul E.
Publicado no Chem Sci (2016)

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

Por 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
Publicado no J Med Chem (2015)

Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex

Por Sutherell, Charlotte L., Tallant, Cynthia, Monteiro, Octovia P., Yapp, Clarence, Fuchs, Julian E., Fedorov, Oleg, Siejka, Paulina, Müller, Suzanne, Knapp, Stefan, Brenton, James D., Brennan, Paul E., Ley, Steven V.
Publicado no J Med Chem (2016)

Fragment Screening Reveals Starting Points for Rational Design of Galactokinase 1 Inhibitors to Treat Classic Galactosemia

Por Mackinnon, Sabrina R., Krojer, Tobias, Foster, William R., Diaz-Saez, Laura, Tang, Manshu, Huber, Kilian V. M., von Delft, Frank, Lai, Kent, Brennan, Paul E., Arruda Bezerra, Gustavo, Yue, Wyatt W.
Publicado no ACS Chem Biol (2021)

RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain

Por Picaud, Sarah, Wells, Christopher, Felletar, Ildiko, Brotherton, Deborah, Martin, Sarah, Savitsky, Pavel, Diez-Dacal, Beatriz, Philpott, Martin, Bountra, Chas, Lingard, Hannah, Fedorov, Oleg, Müller, Susanne, Brennan, Paul E., Knapp, Stefan, Filippakopoulos, Panagis
Publicado em 2013

Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor

Por England, Katherine S., Tumber, Anthony, Krojer, Tobias, Scozzafava, Giuseppe, Ng, Stanley S., Daniel, Michelle, Szykowska, Aleksandra, Che, KaHing, von Delft, Frank, Burgess-Brown, Nicola A., Kawamura, Akane, Schofield, Christopher J., Brennan, Paul E.
Publicado no Medchemcomm (2014)

Discovery of a novel allosteric inhibitor scaffold for polyadenosine-diphosphate-ribose polymerase 14 (PARP14) macrodomain 2

Por Moustakim, Moses, Riedel, Kerstin, Schuller, Marion, Gehring, Andrè P., Monteiro, Octovia P., Martin, Sarah P., Fedorov, Oleg, Heer, Jag, Dixon, Darren J., Elkins, Jonathan M., Knapp, Stefan, Bracher, Franz, Brennan, Paul E.
Publicado no Bioorg Med Chem (2018)

Inhibition of the SUV4-20 H1 histone methyltransferase increases frataxin expression in Friedreich's ataxia patient cells

Por Vilema-Enríquez, Gabriela, Quinlan, Robert, Kilfeather, Peter, Mazzone, Roberta, Saqlain, Saba, del Molino del Barrio, Irene, Donato, Annalidia, Corda, Gabriele, Li, Fengling, Vedadi, Masoud, Németh, Andrea H., Brennan, Paul E., Wade-Martins, Richard
Publicado no J Biol Chem (2021)

[1,2,4]Triazolo[4,3-a]phthalazines: Inhibitors of Diverse Bromodomains

Por Fedorov, Oleg, Lingard, Hannah, Wells, Chris, Monteiro, Octovia P., Picaud, Sarah, Keates, Tracy, Yapp, Clarence, Philpott, Martin, Martin, Sarah J., Felletar, Ildiko, Marsden, Brian D., Filippakopoulos, Panagis, Müller, Susanne, Knapp, Stefan, Brennan, Paul E.
Publicado em 2013