Luminescence-based complementation assay to assess target engagement and cell permeability of glycolate oxidase (HAO1) inhibitors

Authors: Mackinnon, Sabrina R. ^a, Zarganes-Tzitzikas, Tryfon ^b, Adams, Cassandra J. ^c, Brennan, Paul E. ^{c, ⁎}, Yue, Wyatt W. ^{a, ⁎⁎}

Source: In Biochimie January 2025 228:71-81

Regulation of inositol 5-phosphatase activity by the C2 domain of SHIP1 and SHIP2

Authors: Bradshaw, William J., Kennedy, Emma C., Moreira, Tiago, Smith, Luke A., Chalk, Rod, Katis, Vittorio L., Benesch, Justin L.P., Brennan, Paul E., Murphy, Emma J., Gileadi, Opher

Source: In Structure 4 April 2024 32(4):453-466

Discovery of FERM domain protein–protein interaction inhibitors for MSN and CD44 as a potential therapeutic approach for Alzheimer’s disease

Authors: Du, Yuhong, Bradshaw, William J., Leisner, Tina M., Annor-Gyamfi, Joel K., Qian, Kun, Bashore, Frances M., Sikdar, Arunima, Nwogbo, Felix O., Ivanov, Andrey A., Frye, Stephen V., Gileadi, Opher, Brennan, Paul E., Levey, Allan I., Axtman, Alison D., Pearce, Kenneth H., Fu, Haian, Katis, Vittorio L.

Source: In Journal of Biological Chemistry December 2023 299(12)

Structural Premise of Selective Deubiquitinase USP30 Inhibition by Small-Molecule Benzosulfonamides

Authors: O'Brien, Darragh P., Jones, Hannah B.L., Guenther, Franziska, Murphy, Emma J., England, Katherine S., Vendrell, Iolanda, Anderson, Malcolm, Brennan, Paul E., Davis, John B., Pinto-Fernández, Adán, Turnbull, Andrew P., Kessler, Benedikt M.

Source: In Molecular & Cellular Proteomics August 2023 22(8)

Drug repurposing in amyotrophic lateral sclerosis (ALS).

Authors: Carroll, Emily, Scaber, Jakub, Huber, Kilian V. M., Brennan, Paul E., Thompson, Alexander G., Turner, Martin R., Talbot, Kevin

Source: Expert Opinion on Drug Discovery; Apr2025, Vol. 20 Issue 4, p447-464, 18p

Subject Terms: AMYOTROPHIC lateral sclerosis treatment, DRUG repositioning, DRUG discovery, NEURODEGENERATION, EXPERIMENTAL medicine

Male sex chromosomal complement exacerbates the pathogenicity of Th17 cells in a chronic model of central nervous system autoimmunity

Authors: Doss, Prenitha Mercy Ignatius Arokia, Umair, Muhammad, Baillargeon, Joanie, Fazazi, Reda, Fudge, Neva, Akbar, Irshad, Yeola, Asmita Pradeep, Williams, John B., Leclercq, Mickael, Joly-Beauparlant, Charles, Beauchemin, Philippe, Ruda, Gian Filipo, Alpaugh, Melanie, Anderson, Ana C., Brennan, Paul E., Droit, Arnaud, Lassmann, Hans, Moore, Craig S., Rangachari, Manu

Source: In Cell Reports 9 March 2021 34(10)

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

Authors: Thompson, Andrew P., Bitsina, Christina, Gray, Janine L., von Delft, Frank, Brennan, Paul E.

Source: In Journal of Biological Chemistry January-June 2021 296

Structural Dynamics of the Ubiquitin Specific Protease USP30 in Complex with a Cyanopyrrolidine-Containing Covalent Inhibitor.

Authors: O'Brien, Darragh P.¹ (AUTHOR) darragh.obrien@ndm.ox.ac.uk, Jones, Hannah B.L.¹ (AUTHOR), Shi, Yuqi² (AUTHOR), Guenther, Franziska³ (AUTHOR), Vendrell, Iolanda^1,4 (AUTHOR), Viner, Rosa² (AUTHOR), Brennan, Paul E.³ (AUTHOR), Mead, Emma³ (AUTHOR), Zarganes-Tzitzikas, Tryfon³ (AUTHOR), Davis, John B.³ (AUTHOR), Pinto-Fernández, Adán^1,4 (AUTHOR), England, Katherine S.³ (AUTHOR), Murphy, Emma J.³ (AUTHOR), Turnbull, Andrew P.⁵ (AUTHOR) andrew.turnbull@cancer.org.uk, Kessler, Benedikt M.^1,4 (AUTHOR) benedikt.kessler@ndm.ox.ac.uk

Source: Journal of Proteome Research. 2/7/2025, Vol. 24 Issue 2, p479-490. 12p.

The Chemical Probes Portal – 2024: update on this public resource to support best-practice selection and use of small molecules in biomedical research.

Authors: Sanfelice, Domenico, Antolin, Albert A, Crisp, Alisa, Chen, Yi, Bellenie, Benjamin, Brennan, Paul E, Edwards, Aled, Müller, Susanne, Al-Lazikani, Bissan, Workman, Paul

Source: Nucleic Acids Research; 1/6/2025, Vol. 53 Issue D1, pD1663-D1669, 7p

Identification and characterization of human KALRN mRNA and Kalirin protein isoforms.

Authors: Mould, Arne W, Wright, David J, Bornemann, Klaus D, Hengerer, Bastian, Pinnock, Rob, Drydale, Edward, Bancroft, James, Hall, Nicola A L, Delft, Annette von, Brennan, Paul E, Harrison, Paul J, Haerty, Wilfried, Tunbridge, Elizabeth M

Source: Cerebral Cortex; Dec2024, Vol. 34 Issue 12, p1-15, 15p

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

Authors: 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 ^*

Source: In Journal of Biological Chemistry 25 December 2020 295(52):17973-17985

C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays

Authors: Le Bihan, Yann-Vaï, Lanigan, Rachel M., Atrash, Butrus, McLaughlin, Mark G., Velupillai, Srikannathasan, Malcolm, Andrew G., England, Katherine S., Ruda, Gian Filippo, Mok, N. Yi, Tumber, Anthony, Tomlin, Kathy, Saville, Harry, Shehu, Erald, McAndrew, Craig, Carmichael, LeAnne, Bennett, James M., Jeganathan, Fiona, Eve, Paul, Donovan, Adam, Hayes, Angela, Wood, Francesca, Raynaud, Florence I., Fedorov, Oleg, Brennan, Paul E., Burke, Rosemary, van Montfort, Rob L.M., Rossanese, Olivia W., Blagg, Julian, Bavetsias, Vassilios

Source: In European Journal of Medicinal Chemistry 1 September 2019 177:316-337

Covalent Inhibitors of S100A4 Block the Formation of a Pro-Metastasis Non-Muscle Myosin 2A Complex.

Authors: Giroud, Charline¹ (AUTHOR), Szommer, Tamas¹ (AUTHOR), Coxon, Carmen¹ (AUTHOR), Monteiro, Octovia¹ (AUTHOR), Grimes, Thomas^1,2 (AUTHOR), Zarganes-Tzitzikas, Tryfon^1,2 (AUTHOR), Christott, Thomas¹ (AUTHOR), Bennett, James¹ (AUTHOR), Buchan, Karly¹ (AUTHOR), Brennan, Paul E.¹ (AUTHOR), Fedorov, Oleg¹ (AUTHOR) oleg.fedorov@cmd.ox.ac.uk

Source: Journal of Medicinal Chemistry. 11/14/2024, Vol. 67 Issue 21, p18943-18956. 14p.

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

Authors: 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.

Source: In Bioorganic & Medicinal Chemistry 15 July 2018 26(11):2965-2972

Development of chemical probes for the bromodomains of BRD7 and BRD9

Authors: Clark, Peter G.K., Dixon, Darren J., Brennan, Paul E.

Source: In Drug Discovery Today: Technologies March 2016 19:73-80

Unexpected Noncovalent Off-Target Activity of Clinical BTK Inhibitors Leads to Discovery of a Dual NUDT5/14 Antagonist.

Authors: Balıkçı, Esra^1,2 (AUTHOR), Marques, Anne-Sophie M. C.^1,2 (AUTHOR), Bauer, Ludwig G.^1,2 (AUTHOR), Seupel, Raina^1,2 (AUTHOR), Bennett, James^1,2 (AUTHOR), Raux, Brigitt^1,2 (AUTHOR), Buchan, Karly^1,2 (AUTHOR), Simelis, Klemensas^1,2 (AUTHOR), Singh, Usha^1,2 (AUTHOR), Rogers, Catherine^1,2 (AUTHOR), Ward, Jennifer^1,2 (AUTHOR), Cheng, Carol^1,2 (AUTHOR), Szommer, Tamas^1,2 (AUTHOR), Schützenhofer, Kira³ (AUTHOR), Elkins, Jonathan M.^1,2 (AUTHOR), Sloman, David L.⁴ (AUTHOR), Ahel, Ivan³ (AUTHOR), Fedorov, Oleg^1,2 (AUTHOR), Brennan, Paul E.^1,2,5 (AUTHOR), Huber, Kilian V. M.^1,2 (AUTHOR) kilian.huber@cmd.ox.ac.uk

Source: Journal of Medicinal Chemistry. 5/9/2024, Vol. 67 Issue 9, p7245-7259. 15p.

Inflammatory Signaling by NOD-RIPK2 Is Inhibited by Clinically Relevant Type II Kinase Inhibitors

Authors: Canning, Peter, Ruan, Qui, Schwerd, Tobias, Hrdinka, Matous, Maki, Jenny L., Saleh, Danish, Suebsuwong, Chalada, Ray, Soumya, Brennan, Paul E., Cuny, Gregory D., Uhlig, Holm H., Gyrd-Hansen, Mads, Degterev, Alexei, Bullock, Alex N.

Source: In Chemistry & Biology 17 September 2015 22(9):1174-1184

CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses

Authors: Hammitzsch, Ariane, Tallant, Cynthia, Fedorov, Oleg, O’Mahony, Alison, Brennan, Paul E., Hay, Duncan A., Martinez, Fernando O., Al-Mossawi, M. Hussein, de Wit, Jelle, Vecellio, Matteo, Wells, Christopher, Wordsworth, Paul, Müller, Susanne, Knapp, Stefan, Bowness, Paul

Source: Proceedings of the National Academy of Sciences of the United States of America, 2015 Aug . 112(34), 10768-10773.

Access URL: https://www.jstor.org/stable/26464034

K2P channel gating mechanisms revealed by structures of TREK-2 and a complex with Prozac

Authors: Dong, Yin Yao, Pike, Ashley C. W., Mackenzie, Alexandra, McClenaghan, Conor, Aryal, Prafulla, Dong, Liang, Quigley, Andrew, Grieben, Mariana, Goubin, Solenne, Mukhopadhyay, Shubhashish, Ruda, Gian Filippo, Clausen, Michael V., Cao, Lishuang, Brennan, Paul E., Burgess-Brown, Nicola A., Sansom, Mark S. P., Tucker, Stephen J., Carpenter, Elisabeth P.

Source: Science, 2015 Mar . 347(6227), 1256-1259.

Access URL: http://www.jstor.org/stable/24746272

Characterization of covalent inhibitors that disrupt the interaction between the tandem SH2 domains of SYK and FCER1G phospho-ITAM.

Authors: Bashore, Frances M., Katis, Vittorio L., Du, Yuhong, Sikdar, Arunima, Wang, Dongxue, Bradshaw, William J., Rygiel, Karolina A., Leisner, Tina M., Chalk, Rod, Mishra, Swati, Williams, C. Andrew, Gileadi, Opher, Brennan, Paul E., Wiley, Jesse C., Gockley, Jake, Cary, Gregory A., Carter, Gregory W., Young, Jessica E., Pearce, Kenneth H., Fu, Haian

Source: PLoS ONE; 2/15/2024, Vol. 19 Issue 2, p1-24, 24p

Subject Terms: IMMUNOGLOBULIN receptors, ALZHEIMER'S disease, SMALL molecules, RNA sequencing, HIGH throughput screening (Drug development), FC receptors