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Items: 14

1.

A Qualified Success: Discovery of a New Series of ATAD2 Bromodomain Inhibitors with a Novel Binding Mode Using High-Throughput Screening and Hit Qualification.

Bamborough P, Chung CW, Demont EH, Bridges AM, Craggs PD, Dixon DP, Francis P, Furze RC, Grandi P, Jones EJ, Karamshi B, Locke K, Lucas SCC, Michon AM, Mitchell DJ, Pogány P, Prinjha RK, Rau C, Roa AM, Roberts AD, Sheppard RJ, Watson RJ.

J Med Chem. 2019 Aug 22;62(16):7506-7525. doi: 10.1021/acs.jmedchem.9b00673. Epub 2019 Aug 9.

PMID:
31398032
2.

Identification of Novel Trypanosoma cruzi Proteasome Inhibitors Using a Luminescence-Based High-Throughput Screening Assay.

Zmuda F, Sastry L, Shepherd SM, Jones D, Scott A, Craggs PD, Cortes A, Gray DW, Torrie LS, De Rycker M.

Antimicrob Agents Chemother. 2019 Aug 23;63(9). pii: e00309-19. doi: 10.1128/AAC.00309-19. Print 2019 Sep.

3.

Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition.

Wyllie S, Brand S, Thomas M, De Rycker M, Chung CW, Pena I, Bingham RP, Bueren-Calabuig JA, Cantizani J, Cebrian D, Craggs PD, Ferguson L, Goswami P, Hobrath J, Howe J, Jeacock L, Ko EJ, Korczynska J, MacLean L, Manthri S, Martinez MS, Mata-Cantero L, Moniz S, Nühs A, Osuna-Cabello M, Pinto E, Riley J, Robinson S, Rowland P, Simeons FRC, Shishikura Y, Spinks D, Stojanovski L, Thomas J, Thompson S, Viayna Gaza E, Wall RJ, Zuccotto F, Horn D, Ferguson MAJ, Fairlamb AH, Fiandor JM, Martin J, Gray DW, Miles TJ, Gilbert IH, Read KD, Marco M, Wyatt PG.

Proc Natl Acad Sci U S A. 2019 May 7;116(19):9318-9323. doi: 10.1073/pnas.1820175116. Epub 2019 Apr 8.

4.

Kawasaki disease: a prospective population survey in the UK and Ireland from 2013 to 2015.

Tulloh RMR, Mayon-White R, Harnden A, Ramanan AV, Tizard EJ, Shingadia D, Michie CA, Lynn RM, Levin M, Franklin OD, Craggs P, Davidson S, Stirzaker R, Danson M, Brogan PA.

Arch Dis Child. 2019 Jul;104(7):640-646. doi: 10.1136/archdischild-2018-315087. Epub 2018 Aug 13.

PMID:
30104394
5.

A pilot randomised controlled trial investigating a mindfulness-based stress reduction (MBSR) intervention in individuals with pulmonary arterial hypertension (PAH): the PATHWAYS study.

Tulloh RMR, Garratt V, Tagney J, Turner-Cobb J, Marques E, Greenwood R, Howard L, Gin-Sing W, Barton A, Ewings P, Craggs P, Hollingworth W.

Pilot Feasibility Stud. 2018 May 21;4:78. doi: 10.1186/s40814-018-0270-z. eCollection 2018.

6.

The Mechanism of Acetyl Transfer Catalyzed by Mycobacterium tuberculosis GlmU.

Craggs PD, Mouilleron S, Rejzek M, de Chiara C, Young RJ, Field RA, Argyrou A, de Carvalho LPS.

Biochemistry. 2018 Jun 19;57(24):3387-3401. doi: 10.1021/acs.biochem.8b00121. Epub 2018 May 2.

7.

Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe.

Humphreys PG, Bamborough P, Chung CW, Craggs PD, Gordon L, Grandi P, Hayhow TG, Hussain J, Jones KL, Lindon M, Michon AM, Renaux JF, Suckling CJ, Tough DF, Prinjha RK.

J Med Chem. 2017 Jan 26;60(2):695-709. doi: 10.1021/acs.jmedchem.6b01566. Epub 2017 Jan 9.

PMID:
28002667
8.

GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain.

Bamborough P, Barnett HA, Becher I, Bird MJ, Chung CW, Craggs PD, Demont EH, Diallo H, Fallon DJ, Gordon LJ, Grandi P, Hobbs CI, Hooper-Greenhill E, Jones EJ, Law RP, Le Gall A, Lugo D, Michon AM, Mitchell DJ, Prinjha RK, Sheppard RJ, Watson AJ, Watson RJ.

ACS Med Chem Lett. 2016 May 9;7(6):552-7. doi: 10.1021/acsmedchemlett.6b00092. eCollection 2016 Jun 9.

9.

Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors.

Demont EH, Chung CW, Furze RC, Grandi P, Michon AM, Wellaway C, Barrett N, Bridges AM, Craggs PD, Diallo H, Dixon DP, Douault C, Emmons AJ, Jones EJ, Karamshi BV, Locke K, Mitchell DJ, Mouzon BH, Prinjha RK, Roberts AD, Sheppard RJ, Watson RJ, Bamborough P.

J Med Chem. 2015 Jul 23;58(14):5649-73. doi: 10.1021/acs.jmedchem.5b00772. Epub 2015 Jul 9.

PMID:
26155854
10.

Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation.

Lewis HD, Liddle J, Coote JE, Atkinson SJ, Barker MD, Bax BD, Bicker KL, Bingham RP, Campbell M, Chen YH, Chung CW, Craggs PD, Davis RP, Eberhard D, Joberty G, Lind KE, Locke K, Maller C, Martinod K, Patten C, Polyakova O, Rise CE, Rüdiger M, Sheppard RJ, Slade DJ, Thomas P, Thorpe J, Yao G, Drewes G, Wagner DD, Thompson PR, Prinjha RK, Wilson DM.

Nat Chem Biol. 2015 Mar;11(3):189-91. doi: 10.1038/nchembio.1735. Epub 2015 Jan 26.

11.

1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain.

Demont EH, Bamborough P, Chung CW, Craggs PD, Fallon D, Gordon LJ, Grandi P, Hobbs CI, Hussain J, Jones EJ, Le Gall A, Michon AM, Mitchell DJ, Prinjha RK, Roberts AD, Sheppard RJ, Watson RJ.

ACS Med Chem Lett. 2014 Sep 10;5(11):1190-5. doi: 10.1021/ml5002932. eCollection 2014 Nov 13.

12.

BET inhibition silences expression of MYCN and BCL2 and induces cytotoxicity in neuroblastoma tumor models.

Wyce A, Ganji G, Smitheman KN, Chung CW, Korenchuk S, Bai Y, Barbash O, Le B, Craggs PD, McCabe MT, Kennedy-Wilson KM, Sanchez LV, Gosmini RL, Parr N, McHugh CF, Dhanak D, Prinjha RK, Auger KR, Tummino PJ.

PLoS One. 2013 Aug 23;8(8):e72967. doi: 10.1371/journal.pone.0072967. eCollection 2013.

13.

Crystal structures of ASK1-inhibtor complexes provide a platform for structure-based drug design.

Singh O, Shillings A, Craggs P, Wall I, Rowland P, Skarzynski T, Hobbs CI, Hardwick P, Tanner R, Blunt M, Witty DR, Smith KJ.

Protein Sci. 2013 Aug;22(8):1071-7. doi: 10.1002/pro.2298. Epub 2013 Jul 3.

14.

Lead discovery for microsomal prostaglandin E synthase using a combination of high-throughput fluorescent-based assays and RapidFire mass spectrometry.

Leveridge MV, Bardera AI, LaMarr W, Billinton A, Bellenie B, Edge C, Francis P, Christodoulou E, Shillings A, Hibbs M, Fosberry A, Tanner R, Hardwicke P, Craggs P, Sinha Y, Elegbe O, Alvarez-Ruiz E, Martin-Plaza JJ, Barroso-Poveda V, Baddeley S, Chung CW, Hutchinson J.

J Biomol Screen. 2012 Jun;17(5):641-50. doi: 10.1177/1087057111435700. Epub 2012 Feb 14.

PMID:
22337655

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