Publications by authors named "Peter D Craggs"

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Structure- and Property-Based Optimization of Efficient Pan-Bromodomain and Extra Terminal Inhibitors to Identify Oral and Intravenous Candidate I-BET787.
David J Hirst, Paul Bamborough, Niam Al-Mahdi, Davina C Angell, Heather A Barnett, Peter D Craggs

J Med Chem· June 2024

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Structure-Guided Design of a Domain-Selective Bromodomain and Extra Terminal N-Terminal Bromodomain Chemical Probe.
Erin Bradley, Lucia Fusani, Chun-Wa Chung, Peter D Craggs, Emmanuel H Demont

J Med Chem· December 2023

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Development of an intracellular quantitative assay to measure compound binding kinetics.
Charles S Lay, Daniel A Thomas, John P Evans, Matthew Campbell, Kristopher McCombe, Peter D Craggs

Cell Chem Biol· December 2023

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Structure-Guided Design and Synthesis of a Pyridazinone Series of Proteasome Inhibitors.
Michael G Thomas, Kate McGonagle, Paul Rowland, David A Robinson, Peter G Dodd, Peter D Craggs

J Med Chem· August 2023

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Use of NanoBiT and NanoBRET to characterise interleukin-23 receptor dimer formation in living cells.
Charles S Lay, Laura E Kilpatrick, Peter D Craggs, Stephen J Hill

Br J Pharmacol· June 2023

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Characterisation of IL-23 receptor antagonists and disease relevant mutants using fluorescent probes.
Charles S Lay, Albert Isidro-Llobet, Laura E Kilpatrick, Peter D Craggs, Stephen J Hill

Nat Commun· May 2023

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Identification and Optimization of a Ligand-Efficient Benzoazepinone Bromodomain and Extra Terminal (BET) Family Acetyl-Lysine Mimetic into the Oral Candidate Quality Molecule I-BET432.
Philip G Humphreys, Niall A Anderson, Paul Bamborough, Andrew Baxter, Chun-Wa Chung, Peter D Craggs

J Med Chem· November 2022

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Bottlenecks and opportunities in antibiotic discovery against Mycobacterium tuberculosis.
Peter D Craggs, Luiz Pedro S de Carvalho

Curr Opin Microbiol· October 2022

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Modulation of macrophage inflammatory function through selective inhibition of the epigenetic reader protein SP140.
Mohammed Ghiboub, Jan Koster, Peter D Craggs, Andrew Y F Li Yim, Anthony Shillings

BMC Biol· August 2022

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A kinetic intra-cellular assay (KICA) to measure quantitative compound binding kinetics within living cells.
Charles S Lay, Daniel A Thomas, John P Evans, Emma J Jones, Kelly M Gatfield, Peter D Craggs

STAR Protoc· March 2022

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Development of an intracellular quantitative assay to measure compound binding kinetics.
Charles S Lay, Daniel A Thomas, John P Evans, Matthew Campbell, Kristopher McCombe, Peter D Craggs

Cell Chem Biol· February 2022

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Design, Synthesis, and Characterization of I-BET567, a Pan-Bromodomain and Extra Terminal (BET) Bromodomain Oral Candidate.
Philip G Humphreys, Stephen J Atkinson, Paul Bamborough, Rino A Bit, Chun-Wa Chung, Peter D Craggs

J Med Chem· February 2022

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Probing the binding of interleukin-23 to individual receptor components and the IL-23 heteromeric receptor complex in living cells using NanoBRET.
Charles S Lay, Angela Bridges, Joelle Goulding, Stephen J Briddon, Zoja Soloviev, Peter D Craggs

Cell Chem Biol· January 2022

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Optimization of Naphthyridones into Selective TATA-Binding Protein Associated Factor 1 (TAF1) Bromodomain Inhibitors.
Michael A Clegg, Natalie H Theodoulou, Paul Bamborough, Chun-Wa Chung, Peter D Craggs

ACS Med Chem Lett· August 2021

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Reducing False Positives through the Application of Fluorescence Lifetime Technology: A Comparative Study Using TYK2 Kinase as a Model System.
Luke A Greenhough, Gabriella Clarke, Alexander N Phillipou, Faith Mazani, Bhumika Karamshi, Peter D Craggs

SLAS Discov· June 2021

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Design and Synthesis of a Highly Selective and -Capable Inhibitor of the Second Bromodomain of the Bromodomain and Extra Terminal Domain Family of Proteins.
Alex Preston, Stephen Atkinson, Paul Bamborough, Chun-Wa Chung, Peter D Craggs

J Med Chem· September 2020

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Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype.
Christopher R Wellaway, Paul Bamborough, Sharon G Bernard, Chun-Wa Chung, Peter D Craggs

J Med Chem· September 2020

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Application of Atypical Acetyl-lysine Methyl Mimetics in the Development of Selective Inhibitors of the Bromodomain-Containing Protein 7 (BRD7)/Bromodomain-Containing Protein 9 (BRD9) Bromodomains.
Michael A Clegg, Paul Bamborough, Chun-Wa Chung, Peter D Craggs, Laurie Gordon

J Med Chem· June 2020

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Cellular Target Engagement Approaches to Monitor Epigenetic Reader Domain Interactions.
Alexander N Phillipou, Charles S Lay, Charlotte E Carver, Cassie Messenger, John P Evans, Peter D Craggs

SLAS Discov· February 2020

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Discovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening.
Christopher R Wellaway, Dominique Amans, Paul Bamborough, Heather Barnett, Rino A Bit, Peter D Craggs

J Med Chem· January 2020

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Identification of Novel Trypanosoma cruzi Proteasome Inhibitors Using a Luminescence-Based High-Throughput Screening Assay.
Filip Zmuda, Lalitha Sastry, Sharon M Shepherd, Deuan Jones, Alison Scott, Peter D Craggs

Antimicrob Agents Chemother· September 2019

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A Qualified Success: Discovery of a New Series of ATAD2 Bromodomain Inhibitors with a Novel Binding Mode Using High-Throughput Screening and Hit Qualification.
Paul Bamborough, Chun-Wa Chung, Emmanuel H Demont, Angela M Bridges, Peter D Craggs

J Med Chem· August 2019

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Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition.
Susan Wyllie, Stephen Brand, Michael Thomas, Manu De Rycker, Chun-Wa Chung, Peter D Craggs

Proc Natl Acad Sci U S A· May 2019

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The Mechanism of Acetyl Transfer Catalyzed by Mycobacterium tuberculosis GlmU.
Peter D Craggs, Stephane Mouilleron, Martin Rejzek, Cesira de Chiara, Robert J Young

Biochemistry· June 2018

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Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe.
Philip G Humphreys, Paul Bamborough, Chun-Wa Chung, Peter D Craggs, Laurie Gordon

J Med Chem· January 2017

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