P. Craggs

发表

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.

Melanie V. Leveridge, P. Grandi, A. Michon, 2020, Journal of medicinal chemistry.

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

P. Grandi, A. Michon, P. Bamborough, 2015, Journal of medicinal chemistry.

Fluorescent-Based Assays and RapidFire Mass Spectrometry Lead Discovery for Microsomal Prostaglandin E Synthase Using a Combination of High-Throughput

Melanie V. Leveridge, Stuart M. Baddeley, Benjamin R Bellenie, 2012 .

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

David M. Wilson, G. Drewes, D. Eberhard, 2015, Nature chemical biology.

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

P. Grandi, A. Michon, Christina Rau, 2019, Journal of medicinal chemistry.

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

I. Wall, P. Rowland, R. Tanner, 2013, Protein science : a publication of the Protein Society.

The Mechanism of Acetyl Transfer Catalyzed by Mycobacterium tuberculosis GlmU

L. D. de Carvalho, M. Rejžek, R. Field, 2018, Biochemistry.

Modulation of macrophage inflammatory function through selective inhibition of the epigenetic reader protein SP140

D. Zwijnenburg, W. D. de Jonge, R. Prinjha, 2020, bioRxiv.

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

David J. Fallon, P. Grandi, A. Michon, 2014, ACS medicinal chemistry letters.

Bottlenecks and opportunities in antibiotic discovery against Mycobacterium tuberculosis.

L. D. de Carvalho, P. Craggs, L. P. S. de Carvalho, 2022, Current opinion in microbiology.

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.

Darren L. Poole, I. Wall, P. Bamborough, 2022, Journal of medicinal chemistry.

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

Juan A. Bueren-Calabuig, David W. Gray, Frederick R. C. Simeons, 2019, Proceedings of the National Academy of Sciences.

Kinetic intracellular assay measures compound binding kinetics at intracellular targets within living cells

P. Craggs, Charles S Lay, Daniel A. Thomas, 2021, Future Drug Discovery.

BET Inhibition Silences Expression of MYCN and BCL2 and Induces Cytotoxicity in Neuroblastoma Tumor Models

G. Ganji, R. Prinjha, C. Chung, 2013, PloS one.

Reducing False Positives through the Application of Fluorescence Lifetime Technology: A Comparative Study Using TYK2 Kinase as a Model System

P. Rowland, P. Craggs, Bhumika Karamshi, 2021, SLAS discovery : advancing life sciences R & D.

The reaction of hydrogen with nitric oxide at high temperature

J. N. Bradley, P. Craggs, 1975 .

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

P. Grandi, A. Michon, P. Bamborough, 2017, Journal of medicinal chemistry.

Probing the binding of interleukin-23 to individual receptor components and the IL-23 heteromeric receptor complex in living cells using NanoBRET

S. Hill, S. Briddon, Joëlle Goulding, 2021, Cell chemical biology.

Cellular Target Engagement Approaches to Monitor Epigenetic Reader Domain Interactions

Aaron T. Cheng, D. J. Brierley, Antonia J Lewis, 2019, SLAS discovery : advancing life sciences R & D.

Development of an intracellular quantitative assay to measure compound binding kinetics.

Kris D. McCombe, Kristin M. Riching, Daniel A. Thomas, 2021, Cell chemical biology.

Optimization of Naphthyridones into Selective TATA-Binding Protein Associated Factor 1 (TAF1) Bromodomain Inhibitors.

P. Bamborough, R. Prinjha, C. Chung, 2021, ACS medicinal chemistry letters.

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

David W. Gray, D. Gray, L. S. Torrie, 2019, Antimicrobial Agents and Chemotherapy.

Use of NanoBiT and NanoBRET to characterise interleukin‐23 receptor dimer formation in living cells

P. Craggs, Stephen J Hill, Charles S Lay, 2022, British journal of pharmacology.

Discovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening.

Darren L. Poole, Tony W Dean, I. Wall, 2020, Journal of medicinal chemistry.

Modulation of macrophage inflammatory function through selective inhibition of the epigenetic reader protein SP140

D. Zwijnenburg, W. D. de Jonge, R. Prinjha, 2022, BMC Biology.

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.

James M. Woolven, P. Bamborough, R. Prinjha, 2020, Journal of medicinal chemistry.

The Design and Synthesis of a Highly Selective and In Vivo Capable Inhibitor of the Second Bromodomain (BD2) of the Bromodomain and Extra Terminal Domain (BET) Family of Proteins.

P. Grandi, A. Michon, I. Wall, 2020, Journal of medicinal chemistry.

GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain

David J. Fallon, P. Grandi, A. Michon, 2016, ACS medicinal chemistry letters.

Structure-Guided Design and Synthesis of a Pyridazinone Series of Trypanosoma cruzi Proteasome Inhibitors

Peter G. Dodd, Frederick R. C. Simeons, L. Stojanovski, 2023, Journal of medicinal chemistry.

Lead Discovery for Microsomal Prostaglandin E Synthase Using a Combination of High-Throughput Fluorescent-Based Assays and RapidFire Mass Spectrometry

Melanie V. Leveridge, Stuart M. Baddeley, Benjamin R Bellenie, 2012, Journal of biomolecular screening.

Design and Synthesis of a Highly Selective and In Vivo-Capable Inhibitor of the Second Bromodomain of the Bromodomain and Extra Terminal Domain Family of Proteins

P. Grandi, A. Michon, James M. Woolven, 2020, Journal of Medicinal Chemistry.