Publications

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*denotes latest

Oncology

Porcupine inhibitor
2016 EORTC-NCI-AACR: Novel Porcupine inhibitor RXC004: Potent efficacy in animal models of cancer through direct tumour targeting and immunomodulatory mechanisms
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2016 EMBL: A paracrine role for Wnt signalling at the metastatic niche in breast cancer stem cells
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2015 AACR BT: Inhibition of Porcupine reduces Wnt-dependent colony formation and/or proliferation in both autocrine and paracrine cell models
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BTK inhibitor
2016 ASH: RXC005 (REDX08608), a Novel, Potent and Selective, Reversible BTK Inhibitor with Efficacy and Equivalent Potency Against Wild-Type and Mutant C481S BTK
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2016 AACR: Development of novel, selective, reversible inhibitors equipotent against wild-type and C481S Bruton's tyrosine kinase (BTK)
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2015 CHI-Drug Discovery Chemistry: Development of REDX05194, a novel, potent and selective inhibitor of Bruton's tyrosine kinase (BTK) as a potential treatment for B-cell malignancies and rheumatoid arthritis with proven efficacy in a mouse CIA model
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IDO inhibitor
*2017 AACR: Development of 2nd generation indoleamine 2,3-dioxygenase 1 (IDO-1) selective inhibitors
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2016 XXIV EFMC International Symposium on Medicinal: Ligand-Based in Silico Screening for the Discovery of Novel Inhibitors of Indoleamine 2,3-Dioxygenase (IDO1) and Tryptophan 2,3-Dioxygenase (TDO2)
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Pan-Raf inhibitor
2017 AACR: Development of REDX05358, a novel highly selective and potent pan RAF inhibitor and a potential therapeutic for BRAF and RAS mutant tumors
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2016 RSC/SCI Kinase: Next Generation Inhibitors: B-RAF inhibitors with reduced potential for paradoxical activation
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2014 AACR-NCI-EORTC: REDX04988, a novel dual B-RAF/C-RAF inhibitor and a potential therapeutic for BRAF-mutant colorectal cancer
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Immunology

Porcupine inhibitor
*2017 Keystone Symposia: Injury, Inflammation and Fibrosis (2017-C8): Porcupine inhibitors demonstrate suitability for use as novel anti-fibrotic therapeutics
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Infectious Disease

MDR Gram-positive
*2016 DMDG GMP Open Meeting: DMPK Strategy to assess early dose to man (eD2M) predictions for novel tricyclic topoisomerase inhibitors (NTTI) based on efficacy from an in vivo model
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2016 EFMC-ISMC: Design and Synthesis of Novel Tricyclic Topoisomerase Inhibitors (NTTIS) to tackle the threat of multi-drug resistant bacterial infections
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2016 Savage V. J. et al. Efficacy of a Novel Tricyclic Topoisomerase Inhibitor in a Murine Model of Neisseria gonorrhoeae infection. Antimicrob Agents Chemother doi: 10.1128/ACC. 00913-16
2016 Microbiology Society Conference: Novel Inhibitors of Bacterial Topoisomerases with Potent Activity Against Multidrug-Resistant Gram-Positive and Fastidious Gram-Negative Bacteria
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2016 Savage V. J. et al. Biological profiling of novel tricyclic inhibitors of bacterial DNA gyrase and topoisomerase IV. Journal of Antimicrobial Chemotherapy doi: 10.1093/jac/dkw06
2015 ICAAC: Novel Tricyclic Topoisomerase Inhibitors (NTTIs) with Potent Activity against Drug-Resistant Bacteria
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2015 EMBO: Novel Topoisomerase Inhibitors Active Against Drug-Resistant Gram-Positive Bacteria
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2014 BSAC ARM Workshop: Novel Inhibitors of Bacterial DNA Gyrase and Topoisomerase IV: In Vitro and In Vivo Biological Profiles
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2014 Gordon Research Conference: Discovery of Novel Small-Molecule Inhibitors of DNA Gyrase and Topoisomerase IV with Potent Activity against Drug-Resistant Bacteria
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MDR Gram-negative
2016 Cooper I. R. et al. Discovery and structure-activity relationships of a novel isothiazolone class of bacterial type II topoisomerase inhibitors. Bioorg Med Chem Lett doi: 10.1016/j.bmcl.2016.07.061
2016 Charrier C. et al. In vitro biological evaluation of novel broad-spectrum isothiazolone inhibitors of bacterial type II topoisomerases. Journal of Antimicrobial Chemotherapy doi: 10.1093/jac/dkw228
2016 ASM Microbe: In Vitro Biology and Pharmacokinetics Evaluation of Novel Bacterial Topoisomerase Inhibitors
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2016 ECCMID: Biological Profiling of Novel Bacterial Topoisomerase Inhibitors with Broad-Spectrum Antibacterial Activity
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2016 Gordon Research Conference: Novel Bacterial Topoisomerase Inhibitors: In Vitro Biological Evaluation
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2015 ECCMID: In Vitro Evaluation of Novel Bacterial Topoisomerase Inhibitors
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2015 ICAAC: Biological Profiling of Novel Broad-Spectrum Inhibitors of Bacterial Topoisomerases
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2014 Gordon Research Conference: Novel Small-Molecule Inhibitors of DNA Gyrase and Topoisomerase IV with Potent Antimicrobial Activity against Gram-Negative Bacteria
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