I. Rioja

发表

Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A).

David M. Wilson, P. Bamborough, R. Prinjha, 2012, Bioorganic & medicinal chemistry letters.

BET protein inhibition shows efficacy against JAK2V617F-driven neoplasms

Andrew J. Bannister, S. Robson, R. Prinjha, 2014, Leukemia.

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.

Epigenetic pathway targets for the treatment of disease: accelerating progress in the development of pharmacological tools: IUPHAR Review 11

R. Prinjha, D. Tough, I. Rioja, 2014, British journal of pharmacology.

Single doses of p 38 MAP kinase inhibitors or prednisolone affect CRP and IL-6 in patients with active Rheumatoid Arthritis ( RA )

Shuying Yang, K. Ray, I. Rioja, 2013 .

Single doses of p38 MAP kinase inhibitors or prednisolone affect CRP and IL-6 in patients with active Rheumatoid Arthritis (RA)

Shuying Yang, K. Ray, I. Rioja, 2012 .

Bromodomain factor 5 is an essential regulator of transcription in Leishmania

J. Mottram, R. Prinjha, A. Wilkinson, 2022, Nature Communications.

Bromodomain factor 5 is an essential transcriptional regulator of the Leishmania genome

J. Mottram, R. Prinjha, A. Wilkinson, 2021, bioRxiv.

Optimization of a Series of 2,3-Dihydrobenzofurans as Highly Potent, Second Bromodomain (BD2)-Selective, Bromo and Extra-Terminal Domain (BET) Inhibitors.

P. Grandi, I. Wall, James M. Woolven, 2021, Journal of medicinal chemistry.

Joint cytokine quantification in two rodent arthritis models: kinetics of expression, correlation of mRNA and protein levels and response to prednisolone treatment

I. Rioja, J. Buckton, M. Dickson, 2004, Clinical and experimental immunology.

Quantitative Power Doppler Ultrasonography Is a Sensitive Measure of Metacarpophalangeal Joint Synovial Vascularity in Rheumatoid Arthritis and Declines Significantly Following a 2-week Course of Oral Low-dose Corticosteroids

P. Taylor, F. Chiesa, R. Eckersley, 2010, The Journal of Rheumatology.

Identification of a Series of N-Methylpyridine-2-carboxamides as Potent and Selective Inhibitors of the Second Bromodomain (BD2) of the Bromo and Extra Terminal Domain (BET) Proteins.

P. Grandi, A. Michon, I. Wall, 2021, Journal of medicinal chemistry.

Selective inhibitors of bromodomain BD1 and BD2 of BET proteins modulate radiation‐induced profibrotic fibroblast responses

C. Plass, R. Prinjha, P. Schmezer, 2022, International journal of cancer.

Cohesin couples transcriptional bursting probabilities of inducible enhancers and promoters

Mohammad M. Karimi, M. Stumpf, S. Marguerat, 2022, Nature Communications.

Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation

P. Grandi, A. Michon, G. Drewes, 2020, Science.

A pyrroloquinazoline derivative with anti-inflammatory and analgesic activity by dual inhibition of cyclo-oxygenase-2 and 5-lipoxygenase.

P. Molina, M. Alcaraz, I. Rioja, 2002, European journal of pharmacology.

N-terminal BET bromodomain inhibitors disrupt a BRD4-p65 interaction and reduce inducible nitric oxide synthase transcription in pancreatic β-cells

Brian C. Smith, R. Prinjha, Aaron Naatz, 2022, Frontiers in Endocrinology.

GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins.

P. Grandi, P. Bamborough, R. Prinjha, 2020, Journal of medicinal chemistry.

BET bromodomain inhibition reduces maturation and enhances tolerogenic properties of human and mouse dendritic cells.

W. D. de Jonge, P. Tak, R. Prinjha, 2016, Molecular immunology.

Characterization of pristane-induced arthritis, a murine model of chronic disease: response to antirheumatic agents, expression of joint cytokines, and immunopathology.

J. Trill, I. Rioja, P. Wooley, 2004, Arthritis and rheumatism.

Gene expression profiles in the rat streptococcal cell wall-induced arthritis model identified using microarray analysis

I. Rioja, C. Clayton, S. Graham, 2004, Arthritis research & therapy.

Expanding Bromodomain Targeting into Neglected Parasitic Diseases.

D. Simola, P. Bamborough, F. Gamo, 2021, ACS infectious diseases.

A BET Protein Inhibitor Targeting Mononuclear Myeloid Cells Affects Specific Inflammatory Mediators and Pathways in Crohn’s Disease

C. Buskens, W. D. de Jonge, R. Prinjha, 2022, Cells.

Tyrosine Kinase 2 Signalling Drives Pathogenic T cells in Colitis

W. D. de Jonge, R. Prinjha, G. D'Haens, 2020, Journal of Crohn's & colitis.

Fragment-based Scaffold Hopping: Identification of Potent, Selective, and Highly Soluble Bromo and Extra Terminal Domain (BET) Second Bromodomain (BD2) Inhibitors.

P. Grandi, I. Wall, James M. Woolven, 2021, Journal of medicinal chemistry.

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.

Carboxylesterase-1 Assisted Targeting of HDAC Inhibitors to Mononuclear Myeloid Cells in Inflammatory Bowel Disease

W. D. de Jonge, R. Prinjha, P. Mander, 2021, Journal of Crohn's & colitis.

Solid-phase synthesis and inhibitory effects of some pyrido[1,2-c]pyrimidine derivatives on leukocyte formations and experimental inflammation.

P. Molina, M. Alcaraz, I. Rioja, 2001, Journal of medicinal chemistry.

Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives.

David M. Wilson, Melanie V. Leveridge, G. Drewes, 2016, Journal of medicinal chemistry.

Inhibition of leukocyte functions by the alkaloid isaindigotone from Isatis indigotica and some new synthetic derivatives.

P. Molina, M. Alcaraz, I. Rioja, 2001, Journal of natural products.

The Optimisation of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor.

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

Essential bromodomain TcBDF2 as a drug target against Chagas disease

R. Prinjha, E. Serra, V. Alonso, 2022, bioRxiv.

Histone H3 lysine 9 di-methylation as an epigenetic signature of the interferon response

Scott B. Dewell, C. Rice, A. Tarakhovsky, 2012, The Journal of experimental medicine.

IFN-γ Drives Human Monocyte Differentiation into Highly Proinflammatory Macrophages That Resemble a Phenotype Relevant to Psoriasis

W. D. de Jonge, R. Prinjha, H. Eberl, 2021, The Journal of Immunology.

Epigenetic modulation of type-1 diabetes via a dual effect on pancreatic macrophages and β cells

R. Weissleder, C. Benoist, R. Prinjha, 2014, eLife.

BET Inhibition Improves NASH and Liver Fibrosis

Sarah A. Middleton, Pankaj Agarwal, D. Rajpal, 2018, Scientific Reports.

Brd4 bridges the transcriptional regulators, Aire and P-TEFb, to promote elongation of peripheral-tissue antigen transcripts in thymic stromal cells

Mark S. Anderson, A. Tarakhovsky, C. Benoist, 2015, Proceedings of the National Academy of Sciences.

Potential novel biomarkers of disease activity in rheumatoid arthritis patients: CXCL13, CCL23, transforming growth factor alpha, tumor necrosis factor receptor superfamily member 9, and macrophage colony-stimulating factor.

I. Rioja, M. Binks, L. Warnock, 2008, Arthritis and rheumatism.

BET bromodomain inhibition promotes neurogenesis while inhibiting gliogenesis in neural progenitor cells.

H. Mei, R. Prinjha, Zhong Zhong, 2016, Stem cell research.

Signaling function of PRC2 is essential for TCR-driven T cell responses

A. Tarakhovsky, R. Prinjha, M. T. McCabe, 2018, The Journal of experimental medicine.

Bromodomain Proteins Contribute to Maintenance of Bloodstream Form Stage Identity in the African Trypanosome

F. Papavasiliou, R. Prinjha, E. Debler, 2015, PLoS biology.

Combined noncanonical NF-κB agonism and targeted BET bromodomain inhibition reverse HIV latency ex vivo

B. Strahl, A. Sanchez, R. Prinjha, 2022, The Journal of clinical investigation.

Anti-inflammatory Effects of BET Protein Inhibition Through Modulation of Gene Transcription

R. Prinjha, D. Tough, I. Rioja, 2015 .

The structure based design of dual HDAC/BET inhibitors as novel epigenetic probes

Kathryn A. Giblin, G. Drewes, M. Bantscheff, 2014 .

Epigenetic Regulation of T Cell Memory: Recalling Therapeutic Implications.

R. Prinjha, D. Tough, I. Rioja, 2019, Trends in immunology.

A histone-like motif in yellow fever virus contributes to viral replication

B. Garcia, C. Rice, D. Patel, 2020, bioRxiv.

In vitro target validation and in vivo efficacy of p38 MAP kinase inhibition in established chronic collagen-induced arthritis model: a pre-clinical study.

D. Essex, K. Ray, I. Rioja, 2010, Clinical and experimental rheumatology.

Discovery of a Highly Selective BET BD2 Inhibitor from a DNA-Encoded Library Technology Screening Hit.

P. Grandi, I. Wall, R. Prinjha, 2021, Journal of medicinal chemistry.

Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 1. 3-Amino-4-pyridine Carboxylate Derivatives.

Douglas W. Thomson, David M. Wilson, Melanie V. Leveridge, 2016, Journal of medicinal chemistry.

Targeting Histone Deacetylases in Myeloid Cells Inhibits Their Maturation and Inflammatory Function With Limited Effects on Atherosclerosis

W. D. de Jonge, R. Prinjha, P. Mander, 2019, Front. Pharmacol..

Bromodomain inhibitor i-BET858 triggers a unique transcriptional response coupled to enhanced DNA damage, cell cycle arrest and apoptosis in high-grade ovarian carcinoma cells

R. S. Conlan, R. Prinjha, I. Rioja, 2023, Clinical Epigenetics.

In silico enhancer mining reveals SNS-032 and EHMT2 inhibitors as therapeutic candidates in high-grade serous ovarian cancer

R. Prinjha, I. Rioja, L. Francis, 2023, British Journal of Cancer.

A new ditriazine inhibitor of NF-κB modulates chronic inflammation and angiogenesis

I. Rioja, A. Úbeda, R. Riguera, 2002, Naunyn-Schmiedeberg's Archives of Pharmacology.

An anti-inflammatory ditriazine inhibiting leukocyte functions and expression of inducible nitric oxide synthase and cyclo-oxygenase-2.

M. Alcaraz, I. Rioja, C. Peinador, 2000, European journal of pharmacology.

GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family.

P. Grandi, A. Michon, I. Wall, 2020, ACS Medicinal Chemistry Letters.

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.

BET Inhibition Improves NASH and Liver Fibrosis

Sarah A. Middleton, Pankaj Agarwal, D. Rajpal, 2018, Scientific Reports.

INTERNATIONAL UNION OF BASIC AND CLINICAL PHARMACOLOGY REVIEW Epigenetic pathway targets for the treatment of disease: accelerating progress in the development of pharmacological tools: IUPHAR Review 11

R. Prinjha, D. Tough, I. Rioja, 2014 .

BET bromodomain inhibition reduces maturation and enhances tolerogenic properties of human and mouse dendritic cells.

P. Tak, R. Prinjha, D. Tough, 2016, Molecular immunology.

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.