D. Lugo

发表

Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia

S. Robson, G. Drewes, M. Bantscheff, 2011, Nature.

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.

Functional interdependence of BRD4 and DOT1L in MLL leukemia

Andrew J. Bannister, P. Grandi, G. Drewes, 2016, Nature Structural &Molecular Biology.

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.

Acute resistance to BET inhibitors remodels compensatory transcriptional programs via p300 co-activation

R. Prinjha, E. Meduri, B. Huntly, 2022, bioRxiv.

Inhibition of spleen tyrosine kinase as treatment of postoperative ileus

G. Boeckxstaens, W. D. de Jonge, César Ramírez-Molina, 2012, Gut.

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.

BET inhibitor resistance emerges from leukaemia stem cells

Mark A. Dawson, Omar Abdel-Wahab, Alan F. Rubin, 2015, Nature.

Click chemistry enables preclinical evaluation of targeted epigenetic therapies

P. Grandi, G. Drewes, S. Dawson, 2017, Science.

Recurrent mutations, including NPM1c, activate a BRD4-dependent core transcriptional program in acute myeloid leukemia

S. Robson, G. Drewes, L. Bullinger, 2013, Leukemia.

Optimisation of a novel series of potent and orally bioavailable azanaphthyridine SYK inhibitors.

David M. Wilson, J. Liddle, D. Lugo, 2016, Bioorganic & medicinal chemistry letters.

Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy.

Andrew J. Bannister, S. Robson, S. Knapp, 2015, Cancer research.

Protein arginine deiminase 4 inhibition is sufficient for the amelioration of collagen‐induced arthritis

P. Tak, R. Prinjha, V. Holers, 2017, Clinical and experimental immunology.

BRD4 Short Isoform Interacts with RRP1B, SIPA1 and Components of the LINC Complex at the Inner Face of the Nuclear Membrane

N. Crawford, K. Gardner, D. Esposito, 2013, PloS one.

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.

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.

GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain

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

Inhibition of spleen tyrosine kinase as treatment of postoperative ileus

Fleur S. van de Bovenkamp, G. Boeckxstaens, W. D. de Jonge, 2012, Gut.

Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy.

Andrew J. Bannister, S. Robson, S. Knapp, 2015, Cancer research.

Recurrent mutations, including NPM1c, activate a BRD4-dependent core transcriptional program in acute myeloid leukemia

S. Robson, G. Drewes, L. Bullinger, 2013, Leukemia.

Tissue distribution and brain penetration of niraparib in tumor bearing mouse models and its clinical relevance.

G. Fulci, E. Minthorn, D. Lugo, 2021 .