A. K. de Haven Brandon

发表

Preclinical Pharmacology, Antitumor Activity, and Development of Pharmacodynamic Markers for the Novel, Potent AKT Inhibitor CCT128930

P. Workman, M. Walton, M. Garrett, 2010, Molecular Cancer Therapeutics.

The Preclinical Pharmacology and Therapeutic Activity of the Novel CHK1 Inhibitor SAR-020106

Gary Box, Ian Collins, Melanie Valenti, 2010, Molecular Cancer Therapeutics.

CCT244747 Is a Novel Potent and Selective CHK1 Inhibitor with Oral Efficacy Alone and in Combination with Genotoxic Anticancer Drugs

S. Robinson, M. Walton, K. Boxall, 2012, Clinical Cancer Research.

A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease

Gary Box, Julian Blagg, Paul Workman, 2015, Nature chemical biology.

NVP-AUY922: a novel heat shock protein 90 inhibitor active against xenograft tumor growth, angiogenesis, and metastasis.

L. Pearl, X. Barril, M. Drysdale, 2008, Cancer research.

Application of meso scale technology for the measurement of phosphoproteins in human tumor xenografts.

P. Workman, M. Garrett, L. Hunter, 2007, Assay and drug development technologies.

Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns

P. Workman, A. Faisal, M. Valenti, 2012, Leukemia.

Characterisation of CCT271850, a selective, oral and potent MPS1 inhibitor, used to directly measure in vivo MPS1 inhibition vs therapeutic efficacy

A. Faisal, M. Valenti, A. K. de Haven Brandon, 2017, British Journal of Cancer.

Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach.

R. V. van Montfort, A. Faisal, N. Cronin, 2016, Journal of medicinal chemistry.

AT13148 Is a Novel, Oral Multi-AGC Kinase Inhibitor with Potent Pharmacodynamic and Antitumor Activity

P. Jones, P. Workman, M. Walton, 2012, Clinical Cancer Research.

Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737).

S. Robinson, R. V. van Montfort, M. Lamers, 2016, Journal of medicinal chemistry.

Optimization of imidazo [4, 5-b] pyridine-based kinase inhibitors: identification of a dual FLT3/aur

Gary Box, Nathan Brown, Julian Blagg, 2012 .

Quizartinib-resistant FLT3-ITD acute myeloid leukemia cells are sensitive to the FLT3-Aurora kinase inhibitor CCT241736.

A. Faisal, M. Valenti, A. K. de Haven Brandon, 2020, Blood advances.

Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate.

P. Workman, A. Faisal, R. Bayliss, 2010, Journal of medicinal chemistry.

Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo

O. Rossanese, Benjamin R Bellenie, R. V. van Montfort, 2022, Journal of medicinal chemistry.

Combined targeting of MEK and the glucocorticoid receptor for the treatment of RAS-mutant multiple myeloma

N. Carragher, S. Whittaker, A. K. de Haven Brandon, 2020, BMC Cancer.

Pharmacologic characterization of a potent inhibitor of class I phosphatidylinositide 3-kinases.

M. Waterfield, P. Workman, P. Parker, 2007, Cancer research.

Acquired resistance to EGFR tyrosine kinase inhibitors alters the metabolism of human head and neck squamous carcinoma cells and xenograft tumours

M. Leach, H. Parkes, M. Valenti, 2015, British Journal of Cancer.

Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941

P. Workman, Irina S. Chuckowree, P. Clarke, 2009, Molecular Cancer Therapeutics.

Discovery of 3-Alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as Selective, Orally Bioavailable CHK1 Inhibitors

M. Walton, K. Boxall, G. Aherne, 2012, Journal of medicinal chemistry.

Discovery of 4-Amino-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamides As Selective, Orally Active Inhibitors of Protein Kinase B (Akt)†

G. Aherne, M. Garrett, L. Hunter, 2010, Journal of medicinal chemistry.

Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19

Julian Blagg, Paul Workman, Florence I. Raynaud, 2016, Journal of medicinal chemistry.

Orally bioavailable CDK9/2 inhibitor shows mechanism-based therapeutic potential in MYCN-driven neuroblastoma

Charles Y. Lin, J. Bradner, N. Gray, 2020, The Journal of clinical investigation.

Enhanced Efficacy of IGF1R Inhibition in Pediatric Glioblastoma by Combinatorial Targeting of PDGFRα/β

Chris Jones, F. Hofmann, S. Jeay, 2011, Molecular Cancer Therapeutics.

Discovery of Potent, Orally Bioavailable, Small-Molecule Inhibitors of WNT Signaling from a Cell-Based Pathway Screen

F. Rohdich, T. Dale, P. Workman, 2015, Journal of medicinal chemistry.

Dual Blockade of the PI3K/AKT/mTOR (AZD8055) and RAS/MEK/ERK (AZD6244) Pathways Synergistically Inhibits Rhabdomyosarcoma Cell Growth In Vitro and In Vivo

Khin Thway, Melanie Valenti, Torsten Pietsch, 2013, Clinical Cancer Research.

Plasma Metabolomic Changes following PI3K Inhibition as Pharmacodynamic Biomarkers: Preclinical Discovery to Phase I Trial Evaluation

B. Vanhaesebroeck, P. Workman, L. Friedman, 2016, Molecular Cancer Therapeutics.

The clinical development candidate CCT245737 is an orally active CHK1 inhibitor with preclinical activity in RAS mutant NSCLC and Eμ-MYC driven B-cell lymphoma

M. Walton, N. Perkins, K. Boxall, 2015, Oncotarget.

Small-Molecule Activation of p53 Blocks Hypoxia-Inducible Factor 1α and Vascular Endothelial Growth Factor Expression In Vivo and Leads to Tumor Cell Apoptosis in Normoxia and Hypoxia

Gary Box, Margaret Ashcroft, Melanie Valenti, 2009, Molecular and Cellular Biology.

Identification of ovarian high-grade serous carcinoma cell lines that show estrogen-sensitive growth as xenografts in immunocompromised mice

M. Valenti, A. K. de Haven Brandon, G. Box, 2020, Scientific Reports.

Structure-Guided Evolution of Potent and Selective CHK1 Inhibitors through Scaffold Morphing

Gary Box, Ian Collins, Isaac M. Westwood, 2011, Journal of medicinal chemistry.

Modulation of Plasma Metabolite Biomarkers of the MAPK Pathway with MEK Inhibitor RO4987655: Pharmacodynamic and Predictive Potential in Metastatic Melanoma

M. Venturi, D. Skene, P. Workman, 2017, Molecular Cancer Therapeutics.

Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4-d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N2-(2-Ethoxy-4-(4-methyl-4H-1,2,4-triazol-3-yl)phenyl)-6-methyl-N8-neopentylpyrido[3,4-d]pyrimidine-2,8-diamine (BOS172722)

R. V. van Montfort, A. Faisal, N. Cronin, 2018, Journal of medicinal chemistry.

Structure-Based Design of Orally Bioavailable 1H-Pyrrolo[3,2-c]pyridine Inhibitors of Mitotic Kinase Monopolar Spindle 1 (MPS1)

Isaac M. Westwood, Julian Blagg, Florence I. Raynaud, 2013, Journal of medicinal chemistry.

Assessing the mechanism and therapeutic potential of modulators of the human Mediator complex-associated protein kinases

S. Czasch, F. Rohdich, T. Dale, 2016, eLife.

Suppression of interferon gene expression overcomes resistance to MEK inhibition in KRAS-mutant colorectal cancer

A. Rust, C. Isacke, S. Whittaker, 2018, Oncogene.

Discovery of an In Vivo Chemical Probe for BCL6 Inhibition by Optimization of Tricyclic Quinolinones

O. Rossanese, Benjamin R Bellenie, R. V. van Montfort, 2023, Journal of Medicinal Chemistry.

Discovery and validation of biomarkers to support clinical development of NXP800: A first-in-class orally active, small-molecule HSF1 pathway inhibitor

P. Workman, P. Clarke, M. Valenti, 2022, European Journal of Cancer.

Combining TRAIL with PI3 Kinase or HSP90 inhibitors enhances apoptosis in colorectal cancer cells via suppression of survival signaling

P. Workman, P. Clarke, M. Valenti, 2013, Oncotarget.

Characterisation of CCT271850, a selective, oral and potent MPS1 inhibitor, used to directly measure in vivo MPS1 inhibition vs therapeutic efficacy

A. Faisal, M. Valenti, A. K. de Haven Brandon, 2017, British Journal of Cancer.

Signalling involving MET and FAK supports cell division independent of the activity of the cell cycle-regulating CDK4/6 kinases

Paul Workman, Bissan Al-Lazikani, Sibylle Mittnacht, 2019, bioRxiv.

Optimization of Imidazo[4,5-b]pyridine-Based Kinase Inhibitors: Identification of a Dual FLT3/Aurora Kinase Inhibitor as an Orally Bioavailable Preclinical Development Candidate for the Treatment of Acute Myeloid Leukemia

M. Valenti, A. K. de Haven Brandon, Alan T. Henley, 2012, Journal of Medicinal Chemistry.