M. Valenti

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.

Molecular Cancer Therapeutics The Preclinical Pharmacology and Therapeutic Activity of the Novel CHK 1 Inhibitor SAR-020106

M. Walton, K. Boxall, G. Aherne, 2009 .

In vitro and In vivo Pharmacokinetic-Pharmacodynamic Relationships for the Trisubstituted Aminopurine Cyclin-Dependent Kinase Inhibitors Olomoucine, Bohemine and CYC202

S. Clarke, D. Lane, P. Workman, 2005, Clinical Cancer Research.

Combining hit identification strategies: fragment-based and in silico approaches to orally active 2-aminothieno[2,3-d]pyrimidine inhibitors of the Hsp90 molecular chaperone.

X. Barril, B. Davis, M. Drysdale, 2009, Journal of Medicinal Chemistry.

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.

Pharmacokinetic-Pharmacodynamic Relationships for the Heat Shock Protein 90 Molecular Chaperone Inhibitor 17-Allylamino , 17-Demethoxygeldanamycin in Human Ovarian Cancer

P. Workman, I. Judson, M. Walton, 2005 .

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.

The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer .

Gary Box, Paul Workman, Christian Wiesmann, 2008, Journal of medicinal chemistry.

Mechanism of action of the Aurora kinase inhibitor CCT129202 and in vivo quantification of biological activity

P. Workman, F. Chan, R. T. te Poele, 2007, Molecular Cancer Therapeutics.

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.

Mode of cell death induced by the HSP90 inhibitor 17-AAG (tanespimycin) is dependent on the expression of pro-apoptotic BAX

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

A G-quadruplex-interactive potent small-molecule inhibitor of telomerase exhibiting in vitro and in vivo antitumor activity.

S. Neidle, L. Kèlland, M. Valenti, 2002, Molecular pharmacology.

Human ovarian-carcinoma cell lines and companion xenografts: a disease-oriented approach to new platinum anticancer drug discovery

L. Kèlland, M. Valenti, G. Abel, 2004, Cancer Chemotherapy and Pharmacology.

Dependence of Wilms tumor cells on signaling through insulin-like growth factor 1 in an orthotopic xenograft model targetable by specific receptor inhibition

Chris Jones, F. Hofmann, S. Robinson, 2012, Proceedings of the National Academy of Sciences.

Cancer Therapy : Preclinical AT 13148 Is a Novel , Oral Multi-AGC Kinase Inhibitor with Potent Pharmacodynamic and Antitumor Activity

P. Jones, P. Workman, M. Walton, 2012 .

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.

Pharmacokinetic/pharmacodynamic study of ZD9331, a nonpolyglutamatable inhibitor of thymidylate synthase, in a murine model following two curative administration schedules.

G. Aherne, M. Valenti, L. Brunton, 2001, Clinical cancer research : an official journal of the American Association for Cancer Research.

Schedule dependency of orally administered bis-acetato-ammine-dichloro-cyclohexylamine-platinum(IV) (JM216) in vivo.

L. Kèlland, M. Valenti, M. McKeage, 1994, Cancer research.

Preclinical antitumor evaluation of bis-acetato-ammine-dichloro-cyclohexylamine platinum(IV): an orally active platinum drug.

L. Kèlland, M. Valenti, B. Murrer, 1993, 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.

A novel serum protein signature associated with resistance to epidermal growth factor receptor tyrosine kinase inhibitors in head and neck squamous cell carcinoma.

B. Al-Lazikani, K. Harrington, M. Valenti, 2013, European journal of cancer.

An in vitro and in vivo study of the combination of the heat shock protein inhibitor 17-allylamino-17-demethoxygeldanamycin and carboplatin in human ovarian cancer models

P. Workman, I. Judson, M. Walton, 2008, Cancer Chemotherapy and Pharmacology.

Comparison of thymidylate synthase (TS) protein up-regulation after exposure to TS inhibitors in normal and tumor cell lines and tissues.

G. Aherne, M. Valenti, L. Brunton, 2000, Clinical cancer research : an official journal of the American Association for Cancer Research.

Antitumour evaluation of dolastatins 10 and 15 and their measurement in plasma by radioimmunoassay

L. Kèlland, G. Aherne, M. Valenti, 1996, Cancer Chemotherapy and Pharmacology.

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.

Abstract B74: The dual FLT3-Aurora inhibitor CCT241736 overcomes resistance to selective FLT3 inhibition driven by FLT3 ligand and FLT3 point mutations in acute myeloid leukemia.

P. Workman, A. Faisal, M. Valenti, 2011 .

De novo phosphatidylcholine synthesis is required for autophagosome membrane formation and maintenance during autophagy

M. Leach, H. Parkes, R. Fleck, 2019, Autophagy.

Overexpression of BclXL in a human ovarian carcinoma cell line: Paradoxic effects on chemosensitivity in vitro versus in vivo

P. Beale, S. Johnston, L. Kèlland, 2002, International journal of cancer.

BGC 945, a novel tumor-selective thymidylate synthase inhibitor targeted to alpha-folate receptor-overexpressing tumors.

M. Valenti, F. Raynaud, A. Jackman, 2005, Cancer research.

Synthesis and in vitro and in vivo antitumor activity of a series of trans platinum antitumor complexes.

L. Kèlland, M. Valenti, B. Murrer, 1995, Journal of medicinal chemistry.

Selective potentiation of platinum drug cytotoxicity in cisplatin-sensitive and-resistant human ovarian carcinoma cell lines by amphotericin B

L. Kèlland, M. Valenti, S. Sharp, 2004, Cancer Chemotherapy and Pharmacology.

Novel Tumor-Selective Thymidylate Synthase Inhibitor Targeted to A-Folate Receptor – Overexpressing Tumors

M. Valenti, F. Raynaud, A. Jackman, 2005 .

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.

A novel trans-platinum coordination complex possessing in vitro and in vivo antitumor activity.

L. Kèlland, M. Valenti, B. Murrer, 1994, Cancer research.

cis-Amminedichloro(2-methylpyridine) platinum(II) (AMD473), a novel sterically hindered platinum complex: in vivo activity, toxicology, and pharmacokinetics in mice.

L. Kèlland, M. Valenti, F. Raynaud, 1997, Clinical cancer research : an official journal of the American Association for Cancer Research.

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.

The role of murine tumour models and their acquired platinum-resistant counterparts in the evaluation of novel platinum antitumour agents: a cautionary note.

M. Valenti, P. Goddard, K. Harrap, 1991, Annals of oncology : official journal of the European Society for Medical Oncology.

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

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

Preclinical Development Enhanced Efficacy of IGF 1 R Inhibition in Pediatric Glioblastoma by Combinatorial Targeting of PDGFR a / b

Chris Jones, F. Hofmann, S. Jeay, 2011 .

ALK2 inhibitors display beneficial effects in preclinical models of ACVR1 mutant diffuse intrinsic pontine glioma

M. Monje, J. Mora, Chris Jones, 2019, Communications Biology.

ALK2 inhibitors display beneficial effects in preclinical models of ACVR1 mutant diffuse intrinsic pontine glioma

M. Monje, J. Mora, Chris Jones, 2019, Communications Biology.

Molecular pharmacology of phosphatidylinositol 3-kinase inhibition in human glioma

Paul Workman, Lynn Bjerke, Melanie Valenti, 2009, Cell cycle.

FGF7–FGFR2 autocrine signaling increases growth and chemoresistance of fusion‐positive rhabdomyosarcomas

A. Kelsey, M. Valenti, F. Raynaud, 2021, Molecular oncology.

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.

Preclinical antitumor activity and pharmacodynamic studies with the farnesyl protein transferase inhibitor R115777 in human breast cancer.

M. Dowsett, P. Workman, A. Howes, 2001, Clinical cancer research : an official journal of the American Association for Cancer Research.

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.

Establishment of an isogenic human colon tumor model for NQO1 gene expression: application to investigate the role of DT-diaphorase in bioreductive drug activation in vitro and in vivo.

P. Workman, L. Kèlland, M. Valenti, 2000, Molecular pharmacology.

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.

Benzoquinone ansamycin heat shock protein 90 inhibitors modulate multiple functions required for tumor angiogenesis

P. Workman, M. Valenti, S. Eccles, 2006, Molecular Cancer Therapeutics.

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.

The Bcl-2/Bcl-XL Family Inhibitor ABT-737 Sensitizes Ovarian Cancer Cells to Carboplatin

S. Kaye, M. Valenti, S. Eccles, 2007, Clinical Cancer Research.

Antitumor-activity of orally-administered ammine amine platinum (iv) dicarboxylate complexes against a panel of human ovarian-carcinoma xenografts.

L. Kèlland, M. Valenti, C. Giandomenico, 1993, International journal of oncology.

Novel trans platinum complexes: comparative in vitro and in vivo activity against platinum-sensitive and resistant murine tumours.

L. Kèlland, M. Valenti, B. Murrer, 1996, Anticancer research.

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.

ENHANCED EFFICACY OF IGF1R INHIBITION IN PAEDIATRIC GLIOBLASTOMA BY COMBINATORIAL TARGETING OF PDGFRALPHA/BETA

Gary Box, Sergey Popov, Darren Hargrave, 2010 .

The 5-HT3 antagonist, BRL 43694, does not compromise the efficacy of cisplatin in tumour-bearing mice

M. Valenti, P. Goddard, K. Harrap, 2004, Cancer Chemotherapy and Pharmacology.

ALK2 inhibitors display beneficial effects in preclinical models of ACVR1 mutant diffuse intrinsic pontine glioma

M. Monje, J. Mora, Chris Jones, 2019, Communications Biology.

Dual Inhibition of Aurora and FLT3 Kinases by CCT137690: A Novel Treatment Strategy Against FLT3-ITD Positive AML In Vitro and In Vivo

P. Workman, A. Faisal, M. Valenti, 2010 .

Resistance to Selective FLT3 Inhibitors, Driven by FLT3 Ligand and FLT3 Point Mutations, Can Be Overcome with the Dual FLT3-Aurora Kinase Inhibitor CCT241736,

P. Workman, A. Faisal, M. Valenti, 2011 .

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.

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.

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.

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

M. Valenti, A. K. de Haven Brandon, R. Ruddle, 2013, Clinical Cancer Research.

Pharmacokinetic-Pharmacodynamic Relationships for the Heat Shock Protein 90 Molecular Chaperone Inhibitor 17-Allylamino, 17-Demethoxygeldanamycin in Human Ovarian Cancer Xenograft Models

U. Banerji, M. Valenti, Lloyd R. Kelland, 2005, Clinical Cancer Research.

R. V. van Montfort, K. Boxall, G. Aherne, 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.