K. Boxall

发表

Trans‐activation of the DNA‐damage signalling protein kinase Chk2 by T‐loop exchange

Sibylle Mittnacht, Michelle D Garrett, Laurence H Pearl, 2006, The EMBO journal.

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 .

Structure-activity relationships in purine-based inhibitor binding to HSP90 isoforms.

X. Barril, M. Drysdale, P. Workman, 2004, Chemistry & biology.

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.

4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer.

Mike Wood, Brian Dymock, Xavier Barril, 2007, Journal of medicinal chemistry.

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.

The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors.

Paul Workman, Edward McDonald, Chrisostomos Prodromou, 2005, Bioorganic & medicinal chemistry letters.

Design and evaluation of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines as inhibitors of checkpoint and other kinases.

Ian Collins, C. E. Allen, Michelle D Garrett, 2010, Bioorganic & medicinal chemistry letters.

Benzimidazole inhibitors induce a DFG-out conformation of never in mitosis gene A-related kinase 2 (Nek2) without binding to the back pocket and reveal a nonlinear structure-activity relationship.

R. V. van Montfort, K. Boxall, G. Aherne, 2011, Journal of medicinal chemistry.

Naturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug Resistance.

R. V. van Montfort, P. Workman, A. Faisal, 2015, Cancer research.

Microfluidic Mobility Shift Assay for Real-Time Analysis of Peptide N-Palmitoylation

K. Boxall, J. Blagg, A. Magee, 2017, SLAS discovery : advancing life sciences R & D.

Structure-guided design of purine-based probes for selective Nek2 inhibition

I. Hardcastle, R. Griffin, B. Golding, 2016, Oncotarget.

8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors

G. F. Ruda, O. Fedorov, C. Bountra, 2016, Journal of medicinal chemistry.

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.

Solid-phase immunoassays in mechanism-based drug discovery: their application in the development of inhibitors of the molecular chaperone heat-shock protein 90.

P. Workman, K. Boxall, P. Clarke, 2005, Assay and drug development technologies.

Synthetic ansamycins prepared by a ring-expanding Claisen rearrangement. Synthesis and biological evaluation of ring and conformational analogues of the Hsp90 molecular chaperone inhibitor geldanamycin.

A. Slawin, P. Workman, K. Boxall, 2007, Organic & biomolecular chemistry.

Assays for HSP90 and inhibitors.

L. Pearl, P. Workman, M. Walton, 2003, Methods in molecular medicine.

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.

Aurora Isoform Selectivity: Design and Synthesis of Imidazo[4,5-b]pyridine Derivatives as Highly Selective Inhibitors of Aurora-A Kinase in Cells

P. Workman, A. Faisal, K. Boxall, 2013, Journal of medicinal chemistry.

Inhibition of Hsp90 with synthetic macrolactones: synthesis and structural and biological evaluation of ring and conformational analogs of radicicol.

Paul Workman, Chrisostomos Prodromou, Laurence H Pearl, 2006, Chemistry & biology.

CCT241533 is a potent and selective inhibitor of CHK2 that potentiates the cytotoxicity of PARP inhibitors.

L. Pearl, M. Walton, A. Oliver, 2011, Cancer research.

Aminopyrazine Inhibitors Binding to an Unusual Inactive Conformation of the Mitotic Kinase Nek2: SAR and Structural Characterization†

Caterina Barillari, Ian Collins, Samantha Burns, 2010, Journal of medicinal chemistry.

The discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug design

R. V. van Montfort, P. Workman, R. Griffin, 2013, Oncotarget.

2-Arylamino-6-ethynylpurines are cysteine-targeting irreversible inhibitors of Nek2 kinase

I. Hardcastle, R. Griffin, B. Golding, 2020, RSC medicinal chemistry.

A chemical inhibitor of PPM1D that selectively kills cells overexpressing PPM1D

A. Ashworth, P. Workman, C. Lord, 2008, Oncogene.

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.

In vitro biological characterization of a novel, synthetic diaryl pyrazole resorcinol class of heat shock protein 90 inhibitors.

L. Pearl, P. Workman, R. Marais, 2007, Cancer research.

Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.

L. Pearl, A. Oliver, K. Boxall, 2011, Journal of medicinal chemistry.

Is a Potent and Selective Inhibitor of CHK 2 that Potentiates the Cytotoxicity of PARP Inhibitors

L. Pearl, M. Walton, A. Oliver, 2011 .

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

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

A duplexed phenotypic screen for the simultaneous detection of inhibitors of the molecular chaperone heat shock protein 90 and modulators of cellular acetylation

P. Workman, K. Boxall, W. Aherne, 2007, Molecular Cancer Therapeutics.

Fragment-Based Screening Maps Inhibitor Interactions in the ATP-Binding Site of Checkpoint Kinase 2

Ian Collins, Isaac M. Westwood, Nathan Brown, 2013, PloS one.

Identification and characterisation of 2-aminopyridine inhibitors of checkpoint kinase 2.

C. E. Allen, L. Pearl, A. Oliver, 2010, Bioorganic & medicinal chemistry.

Identification of inhibitors of checkpoint kinase 1 through template screening.

Ian Collins, Samantha Burns, David Williams, 2009, Journal of medicinal chemistry.

Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity.

K. Boxall, G. Aherne, R. Bayliss, 2012, Journal of medicinal chemistry.

Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: SAR, structural biology and cellular activity

Swen, K. Boxall, G. Aherne, 2012 .

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.

Inhibition of the heat shock protein 90 molecular chaperone in vitro and in vivo by novel, synthetic, potent resorcinylic pyrazole/isoxazole amide analogues

L. Pearl, X. Barril, M. Drysdale, 2007, Molecular Cancer Therapeutics.

118 2-arylamino-6-ethynylpurines as Potent Irreversible Inhibitors of the Mitotic Kinase Nek2

R. Griffin, K. Boxall, R. Bayliss, 2012 .

Aurora Isoform Selectivity: Design and Synthesis of Imidazo [4, 5-b] pyridine Derivatives as Highly

A. Faisal, K. Boxall, Nathan Brown, 2013 .

Trans‐activation of the DNA‐damage signalling protein kinase Chk2 by T‐loop exchange

L. Pearl, A. Oliver, A. Paul, 2006, The EMBO journal.

R. V. van Montfort, K. Boxall, G. Aherne, 2016, 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.