Additional Publications

Additional publications.

Sareum programmes

TYK2/JAK1: Publications

1 December 2019

A New Regulatory Switch in a JAK Protein Kinase.

Publication: AACR-EORTC-NCI (2019)

Authors: J Reader, T Mitchell et al

1 October 2014

Inhibition of TYK2 and JAK1 Ameliorates Imiquimod-Induced Psoriasis-like Dermatitis by Inhibiting IL-22 and the IL-23/IL-17 Axis

Publication: J Immunol (2014)

Authors: Works MG, Yin F, Yin CC, Yiu Y, Shew K, Tran TT, Dunlap N, Lam J, Mitchell T, Reader J, Stein PL, D’Andrea A. J Immunol.

1 December 2019

A New Regulatory Switch in a JAK Protein Kinase

Publication: Proteins: Structure, Function & Bioinformatics (2011)

Authors: Tsui, V., Gibbons, P., Ultsch, M., Motara, K., Chang, C., Blair, W., Pulk, R., Stanley, M., Starovasnik, M., Willimas, D., Lamers, M., Leonard, P., Magnuson, S., Liang, J. & Eigenbrot, C

Sareum programmes

Chk1: Publications

15 January 2023

A Phase I/II Trial of Oral SRA737 (a Chk1 Inhibitor) Given in Combination with Low-Dose Gemcitabine in Patients with Advanced Cancer.

Publication: Clin Cancer Res, 15 November 2022

Authors: R Jones R Plummer, V Moreno, L Carter, D Roda, E Garralda, R Kristeleit, D Sarker, T Arkenau, P Roxburgh, HS Walter, S Blagden, A Anthoney, BJ Klencke, MM Kowalski & U Banerji

1 July 2021

A study of combinatorial growth inhibition, cell death and DNA damage repair caused by CHK1 inhibitor SRA737 and WEE1 inhibitor adavosertib in TP53 mutated cell line

Publication: AACR Annual Meeting 2021

Authors: A Stewart, L Pickard, A Hallsworth, S Sauvaigo, G Muggiolu, F Raynaud, U BANERJI

15 April 2020

CHK1 Inhibition Is Synthetically Lethal with Loss of B-Family DNA Polymerase Function in Human Lung and Colorectal Cancer Cells

Publication: Cancer Research (2020)

Authors: R Rogers, M Walton, D Cherry, I Collins, P Clarke, M & P Workman

27 August 2019

Combination treatment of the oral CHK1 inhibitor, SRA737 and low dose gemcitabine, enhances the effect of PD-L1 blockade by modulating the immune microenvironment in small cell lung cancer

Publication: J Thoracic Oncology 27 Aug 2019

Authors: T Sen et. al

19 July 2018

The CHK1 inhibitor SRA737 synergizes with PARP1 inhibitors to kill carcinoma cells

Publication: Cancer Biology & Therapy 2018

Authors: L Booth, J Roberts, A Poklepovic & P Dent

25 January 2017

An orally bioavailable Chk1 inhibitor, CCT244747, sensitizes bladder and head and neck cancer cell lines to radiation

Publication: Radiother Oncol (2017)

Authors: R Patel, HE Barker, J Kyula, M McLaughlin, MT Dillon, U Schick, H Hafsi, A Thompson, V Khoo, K Harrington & S Zaidi

15 September 2016

DNA replication stress mediates APOBEC3 family mutagenesis in breast cancer

Publication: Genome Biology (2016)

Authors: N Kanu, MA Cerone, G Goh, L-P Zalmas, J Bartkova, M Dietzen, N McGranahan, R Rogers, EK Law, I Gromova, M Kschischo, MI Walton, OW Rossanese, J Bartek, RS Harris, S Venkatesan and C Swanton

1 September 2016

CHK1 inhibition radiosensitises head and neck cancers to paclitaxel-based chemoradiotherapy

Publication: Mol Cancer Therapeutics (2016)

Authors: HE Barker, R Patel, M McLaughlin, U Schick, S Zaidi, CM Nutting, KL Newbold, S Bhide, KJ Harrington

11 May 2016

Multi-parameter 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)

Publication: J. Med. Chem. 2016

Authors: JD Osborne, TP Matthews, T McHardy, N Proisy, K-M J Cheung, M Lainchbury, N Brown, MI Walton, PD Eve, KJ Boxall, A Hayes, AT Henley, MR Valenti, AK De Haven Brandon, G Box, Y Jamin, SP Robinson, IM Westwood, RLM van Montfort, PM Leonard, MBAC Lamers, JC Reader, GW Aherne, FI Raynaud, SA Eccles, MD Garrett and I Collins

22 July 2015

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

Publication: Oncotarget 2015

Authors: MI Walton, PD Eve, A Hayes, AT Henley, MR Valenti, AK De Haven Brandon, G Box, KJ Boxall, M Tall, K Swales, TP Matthews, T McHardy, M Lainchbury, J Osborne, JE Hunter, ND Perkins, GW Aherne, JC Reader, FI Raynaud, SA Eccles, I Collins and MD Garrett

18 April 2013

Structure-based design, discovery and development of checkpoint kinase inhibitors as potential anticancer therapies

Publication: Expert Opin Drug Discov. 2013

Authors: Matthews TP, Jones AM, Collins I

15 March 2013

Targeted radiosensitization by the Chk1 inhibitor SAR-020106

Publication: International Journal of Radiation Oncology Biology Physics, 2013

Authors: GR Borst, M McLaughlin, JN Kyula, S Neijenhuis, A Khan, J Good … & KJ Harrington

19 October 2012

Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino) pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors

Publication: Journal of Medicinal Chemistry 2012

Authors: Lainchbury M, Matthews TP, McHardy T, Boxall KJ, Walton MI, Eve PD, … & Collins, I

15 October 2012

CCT244747 is a novel potent and selective CHK1 inhibitor with oral efficacy alone and in combination with genotoxic anticancer drugs

Publication: Clinical Cancer Research 2012

Authors: Walton MI, Eve PD, Hayes A, Valenti MR, Alexis K, Box G, … & Garrett MD

23 November 2011

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

Publication: J. Med. Chem., 2011

Authors: JC Reader, TP Matthews, S Klair, K-MJ Cheung, J Scanlon, N Proisy, G Addison, J Ellard, N Piton, S Taylor, M Cherry, M Fisher, K Boxall, S Burns, MI Walton, IM Westwood, A Hayes, P Eve, M Valenti, A de Haven Brandon, G Box, RLM van Montfort, DH Williams, GW Aherne, FI Raynaud, SA Eccles, MD Garrett and Ian Collins

1 November 2011

CCT244747 is a novel, potent and selective inhibitor of CHK1 with oral efficacy both alone in neuroblastoma and in combination with genotoxic chemotherapeutic agents

Publication: AACR NCI EORTC “Molecular Targets and Cancer Therapeutics”

Authors: MI. Walton, PE. Eve, A Hayes, MR. Valenti, AK. de Haven Brandon, G Box, A Hallsworth, EL. Smith, KJ. Boxall, M Lainchbury, TP. Matthews, Y Jamin, SP Robinson, GW Aherne, JC. Reader, L Chesler, FI. Raynaud, SE Eccles, I Collins, MD Garrett

23 November 2011

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

Publication: AACR NCI EORTC “Molecular Targets and Cancer Therapeutics”

Authors: TP Matthews, S Klair, K-MJ Cheung, J Scanlon, M Lainchbury, N Piton, M Fisher, M Cherry, K Boxall, MI. Walton, IM Westwood, A Hayes, P Eve, M Valenti, A de Haven Brandon, G Box, RLM van Montfort, DH. Williams, W Aherne, FI Raynaud, SA Eccles, MD Garrett, JC. Reader, I Collins

15 July 2010

Design and Evaluation of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines as Inhibitors of Checkpoint and Other Kinases

Publication: Bioorg & Med Chem Lett (2010)

Authors: Matthews, T.P., McHardy, T., Klair, S., Boxhall, K., Fisher, M., Cherry, M., Allen, C.E., Addison, G.J., Ellard, J., Aherne, G.W., Westwood, I.M, van Montfort, R., Garrett, M.D., Reader, J.C. & Collins, I

1 January 2010

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

Publication: Mol Cancer Ther (2010)

Authors: Walton, M.I., Eve, P.D., Hayes, A., Valenti, M., De Haven Brandon, A., Box, G., Boxall, K.J., Aherne, G.W., Eccles, S.A., Raynauld, F.I., Williams, D.H., Reader, J.C., Collins, I., Garrett, M.D

2 July 2009

Identification of Inhibitors of Checkpoint Kinase 1 through Template Screening

Publication: J Medicinal Chemistry (2009)

Authors: Matthews, T.P., Klair, S., Burns, S., Boxall, K., Cherry, M., Fisher, M., Westwood, I.M., Walton, M.I., McHardy, T., Kwai-Ming, J.C., Van Montfort, R., Williams, D., Aherne, G.W., Garrett, M.D., Reader, J and Collins, I

1 May 2008

Identification and Structure-guided Optimisation of Novel Inhibitors of Checkpoint Kinase 1 (Chk1) through Combined Biochemical and Crystallographic Screening

Publication: AACR Annual Meeting, San Diego, CA, Apr 12-16, 2008

Authors: Reader, J., Williams, D., Klair, S., Cherry, M., Fisher, M., Scanlon, J., Piton, N., Addison, G., Lamers, M., et al

Sareum Expertise

Publications

1 January 2010

Introduction to Fragment-based Drug Discovery

Publication: Fragment-Based Drug Discovery: Practical Aspects”, E.R. Zartler & M.J. Shapiro, Eds, John Wiley & Sons (2008)

Authors: T Mitchell & M Cherry

2007

Fragment-Based Drug Design

Publication: MedChem News(Japan), (2007)

Authors: Tim Mitchell

2005

Finding protein kinase hits using structural information

Publication: M. Innovations in Pharmaceutical Technology, (2005)

Authors: Cherry, M., Reader, J. and Williams

2005

The design of a new potent and selective ligand for the BRS3 receptor

Publication: J Peptide Research, (2005)

Authors: Boyle, R.G., Humphries, J., Mitchell, T., Showell, G.A., Iijima, H., Shimada, H., Arai, T., Ueno, H., Usui, H., Sakaki, T., Wada, E. and Wada, K

2004

Automation in medicinal chemistry

Publication: C. Current Topics in Medicinal Chemistry, (2004)

Authors: Reader, John

2003

Solid phase synthesis of tetrahydro-1,4-benzodiazepin-2-ones

Publication: Tetrahedron Letters, (2003)

Authors: Hone, Neal D.; Wilson, William; Reader, John C

2005

Solid-phase synthesis of dibenzoxazepinones

Publication: Tetrahedron Letters, (2003)

Authors: Hone, Neal D., Salter, James I., Reader, John C