Balb/c mice as a preclinical model for raltitrexed-induced gastrointestinal toxicity

Autor: Sj, Clarke, Dc, Farrugia, Gw, Aherne, David Mark Pritchard, Benstead J, Al, Jackman

Publikováno v: Europe PubMed Central

Raltitrexed (RTX) is an antifolate thymidylate synthase (TS) inhibitor used for the treatment of advanced colorectal cancer. RTX induces proliferating tissue toxicities that are largely confined to the intestine, with diarrhea being a severe side eff

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid_dedup__::1070d66ffdce9a96e42bf7eff8b38648
http://europepmc.org/abstract/med/10656460

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.

Autor: Walton MI; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, UK., Eve PD; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, UK., Hayes A; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, UK., Henley AT; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, UK., Valenti MR; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, UK., De Haven Brandon AK; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, UK., Box G; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, UK., Boxall KJ; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, UK., Tall M; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, UK., Swales K; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, UK., Matthews TP; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, UK., McHardy T; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, UK., Lainchbury M; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, UK., Osborne J; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, UK., Hunter JE; Institute for Cell and Molecular Biosciences, Medical School, Newcastle University, Newcastle Upon Tyne, UK., Perkins ND; Institute for Cell and Molecular Biosciences, Medical School, Newcastle University, Newcastle Upon Tyne, UK., Aherne GW; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, UK., Reader JC; Sareum Ltd, Cambridge, UK., Raynaud FI; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, UK., Eccles SA; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, UK., Collins I; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, UK., Garrett MD; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, UK.; School of Biosciences, University of Kent, Canterbury, Kent, UK.

Publikováno v: Oncotarget [Oncotarget] 2016 Jan 19; Vol. 7 (3), pp. 2329-42.

Fragment-based screening maps inhibitor interactions in the ATP-binding site of checkpoint kinase 2.

Autor: Silva-Santisteban MC; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, Haddow Laboratories, Sutton, Surrey, United Kingdom., Westwood IM, Boxall K, Brown N, Peacock S, McAndrew C, Barrie E, Richards M, Mirza A, Oliver AW, Burke R, Hoelder S, Jones K, Aherne GW, Blagg J, Collins I, Garrett MD, van Montfort RL

Publikováno v: PloS one [PLoS One] 2013 Jun 12; Vol. 8 (6), pp. e65689. Date of Electronic Publication: 2013 Jun 12 (Print Publication: 2013).

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

Autor: Walton MI; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, Sutton, United Kingdom. Mike.Walton@icr.ac.uk, Eve PD, Hayes A, Valenti MR, De Haven Brandon AK, Box G, Hallsworth A, Smith EL, Boxall KJ, Lainchbury M, Matthews TP, Jamin Y, Robinson SP, Aherne GW, Reader JC, Chesler L, Raynaud FI, Eccles SA, Collins I, Garrett MD

Publikováno v: Clinical cancer research : an official journal of the American Association for Cancer Research [Clin Cancer Res] 2012 Oct 15; Vol. 18 (20), pp. 5650-61. Date of Electronic Publication: 2012 Aug 28.

Mechanism-based screen for G1/S checkpoint activators identifies a selective activator of EIF2AK3/PERK signalling.

Autor: Stockwell SR; Research Department of Cancer Biology, UCL Cancer Institute, London, United Kingdom., Platt G, Barrie SE, Zoumpoulidou G, Te Poele RH, Aherne GW, Wilson SC, Sheldrake P, McDonald E, Venet M, Soudy C, Elustondo F, Rigoreau L, Blagg J, Workman P, Garrett MD, Mittnacht S

Publikováno v: PloS one [PLoS One] 2012; Vol. 7 (1), pp. e28568. Date of Electronic Publication: 2012 Jan 12.