Zobrazeno 1 - 10 of 38 pro vyhledávání: '"Van Montfort RL"'
1
Exploiting Protein Conformational Change to Optimize Adenosine-Derived Inhibitors of HSP70
Autor: Cheeseman, MD, Westwood, IM, Barbeau, O, Rowlands, M, Dobson, S, Jones, AM, Jeganathan, F, Burke, R, Kadi, N, Workman, P, Collins, I, van Montfort, RL, Jones, K
HSP70 is a molecular chaperone and a key component of the heat-shock response. Because of its proposed importance in oncology, this protein has become a popular target for drug discovery, efforts which have as yet brought little success. This study d
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=od_______128::0133f6371bc3d56bc5e234214a979624
https://e-space.mmu.ac.uk/613362/
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3
Akademický článek
An Irreversible Inhibitor of HSP72 that Unexpectedly Targets Lysine-56.
Autor: Pettinger J; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, SW7 3RP, UK., Le Bihan YV; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, SW7 3RP, UK.; Division of Structural Biology, The Institute of Cancer Research, London, SW7 3RP, UK., Widya M; Proteomics Core Facility, The Institute of Cancer Research, London, SW7 3RP, UK., van Montfort RL; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, SW7 3RP, UK.; Division of Structural Biology, The Institute of Cancer Research, London, SW7 3RP, UK., Jones K; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, SW7 3RP, UK., Cheeseman MD; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, SW7 3RP, UK.
Publikováno v: Angewandte Chemie (International ed. in English) [Angew Chem Int Ed Engl] 2017 Mar 20; Vol. 56 (13), pp. 3536-3540. Date of Electronic Publication: 2017 Feb 22.
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4
Akademický článek
Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen.
Autor: Cheeseman MD; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SW7 3RP, United Kingdom., Chessum NE; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SW7 3RP, United Kingdom., Rye CS; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SW7 3RP, United Kingdom., Pasqua AE; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SW7 3RP, United Kingdom., Tucker MJ; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SW7 3RP, United Kingdom., Wilding B; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SW7 3RP, United Kingdom., Evans LE; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SW7 3RP, United Kingdom., Lepri S; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SW7 3RP, United Kingdom., Richards M; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SW7 3RP, United Kingdom., Sharp SY; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SW7 3RP, United Kingdom., Ali S; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SW7 3RP, United Kingdom.; Division of Structural Biology at The Institute of Cancer Research , London SW7 3RP, United Kingdom., Rowlands M; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SW7 3RP, United Kingdom., O'Fee L; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SW7 3RP, United Kingdom., Miah A; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SW7 3RP, United Kingdom., Hayes A; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SW7 3RP, United Kingdom., Henley AT; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SW7 3RP, United Kingdom., Powers M; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SW7 3RP, United Kingdom., Te Poele R; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SW7 3RP, United Kingdom., De Billy E; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SW7 3RP, United Kingdom., Pellegrino L; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SW7 3RP, United Kingdom., Raynaud F; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SW7 3RP, United Kingdom., Burke R; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SW7 3RP, United Kingdom., van Montfort RL; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SW7 3RP, United Kingdom.; Division of Structural Biology at The Institute of Cancer Research , London SW7 3RP, United Kingdom., Eccles SA; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SW7 3RP, United Kingdom., Workman P; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SW7 3RP, United Kingdom., Jones K; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SW7 3RP, United Kingdom.
Publikováno v: Journal of medicinal chemistry [J Med Chem] 2017 Jan 12; Vol. 60 (1), pp. 180-201. Date of Electronic Publication: 2016 Dec 22.
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5
Akademický článek
Structure of the Epigenetic Oncogene MMSET and Inhibition by N-Alkyl Sinefungin Derivatives.
Autor: Tisi D; Astex Pharmaceuticals , 436 Cambridge Science Park, Milton Road, Cambridge, United Kingdom CB4 0QA., Chiarparin E; Astex Pharmaceuticals , 436 Cambridge Science Park, Milton Road, Cambridge, United Kingdom CB4 0QA., Tamanini E; Astex Pharmaceuticals , 436 Cambridge Science Park, Milton Road, Cambridge, United Kingdom CB4 0QA., Pathuri P; Astex Pharmaceuticals , 436 Cambridge Science Park, Milton Road, Cambridge, United Kingdom CB4 0QA., Coyle JE; Astex Pharmaceuticals , 436 Cambridge Science Park, Milton Road, Cambridge, United Kingdom CB4 0QA., Hold A; Astex Pharmaceuticals , 436 Cambridge Science Park, Milton Road, Cambridge, United Kingdom CB4 0QA., Holding FP; Astex Pharmaceuticals , 436 Cambridge Science Park, Milton Road, Cambridge, United Kingdom CB4 0QA., Amin N; Astex Pharmaceuticals , 436 Cambridge Science Park, Milton Road, Cambridge, United Kingdom CB4 0QA., Martin AC; Astex Pharmaceuticals , 436 Cambridge Science Park, Milton Road, Cambridge, United Kingdom CB4 0QA., Rich SJ; Astex Pharmaceuticals , 436 Cambridge Science Park, Milton Road, Cambridge, United Kingdom CB4 0QA., Berdini V; Astex Pharmaceuticals , 436 Cambridge Science Park, Milton Road, Cambridge, United Kingdom CB4 0QA., Yon J; Astex Pharmaceuticals , 436 Cambridge Science Park, Milton Road, Cambridge, United Kingdom CB4 0QA., Acklam P; CRUK Cancer Therapeutics Unit, Institute of Cancer Research , 15 Cotswold Road, Belmont, Sutton, Surrey, United Kingdom SM2 5NG., Burke R; CRUK Cancer Therapeutics Unit, Institute of Cancer Research , 15 Cotswold Road, Belmont, Sutton, Surrey, United Kingdom SM2 5NG., Drouin L; CRUK Cancer Therapeutics Unit, Institute of Cancer Research , 15 Cotswold Road, Belmont, Sutton, Surrey, United Kingdom SM2 5NG., Harmer JE; CRUK Cancer Therapeutics Unit, Institute of Cancer Research , 15 Cotswold Road, Belmont, Sutton, Surrey, United Kingdom SM2 5NG., Jeganathan F; CRUK Cancer Therapeutics Unit, Institute of Cancer Research , 15 Cotswold Road, Belmont, Sutton, Surrey, United Kingdom SM2 5NG., van Montfort RL; CRUK Cancer Therapeutics Unit, Institute of Cancer Research , 15 Cotswold Road, Belmont, Sutton, Surrey, United Kingdom SM2 5NG., Newbatt Y; CRUK Cancer Therapeutics Unit, Institute of Cancer Research , 15 Cotswold Road, Belmont, Sutton, Surrey, United Kingdom SM2 5NG., Tortorici M; CRUK Cancer Therapeutics Unit, Institute of Cancer Research , 15 Cotswold Road, Belmont, Sutton, Surrey, United Kingdom SM2 5NG., Westlake M; CRUK Cancer Therapeutics Unit, Institute of Cancer Research , 15 Cotswold Road, Belmont, Sutton, Surrey, United Kingdom SM2 5NG., Wood A; CRUK Cancer Therapeutics Unit, Institute of Cancer Research , 15 Cotswold Road, Belmont, Sutton, Surrey, United Kingdom SM2 5NG., Hoelder S; CRUK Cancer Therapeutics Unit, Institute of Cancer Research , 15 Cotswold Road, Belmont, Sutton, Surrey, United Kingdom SM2 5NG., Heightman TD; Astex Pharmaceuticals , 436 Cambridge Science Park, Milton Road, Cambridge, United Kingdom CB4 0QA.
Publikováno v: ACS chemical biology [ACS Chem Biol] 2016 Nov 18; Vol. 11 (11), pp. 3093-3105. Date of Electronic Publication: 2016 Sep 27.
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6
Akademický článek
A fragment-based approach applied to a highly flexible target: Insights and challenges towards the inhibition of HSP70 isoforms.
Autor: Jones AM; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London SM2 5NG, United Kingdom., Westwood IM; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London SM2 5NG, United Kingdom.; Division of Structural Biology, The Institute of Cancer Research, London SW3 6JB, United Kingdom., Osborne JD; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London SM2 5NG, United Kingdom., Matthews TP; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London SM2 5NG, United Kingdom., Cheeseman MD; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London SM2 5NG, United Kingdom., Rowlands MG; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London SM2 5NG, United Kingdom., Jeganathan F; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London SM2 5NG, United Kingdom., Burke R; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London SM2 5NG, United Kingdom., Lee D; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London SM2 5NG, United Kingdom., Kadi N; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London SM2 5NG, United Kingdom., Liu M; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London SM2 5NG, United Kingdom., Richards M; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London SM2 5NG, United Kingdom., McAndrew C; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London SM2 5NG, United Kingdom., Yahya N; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London SM2 5NG, United Kingdom., Dobson SE; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London SM2 5NG, United Kingdom.; Division of Structural Biology, The Institute of Cancer Research, London SW3 6JB, United Kingdom., Jones K; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London SM2 5NG, United Kingdom., Workman P; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London SM2 5NG, United Kingdom., Collins I; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London SM2 5NG, United Kingdom., van Montfort RL; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London SM2 5NG, United Kingdom.; Division of Structural Biology, The Institute of Cancer Research, London SW3 6JB, United Kingdom.
Publikováno v: Scientific reports [Sci Rep] 2016 Oct 06; Vol. 6, pp. 34701. Date of Electronic Publication: 2016 Oct 06.
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7
Akademický článek
Synthesis of a Ribose-Incorporating Medium Ring Scaffold via a Challenging Ring-Closing Metathesis Reaction.
Autor: Rankin SS; Cancer Research UK Cancer Therapeutics Unit The Institute of Cancer Research SM2 5NG London United Kingdom., Caldwell JJ; Cancer Research UK Cancer Therapeutics Unit The Institute of Cancer Research SM2 5NG London United Kingdom., Cronin NB; Division of Structural Biology The Institute of Cancer Research SW7 3RP London United Kingdom., van Montfort RL; Division of Structural Biology The Institute of Cancer Research SW7 3RP London United Kingdom., Collins I; Cancer Research UK Cancer Therapeutics Unit The Institute of Cancer Research SM2 5NG London United Kingdom.
Publikováno v: European journal of organic chemistry [European J Org Chem] 2016 Sep; Vol. 2016 (26), pp. 4496-4507. Date of Electronic Publication: 2016 Aug 15.
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8
Akademický článek
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).
Autor: Osborne JD, Matthews TP, McHardy T, Proisy N, Cheung KM, Lainchbury M, Brown N, Walton MI, Eve PD, Boxall KJ, Hayes A, Henley AT, Valenti MR, De Haven Brandon AK, Box G, Jamin Y, Robinson SP, Westwood IM, van Montfort RL, Leonard PM; Sareum Ltd. , Cambridge CB22 3FX, U.K., Lamers MB; Sareum Ltd. , Cambridge CB22 3FX, U.K., Reader JC; Sareum Ltd. , Cambridge CB22 3FX, U.K., Aherne GW, Raynaud FI, Eccles SA, Garrett MD, Collins I
Publikováno v: Journal of medicinal chemistry [J Med Chem] 2016 Jun 09; Vol. 59 (11), pp. 5221-37. Date of Electronic Publication: 2016 May 23.
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9
Akademický článek
Exploiting Protein Conformational Change to Optimize Adenosine-Derived Inhibitors of HSP70.
Autor: Cheeseman MD; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , London SW7 3RP, U.K., Westwood IM; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , London SW7 3RP, U.K.; Division of Structural Biology, The Institute of Cancer Research , London SW7 3RP, U.K., Barbeau O; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , London SW7 3RP, U.K., Rowlands M; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , London SW7 3RP, U.K., Dobson S; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , London SW7 3RP, U.K.; Division of Structural Biology, The Institute of Cancer Research , London SW7 3RP, U.K., Jones AM; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , London SW7 3RP, U.K., Jeganathan F; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , London SW7 3RP, U.K., Burke R; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , London SW7 3RP, U.K., Kadi N; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , London SW7 3RP, U.K., Workman P; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , London SW7 3RP, U.K., Collins I; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , London SW7 3RP, U.K., van Montfort RL; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , London SW7 3RP, U.K.; Division of Structural Biology, The Institute of Cancer Research , London SW7 3RP, U.K., Jones K; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , London SW7 3RP, U.K.
Publikováno v: Journal of medicinal chemistry [J Med Chem] 2016 May 26; Vol. 59 (10), pp. 4625-36. Date of Electronic Publication: 2016 May 11.
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10
Akademický článek
Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach.
Autor: Innocenti P; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , 15 Cotswold Road, Sutton, London, SM2 5NG, United Kingdom., Woodward HL; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , 15 Cotswold Road, Sutton, London, SM2 5NG, United Kingdom., Solanki S; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , 15 Cotswold Road, Sutton, London, SM2 5NG, United Kingdom., Naud S; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , 15 Cotswold Road, Sutton, London, SM2 5NG, United Kingdom., Westwood IM; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , 15 Cotswold Road, Sutton, London, SM2 5NG, United Kingdom., Cronin N, Hayes A; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , 15 Cotswold Road, Sutton, London, SM2 5NG, United Kingdom., Roberts J; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , 15 Cotswold Road, Sutton, London, SM2 5NG, United Kingdom., Henley AT; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , 15 Cotswold Road, Sutton, London, SM2 5NG, United Kingdom., Baker R; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , 15 Cotswold Road, Sutton, London, SM2 5NG, United Kingdom., Faisal A; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , 15 Cotswold Road, Sutton, London, SM2 5NG, United Kingdom., Mak GW; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , 15 Cotswold Road, Sutton, London, SM2 5NG, United Kingdom., Box G; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , 15 Cotswold Road, Sutton, London, SM2 5NG, United Kingdom., Valenti M; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , 15 Cotswold Road, Sutton, London, SM2 5NG, United Kingdom., De Haven Brandon A; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , 15 Cotswold Road, Sutton, London, SM2 5NG, United Kingdom., O'Fee L; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , 15 Cotswold Road, Sutton, London, SM2 5NG, United Kingdom., Saville H; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , 15 Cotswold Road, Sutton, London, SM2 5NG, United Kingdom., Schmitt J; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , 15 Cotswold Road, Sutton, London, SM2 5NG, United Kingdom., Matijssen B; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , 15 Cotswold Road, Sutton, London, SM2 5NG, United Kingdom., Burke R; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , 15 Cotswold Road, Sutton, London, SM2 5NG, United Kingdom., van Montfort RL; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , 15 Cotswold Road, Sutton, London, SM2 5NG, United Kingdom., Raynaud FI; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , 15 Cotswold Road, Sutton, London, SM2 5NG, United Kingdom., Eccles SA; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , 15 Cotswold Road, Sutton, London, SM2 5NG, United Kingdom., Linardopoulos S; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , 15 Cotswold Road, Sutton, London, SM2 5NG, United Kingdom., Blagg J; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , 15 Cotswold Road, Sutton, London, SM2 5NG, United Kingdom., Hoelder S; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , 15 Cotswold Road, Sutton, London, SM2 5NG, United Kingdom.
Publikováno v: Journal of medicinal chemistry [J Med Chem] 2016 Apr 28; Vol. 59 (8), pp. 3671-88. Date of Electronic Publication: 2016 Apr 07.
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