A RIPK1-specific PROTAC degrader achieves potent antitumor activity by enhancing immunogenic cell death.

Autor: Mannion J; The Breast Cancer Now Toby Robins Research Centre, The Institute of Cancer Research, Fulham Road, London SW3 6JB, UK., Gifford V; The Breast Cancer Now Toby Robins Research Centre, The Institute of Cancer Research, Fulham Road, London SW3 6JB, UK., Bellenie B; Centre for Cancer Drug Discovery at the Institute of Cancer Research, London SM2 5NG, UK., Fernando W; The Breast Cancer Now Toby Robins Research Centre, The Institute of Cancer Research, Fulham Road, London SW3 6JB, UK., Ramos Garcia L; The Breast Cancer Now Toby Robins Research Centre, The Institute of Cancer Research, Fulham Road, London SW3 6JB, UK., Wilson R; The Breast Cancer Now Toby Robins Research Centre, The Institute of Cancer Research, Fulham Road, London SW3 6JB, UK., John SW; The Breast Cancer Now Toby Robins Research Centre, The Institute of Cancer Research, Fulham Road, London SW3 6JB, UK., Udainiya S; The Breast Cancer Now Toby Robins Research Centre, The Institute of Cancer Research, Fulham Road, London SW3 6JB, UK., Patin EC; Division of Radiotherapy and Imaging, The Institute of Cancer Research, London SW3 6JB, UK., Tiu C; The Breast Cancer Now Toby Robins Research Centre, The Institute of Cancer Research, Fulham Road, London SW3 6JB, UK., Smith A; The Breast Cancer Now Toby Robins Research Centre, The Institute of Cancer Research, Fulham Road, London SW3 6JB, UK., Goicoechea M; The Breast Cancer Now Toby Robins Research Centre, The Institute of Cancer Research, Fulham Road, London SW3 6JB, UK., Craxton A; MRC Toxicology Unit, University of Cambridge, Gleeson Building, Cambridge CB2 1QR, UK., Moraes de Vasconcelos N; The Breast Cancer Now Toby Robins Research Centre, The Institute of Cancer Research, Fulham Road, London SW3 6JB, UK., Guppy N; The Breast Cancer Now Toby Robins Research Centre, The Institute of Cancer Research, Fulham Road, London SW3 6JB, UK., Cheung KJ; Centre for Cancer Drug Discovery at the Institute of Cancer Research, London SM2 5NG, UK., Cundy NJ; Centre for Cancer Drug Discovery at the Institute of Cancer Research, London SM2 5NG, UK., Pierrat O; Centre for Cancer Drug Discovery at the Institute of Cancer Research, London SM2 5NG, UK., Brennan A; Centre for Cancer Drug Discovery at the Institute of Cancer Research, London SM2 5NG, UK., Roumeliotis TI; Functional Proteomics Group, The Institute of Cancer Research, London SW3 6JB, UK., Benstead-Hume G; Functional Proteomics Group, The Institute of Cancer Research, London SW3 6JB, UK., Alexander J; The Breast Cancer Now Toby Robins Research Centre, The Institute of Cancer Research, Fulham Road, London SW3 6JB, UK., Muirhead G; The Breast Cancer Now Toby Robins Research Centre, The Institute of Cancer Research, Fulham Road, London SW3 6JB, UK., Layzell S; Institute of Immunity and Transplantation, University College London, London NW3 2PP, UK., Lyu W; Department of Immunology and Microbiology, LEO Foundation Skin Immunology Research Center, University of Copenhagen, Copenhagen, Denmark., Roulstone V; Division of Radiotherapy and Imaging, The Institute of Cancer Research, London SW3 6JB, UK., Allen M; Biological Services Unit, The Institute of Cancer Research, London SW3 6JB, UK., Baldock H; Biological Services Unit, The Institute of Cancer Research, London SW3 6JB, UK., Legrand A; The Breast Cancer Now Toby Robins Research Centre, The Institute of Cancer Research, Fulham Road, London SW3 6JB, UK., Gabel F; Centre for Cancer Drug Discovery at the Institute of Cancer Research, London SM2 5NG, UK., Serrano-Aparicio N; Centre for Cancer Drug Discovery at the Institute of Cancer Research, London SM2 5NG, UK., Starling C; The Breast Cancer Now Toby Robins Research Centre, The Institute of Cancer Research, Fulham Road, London SW3 6JB, UK., Guo H; Department of Microbiology and Immunology, LSU Health Shreveport, Shreveport, LA, USA., Upton J; Department of Biological Sciences, Auburn University, Auburn, AL, USA., Gyrd-Hansen M; Department of Immunology and Microbiology, LEO Foundation Skin Immunology Research Center, University of Copenhagen, Copenhagen, Denmark., MacFarlane M; MRC Toxicology Unit, University of Cambridge, Gleeson Building, Cambridge CB2 1QR, UK., Seddon B; Institute of Immunity and Transplantation, University College London, London NW3 2PP, UK., Raynaud F; Centre for Cancer Drug Discovery at the Institute of Cancer Research, London SM2 5NG, UK., Roxanis I; The Breast Cancer Now Toby Robins Research Centre, The Institute of Cancer Research, Fulham Road, London SW3 6JB, UK., Harrington K; Division of Radiotherapy and Imaging, The Institute of Cancer Research, London SW3 6JB, UK., Haider S; The Breast Cancer Now Toby Robins Research Centre, The Institute of Cancer Research, Fulham Road, London SW3 6JB, UK., Choudhary JS; Functional Proteomics Group, The Institute of Cancer Research, London SW3 6JB, UK., Hoelder S; Centre for Cancer Drug Discovery at the Institute of Cancer Research, London SM2 5NG, UK., Tenev T; The Breast Cancer Now Toby Robins Research Centre, The Institute of Cancer Research, Fulham Road, London SW3 6JB, UK. Electronic address: tencho.tenev@icr.ac.uk., Meier P; The Breast Cancer Now Toby Robins Research Centre, The Institute of Cancer Research, Fulham Road, London SW3 6JB, UK. Electronic address: pmeier@icr.ac.uk.

Publikováno v: Immunity [Immunity] 2024 Jul 09; Vol. 57 (7), pp. 1514-1532.e15. Date of Electronic Publication: 2024 May 23.

Discovery of an In Vivo Chemical Probe for BCL6 Inhibition by Optimization of Tricyclic Quinolinones.

Autor: Harnden AC, Davis OA, Box GM, Hayes A, Johnson LD, Henley AT, de Haven Brandon AK, Valenti M, Cheung KJ, Brennan A, Huckvale R, Pierrat OA, Talbot R, Bright MD, Akpinar HA, Miller DSJ, Tarantino D, Gowan S, de Klerk S, McAndrew PC, Le Bihan YV, Meniconi M, Burke R, Kirkin V, van Montfort RLM, Raynaud FI, Rossanese OW, Bellenie BR, Hoelder S

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2023 Apr 27; Vol. 66 (8), pp. 5892-5906. Date of Electronic Publication: 2023 Apr 07.

Discovering cell-active BCL6 inhibitors: effectively combining biochemical HTS with multiple biophysical techniques, X-ray crystallography and cell-based assays.

Autor: Pierrat OA; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., Liu M; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., Collie GW; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK.; Division of Structural Biology, The Institute of Cancer Research, London, SW3 6JB, UK., Shetty K; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK.; Division of Structural Biology, The Institute of Cancer Research, London, SW3 6JB, UK., Rodrigues MJ; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK.; Division of Structural Biology, The Institute of Cancer Research, London, SW3 6JB, UK., Le Bihan YV; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK.; Division of Structural Biology, The Institute of Cancer Research, London, SW3 6JB, UK., Gunnell EA; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK.; Division of Structural Biology, The Institute of Cancer Research, London, SW3 6JB, UK., McAndrew PC; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., Stubbs M; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., Rowlands MG; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., Yahya N; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., Shehu E; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., Talbot R; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., Pickard L; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., Bellenie BR; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., Cheung KJ; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., Drouin L; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., Innocenti P; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., Woodward H; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., Davis OA; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., Lloyd MG; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., Varela A; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., Huckvale R; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., Broccatelli F; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., Carter M; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., Galiwango D; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., Hayes A; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., Raynaud FI; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., Bryant C; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., Whittaker S; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., Rossanese OW; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., Hoelder S; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., Burke R; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK., van Montfort RLM; Division of Cancer Therapeutics, Centre for Cancer Drug Discovery, The Institute of Cancer Research, London, SM2 5NG, UK. rob.vanmontfort@icr.ac.uk.; Division of Structural Biology, The Institute of Cancer Research, London, SW3 6JB, UK. rob.vanmontfort@icr.ac.uk.

Publikováno v: Scientific reports [Sci Rep] 2022 Nov 03; Vol. 12 (1), pp. 18633. Date of Electronic Publication: 2022 Nov 03.

Optimizing Shape Complementarity Enables the Discovery of Potent Tricyclic BCL6 Inhibitors.

Autor: Davis OA; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K.., Cheung KJ; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K.., Brennan A; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K.., Lloyd MG; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K.., Rodrigues MJ; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K..; Division of Structural Biology, The Institute of Cancer Research, London SM2 5NG, U.K.., Pierrat OA; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K.., Collie GW; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K..; Division of Structural Biology, The Institute of Cancer Research, London SM2 5NG, U.K.., Le Bihan YV; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K..; Division of Structural Biology, The Institute of Cancer Research, London SM2 5NG, U.K.., Huckvale R; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K.., Harnden AC; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K.., Varela A; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K.., Bright MD; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K.., Eve P; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K.., Hayes A; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K.., Henley AT; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K.., Carter MD; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K.., McAndrew PC; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K.., Talbot R; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K.., Burke R; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K.., van Montfort RLM; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K..; Division of Structural Biology, The Institute of Cancer Research, London SM2 5NG, U.K.., Raynaud FI; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K.., Rossanese OW; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K.., Meniconi M; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K.., Bellenie BR; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K.., Hoelder S; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K..

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2022 Jun 23; Vol. 65 (12), pp. 8169-8190. Date of Electronic Publication: 2022 Jun 03.

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