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.

Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo .

Autor: 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., Cheung KJ; Cancer Research UK Cancer Therapeutics Unit, 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., Talbot R; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Box GM; 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., de Haven Brandon AK; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Hallsworth AE; 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., Akpinar HA; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Miller DSJ; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Tarantino D; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Gowan S; 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., Gunnell EA; 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., Brennan A; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Davis OA; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Johnson LD; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., de Klerk S; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., McAndrew C; Cancer Research UK Cancer Therapeutics Unit, 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., Meniconi M; 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., Kirkin V; 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., 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. 8191-8207. Date of Electronic Publication: 2022 Jun 02.

Paramagnetic Lanthanide NMR Probes Signalling Changes in Zinc Concentration by Emission and Chemical Shift: A Proof of Concept Study.

Autor: Harnden AC; Department of Chemistry, Durham University, South Road, Durham, DH1 3LE, UK., Batsanov AS; Department of Chemistry, Durham University, South Road, Durham, DH1 3LE, UK., Parker D; Department of Chemistry, Durham University, South Road, Durham, DH1 3LE, UK.

Publikováno v: Chemistry (Weinheim an der Bergstrasse, Germany) [Chemistry] 2019 Apr 26; Vol. 25 (24), pp. 6212-6225. Date of Electronic Publication: 2019 Apr 04.

Simultaneous Triple Imaging with Two PARASHIFT Probes: Encoding Anatomical, pH and Temperature Information using Magnetic Resonance Shift Imaging.

Autor: Finney KNA; Department of Chemistry, Durham University, South Road, Durham, DH1 3LE, UK., Harnden AC; Department of Chemistry, Durham University, South Road, Durham, DH1 3LE, UK., Rogers NJ; Department of Chemistry, Durham University, South Road, Durham, DH1 3LE, UK., Senanayake PK; Department of Chemistry, Durham University, South Road, Durham, DH1 3LE, UK., Blamire AM; Institute of Cellular Medicine and Newcastle MR Centre, Newcastle University, Newcastle upon Tyne, NE4 5PL, UK., O'Hogain D; Institute of Cellular Medicine and Newcastle MR Centre, Newcastle University, Newcastle upon Tyne, NE4 5PL, UK., Parker D; Department of Chemistry, Durham University, South Road, Durham, DH1 3LE, UK.

Publikováno v: Chemistry (Weinheim an der Bergstrasse, Germany) [Chemistry] 2017 Jun 12; Vol. 23 (33), pp. 7976-7989. Date of Electronic Publication: 2017 May 22.