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Page 1
Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo.
Huckvale R, Harnden AC, Cheung KJ, Pierrat OA, Talbot R, Box GM, Henley AT, de Haven Brandon AK, Hallsworth AE, Bright MD, Akpinar HA, Miller DSJ, Tarantino D, Gowan S, Hayes A, Gunnell EA, Brennan A, Davis OA, Johnson LD, de Klerk S, McAndrew C, Le Bihan YV, Meniconi M, Burke R, Kirkin V, van Montfort RLM, Raynaud FI, Rossanese OW, Bellenie BR, Hoelder S. Huckvale R, et al. Among authors: gunnell ea. J Med Chem. 2022 Jun 23;65(12):8191-8207. doi: 10.1021/acs.jmedchem.1c02175. Epub 2022 Jun 2. J Med Chem. 2022. PMID: 35653645 Free PMC article.
Into Deep Water: Optimizing BCL6 Inhibitors by Growing into a Solvated Pocket.
Lloyd MG, Huckvale R, Cheung KJ, Rodrigues MJ, Collie GW, Pierrat OA, Gatti Iou M, Carter M, Davis OA, McAndrew PC, Gunnell E, Le Bihan YV, Talbot R, Henley AT, Johnson LD, Hayes A, Bright MD, Raynaud FI, Meniconi M, Burke R, van Montfort RLM, Rossanese OW, Bellenie BR, Hoelder S. Lloyd MG, et al. J Med Chem. 2021 Dec 9;64(23):17079-17097. doi: 10.1021/acs.jmedchem.1c00946. Epub 2021 Nov 30. J Med Chem. 2021. PMID: 34846884 Free PMC article.
Discovering cell-active BCL6 inhibitors: effectively combining biochemical HTS with multiple biophysical techniques, X-ray crystallography and cell-based assays.
Pierrat OA, Liu M, Collie GW, Shetty K, Rodrigues MJ, Le Bihan YV, Gunnell EA, McAndrew PC, Stubbs M, Rowlands MG, Yahya N, Shehu E, Talbot R, Pickard L, Bellenie BR, Cheung KJ, Drouin L, Innocenti P, Woodward H, Davis OA, Lloyd MG, Varela A, Huckvale R, Broccatelli F, Carter M, Galiwango D, Hayes A, Raynaud FI, Bryant C, Whittaker S, Rossanese OW, Hoelder S, Burke R, van Montfort RLM. Pierrat OA, et al. Among authors: gunnell ea. Sci Rep. 2022 Nov 3;12(1):18633. doi: 10.1038/s41598-022-23264-z. Sci Rep. 2022. PMID: 36329085 Free PMC article.