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Page 1
A Degron Blocking Strategy Towards Improved CRL4CRBN Recruiting PROTAC Selectivity.
Bouguenina H, Scarpino A, O'Hanlon JA, Warne J, Wang HZ, Wah Hak LC, Sadok A, McAndrew PC, Stubbs M, Pierrat OA, Hahner T, Cabry MP, Le Bihan YV, Mitsopoulos C, Sialana FJ, Roumeliotis TI, Burke R, van Montfort RLM, Choudhari J, Chopra R, Caldwell JJ, Collins I. Bouguenina H, et al. Among authors: van montfort rlm. Chembiochem. 2023 Dec 1;24(23):e202300351. doi: 10.1002/cbic.202300351. Epub 2023 Oct 10. Chembiochem. 2023. PMID: 37418539
iTAG an optimized IMiD-induced degron for targeted protein degradation in human and murine cells.
Bouguenina H, Nicolaou S, Le Bihan YV, Bowling EA, Calderon C, Caldwell JJ, Harrington B, Hayes A, McAndrew PC, Mitsopoulos C, Sialana FJ, Scarpino A, Stubbs M, Thapaliya A, Tyagi S, Wang HZ, Wood F, Burke R, Raynaud F, Choudhary J, van Montfort RLM, Sadok A, Westbrook TF, Collins I, Chopra R. Bouguenina H, et al. Among authors: van montfort rlm. iScience. 2023 Jun 7;26(7):107059. doi: 10.1016/j.isci.2023.107059. eCollection 2023 Jul 21. iScience. 2023. PMID: 37360684 Free PMC article.
Erratum: iTAG an optimized IMiD-induced degron for targeted protein degradation in human and murine cells.
Bouguenina H, Nicolaou S, Bihan YL, Bowling EA, Calderon C, Caldwell JJ, Harrington B, Hayes A, McAndrew PC, Mitsopoulos C, Sialana FJ, Scarpino A, Stubbs M, Thapaliya A, Tyagi S, Wang HZ, Wood F, Burke R, Raynaud F, Choudhary J, van Montfort RLM, Sadok A, Westbrook TF, Collins I, Chopra R. Bouguenina H, et al. Among authors: van montfort rlm. iScience. 2024 Apr 14;27(5):109727. doi: 10.1016/j.isci.2024.109727. eCollection 2024 May 17. iScience. 2024. PMID: 38646177 Free PMC article.
Discovery of an In Vivo Chemical Probe for BCL6 Inhibition by Optimization of Tricyclic Quinolinones.
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. Harnden AC, et al. Among authors: van montfort rlm. J Med Chem. 2023 Apr 27;66(8):5892-5906. doi: 10.1021/acs.jmedchem.3c00155. Epub 2023 Apr 7. J Med Chem. 2023. PMID: 37026591 Free PMC article.
Determination of Ligand-Binding Affinity (Kd) Using Transverse Relaxation Rate (R2) in the Ligand-Observed 1H NMR Experiment and Applications to Fragment-Based Drug Discovery.
Liu M, Mirza A, McAndrew PC, Thapaliya A, Pierrat OA, Stubbs M, Hahner T, Chessum NEA, Innocenti P, Caldwell J, Cheeseman MD, Bellenie BR, van Montfort RLM, Newton GK, Burke R, Collins I, Hoelder S. Liu M, et al. Among authors: van montfort rlm. J Med Chem. 2023 Aug 10;66(15):10617-10627. doi: 10.1021/acs.jmedchem.3c00758. Epub 2023 Jul 19. J Med Chem. 2023. PMID: 37467168 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: van montfort rlm. Sci Rep. 2022 Nov 3;12(1):18633. doi: 10.1038/s41598-022-23264-z. Sci Rep. 2022. PMID: 36329085 Free PMC article.
Optimizing Shape Complementarity Enables the Discovery of Potent Tricyclic BCL6 Inhibitors.
Davis OA, Cheung KJ, Brennan A, Lloyd MG, Rodrigues MJ, Pierrat OA, Collie GW, Le Bihan YV, Huckvale R, Harnden AC, Varela A, Bright MD, Eve P, Hayes A, Henley AT, Carter MD, McAndrew PC, Talbot R, Burke R, van Montfort RLM, Raynaud FI, Rossanese OW, Meniconi M, Bellenie BR, Hoelder S. Davis OA, et al. Among authors: van montfort rlm. J Med Chem. 2022 Jun 23;65(12):8169-8190. doi: 10.1021/acs.jmedchem.1c02174. Epub 2022 Jun 3. J Med Chem. 2022. PMID: 35657291 Free PMC article.
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: van montfort rlm. 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. Among authors: van montfort rlm. 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.
Achieving In Vivo Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 Degraders.
Bellenie BR, Cheung KJ, Varela A, Pierrat OA, Collie GW, Box GM, Bright MD, Gowan S, Hayes A, Rodrigues MJ, Shetty KN, Carter M, Davis OA, Henley AT, Innocenti P, Johnson LD, Liu M, de Klerk S, Le Bihan YV, Lloyd MG, McAndrew PC, Shehu E, Talbot R, Woodward HL, Burke R, Kirkin V, van Montfort RLM, Raynaud FI, Rossanese OW, Hoelder S. Bellenie BR, et al. Among authors: van montfort rlm. J Med Chem. 2020 Apr 23;63(8):4047-4068. doi: 10.1021/acs.jmedchem.9b02076. Epub 2020 Apr 10. J Med Chem. 2020. PMID: 32275432 Free PMC article.
50 results