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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: mcandrew pc. Chembiochem. 2023 Dec 1;24(23):e202300351. doi: 10.1002/cbic.202300351. Epub 2023 Oct 10. Chembiochem. 2023. PMID: 37418539
The discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug design.
Couty S, Westwood IM, Kalusa A, Cano C, Travers J, Boxall K, Chow CL, Burns S, Schmitt J, Pickard L, Barillari C, McAndrew PC, Clarke PA, Linardopoulos S, Griffin RJ, Aherne GW, Raynaud FI, Workman P, Jones K, van Montfort RL. Couty S, et al. Among authors: mcandrew pc. Oncotarget. 2013 Oct;4(10):1647-61. doi: 10.18632/oncotarget.1255. Oncotarget. 2013. PMID: 24072592 Free PMC article.
Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766).
Chessum NEA, Sharp SY, Caldwell JJ, Pasqua AE, Wilding B, Colombano G, Collins I, Ozer B, Richards M, Rowlands M, Stubbs M, Burke R, McAndrew PC, Clarke PA, Workman P, Cheeseman MD, Jones K. Chessum NEA, et al. Among authors: mcandrew pc. J Med Chem. 2018 Feb 8;61(3):918-933. doi: 10.1021/acs.jmedchem.7b01406. Epub 2018 Jan 5. J Med Chem. 2018. PMID: 29240418 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: mcandrew pc. 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.
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: mcandrew pc. 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.
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: mcandrew pc. Sci Rep. 2022 Nov 3;12(1):18633. doi: 10.1038/s41598-022-23264-z. Sci Rep. 2022. PMID: 36329085 Free PMC article.
Discovery of 2-(3-Benzamidopropanamido)thiazole-5-carboxylate Inhibitors of the Kinesin HSET (KIFC1) and the Development of Cellular Target Engagement Probes.
Saint-Dizier F, Matthews TP, Gregson AM, Prevet H, McHardy T, Colombano G, Saville H, Rowlands M, Ewens C, McAndrew PC, Tomlin K, Guillotin D, Mak GW, Drosopoulos K, Poursaitidis I, Burke R, van Montfort R, Linardopoulos S, Collins I. Saint-Dizier F, et al. Among authors: mcandrew pc. J Med Chem. 2023 Feb 23;66(4):2622-2645. doi: 10.1021/acs.jmedchem.2c01591. Epub 2023 Feb 7. J Med Chem. 2023. PMID: 36749938 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: mcandrew pc. 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.
18 results