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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: caldwell jj. Chembiochem. 2023 Dec 1;24(23):e202300351. doi: 10.1002/cbic.202300351. Epub 2023 Oct 10. Chembiochem. 2023. PMID: 37418539
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: caldwell jj. 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.
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: caldwell jj. 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.
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. 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.
41 results