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A fragment-based approach applied to a highly flexible target: Insights and challenges towards the inhibition of HSP70 isoforms.
Jones AM, Westwood IM, Osborne JD, Matthews TP, Cheeseman MD, Rowlands MG, Jeganathan F, Burke R, Lee D, Kadi N, Liu M, Richards M, McAndrew C, Yahya N, Dobson SE, Jones K, Workman P, Collins I, van Montfort RL. Jones AM, et al. Among authors: cheeseman md. Sci Rep. 2016 Oct 6;6:34701. doi: 10.1038/srep34701. Sci Rep. 2016. PMID: 27708405 Free PMC article.
Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen.
Cheeseman MD, Chessum NE, Rye CS, Pasqua AE, Tucker MJ, Wilding B, Evans LE, Lepri S, Richards M, Sharp SY, Ali S, Rowlands M, O'Fee L, Miah A, Hayes A, Henley AT, Powers M, Te Poele R, De Billy E, Pellegrino L, Raynaud F, Burke R, van Montfort RL, Eccles SA, Workman P, Jones K. Cheeseman MD, et al. J Med Chem. 2017 Jan 12;60(1):180-201. doi: 10.1021/acs.jmedchem.6b01055. Epub 2016 Dec 22. J Med Chem. 2017. PMID: 28004573 Free PMC article.
An Irreversible Inhibitor of HSP72 that Unexpectedly Targets Lysine-56.
Pettinger J, Le Bihan YV, Widya M, van Montfort RL, Jones K, Cheeseman MD. Pettinger J, et al. Among authors: cheeseman md. Angew Chem Int Ed Engl. 2017 Mar 20;56(13):3536-3540. doi: 10.1002/anie.201611907. Epub 2017 Feb 22. Angew Chem Int Ed Engl. 2017. PMID: 28225177 Free PMC article.
Lysine-Targeting Covalent Inhibitors.
Pettinger J, Jones K, Cheeseman MD. Pettinger J, et al. Among authors: cheeseman md. Angew Chem Int Ed Engl. 2017 Nov 27;56(48):15200-15209. doi: 10.1002/anie.201707630. Epub 2017 Oct 27. Angew Chem Int Ed Engl. 2017. PMID: 28853194 Review.
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: cheeseman md. 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.
24 results