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Page 1
Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation.
Lewis HD, Liddle J, Coote JE, Atkinson SJ, Barker MD, Bax BD, Bicker KL, Bingham RP, Campbell M, Chen YH, Chung CW, Craggs PD, Davis RP, Eberhard D, Joberty G, Lind KE, Locke K, Maller C, Martinod K, Patten C, Polyakova O, Rise CE, Rüdiger M, Sheppard RJ, Slade DJ, Thomas P, Thorpe J, Yao G, Drewes G, Wagner DD, Thompson PR, Prinjha RK, Wilson DM. Lewis HD, et al. Among authors: thorpe j. Nat Chem Biol. 2015 Mar;11(3):189-91. doi: 10.1038/nchembio.1735. Epub 2015 Jan 26. Nat Chem Biol. 2015. PMID: 25622091 Free PMC article.
Structure guided drug design to develop kallikrein 5 inhibitors to treat Netherton syndrome.
Walker AL, Bingham RP, Edgar EV, Ferrie A, Holmes DS, Liddle J, Polyakova O, Rella M, Smith KJ, Thorpe JH, Wang Y, White GV, Young RJ, Hovnanian A. Walker AL, et al. Among authors: thorpe jh. Bioorg Med Chem Lett. 2019 Jun 15;29(12):1454-1458. doi: 10.1016/j.bmcl.2019.04.022. Epub 2019 Apr 12. Bioorg Med Chem Lett. 2019. PMID: 31005442
Design and development of a series of borocycles as selective, covalent kallikrein 5 inhibitors.
Walker AL, Denis A, Bingham RP, Bouillot A, Edgar EV, Ferrie A, Holmes DS, Laroze A, Liddle J, Fouchet MH, Moquette A, Nassau P, Pearce AC, Polyakova O, Smith KJ, Thomas P, Thorpe JH, Trottet L, Wang Y, Hovnanian A. Walker AL, et al. Among authors: thorpe jh. Bioorg Med Chem Lett. 2019 Oct 15;29(20):126675. doi: 10.1016/j.bmcl.2019.126675. Epub 2019 Sep 7. Bioorg Med Chem Lett. 2019. PMID: 31521475
Corrigendum to 'Design and development of a series of borocycles as selective, covalent kallikrein 5 inhibitors' [Bioorg. Med. Chem. Lett. 29 (2019) 126675].
Walker AL, Denis A, Bingham RP, Bouillot A, Edgar EV, Ferrie A, Holmes DS, Laroze A, Liddle J, Fouchet MH, Moquette A, Nassau P, Pearce AC, Polyakova O, Smith KJ, Thomas P, Thorpe JH, Trottet L, Wang Y, Hovnanian A. Walker AL, et al. Among authors: thorpe jh. Bioorg Med Chem Lett. 2020 Jan 15;30(2):126771. doi: 10.1016/j.bmcl.2019.126771. Epub 2019 Dec 16. Bioorg Med Chem Lett. 2020. PMID: 31859161 No abstract available.
Evaluation of a crystallographic surrogate for kallikrein 5 in the discovery of novel inhibitors for Netherton syndrome.
Thorpe JH, Edgar EV, Smith KJ, Lewell XQ, Rella M, White GV, Polyakova O, Nassau P, Walker AL, Holmes DS, Pearce AC, Wang Y, Liddle J, Hovnanian A. Thorpe JH, et al. Acta Crystallogr F Struct Biol Commun. 2019 May 1;75(Pt 5):385-391. doi: 10.1107/S2053230X19003169. Epub 2019 Apr 26. Acta Crystallogr F Struct Biol Commun. 2019. PMID: 31045568 Free PMC article.
A Potent and Selective Kallikrein-5 Inhibitor Delivers High Pharmacological Activity in Skin from Patients with Netherton Syndrome.
Liddle J, Beneton V, Benson M, Bingham R, Bouillot A, Boullay AB, Brook E, Cryan J, Denis A, Edgar E, Ferrie A, Fouchet MH, Grillot D, Holmes DS, Howes A, Krysa G, Laroze A, Lennon M, McClure F, Moquette A, Nicodeme E, Santiago B, Santos L, Smith KJ, Thorpe JH, Thripp G, Trottet L, Walker AL, Ward SA, Wang Y, Wilson S, Pearce AC, Hovnanian A. Liddle J, et al. Among authors: thorpe jh. J Invest Dermatol. 2021 Sep;141(9):2272-2279. doi: 10.1016/j.jid.2021.01.029. Epub 2021 Mar 18. J Invest Dermatol. 2021. PMID: 33744298 Free article.
Structure-based optimisation of orally active & reversible MetAP-2 inhibitors maintaining a tight 'molecular budget'.
Hirst DJ, Brandt M, Bruton G, Christodoulou E, Cutler L, Deeks N, Goodacre JD, Jack T, Lindon M, Miah A, Page K, Parr N, Shukla L, Sims M, Thomas P, Thorpe J, Holmes DS. Hirst DJ, et al. Among authors: thorpe j. Bioorg Med Chem Lett. 2020 Nov 1;30(21):127533. doi: 10.1016/j.bmcl.2020.127533. Epub 2020 Sep 10. Bioorg Med Chem Lett. 2020. PMID: 32919012
Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase.
Harris PA, Faucher N, George N, Eidam PM, King BW, White GV, Anderson NA, Bandyopadhyay D, Beal AM, Beneton V, Berger SB, Campobasso N, Campos S, Capriotti CA, Cox JA, Daugan A, Donche F, Fouchet MH, Finger JN, Geddes B, Gough PJ, Grondin P, Hoffman BL, Hoffman SJ, Hutchinson SE, Jeong JU, Jigorel E, Lamoureux P, Leister LK, Lich JD, Mahajan MK, Meslamani J, Mosley JE, Nagilla R, Nassau PM, Ng SL, Ouellette MT, Pasikanti KK, Potvain F, Reilly MA, Rivera EJ, Sautet S, Schaeffer MC, Sehon CA, Sun H, Thorpe JH, Totoritis RD, Ward P, Wellaway N, Wisnoski DD, Woolven JM, Bertin J, Marquis RW. Harris PA, et al. Among authors: thorpe jh. J Med Chem. 2019 May 23;62(10):5096-5110. doi: 10.1021/acs.jmedchem.9b00318. Epub 2019 May 2. J Med Chem. 2019. PMID: 31013427
661 results