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Kynurenine-3-monooxygenase inhibition prevents multiple organ failure in rodent models of acute pancreatitis.
Mole DJ, Webster SP, Uings I, Zheng X, Binnie M, Wilson K, Hutchinson JP, Mirguet O, Walker A, Beaufils B, Ancellin N, Trottet L, Bénéton V, Mowat CG, Wilkinson M, Rowland P, Haslam C, McBride A, Homer NZ, Baily JE, Sharp MG, Garden OJ, Hughes J, Howie SE, Holmes DS, Liddle J, Iredale JP. Mole DJ, et al. Among authors: holmes ds. Nat Med. 2016 Feb;22(2):202-9. doi: 10.1038/nm.4020. Epub 2016 Jan 11. Nat Med. 2016. PMID: 26752518 Free PMC article.
The discovery of potent and selective kynurenine 3-monooxygenase inhibitors for the treatment of acute pancreatitis.
Liddle J, Beaufils B, Binnie M, Bouillot A, Denis AA, Hann MM, Haslam CP, Holmes DS, Hutchinson JP, Kranz M, McBride A, Mirguet O, Mole DJ, Mowat CG, Pal S, Rowland P, Trottet L, Uings IJ, Walker AL, Webster SP. Liddle J, et al. Among authors: holmes ds. Bioorg Med Chem Lett. 2017 May 1;27(9):2023-2028. doi: 10.1016/j.bmcl.2017.02.078. Epub 2017 Mar 9. Bioorg Med Chem Lett. 2017. PMID: 28336141 Free article.
Development of a Series of Kynurenine 3-Monooxygenase Inhibitors Leading to a Clinical Candidate for the Treatment of Acute Pancreatitis.
Walker AL, Ancellin N, Beaufils B, Bergeal M, Binnie M, Bouillot A, Clapham D, Denis A, Haslam CP, Holmes DS, Hutchinson JP, Liddle J, McBride A, Mirguet O, Mowat CG, Rowland P, Tiberghien N, Trottet L, Uings I, Webster SP, Zheng X, Mole DJ. Walker AL, et al. Among authors: holmes ds. J Med Chem. 2017 Apr 27;60(8):3383-3404. doi: 10.1021/acs.jmedchem.7b00055. Epub 2017 Apr 11. J Med Chem. 2017. PMID: 28398044 Free article.
Targeting the Regulatory Site of ER Aminopeptidase 1 Leads to the Discovery of a Natural Product Modulator of Antigen Presentation.
Liddle J, Hutchinson JP, Kitchen S, Rowland P, Neu M, Cecconie T, Holmes DS, Jones E, Korczynska J, Koumantou D, Lea JD, Nickels L, Pemberton M, Phillipou A, Schneck JL, Sheehan H, Tinworth CP, Uings I, Wojno-Picon J, Young RJ, Stratikos E. Liddle J, et al. Among authors: holmes ds. J Med Chem. 2020 Mar 26;63(6):3348-3358. doi: 10.1021/acs.jmedchem.9b02123. Epub 2020 Mar 9. J Med Chem. 2020. PMID: 32109056
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: holmes ds. 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.
Development of a small molecule that corrects misfolding and increases secretion of Z α1 -antitrypsin.
Lomas DA, Irving JA, Arico-Muendel C, Belyanskaya S, Brewster A, Brown M, Chung CW, Dave H, Denis A, Dodic N, Dossang A, Eddershaw P, Klimaszewska D, Haq I, Holmes DS, Hutchinson JP, Jagger AM, Jakhria T, Jigorel E, Liddle J, Lind K, Marciniak SJ, Messer J, Neu M, Olszewski A, Ordonez A, Ronzoni R, Rowedder J, Rüdiger M, Skinner S, Smith KJ, Terry R, Trottet L, Uings I, Wilson S, Zhu Z, Pearce AC. Lomas DA, et al. Among authors: holmes ds. EMBO Mol Med. 2021 Mar 5;13(3):e13167. doi: 10.15252/emmm.202013167. Epub 2021 Jan 29. EMBO Mol Med. 2021. PMID: 33512066 Free PMC article.
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. Among authors: holmes ds. 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.
246 results