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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: edgar e. 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.
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.
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. 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. 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.
In Vivo Half-Life Extension of BMP1/TLL Metalloproteinase Inhibitors Using Small-Molecule Human Serum Albumin Binders.
Vantourout JC, Mason AM, Yuen J, Simpson GL, Evindar G, Kuai L, Hobbs M, Edgar E, Needle S, Bai X, Wilson S, Scott-Stevens P, Traylen W, Lambert K, Young N, Bunally S, Summerfield SG, Snell R, Lad R, Shi E, Skinner S, Shewchuk L, Watson AJB, Chung CW, Pal S, Holt DA, Kallander LS, Prendergast J, Rivera K, Washburn DG, Harpel MR, Arico-Muendel C, Isidro-Llobet A. Vantourout JC, et al. Among authors: edgar e. Bioconjug Chem. 2021 Feb 17;32(2):279-289. doi: 10.1021/acs.bioconjchem.0c00662. Epub 2021 Feb 1. Bioconjug Chem. 2021. PMID: 33523652
Pharmacological characterisation and inhibitory effects of (2R,3R,4S,5R)-2-(6-amino-2-{[(1S)-2-hydroxy-1-(phenylmethyl)ethyl]amino}-9H-purin-9-yl)-5-(2-ethyl-2H-tetrazol-5-yl)tetrahydro-3,4-furandiol, a novel ligand that demonstrates both adenosine A(2A) receptor agonist and adenosine A(3) receptor antagonist activity.
Bevan N, Butchers PR, Cousins R, Coates J, Edgar EV, Morrison V, Sheehan MJ, Reeves J, Wilson DJ. Bevan N, et al. Eur J Pharmacol. 2007 Jun 14;564(1-3):219-25. doi: 10.1016/j.ejphar.2007.01.094. Epub 2007 Feb 16. Eur J Pharmacol. 2007. PMID: 17382926
Pharmacological and structural understanding of the Trypanosoma cruzi proteasome provides key insights for developing site-specific inhibitors.
Eadsforth TC, Torrie LS, Rowland P, Edgar EV, MacLean LM, Paterson C, Robinson DA, Shepherd SM, Thomas J, Thomas MG, Gray DW, Postis VLG, De Rycker M. Eadsforth TC, et al. Among authors: edgar ev. J Biol Chem. 2024 Dec 9;301(1):108049. doi: 10.1016/j.jbc.2024.108049. Online ahead of print. J Biol Chem. 2024. PMID: 39638245 Free article.
59 results