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Page 1
Optimisation of a novel series of ENaC inhibitors, leading to the selection of the long-acting inhaled clinical candidate ETD001, a potential new treatment for cystic fibrosis.
Danahay H, Gosling M, Fox R, Lilley S, Charlton H, Hargrave JD, Schofield TB, Hay DA, Went N, McMahon P, Marlin F, Scott J, Vile J, Hewison S, Ellam S, Brown S, Sabater J, Kennet G, Lightowler S, Collingwood SP. Danahay H, et al. Among authors: collingwood sp. Eur J Med Chem. 2024 Nov 8;282:117040. doi: 10.1016/j.ejmech.2024.117040. Online ahead of print. Eur J Med Chem. 2024. PMID: 39561495 Free article.
ETD001: A novel inhaled ENaC blocker with an extended duration of action in vivo.
Danahay H, McCarthy C, Schofield T, Fox R, Charlton H, Lilley S, Sabater J, Salathe M, Baumlin N, Collingwood SP, Gosling M. Danahay H, et al. Among authors: collingwood sp. J Cyst Fibros. 2024 Jun 7:S1569-1993(24)00081-X. doi: 10.1016/j.jcf.2024.06.002. Online ahead of print. J Cyst Fibros. 2024. PMID: 38851923 Free article.
Discovery of Icenticaftor (QBW251), a Cystic Fibrosis Transmembrane Conductance Regulator Potentiator with Clinical Efficacy in Cystic Fibrosis and Chronic Obstructive Pulmonary Disease.
Grand DL, Gosling M, Baettig U, Bahra P, Bala K, Brocklehurst C, Budd E, Butler R, Cheung AK, Choudhury H, Collingwood SP, Cox B, Danahay H, Edwards L, Everatt B, Glaenzel U, Glotin AL, Groot-Kormelink P, Hall E, Hatto J, Howsham C, Hughes G, King A, Koehler J, Kulkarni S, Lightfoot M, Nicholls I, Page C, Pergl-Wilson G, Popa MO, Robinson R, Rowlands D, Sharp T, Spendiff M, Stanley E, Steward O, Taylor RJ, Tranter P, Wagner T, Watson H, Williams G, Wright P, Young A, Sandham DA. Grand DL, et al. Among authors: collingwood sp. J Med Chem. 2021 Jun 10;64(11):7241-7260. doi: 10.1021/acs.jmedchem.1c00343. Epub 2021 May 24. J Med Chem. 2021. PMID: 34028270
Potentiating TMEM16A does not stimulate airway mucus secretion or bronchial and pulmonary arterial smooth muscle contraction.
Danahay H, Fox R, Lilley S, Charlton H, Adley K, Christie L, Ansari E, Ehre C, Flen A, Tuvim MJ, Dickey BF, Williams C, Beaudoin S, Collingwood SP, Gosling M. Danahay H, et al. Among authors: collingwood sp. FASEB Bioadv. 2020 Jul 1;2(8):464-477. doi: 10.1096/fba.2020-00035. eCollection 2020 Aug. FASEB Bioadv. 2020. PMID: 32821878 Free PMC article.
Optimization of Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for Duration of Action, as an Inhaled Therapy for Lung Remodeling in Pulmonary Arterial Hypertension.
Shaw DE, Baig F, Bruce I, Chamoin S, Collingwood SP, Cross S, Dayal S, Drückes P, Furet P, Furminger V, Haggart D, Hussey M, Konstantinova I, Loren JC, Molteni V, Roberts S, Reilly J, Saunders AM, Stringer R, Sviridenko L, Thomas M, Thomson CG, Tomlins C, Wen B, Yeh V, Pearce AC. Shaw DE, et al. Among authors: collingwood sp. J Med Chem. 2016 Sep 8;59(17):7901-14. doi: 10.1021/acs.jmedchem.6b00703. Epub 2016 Aug 19. J Med Chem. 2016. PMID: 27502700
NVP-QBE170: an inhaled blocker of the epithelial sodium channel with a reduced potential to induce hyperkalaemia.
Coote KJ, Paisley D, Czarnecki S, Tweed M, Watson H, Young A, Sugar R, Vyas M, Smith NJ, Baettig U, Groot-Kormelink PJ, Gosling M, Lock R, Ethell B, Williams G, Schumacher A, Harris J, Abraham WM, Sabater J, Poll CT, Faller T, Collingwood SP, Danahay H. Coote KJ, et al. Among authors: collingwood sp. Br J Pharmacol. 2015 Jun;172(11):2814-26. doi: 10.1111/bph.13075. Epub 2015 Apr 23. Br J Pharmacol. 2015. PMID: 25573195 Free PMC article.
Discovery of a novel chemotype of potent human ENaC blockers using a bioisostere approach. Part 1: quaternary amines.
Hunt T, Atherton-Watson HC, Axford J, Collingwood SP, Coote KJ, Cox B, Czarnecki S, Danahay H, Devereux N, Howsham C, Hunt P, Paddock V, Paisley D, Young A. Hunt T, et al. Among authors: collingwood sp. Bioorg Med Chem Lett. 2012 Jan 15;22(2):929-32. doi: 10.1016/j.bmcl.2011.12.016. Epub 2011 Dec 8. Bioorg Med Chem Lett. 2012. PMID: 22197144
13 results