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Items: 14

1.

Translation of Inhaled Drug Optimization Strategies into Clinical Pharmacokinetics and Pharmacodynamics Using GSK2292767A, a Novel Inhaled Phosphoinositide 3-Kinase δ Inhibitor.

Begg M, Edwards CD, Hamblin JN, Pefani E, Wilson R, Gilbert J, Vitulli G, Mallett D, Morrell J, Hingle MI, Uddin S, Ehtesham F, Marotti M, Harrell A, Newman CF, Fernando D, Clark J, Cahn A, Hessel EM.

J Pharmacol Exp Ther. 2019 Jun;369(3):443-453. doi: 10.1124/jpet.119.257311. Epub 2019 Apr 2.

PMID:
30940692
2.

Relationship between Pharmacokinetics and Pharmacodynamic Responses in Healthy Smokers Informs a Once-Daily Dosing Regimen for Nemiralisib.

Begg M, Wilson R, Hamblin JN, Montembault M, Green J, Deans A, Amour A, Worsley S, Fantom K, Cui Y, Dear G, Ahmad S, Kielkowska A, Clark J, Boyce M, Cahn A, Hessel EM.

J Pharmacol Exp Ther. 2019 Jun;369(3):337-344. doi: 10.1124/jpet.118.255109. Epub 2019 Mar 18.

PMID:
30886125
3.

Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase δ through a Deconstruction and Regrowth Approach.

Barton N, Convery M, Cooper AWJ, Down K, Hamblin JN, Inglis G, Peace S, Rowedder J, Rowland P, Taylor JA, Wellaway N.

J Med Chem. 2018 Dec 27;61(24):11061-11073. doi: 10.1021/acs.jmedchem.8b01556. Epub 2018 Dec 21.

PMID:
30532965
4.

A Multicentre, Randomized, Double-Blind, Placebo-Controlled, Crossover Study To Investigate the Efficacy, Safety, Tolerability, and Pharmacokinetics of Repeat Doses of Inhaled Nemiralisib in Adults with Persistent, Uncontrolled Asthma.

Khindri S, Cahn A, Begg M, Montembault M, Leemereise C, Cui Y, Hogg A, Wajdner H, Yang S, Robertson J, Hamblin JN, Ludwig-Sengpiel A, Kornmann O, Hessel EM.

J Pharmacol Exp Ther. 2018 Dec;367(3):405-413. doi: 10.1124/jpet.118.249516. Epub 2018 Sep 14.

PMID:
30217958
5.

PI3Kδ hyper-activation promotes development of B cells that exacerbate Streptococcus pneumoniae infection in an antibody-independent manner.

Stark AK, Chandra A, Chakraborty K, Alam R, Carbonaro V, Clark J, Sriskantharajah S, Bradley G, Richter AG, Banham-Hall E, Clatworthy MR, Nejentsev S, Hamblin JN, Hessel EM, Condliffe AM, Okkenhaug K.

Nat Commun. 2018 Aug 9;9(1):3174. doi: 10.1038/s41467-018-05674-8.

6.

Safety, Tolerability, and Pharmacokinetics of Single and Repeat Doses of Nemiralisib Administered via the Ellipta Dry Powder Inhaler to Healthy Subjects.

Wilson R, Jarvis E, Montembault M, Hamblin JN, Hessel EM, Cahn A.

Clin Ther. 2018 Aug;40(8):1410-1417. doi: 10.1016/j.clinthera.2018.06.011. Epub 2018 Jul 25.

PMID:
30055824
7.

Safety, pharmacokinetics and dose-response characteristics of GSK2269557, an inhaled PI3Kδ inhibitor under development for the treatment of COPD.

Cahn A, Hamblin JN, Begg M, Wilson R, Dunsire L, Sriskantharajah S, Montembault M, Leemereise CN, Galinanes-Garcia L, Watz H, Kirsten AM, Fuhr R, Hessel EM.

Pulm Pharmacol Ther. 2017 Oct;46:69-77. doi: 10.1016/j.pupt.2017.08.008. Epub 2017 Aug 17.

8.

Optimization of Novel Indazoles as Highly Potent and Selective Inhibitors of Phosphoinositide 3-Kinase δ for the Treatment of Respiratory Disease.

Down K, Amour A, Baldwin IR, Cooper AW, Deakin AM, Felton LM, Guntrip SB, Hardy C, Harrison ZA, Jones KL, Jones P, Keeling SE, Le J, Livia S, Lucas F, Lunniss CJ, Parr NJ, Robinson E, Rowland P, Smith S, Thomas DA, Vitulli G, Washio Y, Hamblin JN.

J Med Chem. 2015 Sep 24;58(18):7381-99. doi: 10.1021/acs.jmedchem.5b00767. Epub 2015 Sep 3.

PMID:
26301626
9.

Pyrazolopyridines as potent PDE4B inhibitors: 5-heterocycle SAR.

Mitchell CJ, Ballantine SP, Coe DM, Cook CM, Delves CJ, Dowle MD, Edlin CD, Hamblin JN, Holman S, Johnson MR, Jones PS, Keeling SE, Kranz M, Lindvall M, Lucas FS, Neu M, Solanke YE, Somers DO, Trivedi NA, Wiseman JO.

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5803-6. doi: 10.1016/j.bmcl.2010.07.136. Epub 2010 Aug 5.

PMID:
20732811
10.

Pyrazolopyridines as a novel structural class of potent and selective PDE4 inhibitors.

Hamblin JN, Angell TD, Ballantine SP, Cook CM, Cooper AW, Dawson J, Delves CJ, Jones PS, Lindvall M, Lucas FS, Mitchell CJ, Neu MY, Ranshaw LE, Solanke YE, Somers DO, Wiseman JO.

Bioorg Med Chem Lett. 2008 Jul 15;18(14):4237-41. doi: 10.1016/j.bmcl.2008.05.052. Epub 2008 May 17.

PMID:
18539455
11.

Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides.

Chan C, Borthwick AD, Brown D, Burns-Kurtis CL, Campbell M, Chaudry L, Chung CW, Convery MA, Hamblin JN, Johnstone L, Kelly HA, Kleanthous S, Patikis A, Patel C, Pateman AJ, Senger S, Shah GP, Toomey JR, Watson NS, Weston HE, Whitworth C, Young RJ, Zhou P.

J Med Chem. 2007 Apr 5;50(7):1546-57. Epub 2007 Mar 6.

PMID:
17338508
12.

Design and synthesis of orally active pyrrolidin-2-one-based factor Xa inhibitors.

Watson NS, Brown D, Campbell M, Chan C, Chaudry L, Convery MA, Fenwick R, Hamblin JN, Haslam C, Kelly HA, King NP, Kurtis CL, Leach AR, Manchee GR, Mason AM, Mitchell C, Patel C, Patel VK, Senger S, Shah GP, Weston HE, Whitworth C, Young RJ.

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3784-8. Epub 2006 May 11.

PMID:
16697194
13.

Dimeric zanamivir conjugates with various linking groups are potent, long-lasting inhibitors of influenza neuraminidase including H5N1 avian influenza.

Macdonald SJ, Cameron R, Demaine DA, Fenton RJ, Foster G, Gower D, Hamblin JN, Hamilton S, Hart GJ, Hill AP, Inglis GG, Jin B, Jones HT, McConnell DB, McKimm-Breschkin J, Mills G, Nguyen V, Owens IJ, Parry N, Shanahan SE, Smith D, Watson KG, Wu WY, Tucker SP.

J Med Chem. 2005 Apr 21;48(8):2964-71.

PMID:
15828835
14.

Potent and long-acting dimeric inhibitors of influenza virus neuraminidase are effective at a once-weekly dosing regimen.

Macdonald SJ, Watson KG, Cameron R, Chalmers DK, Demaine DA, Fenton RJ, Gower D, Hamblin JN, Hamilton S, Hart GJ, Inglis GG, Jin B, Jones HT, McConnell DB, Mason AM, Nguyen V, Owens IJ, Parry N, Reece PA, Shanahan SE, Smith D, Wu WY, Tucker SP.

Antimicrob Agents Chemother. 2004 Dec;48(12):4542-9.

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