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Paul Faulder

Explore the profile of Paul Faulder including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 7
Citations 99
Followers 0
Related Specialties
Chemistry
Biochemistry
Top 10 Co-Authors
Jason G Kettle
Gary Fairley
Kurt G Pike
Iris Treinies
Ian R Baldwin
Chris Ioannou
Helen Plant
Florence Raynaud
Olga Plotnikova
Julie Tucker
Published In
J Med Chem
Bioorg Med Chem Lett
ACS Med Chem Lett
Bioorg Med Chem
Medchemcomm
Affiliations
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Recent Articles
1.
Identification and optimization of a novel series of selective PIP5K inhibitors
Andrews D, Cartic S, Cosulich S, Divecha N, Faulder P, Flemington V, et al.
Bioorg Med Chem . 2021 Dec; 54:116557. PMID: 34922306
Phosphatidyl inositol (4,5)-bisphosphate (PI(4,5)P) plays several key roles in human biology and the lipid kinase that produces PI(4,5)P, PIP5K, has been hypothesized to provide a potential therapeutic target of interest...
2.
From PIM1 to PI3Kδ via GSK3β: Target Hopping through the Kinome
Henley Z, Bax B, Inglesby L, Champigny A, Gaines S, Faulder P, et al.
ACS Med Chem Lett . 2017 Oct; 8(10):1093-1098. PMID: 29057057
Selective inhibitors of phosphoinositide 3-kinase delta are of interest for the treatment of inflammatory diseases. Initial optimization of a 3-substituted indazole hit compound targeting the kinase PIM1 focused on improving...
3.
Discovery of 4,6-disubstituted pyrimidines as potent inhibitors of the heat shock factor 1 (HSF1) stress pathway and CDK9
Rye C, Chessum N, Lamont S, Pike K, Faulder P, Demeritt J, et al.
Medchemcomm . 2016 Oct; 7(8):1580-1586. PMID: 27746890
Heat shock factor 1 (HSF1) is a transcription factor that plays key roles in cancer, including providing a mechanism for cell survival under proteotoxic stress. Therefore, inhibition of the HSF1-stress...
4.
Small molecule binding sites on the Ras:SOS complex can be exploited for inhibition of Ras activation
Winter J, Anderson M, Blades K, Brassington C, Breeze A, Chresta C, et al.
J Med Chem . 2015 Feb; 58(5):2265-74. PMID: 25695162
Constitutively active mutant KRas displays a reduced rate of GTP hydrolysis via both intrinsic and GTPase-activating protein-catalyzed mechanisms, resulting in the perpetual activation of Ras pathways. We describe a fragment...
5.
Inhibiting NF-κB-inducing kinase (NIK): discovery, structure-based design, synthesis, structure-activity relationship, and co-crystal structures
Li K, McGee L, Fisher B, Sudom A, Liu J, Rubenstein S, et al.
Bioorg Med Chem Lett . 2013 Feb; 23(5):1238-44. PMID: 23374866
The discovery, structure-based design, synthesis, and optimization of NIK inhibitors are described. Our work began with an HTS hit, imidazopyridinyl pyrimidinamine 1. We utilized homology modeling and conformational analysis to...
6.
4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy
Liddle J, Bamborough P, Barker M, Campos S, Chung C, Cousins R, et al.
Bioorg Med Chem Lett . 2012 Jul; 22(16):5222-6. PMID: 22801646
The lead optimization of a series of potent azaindole IKK2 inhibitors is described. Optimization of the human whole blood activity and selectivity over IKK1 in parallel led to the discovery...
7.
Diverse heterocyclic scaffolds as allosteric inhibitors of AKT
Kettle J, Brown S, Crafter C, Davies B, Dudley P, Fairley G, et al.
J Med Chem . 2012 Jan; 55(3):1261-73. PMID: 22248236
Wide-ranging exploration of potential replacements for a quinoline-based inhibitor of activation of AKT kinase led to number of alternative, novel scaffolds with potentially improved potency and physicochemical properties. Examples showed...