Graeme R Robb
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Explore the profile of Graeme R Robb including associated specialties, affiliations and a list of published articles.
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26
Citations
311
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Recent Articles
11.
Degorce S, Anjum R, Bloecher A, Carbajo R, Dillman K, Drew L, et al.
J Med Chem
. 2019 Oct;
62(21):9918-9930.
PMID: 31622099
In this article, we report the discovery of a series of 5-azaquinazolines as selective IRAK4 inhibitors. From modestly potent quinazoline , we introduced a 5-aza substitution to mask the 4-NH...
12.
Balazs A, Carbajo R, Davies N, Dong Y, Hird A, Johannes J, et al.
J Med Chem
. 2019 Jul;
62(21):9418-9437.
PMID: 31361481
The three-dimensional conformations adopted by a free ligand in solution impact bioactivity and physicochemical properties. Solution 1D NMR spectra inherently contain information on ligand conformational flexibility and three-dimensional shape, as...
13.
McCoull W, Cheung T, Anderson E, Barton P, Burgess J, Byth K, et al.
ACS Chem Biol
. 2018 Oct;
13(11):3131-3141.
PMID: 30335946
B-cell lymphoma 6 (BCL6) inhibition is a promising mechanism for treating hematological cancers but high quality chemical probes are necessary to evaluate its therapeutic potential. Here we report potent BCL6...
14.
Degorce S, Anjum R, Dillman K, Drew L, Groombridge S, Halsall C, et al.
Bioorg Med Chem
. 2018 Feb;
26(4):913-924.
PMID: 29398441
We have developed a series of orally efficacious IRAK4 inhibitors, based on a scaffold hopping strategy and using rational structure based design. Efforts to tackle low permeability and high efflux...
15.
Scott J, Degorce S, Anjum R, Culshaw J, Davies R, Davies N, et al.
J Med Chem
. 2017 Nov;
60(24):10071-10091.
PMID: 29172502
Herein we report the optimization of a series of pyrrolopyrimidine inhibitors of interleukin-1 receptor associated kinase 4 (IRAK4) using X-ray crystal structures and structure based design to identify and optimize...
16.
McCoull W, Abrams R, Anderson E, Blades K, Barton P, Box M, et al.
J Med Chem
. 2017 Jul;
60(14):6459.
PMID: 28714680
No abstract available.
17.
McCoull W, Abrams R, Anderson E, Blades K, Barton P, Box M, et al.
J Med Chem
. 2017 May;
60(10):4386-4402.
PMID: 28485934
Inhibition of the protein-protein interaction between B-cell lymphoma 6 (BCL6) and corepressors has been implicated as a therapeutic target in diffuse large B-cell lymphoma (DLBCL) cancers and profiling of potent...
18.
Waring M, Chen H, Rabow A, Walker G, Bobby R, Boiko S, et al.
Nat Chem Biol
. 2016 Oct;
12(12):1097-1104.
PMID: 27775716
Proteins of the bromodomain and extraterminal (BET) family, in particular bromodomain-containing protein 4 (BRD4), are of great interest as biological targets. BET proteins contain two separate bromodomains, and existing inhibitors...
19.
Raubo P, Andrews D, McKelvie J, Robb G, Smith J, Swarbrick M, et al.
Bioorg Med Chem Lett
. 2015 Jun;
25(16):3189-93.
PMID: 26087940
The discovery and optimisation of novel, potent and selective small molecule inhibitors of the α-isoform of type III phosphatidylinositol-4-kinase (PI4Kα) are described. Lead compounds show cellular activity consistent with their...
20.
Johannes J, Almeida L, Barlaam B, Boriack-Sjodin P, Casella R, Croft R, et al.
ACS Med Chem Lett
. 2015 Mar;
6(3):254-9.
PMID: 25815142
The canonical Wnt pathway plays an important role in embryonic development, adult tissue homeostasis, and cancer. Germline mutations of several Wnt pathway components, such as Axin, APC, and ß-catenin, can...