Adam M Gilbert
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Explore the profile of Adam M Gilbert including associated specialties, affiliations and a list of published articles.
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Recent Articles
21.
Dahal U, Obach R, Gilbert A
Chem Res Toxicol
. 2013 Oct;
26(11):1739-45.
PMID: 24164572
Despite several advantages of covalent inhibitors (such as increased biochemical efficiency, longer duration of action on the target, and lower efficacious doses) over their reversible binding counterparts, there is a...
22.
Gilbert A, Bursavich M, Lombardi S, Adedoyin A, Dwyer J, Hughes Z, et al.
Bioorg Med Chem Lett
. 2010 Dec;
21(1):195-9.
PMID: 21126874
A series of 3-(pyridin-2-yl-ethynyl)benzamide negative allosteric modulators of the metabotropic glutamate receptor 5 (mGluR5 NAMs) have been prepared. Starting from HTS hit 1 (IC(50): 926 nM), potent mGluR5 NAMs showing...
23.
Gilbert A, Bikker J, ONeil S
Expert Opin Ther Pat
. 2010 Nov;
21(1):1-12.
PMID: 21110709
Importance Of The Field: Aggrecanases are members of a disintegrin and metalloprotease with thrombospondin motif family of zinc metalloproteases involved in the cleavage of aggrecan fragments in cartilage. Inhibition of...
24.
Gao Y, Deng K, Cao Z, Graziani E, Gilbert A, Koehn F, et al.
J Neurochem
. 2010 Mar;
113(5):1331-42.
PMID: 20345749
One of the major barriers to successful axon regeneration in the adult CNS is the presence of inhibitory molecules that originate from the myelin sheath and glial scar. So far,...
25.
Bursavich M, Brooijmans N, Feldberg L, Hollander I, Kim S, Lombardi S, et al.
Bioorg Med Chem Lett
. 2010 Mar;
20(8):2586-90.
PMID: 20303263
A series of benzofuran-3-one indole phosphatidylinositol-3-kinases (PI3K) inhibitors identified via HTS has been prepared. The optimized inhibitors possess single digit nanomolar activity against p110alpha (PI3K-alpha), good pharmaceutical properties, selectivity versus...
26.
Gilbert A, Nowak P, Brooijmans N, Bursavich M, Dehnhardt C, Santos E, et al.
Bioorg Med Chem Lett
. 2009 Dec;
20(2):636-9.
PMID: 19969455
Series of purine and pyrazolo[3,4-d]pyrimidine inhibitors of phosphatidylinositol-3-kinases (PI3K) have been prepared. The optimized purine inhibitors show good potency in a PI3K p110alpha (PI3K-alpha) fluorescence polarization assay with good selectivity...
27.
Venkatesan A, Dehnhardt C, Chen Z, Santos E, dos Santos O, Bursavich M, et al.
Bioorg Med Chem Lett
. 2009 Dec;
20(2):653-6.
PMID: 19954970
This article describes the syntheses and SAR of a series of imidazolopyrimidine derivatives, which are evaluated as inhibitors of PI3-Kinase (PI3K) and mTOR. These compounds were found to be ATP...
28.
Gilbert A, Bursavich M, Alon N, Bhat B, Bex F, Cain M, et al.
Bioorg Med Chem Lett
. 2009 Nov;
20(1):366-70.
PMID: 19897365
A series of (hetero)arylpyrimidines agonists of the Wnt-beta-catenin cellular messaging system have been prepared. These compounds show activity in U2OS cells transfected with Wnt-3a, TCF-luciferase, Dkk-1 and tk-Renilla. Selected compounds...
29.
Pelletier J, Lundquist 4th J, Gilbert A, Alon N, Bex F, Bhat B, et al.
J Med Chem
. 2009 Oct;
52(22):6962-5.
PMID: 19856966
A high-throughput screening campaign to discover small molecule leads for the treatment of bone disorders concluded with the discovery of a compound with a 2-aminopyrimidine template that targeted the Wnt...
30.
Gilbert A, Bursavich M, Lombardi S, Georgiadis K, Reifenberg E, Flannery C, et al.
Bioorg Med Chem Lett
. 2008 Nov;
18(24):6454-7.
PMID: 18974001
N-((8-Hydroxy-5-substituted-quinolin-7-yl)(phenyl)methyl)-2-phenyloxy/amino-acetamide inhibitors of ADAMTS-5 (Aggrecanase-2) have been prepared. Selected compounds 10, 14, 25, and 53 show sub-microM ADAMTS-5 potency and good selectivity over the related metalloproteases ADAMTS-4 (Aggrecanase-1), MMP-13, and...