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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Citations
771
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Recent Articles
11.
Thorarensen A, Dowty M, Banker M, Juba B, Jussif J, Lin T, et al.
J Med Chem
. 2017 Feb;
60(5):1971-1993.
PMID: 28139931
Significant work has been dedicated to the discovery of JAK kinase inhibitors resulting in several compounds entering clinical development and two FDA approved NMEs. However, despite significant effort during the...
12.
Zhang Q, Jiang F, Zhao B, Lin H, Tian Y, Xie M, et al.
Sci Rep
. 2016 Dec;
6:38573.
PMID: 27934919
Inducing α-helicity through side-chain cross-linking is a strategy that has been pursued to improve peptide conformational rigidity and bio-availability. Here we describe the preparation of small peptides tethered to chiral...
13.
Telliez J, Dowty M, Wang L, Jussif J, Lin T, Li L, et al.
ACS Chem Biol
. 2016 Oct;
11(12):3442-3451.
PMID: 27791347
PF-06651600, a newly discovered potent JAK3-selective inhibitor, is highly efficacious at inhibiting γc cytokine signaling, which is dependent on both JAK1 and JAK3. PF-06651600 allowed the comparison of JAK3-selective inhibition...
14.
Leung L, Yang X, Strelevitz T, Montgomery J, Brown M, Zientek M, et al.
Drug Metab Dispos
. 2016 Oct;
45(1):1-7.
PMID: 27784718
The concept of target-specific covalent enzyme inhibitors appears attractive from both an efficacy and a selectivity viewpoint considering the potential for enhanced biochemical efficiency associated with an irreversible mechanism. Aside...
15.
Ahn K, Boehm M, Brown M, Calloway J, Che Y, Chen J, et al.
ACS Chem Biol
. 2016 Jul;
11(9):2529-40.
PMID: 27391855
Lysophospholipase-like 1 (LYPLAL1) is an uncharacterized metabolic serine hydrolase. Human genome-wide association studies link variants of the gene encoding this enzyme to fat distribution, waist-to-hip ratio, and nonalcoholic fatty liver...
16.
Bunnage M, Gilbert A, Jones L, Hett E
Nat Chem Biol
. 2015 May;
11(6):368-72.
PMID: 25978985
No abstract available.
17.
Flanagan M, Abramite J, Anderson D, Aulabaugh A, Dahal U, Gilbert A, et al.
J Med Chem
. 2014 Nov;
57(23):10072-9.
PMID: 25375838
Interest in drugs that covalently modify their target is driven by the desire for enhanced efficacy that can result from the silencing of enzymatic activity until protein resynthesis can occur,...
18.
Gilbert A
Pharm Pat Anal
. 2014 Oct;
3(4):375-86.
PMID: 25291312
Despite concerns of off-target selectivity and cytotoxicity, there has been a resurgence in interest in irreversible kinase inhibitors resulting in more than 60 disclosed patent and patent applications over the...
19.
Lanning B, Whitby L, Dix M, Douhan J, Gilbert A, Hett E, et al.
Nat Chem Biol
. 2014 Jul;
10(9):760-767.
PMID: 25038787
Kinases are principal components of signal transduction pathways and the focus of intense basic and drug discovery research. Irreversible inhibitors that covalently modify non-catalytic cysteines in kinase active sites have...
20.
Chekler E, Unwalla R, Khan T, Tangirala R, Johnson M, St Andre M, et al.
J Med Chem
. 2014 Feb;
57(6):2462-71.
PMID: 24527807
We present a novel series of selective androgen receptor modulators (SARMs) which shows excellent biological activity and physical properties. 1-(2-Hydroxy-2-methyl-3-phenoxypropanoyl)-indoline-4-carbonitriles showed potent binding to the androgen receptor (AR) and activated...