Gary L Schieven
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Explore the profile of Gary L Schieven including associated specialties, affiliations and a list of published articles.
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41
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1116
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Recent Articles
11.
Liu C, Lin J, Hynes J, Wu H, Wrobleski S, Lin S, et al.
J Med Chem
. 2015 Sep;
58(19):7775-84.
PMID: 26359680
In search for prodrugs to address the issue of pH-dependent solubility and exposure associated with 1 (BMS-582949), a previously disclosed phase II clinical p38α MAP kinase inhibitor, a structurally novel...
12.
Duan J, Lu Z, Jiang B, Yang B, Doweyko L, Nirschl D, et al.
Bioorg Med Chem Lett
. 2014 Dec;
24(24):5721-5726.
PMID: 25453808
A new class of Janus kinase (JAK) inhibitors was discovered using a rationally designed pyrrolo[1,2-b]pyridazine-3-carboxamide scaffold. Preliminary studies identified (R)-(2,2-dimethylcyclopentyl)amine as a preferred C4 substituent on the pyrrolopyridazine core (3b)....
13.
Wrobleski S, Lin S, Murali Dhar T, Dyckman A, Li T, Pitt S, et al.
Bioorg Med Chem Lett
. 2013 Jun;
23(14):4120-6.
PMID: 23746475
A novel series of p38 MAP kinase inhibitors with high selectivity for the p38α isoform over the other family members including the highly homologous p38β isoform has been identified. X-ray...
14.
Liu C, Lin J, Everlof G, Gesenberg C, Zhang H, Marathe P, et al.
Bioorg Med Chem Lett
. 2013 Apr;
23(10):3028-33.
PMID: 23578688
A series of carbamoylmethylene linked prodrugs of 1 (BMS-582949), a clinical p38α inhibitor, were synthesized and evaluated. Though the phosphoryloxymethylene carbamates (3, 4, and 5) and α-aminoacyloxymethylene carbamates (22, 23,...
15.
Dyckman A, Li T, Pitt S, Zhang R, Shen D, McIntyre K, et al.
Bioorg Med Chem Lett
. 2011 Jun;
21(15):4633-7.
PMID: 21705217
Pyrrolo[2,1-f][1,2,4]triazine based inhibitors of p38α have been prepared exploring functional group modifications at the C6 position. Incorporation of aryl and heteroaryl ketones at this position led to potent inhibitors with...
16.
Das J, Moquin R, Dyckman A, Li T, Pitt S, Zhang R, et al.
Bioorg Med Chem Lett
. 2010 Nov;
20(23):6886-9.
PMID: 21035336
The synthesis and structure-activity relationships (SAR) of p38α MAP kinase inhibitors based on a 5-amino-pyrazole scaffold are described. These studies led to the identification of compound 2j as a potent...
17.
Liu C, Lin J, Wrobleski S, Lin S, Hynes J, Wu H, et al.
J Med Chem
. 2010 Sep;
53(18):6629-39.
PMID: 20804198
The discovery and characterization of 7k (BMS-582949), a highly selective p38α MAP kinase inhibitor that is currently in phase II clinical trials for the treatment of rheumatoid arthritis, is described....
18.
Lin S, Wrobleski S, Hynes Jr J, Pitt S, Zhang R, Fan Y, et al.
Bioorg Med Chem Lett
. 2010 Aug;
20(19):5864-8.
PMID: 20732813
The design, synthesis, and structure-activity relationships (SAR) of a series of 2-aminothiazol-5-yl-pyrimidines as novel p38α MAP kinase inhibitors are described. These efforts led to the identification of 41 as a...
19.
Krejsa C, Franklin C, White C, Ledbetter J, Schieven G, Kavanagh T
J Biol Chem
. 2010 Mar;
285(21):16116-24.
PMID: 20332089
Glutamate cysteine ligase (GCL) catalyzes the rate-limiting step in the formation of the cellular antioxidant glutathione (GSH). The GCL holoenzyme consists of two separately coded proteins, a catalytic subunit (GCLC)...
20.
Schieven G
Curr Top Med Chem
. 2009 Sep;
9(11):1038-48.
PMID: 19747121
The p38 kinase plays a central role in inflammation, and it has been the subject of extensive efforts in both basic research and drug discovery. This review summarizes the biology...