E J Jacobsen
Overview
Explore the profile of E J Jacobsen including associated specialties, affiliations and a list of published articles.
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24
Citations
202
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Recent Articles
1.
Chrencik J, Patny A, Leung I, Korniski B, Emmons T, Hall T, et al.
J Mol Biol
. 2010 May;
400(3):413-33.
PMID: 20478313
Janus kinases (JAKs) are critical regulators of cytokine pathways and attractive targets of therapeutic value in both inflammatory and myeloproliferative diseases. Although the crystal structures of active JAK1 and JAK2...
2.
Tollefson M, Acker B, Jacobsen E, Hughes R, Walker J, Fox D, et al.
Bioorg Med Chem Lett
. 2010 May;
20(10):3120-4.
PMID: 20443228
1H-Pyrazolo[4,3-d]pyrimidines are a class of potent and selective second generation phosphodiesterase 5 (PDE5) inhibitors. This work explores the potency, selectivity and efficacy of 1-(2-ethoxyethyl)-1H-pyrazolo[4,5-d]pyrimidines as PDE5 inhibitors resulting in the...
3.
Tollefson M, Acker B, Jacobsen E, Hughes R, Walker J, Fox D, et al.
Bioorg Med Chem Lett
. 2010 Apr;
20(10):3125-8.
PMID: 20400309
1H-Pyrazolo[4,3-d]pyrimidines were previously disclosed as a potent second generation class of phosphodiesterase 5 (PDE5) inhibitors. This work explores the advancement of more selective and potent PDE5 inhibitors resulting from the...
4.
Jacobsen E, Mitchell M, Hendges S, Belonga K, Skaletzky L, Stelzer L, et al.
J Med Chem
. 1999 May;
42(9):1525-36.
PMID: 10229623
The synthesis and enzyme inhibition data for a series of thiadiazole urea matrix metalloproteinase (MMP) inhibitors are described. A broad screening effort was utilized to identify several thiadiazoles which were...
5.
Jacobsen E, Stelzer L, TenBrink R, Belonga K, CARTER D, Im H, et al.
J Med Chem
. 1999 Apr;
42(7):1123-44.
PMID: 10197957
A series of imidazo[1,5-a]quinoxaline piperazine ureas appended with a tert-butyl ester side chain at the 3-position was developed. Analogues within this series have high affinity for the gamma-aminobutyric acid A...
6.
Stockman B, Waldon D, Gates J, SCAHILL T, Kloosterman D, Mizsak S, et al.
Protein Sci
. 1998 Nov;
7(11):2281-6.
PMID: 9827994
Unregulated or overexpressed matrix metalloproteinases (MMPs), including stromelysin, collagenase, and gelatinase. have been implicated in several pathological conditions including arthritis and cancer. Small-molecule MMP inhibitors may have therapeutic value in...
7.
Im H, Im W, Pregenzer J, Stratman N, VonVoigtlander P, Jacobsen E
Br J Pharmacol
. 1998 May;
123(8):1490-4.
PMID: 9605552
1. Imidazoquinoxaline PNU-97775 and imidazoquinoline PNU-101017 are benzodiazepine site ligands with a second low affinity binding site on GABA(A) receptors, the occupancy of which at high drug concentrations reverses their...
8.
Hall E, Andrus P, Fleck T, Oostveen J, CARTER D, Jacobsen E
J Cereb Blood Flow Metab
. 1997 Aug;
17(8):875-83.
PMID: 9290585
PNU-101017 is a novel, imidazoquinoline amide and benzodiazepine receptor partial agonist that has high affinity for the GABAA receptor subtypes containing the alpha 1 and alpha 3 or alpha 5...
9.
Tang A, Franklin S, CARTER D, Sethy V, Needham L, Jacobsen E, et al.
Psychopharmacology (Berl)
. 1997 Jun;
131(3):255-63.
PMID: 9203236
PNU-101017 is a chemically novel ligand at the benzodiazepine recognition site of cloned GABAA receptors. It was reported to potentiate GABA-mediated chloride current in cultured cells with a moderate intrinsic...
10.
Mickelson J, Jacobsen E, CARTER D, Im H, Im W, Schreur P, et al.
J Med Chem
. 1996 Nov;
39(23):4654-66.
PMID: 8917654
A series of tetracyclic imidazoquinoxaline analogs was developed which constrain the carbonyl group of the partial agonist 3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-5-[(dimethylamino)carbonyl] - 4,5-dihydroimidazo[1,5-alpha]quinoxaline (2, U-91571) away from the benzene ring. These analogs orient...