Judith C Fleming
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Explore the profile of Judith C Fleming including associated specialties, affiliations and a list of published articles.
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10
Citations
122
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Recent Articles
1.
Methot J, Hoffman D, Witter D, Stanton M, Harrington P, Hamblett C, et al.
ACS Med Chem Lett
. 2014 Jun;
5(4):340-5.
PMID: 24900838
The identification and in vitro and in vivo characterization of a potent SHI-1:2 are described. Kinetic analysis indicated that biaryl inhibitors exhibit slow binding kinetics in isolated HDAC1 and HDAC2...
2.
Kattar S, Surdi L, Zabierek A, Methot J, Middleton R, Hughes B, et al.
Bioorg Med Chem Lett
. 2009 Jan;
19(4):1168-72.
PMID: 19138845
The successful application of both solid and solution phase library synthesis, combined with tight integration into the medicinal chemistry effort, resulted in the efficient optimization of a novel structural series...
3.
Methot J, Hamblett C, Mampreian D, Jung J, Harsch A, Szewczak A, et al.
Bioorg Med Chem Lett
. 2008 Oct;
18(23):6104-9.
PMID: 18951790
A potent family of spirocyclic nicotinyl aminobenzamide selective HDAC1/HDAC2 inhibitors (SHI-1:2) is profiled. The incorporation of a biaryl zinc-binding motif into a nicotinyl scaffold resulted in enhanced potency and selectivity...
4.
Wilson K, Witter D, Grimm J, Siliphaivanh P, Otte K, Kral A, et al.
Bioorg Med Chem Lett
. 2008 Feb;
18(6):1859-63.
PMID: 18304810
An HTS screening campaign identified a series of low molecular weight phenols that showed excellent selectivity (>100-fold) for HDAC1/HDAC2 over other Class I and Class II HDACs. Evolution and optimization...
5.
Witter D, Harrington P, Wilson K, Chenard M, Fleming J, Haines B, et al.
Bioorg Med Chem Lett
. 2007 Dec;
18(2):726-31.
PMID: 18060775
A class of biaryl benzamides was identified and optimized as selective HDAC1&2 inhibitors (SHI-1:2). These agents exhibit selectivity over class II HDACs 4-7, as well as class I HDACs 3...
6.
Hubbs J, Zhou H, Kral A, Fleming J, Dahlberg W, Hughes B, et al.
Bioorg Med Chem Lett
. 2007 Nov;
18(1):34-8.
PMID: 18042381
Ongoing clinical studies indicate that inhibitors of Class I and Class II histone deacetylase (HDAC) enzymes show great promise for the treatment of cancer. Zolinza (SAHA, Zolinza) was recently approved...
7.
Hamblett C, Methot J, Mampreian D, Sloman D, Stanton M, Kral A, et al.
Bioorg Med Chem Lett
. 2007 Sep;
17(19):5300-9.
PMID: 17761416
This communication highlights the development of a nicotinamide series of histone deacetylase inhibitors within the benzamide structural class. Extensive exploration around the nicotinamide core led to the discovery of a...
8.
Siliphaivanh P, Harrington P, Witter D, Otte K, Tempest P, Kattar S, et al.
Bioorg Med Chem Lett
. 2007 Jun;
17(16):4619-24.
PMID: 17555962
Histone deacetylase (HDAC) inhibitors that target Class I and Class II HDACs are of synthetic and therapeutic interest and ongoing clinical studies indicate that they show great promise for the...
9.
Fleming J, Tartaglini E, Kawatsuji R, Yao D, Fujiwara Y, Bednarski J, et al.
Mol Genet Metab
. 2003 Oct;
80(1-2):234-41.
PMID: 14567973
Thiamine-responsive megaloblastic anemia with diabetes and deafness (TRMA) is an autosomal recessive disease caused by mutations in the high-affinity thiamine transporter gene SLC19A2. To study the role of thiamine transport...
10.
Boros L, Steinkamp M, Fleming J, Lee W, Cascante M, Neufeld E
Blood
. 2003 Aug;
102(10):3556-61.
PMID: 12893755
Fibroblasts from patients with thiamine-responsive megaloblastic anemia (TRMA) syndrome with diabetes and deafness undergo apoptotic cell death in the absence of supplemental thiamine in their cultures. The basis of megaloblastosis...