David J Richard
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Explore the profile of David J Richard including associated specialties, affiliations and a list of published articles.
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15
Citations
146
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Recent Articles
1.
Ericsson A, Richard D, Wilker E, Lancia Jr D, Fessler S, Troccolo P, et al.
Exp Hematol
. 2024 Nov;
141():104673.
PMID: 39549740
Anemia in patients with sickle cell disease (SCD) increases 2,3-diphosphoglycerate (2,3-DPG), decreasing hemoglobin-oxygen (HbO) affinity to improve oxygen offloading and promote hemoglobin polymerization (sickling) of red blood cells (RBCs). We...
2.
Richard D, Lena R, Bannister T, Blake N, Pierceall W, Carlson N, et al.
Bioorg Med Chem
. 2013 Sep;
21(21):6642-9.
PMID: 23993674
Anti-apoptotic Bcl-2 family proteins are important oncology therapeutic targets. To date, BH3 mimetics that abrogate anti-apoptotic activity have largely been directed at Bcl-2 and/or Bcl-xL. One observed mechanism of resistance...
3.
Zask A, Verheijen J, Richard D
Expert Opin Ther Pat
. 2011 May;
21(7):1109-27.
PMID: 21591993
Introduction: The mammalian target of rapamycin (mTOR) is a protein kinase and a key component of the PI3K/Akt/mTOR signaling pathway, and is deregulated in half of all human cancers. Rapamycin...
4.
Richard D, Verheijen J, Zask A
Curr Opin Drug Discov Devel
. 2010 Jul;
13(4):428-40.
PMID: 20597028
mTOR is a serine-threonine kinase that plays a key role in the regulation of cellular growth. The mTOR pathway consists of two distinct complexes: mTOR/Raptor (mTORC1) and mTOR/Rictor (mTORC2). In...
5.
Zask A, Verheijen J, Richard D, Kaplan J, Curran K, Toral-Barza L, et al.
Bioorg Med Chem Lett
. 2010 Mar;
20(8):2644-7.
PMID: 20227881
Incorporation of bridged morpholines in monocyclic triazine PI3K/mTOR inhibitors gave compounds with increased mTOR selectivity relative to the corresponding morpholine analogs. Compounds with ureidophenyl groups gave highly potent and selective...
6.
Richard D, Verheijen J, Yu K, Zask A
Bioorg Med Chem Lett
. 2010 Mar;
20(8):2654-7.
PMID: 20223664
Potent inhibitors of the mammalian target of rapamycin (mTOR) which contain the triazine scaffold and the (R)-3-methyl morpholine moiety have been identified. Such compounds also demonstrated good selectivity over the...
7.
Verheijen J, Richard D, Curran K, Kaplan J, Yu K, Zask A
Bioorg Med Chem Lett
. 2010 Mar;
20(8):2648-53.
PMID: 20223663
Isosteric replacement of one of the 3,5-ethylene-bridged morpholines in 2-arylureidophenyl-4,6-di(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines led to significant improvements in human microsomal stability. 3-R-Me-morpholine and tetrahydropyran were identified as preferred isosteres for the bridged morpholine....
8.
Curran K, Verheijen J, Kaplan J, Richard D, Toral-Barza L, Hollander I, et al.
Bioorg Med Chem Lett
. 2010 Jan;
20(4):1440-4.
PMID: 20089401
A series of pyrazolopyrimidine mammalian Target Of Rapamycin (mTOR) inhibitors with various substituents at the 1-position have been prepared, resulting in compounds with excellent potency, selectivity and microsomal stability. Combination...
9.
Zask A, Kaplan J, Verheijen J, Richard D, Curran K, Brooijmans N, et al.
J Med Chem
. 2009 Nov;
52(24):7942-5.
PMID: 19916508
Dramatic improvements in mTOR-targeting selectivity were achieved by replacing morpholine in pyrazolopyrimidine inhibitors with bridged morpholines. Analogues with subnanomolar mTOR IC(50) values and up to 26000-fold selectivity versus PI3Kalpha were...
10.
Richard D, Verheijen J, Curran K, Kaplan J, Toral-Barza L, Hollander I, et al.
Bioorg Med Chem Lett
. 2009 Nov;
19(24):6830-5.
PMID: 19896845
A series of highly potent and selective pyrazolopyrimidine mTOR inhibitors which contain water-solubilizing groups attached to the 6-arylureidophenyl moiety have been prepared. Such derivatives displayed superior potency to those in...