[HTML][HTML] Pharmacological inhibition of nicotinamide phosphoribosyltransferase (NAMPT), an enzyme essential for NAD+ biosynthesis, in human cancer cells …
…, J Gillig, S Parthasarathy, TP Burkholder… - Journal of Biological …, 2013 - ASBMB
Nicotinamide phosphoribosyltransferase (NAMPT) catalyzes the first rate-limiting step in
converting nicotinamide to NAD + , essential for cellular metabolism, energy production, and …
converting nicotinamide to NAD + , essential for cellular metabolism, energy production, and …
Substituted 3-Imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino- [6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as Highly Selective and Potent Inhibitors of …
…, K Furness, J Brozinick, TP Burkholder… - Journal of medicinal …, 2004 - ACS Publications
Glycogen synthase kinase-3 (GSK3) is involved in signaling from the insulin receptor.
Inhibitors of GSK3 are expected to effect lowering of plasma glucose similar to insulin, making …
Inhibitors of GSK3 are expected to effect lowering of plasma glucose similar to insulin, making …
[HTML][HTML] Discovery and characterization of LY2784544, a small-molecule tyrosine kinase inhibitor of JAK2V617F
…, MS Dowless, PW Iversen, TP Burkholder - Blood cancer …, 2013 - nature.com
Owing to the prevalence of the JAK2V617F mutation in myeloproliferative neoplasms (MPNs),
its constitutive activity, and ability to recapitulate the MPN phenotype in mouse models, …
its constitutive activity, and ability to recapitulate the MPN phenotype in mouse models, …
Discovery of a highly selective NAMPT inhibitor that demonstrates robust efficacy and improved retinal toxicity with nicotinic acid coadministration
…, MS Kuo, S Geeganage, TP Burkholder - Molecular cancer …, 2017 - AACR
NAMPT, an enzyme essential for NAD + biosynthesis, has been extensively studied as an
anticancer target for developing potential novel therapeutics. Several NAMPT inhibitors have …
anticancer target for developing potential novel therapeutics. Several NAMPT inhibitors have …
Synthesis via vinyl sulfones. 38. Total synthesis of the cephalotaxus alkaloids dl-cephalotaxine, dl-11-hydroxycephalotaxine, and dl-drupacine
TP Burkholder, PL Fuchs - Journal of the American Chemical …, 1990 - ACS Publications
This paper reports the chemical details of our total synthesis of¿/-cephalotaxine (1) and the
completion of the first total synthesis of dl-11-hydroxycephalotaxine (3) and¿/-drupacine (4). …
completion of the first total synthesis of dl-11-hydroxycephalotaxine (3) and¿/-drupacine (4). …
Development and a practical synthesis of the JAK2 inhibitor LY2784544
…, PM Pollock, DM Coppert, TP Burkholder… - … Process Research & …, 2012 - ACS Publications
The route selection and process research and development of a practical synthesis for JAK2
inhibitor LY2784544 is described. The first-generation synthesis route, similar to that used …
inhibitor LY2784544 is described. The first-generation synthesis route, similar to that used …
The development of potent and selective bisarylmaleimide GSK3 inhibitors
TA Engler, S Malhotra, TP Burkholder, JR Henry… - Bioorganic & medicinal …, 2005 - Elsevier
Many 3-aryl-4-(1,2,3,4-tetrahydro[1,4]diazepino[6,7,1-hi]indol-7-yl)maleimides exhibit potent
GSK3 inhibitory activity (<100nM IC 50 ), although few show significant selectivity (>100×) …
GSK3 inhibitory activity (<100nM IC 50 ), although few show significant selectivity (>100×) …
An acyliminium ion route to cis and trans “anti” phe-gly dipeptide mimetics
GA Flynn, TP Burkholder, EW Huber, P Bey - Bioorganic & Medicinal …, 1991 - Elsevier
The synthesis of two series of constrained mimetics of the dipeptide phenylalanylglycine
oriented in the “anti” conformation (X 1 = 180) are described. These benzolactams differ about …
oriented in the “anti” conformation (X 1 = 180) are described. These benzolactams differ about …
Discovery of chiral dihydropyridopyrimidinones as potent, selective and orally bioavailable inhibitors of AKT
…, T Raub, M Lai, S Geeganage, TP Burkholder - Bioorganic & medicinal …, 2018 - Elsevier
During the course of our research efforts to develop potent and selective AKT inhibitors, we
discovered enatiomerically pure substituted dihydropyridopyrimidinones (DHP) as potent …
discovered enatiomerically pure substituted dihydropyridopyrimidinones (DHP) as potent …
[HTML][HTML] Developing and applying a gene functional association network for anti-angiogenic kinase inhibitor activity assessment in an angiogenesis co-culture model
…, T Wei, L Yan, F Lawrence, HR Qian, TP Burkholder… - Bmc Genomics, 2008 - Springer
Background Tumor angiogenesis is a highly regulated process involving intercellular
communication as well as the interactions of multiple downstream signal transduction pathways. …
communication as well as the interactions of multiple downstream signal transduction pathways. …