T. O'Brien

发表

Metabolite profiling stratifies pancreatic ductal adenocarcinomas into subtypes with distinct sensitivities to metabolic inhibitors

Anneleen Daemen, Deepak Sampath, Gerard Manning, 2015, Proceedings of the National Academy of Sciences.

Retinal toxicity, in vivo and in vitro, associated with inhibition of nicotinamide phosphoribosyltransferase.

D. Sampath, P. Dragovich, T. O'Brien, 2015, Toxicological sciences : an official journal of the Society of Toxicology.

Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).

Karl H. Clodfelter, P. Bauer, N. Kley, 2013, Bioorganic & medicinal chemistry letters.

Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pK a Polar Moiety.

Xianrui Zhao, Ignacio Aliagas, Ronen Marmorstein, 2015, ACS medicinal chemistry letters.

Drug Discovery in Apoptosis

V. Dixit, T. O'Brien, 2009 .

Monitoring and Targeting Anti-VEGF Induced Hypoxia within the Viable Tumor by 19F–MRI and Multispectral Analysis

M. Hedehus, F. Peale, R. Carano, 2017, Neoplasia.

Fragment-based identification of amides derived from trans-2-(pyridin-3-yl)cyclopropanecarboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).

Brandon J. Bravo, Qiang Zhao, N. Skelton, 2013, Journal of medicinal chemistry.

Discovery of 2-(cyclohexylmethylamino)pyrimidines as a new class of reversible valosine containing protein inhibitors.

A. Isacchi, E. Felder, R. D'Alessio, 2014, Journal of medicinal chemistry.

Supplementation of nicotinic acid with NAMPT inhibitors results in loss of in vivo efficacy in NAPRT1-deficient tumor models.

Leslie B. Lee, D. Sampath, P. Jackson, 2013, Neoplasia.

IdentificationofPreferredChemotherapeuticsforCombining with a CHK1 Inhibitor

Marie Evangelista, S. Malek, P. Jackson, 2013 .

Cardiotoxicity Associated with Nicotinamide Phosphoribosyltransferase Inhibitors in Rodents and in Rat and Human-Derived Cells Lines

A. Bruening-Wright, D. Sampath, P. Dragovich, 2017, Cardiovascular Toxicology.

Abstract 964: Inhibiting glycolysis with an LDHA inhibitor: A new solution to an old problem

Marie Evangelista, G. Hatzivassiliou, D. Sampath, 2014 .

Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice.

Marie Evangelista, BinQing Wei, M. Ultsch, 2016, ACS medicinal chemistry letters.

Double genetic disruption of lactate dehydrogenases A and B is required to ablate the “Warburg effect” restricting tumor growth to oxidative metabolism

P. Oefner, J. Pouysségur, G. Koehl, 2018, The Journal of Biological Chemistry.

Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition.

M. Belvin, A. Daemen, BinQing Wei, 2016, Nature chemical biology.

Small Molecule Therapeutics Identi fi cationof PreferredChemotherapeutics forCombining with a CHK 1 Inhibitor

S. Malek, P. Jackson, Katarzyna Kowanetz, 2013 .

Chemically Diverse Group I p21-Activated Kinase (PAK) Inhibitors Impart Acute Cardiovascular Toxicity with a Narrow Therapeutic Window.

I. Aliagas, K. Hoeflich, Weiru Wang, 2016, Journal of medicinal chemistry.

Inhibition of nicotinamide phosphoribosyltransferase (NAMPT) as a therapeutic strategy in cancer.

Deepak Sampath, Tanja S. Zabka, D. Sampath, 2015, Pharmacology & therapeutics.

Dependence of tumor cell lines and patient-derived tumors on the NAD salvage pathway renders them sensitive to NAMPT inhibition with GNE-618.

Leslie B. Lee, D. Sampath, P. Jackson, 2013, Neoplasia.

Therapeutic strategies within the ubiquitin proteasome system

T. O'Brien, A. G. Eldridge, 2010, Cell Death and Differentiation.

Metabolic Response to NAD Depletion across Cell Lines Is Highly Variable

M. Belvin, A. Daemen, G. Hatzivassiliou, 2016, PloS one.

Chk1 inhibition in p53-deficient cell lines drives rapid chromosome fragmentation followed by caspase-independent cell death

J. Zha, L. Rangell, P. Jackson, 2013, Cell cycle.

Loss of NAPRT1 Expression by Tumor-Specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors

R. Bourgon, K. Walter, T. Pham, 2013, Clinical Cancer Research.

Predictive Biomarkers and Personalized Medicine Loss of NAPRT 1 Expression by Tumor-Speci fi c Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors

R. Bourgon, H. Koeppen, P. Haverty, 2013 .

Discovery of potent and efficacious urea-containing nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with reduced CYP2C9 inhibition properties.

Yang Xiao, Lei Zhang, Karl H. Clodfelter, 2013, Bioorganic & medicinal chemistry letters.

Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors.

N. Skelton, D. Sampath, K. Bair, 2016, Journal of medicinal chemistry.

Identification of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with no evidence of CYP3A4 time-dependent inhibition and improved aqueous solubility.

Karl H. Clodfelter, N. Skelton, D. Sampath, 2015, Bioorganic & medicinal chemistry letters.

Depletion of the Central Metabolite NAD Leads to Oncosis-mediated Cell Death*

L. Rangell, T. O'Brien, M. Reichelt, 2014, The Journal of Biological Chemistry.

Small molecule inhibition of group I p21-activated kinases in breast cancer induces apoptosis and potentiates the activity of microtubule stabilizing agents

I. Ellis, S. Chin, C. Caldas, 2015, Breast Cancer Research.

Identification of 2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-derived ureas as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).

Yang Xiao, Lei Zhang, Deepak Sampath, 2013, Bioorganic & medicinal chemistry letters.

Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.

Karl H. Clodfelter, P. Bauer, N. Kley, 2013, Journal of medicinal chemistry.

Structure-based Optimization of Hydroxylactam as Potent, Cell-Active Inhibitors of Lactate Dehydrogenase.

BinQing Wei, M. Ultsch, C. Eigenbrot, 2022, Bioorganic & medicinal chemistry letters.

Structural Basis for Resistance to Diverse Classes of NAMPT Inhibitors

D. Sampath, K. Bair, Weiru Wang, 2014, PloS one.

Fragment-based design of 3-aminopyridine-derived amides as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).

Brandon J. Bravo, Qiang Zhao, N. Skelton, 2014, Bioorganic & medicinal chemistry letters.

Small molecule inhibition of group I p21-activated kinases in breast cancer induces apoptosis and potentiates the activity of microtubule stabilizing agents

I. Ellis, S. Chin, C. Caldas, 2015, Breast Cancer Research.

Inhibition of nicotinamide phosphoribosyltransferase (NAMPT) as a therapeutic strategy in cancer.

D. Sampath, P. Dragovich, T. O'Brien, 2015, Pharmacology & therapeutics.

Fragment-based identification of amides derived from trans-2-(pyridin-3-yl)cyclopropanecarboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).

Brandon J. Bravo, Qiang Zhao, N. Skelton, 2013, Journal of medicinal chemistry.

Identification of Preferred Chemotherapeutics for Combining with a CHK1 Inhibitor

S. Malek, P. Jackson, Katarzyna Kowanetz, 2013, Molecular Cancer Therapeutics.