List of works - Thomas O'Brien

2-Aminobenzimidazoles as potent Aurora kinase inhibitors.

scientific article

Alkylsulfanyl-1,2,4-triazoles, a new class of allosteric valosine containing protein inhibitors. Synthesis and structure-activity relationships

scientific article published on 04 January 2013

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

scientific article

Covalent and allosteric inhibitors of the ATPase VCP/p97 induce cancer cell death

scientific article

Crystal structures of a ligand-free and malonate-bound human caspase-1: implications for the mechanism of substrate binding.

scientific article published in August 2004

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

scientific article published on October 2013

Depletion of the central metabolite NAD leads to oncosis-mediated cell death.

scientific article

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

scientific article

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

scientific article

Discovery of a potent and selective aurora kinase inhibitor

scientific article

Fragment-Based Drug Discovery

article

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

scientific article published on 22 January 2014

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

scientific article

Identification of potent and novel small-molecule inhibitors of caspase-3

scientific article published on 01 November 2003

Loss of NAPRT1 expression by tumor-specific promoter methylation provides a novel predictive biomarker for NAMPT inhibitors

scientific article

Metabolic Response to NAD Depletion across Cell Lines Is Highly Variable

scientific article

Metabolic response of prostate cancer to nicotinamide phophoribosyltransferase inhibition in a hyperpolarized MR/PET compatible bioreactor

scientific article published on 14 July 2015

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

scientific article

Mouse Aurora A: expression in Escherichia coli and purification.

scientific article published on 12 March 2007

Pharmacological Inhibition of the Histone Lysine Demethylase KDM1A Suppresses the Growth of Multiple Acute Myeloid Leukemia Subtypes.

scientific article published on 2 February 2016

Prospects for caspase inhibitors.

scientific article published on February 2004

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

scientific article published on 11 December 2014

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

scientific article

Structural analysis of caspase-1 inhibitors derived from Tethering.

scientific article published on 9 April 2005

Structural basis for resistance to diverse classes of NAMPT inhibitors

scientific article

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

scientific article

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

scientific article published on December 2013

Targeting p21-activated kinase 1 (PAK1) to induce apoptosis of tumor cells

scientific article

Tethering identifies fragment that yields potent inhibitors of human caspase-1

scientific article published on 04 November 2005

Therapeutic strategies within the ubiquitin proteasome system.

scientific article published on January 2010

List of works by Thomas O'Brien

2-Aminobenzimidazoles as potent Aurora kinase inhibitors.

Alkylsulfanyl-1,2,4-triazoles, a new class of allosteric valosine containing protein inhibitors. Synthesis and structure-activity relationships

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

Covalent and allosteric inhibitors of the ATPase VCP/p97 induce cancer cell death

Crystal structures of a ligand-free and malonate-bound human caspase-1: implications for the mechanism of substrate binding.

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

Depletion of the central metabolite NAD leads to oncosis-mediated cell death.

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

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

Discovery of a potent and selective aurora kinase inhibitor

Fragment-Based Drug Discovery

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

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

Identification of potent and novel small-molecule inhibitors of caspase-3

Loss of NAPRT1 expression by tumor-specific promoter methylation provides a novel predictive biomarker for NAMPT inhibitors

Metabolic Response to NAD Depletion across Cell Lines Is Highly Variable

Metabolic response of prostate cancer to nicotinamide phophoribosyltransferase inhibition in a hyperpolarized MR/PET compatible bioreactor

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

Mouse Aurora A: expression in Escherichia coli and purification.

Pharmacological Inhibition of the Histone Lysine Demethylase KDM1A Suppresses the Growth of Multiple Acute Myeloid Leukemia Subtypes.

Prospects for caspase inhibitors.

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

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

Structural analysis of caspase-1 inhibitors derived from Tethering.

Structural basis for resistance to diverse classes of NAMPT inhibitors

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

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

Targeting p21-activated kinase 1 (PAK1) to induce apoptosis of tumor cells

Tethering identifies fragment that yields potent inhibitors of human caspase-1

Therapeutic strategies within the ubiquitin proteasome system.