List of works - Julen Oyarzabal

A First-in-Class Small-Molecule that Acts as a Dual Inhibitor of HDAC and PDE5 and that Rescues Hippocampal Synaptic Impairment in Alzheimer's Disease Mice.

scientific article published on 23 August 2016

A cell-based screen identifies ATR inhibitors with synthetic lethal properties for cancer-associated mutations.

scientific article published on 8 May 2011

An integrated one-step system to extract, analyze and annotate all relevant information from image-based cell screening of chemical libraries

scientific article

Assessment of additive/nonadditive effects in structure-activity relationships: implications for iterative drug design

scientific article

Biologically Relevant Chemical Space Navigator: From Patent and Structure–Activity Relationship Analysis to Library Acquisition and Design ⬇️

scientific article published on December 5, 2012

Chemical interrogation of FOXO3a nuclear translocation identifies potent and selective inhibitors of phosphoinositide 3-kinases

scientific article published on 18 August 2009

Computational medicinal chemistry in fragment-based drug discovery: what, how and when.

scientific article published on January 2011

Concomitant histone deacetylase and phosphodiesterase 5 inhibition synergistically prevents the disruption in synaptic plasticity and it reverses cognitive impairment in a mouse model of Alzheimer's disease

scientific article

Conformational Selection versus Induced Fit in Kinases: The Case of PI3K‐γ ⬇️

scientific article published on January 16, 2012

Decreased levels of guanosine 3', 5'-monophosphate (cGMP) in cerebrospinal fluid (CSF) are associated with cognitive decline and amyloid pathology in Alzheimer's disease

scientific article published in June 2015

Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.

scientific article published on 8 September 2016

Design, Synthesis, and Biological Evaluation of Novel Matrix Metalloproteinase Inhibitors As Potent Antihemorrhagic Agents: From Hit Identification to an Optimized Lead

scientific article published on 25 February 2015

Detailed Exploration around 4-Aminoquinolines Chemical Space to Navigate the Lysine Methyltransferase G9a and DNA Methyltransferase Biological Spaces

scientific article published on 19 July 2018

Development and Validation of Molecular Overlays Derived from Three-Dimensional Hydrophobic Similarity with PharmScreen

article

Discovery and safety profiling of a potent preclinical candidate, (4-[4-[[(3R)-3-(hydroxycarbamoyl)-8-azaspiro[4.5]decan-3-yl]sulfonyl]phenoxy]-N-methylbenzamide) (CM-352), for the prevention and treatment of hemorrhage

scientific article published on 25 February 2015

Discovery of 1,5-disubstituted pyridones: a new class of positive allosteric modulators of the metabotropic glutamate 2 receptor

scientific article published on 23 August 2010

Discovery of Reversible DNA Methyltransferase and Lysine Methyltransferase G9a Inhibitors with Antitumoral in Vivo Efficacy

scientific article published on 19 July 2018

Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies

scientific article

Discovery of in Vivo Chemical Probes for Treating Alzheimer's Disease: Dual Phosphodiesterase 5 (PDE5) and Class I Histone Deacetylase Selective Inhibitors

scientific article published on 21 December 2018

Discovery of mitogen-activated protein kinase-interacting kinase 1 inhibitors by a comprehensive fragment-oriented virtual screening approach.

scientific article

Discovery of selective ligands for telomeric RNA G-quadruplexes (TERRA) through 19F-NMR based fragment screening

scientific article

Endogenous retroelement activation by epigenetic therapy reverses the Warburg effect and elicits mitochondrial-mediated cancer cell death

scientific article published on 18 December 2020

Erratum: Salermide, a Sirtuin inhibitor with a strong cancer-specific proapoptotic effect

scholarly article published in Oncogene

Fatty acid amide hydrolase inhibition for the symptomatic relief of Parkinson's disease.

scientific article published on 15 June 2016

Fluoroalkyl alpha,beta-unsaturated imines. Valuable synthetic intermediates from primary fluorinated enamine phosphonates

scientific article published on 01 March 2002

Fragment-hopping-based discovery of a novel chemical series of proto-oncogene PIM-1 kinase inhibitors

scientific article

Hit to lead evaluation of 1,2,3-triazolo[4,5-b]pyridines as PIM kinase inhibitors

scientific article

Hsp70 protects from stroke in atrial fibrillation patients by preventing thrombosis without increased bleeding risk

scientific article published on 14 March 2016

ICAM-1 peptide inhibitors of T-cell adhesion bind to the allosteric site of LFA-1. An NMR characterization

scientific article published on 14 September 2007

Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor.

scientific article

Imidazo[1,2-a]pyrazines as novel PI3K inhibitors

scientific article published on 28 January 2012

Impact of Scaffold Exploration on Novel Dual-Acting Histone Deacetylases and Phosphodiesterase 5 Inhibitors for the Treatment of Alzheimer's Disease

scientific article

In vivo, in vitro and in silico methods for small molecule transfer across the BBB.

scientific article

Information Retrieval and Text Mining Technologies for Chemistry.

scientific article

Inhibition of FOXP3/NFAT Interaction Enhances T Cell Function after TCR Stimulation.

scientific article

Monoacylglycerol lipase inhibitor JZL184 is neuroprotective and alters glial cell phenotype in the chronic MPTP mouse model

scientific article published on 28 May 2014

Multitarget Approach for the Treatment of Alzheimer's Disease: Inhibition of Phosphodiesterase 9 (PDE9) and Histone Deacetylases (HDACs) Covering Diverse Selectivity Profiles

scientific article published on 04 September 2019

Novel Scaffold FingerPrint (SFP): applications in scaffold hopping and scaffold-based selection of diverse compounds.

scientific article published on 13 January 2015

Novel approach for chemotype hopping based on annotated databases of chemically feasible fragments and a prospective case study: new melanin concentrating hormone antagonists.

scientific article published in April 2009

Optimizing the performance of in silico ADMET general models according to local requirements: MARS approach. solubility estimations as case study.

scientific article

Pharmacokinetic investigation of sildenafil using positron emission tomography and determination of its effect on cerebrospinal fluid cGMP levels

scientific article published on 7 December 2015

Phosphodiesterase inhibition in cognitive decline

scientific article

Pim 1 kinase inhibitor ETP-45299 suppresses cellular proliferation and synergizes with PI3K inhibition

scientific article published on 3 November 2010

Preparation of fluoroalkyl imines, amines, enamines, ketones, alpha-amino carbonyls, and alpha-amino acids from primary enamine phosphonates

scientific article published in December 2004

Rapid identification of ETP-46992, orally bioavailable PI3K inhibitor, selective versus mTOR.

scientific article

Repurposing ciclopirox as a pharmacological chaperone in a model of congenital erythropoietic porphyria

scientific article published on 01 September 2018

Salermide, a Sirtuin inhibitor with a strong cancer-specific proapoptotic effect.

scientific article

Synthesis of fluoroalkylated beta-aminophosphonates and pyridines from primary beta-enaminophosphonates

scientific article published on 20 May 2008

Tadalafil crosses the blood-brain barrier and reverses cognitive dysfunction in a mouse model of AD.

scientific article

The Markyt visualisation, prediction and benchmark platform for chemical and gene entity recognition at BioCreative/CHEMDNER challenge

scientific article

Towards the understanding of the activity of G9a inhibitors: an activity landscape and molecular modeling approach

scientific article published on 14 February 2020

Two Affinity Sites of the Cannabinoid Subtype 2 Receptor Identified by a Novel Homogeneous Binding Assay.

scientific article published on 29 June 2016

Using Novel Descriptor Accounting for Ligand–Receptor Interactions To Define and Visually Explore Biologically Relevant Chemical Space ⬇️

scientific article published on April 19, 2012

Zebrafish: Speeding Up the Cancer Drug Discovery Process

article

List of works by Julen Oyarzabal

A First-in-Class Small-Molecule that Acts as a Dual Inhibitor of HDAC and PDE5 and that Rescues Hippocampal Synaptic Impairment in Alzheimer's Disease Mice.

A cell-based screen identifies ATR inhibitors with synthetic lethal properties for cancer-associated mutations.

An integrated one-step system to extract, analyze and annotate all relevant information from image-based cell screening of chemical libraries

Assessment of additive/nonadditive effects in structure-activity relationships: implications for iterative drug design

Biologically Relevant Chemical Space Navigator: From Patent and Structure–Activity Relationship Analysis to Library Acquisition and Design ⬇️

Chemical interrogation of FOXO3a nuclear translocation identifies potent and selective inhibitors of phosphoinositide 3-kinases

Computational medicinal chemistry in fragment-based drug discovery: what, how and when.

Concomitant histone deacetylase and phosphodiesterase 5 inhibition synergistically prevents the disruption in synaptic plasticity and it reverses cognitive impairment in a mouse model of Alzheimer's disease

Conformational Selection versus Induced Fit in Kinases: The Case of PI3K‐γ ⬇️

Decreased levels of guanosine 3', 5'-monophosphate (cGMP) in cerebrospinal fluid (CSF) are associated with cognitive decline and amyloid pathology in Alzheimer's disease

Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.

Design, Synthesis, and Biological Evaluation of Novel Matrix Metalloproteinase Inhibitors As Potent Antihemorrhagic Agents: From Hit Identification to an Optimized Lead

Detailed Exploration around 4-Aminoquinolines Chemical Space to Navigate the Lysine Methyltransferase G9a and DNA Methyltransferase Biological Spaces

Development and Validation of Molecular Overlays Derived from Three-Dimensional Hydrophobic Similarity with PharmScreen

Discovery and safety profiling of a potent preclinical candidate, (4-[4-[[(3R)-3-(hydroxycarbamoyl)-8-azaspiro[4.5]decan-3-yl]sulfonyl]phenoxy]-N-methylbenzamide) (CM-352), for the prevention and treatment of hemorrhage

Discovery of 1,5-disubstituted pyridones: a new class of positive allosteric modulators of the metabotropic glutamate 2 receptor

Discovery of Reversible DNA Methyltransferase and Lysine Methyltransferase G9a Inhibitors with Antitumoral in Vivo Efficacy

Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies

Discovery of in Vivo Chemical Probes for Treating Alzheimer's Disease: Dual Phosphodiesterase 5 (PDE5) and Class I Histone Deacetylase Selective Inhibitors

Discovery of mitogen-activated protein kinase-interacting kinase 1 inhibitors by a comprehensive fragment-oriented virtual screening approach.

Discovery of selective ligands for telomeric RNA G-quadruplexes (TERRA) through 19F-NMR based fragment screening

Endogenous retroelement activation by epigenetic therapy reverses the Warburg effect and elicits mitochondrial-mediated cancer cell death

Erratum: Salermide, a Sirtuin inhibitor with a strong cancer-specific proapoptotic effect

Fatty acid amide hydrolase inhibition for the symptomatic relief of Parkinson's disease.

Fluoroalkyl alpha,beta-unsaturated imines. Valuable synthetic intermediates from primary fluorinated enamine phosphonates

Fragment-hopping-based discovery of a novel chemical series of proto-oncogene PIM-1 kinase inhibitors

Hit to lead evaluation of 1,2,3-triazolo[4,5-b]pyridines as PIM kinase inhibitors

Hsp70 protects from stroke in atrial fibrillation patients by preventing thrombosis without increased bleeding risk

ICAM-1 peptide inhibitors of T-cell adhesion bind to the allosteric site of LFA-1. An NMR characterization

Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor.

Imidazo[1,2-a]pyrazines as novel PI3K inhibitors

Impact of Scaffold Exploration on Novel Dual-Acting Histone Deacetylases and Phosphodiesterase 5 Inhibitors for the Treatment of Alzheimer's Disease

In vivo, in vitro and in silico methods for small molecule transfer across the BBB.

Information Retrieval and Text Mining Technologies for Chemistry.

Inhibition of FOXP3/NFAT Interaction Enhances T Cell Function after TCR Stimulation.

Monoacylglycerol lipase inhibitor JZL184 is neuroprotective and alters glial cell phenotype in the chronic MPTP mouse model

Multitarget Approach for the Treatment of Alzheimer's Disease: Inhibition of Phosphodiesterase 9 (PDE9) and Histone Deacetylases (HDACs) Covering Diverse Selectivity Profiles

Novel Scaffold FingerPrint (SFP): applications in scaffold hopping and scaffold-based selection of diverse compounds.

Novel approach for chemotype hopping based on annotated databases of chemically feasible fragments and a prospective case study: new melanin concentrating hormone antagonists.

Optimizing the performance of in silico ADMET general models according to local requirements: MARS approach. solubility estimations as case study.

Pharmacokinetic investigation of sildenafil using positron emission tomography and determination of its effect on cerebrospinal fluid cGMP levels

Phosphodiesterase inhibition in cognitive decline

Pim 1 kinase inhibitor ETP-45299 suppresses cellular proliferation and synergizes with PI3K inhibition

Preparation of fluoroalkyl imines, amines, enamines, ketones, alpha-amino carbonyls, and alpha-amino acids from primary enamine phosphonates

Rapid identification of ETP-46992, orally bioavailable PI3K inhibitor, selective versus mTOR.

Repurposing ciclopirox as a pharmacological chaperone in a model of congenital erythropoietic porphyria

Salermide, a Sirtuin inhibitor with a strong cancer-specific proapoptotic effect.

Synthesis of fluoroalkylated beta-aminophosphonates and pyridines from primary beta-enaminophosphonates

Tadalafil crosses the blood-brain barrier and reverses cognitive dysfunction in a mouse model of AD.

The Markyt visualisation, prediction and benchmark platform for chemical and gene entity recognition at BioCreative/CHEMDNER challenge

Towards the understanding of the activity of G9a inhibitors: an activity landscape and molecular modeling approach

Two Affinity Sites of the Cannabinoid Subtype 2 Receptor Identified by a Novel Homogeneous Binding Assay.

Using Novel Descriptor Accounting for Ligand–Receptor Interactions To Define and Visually Explore Biologically Relevant Chemical Space ⬇️

Zebrafish: Speeding Up the Cancer Drug Discovery Process