about
Hit to lead evaluation of 1,2,3-triazolo[4,5-b]pyridines as PIM kinase inhibitorsFragment-hopping-based discovery of a novel chemical series of proto-oncogene PIM-1 kinase inhibitorsThe Markyt visualisation, prediction and benchmark platform for chemical and gene entity recognition at BioCreative/CHEMDNER challengeOptimizing the performance of in silico ADMET general models according to local requirements: MARS approach. solubility estimations as case study.Assessment of additive/nonadditive effects in structure-activity relationships: implications for iterative drug design.In vivo, in vitro and in silico methods for small molecule transfer across the BBB.An integrated one-step system to extract, analyze and annotate all relevant information from image-based cell screening of chemical libraries.Discovery of mitogen-activated protein kinase-interacting kinase 1 inhibitors by a comprehensive fragment-oriented virtual screening approach.Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies.Biologically relevant chemical space navigator: from patent and structure-activity relationship analysis to library acquisition and design.Discovery of selective ligands for telomeric RNA G-quadruplexes (TERRA) through 19F-NMR based fragment screening.Novel Scaffold FingerPrint (SFP): applications in scaffold hopping and scaffold-based selection of diverse compounds.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.A cell-based screen identifies ATR inhibitors with synthetic lethal properties for cancer-associated mutations.Chemical interrogation of FOXO3a nuclear translocation identifies potent and selective inhibitors of phosphoinositide 3-kinasesComputational medicinal chemistry in fragment-based drug discovery: what, how and when.Phosphodiesterase inhibition in cognitive decline.Information Retrieval and Text Mining Technologies for Chemistry.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.Fatty acid amide hydrolase inhibition for the symptomatic relief of Parkinson's disease.Rapid identification of ETP-46992, orally bioavailable PI3K inhibitor, selective versus mTOR.Imidazo[1,2-a]pyrazines as novel PI3K inhibitors.Pim 1 kinase inhibitor ETP-45299 suppresses cellular proliferation and synergizes with PI3K inhibition.Salermide, a Sirtuin inhibitor with a strong cancer-specific proapoptotic effect.Pharmacokinetic investigation of sildenafil using positron emission tomography and determination of its effect on cerebrospinal fluid cGMP levels.Discovery of 1,5-disubstituted pyridones: a new class of positive allosteric modulators of the metabotropic glutamate 2 receptorDiscovery 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.Tadalafil crosses the blood-brain barrier and reverses cognitive dysfunction in a mouse model of AD.Preparation of fluoroalkyl imines, amines, enamines, ketones, alpha-amino carbonyls, and alpha-amino acids from primary enamine phosphonates.Monoacylglycerol lipase inhibitor JZL184 is neuroprotective and alters glial cell phenotype in the chronic MPTP mouse model.Inhibition of FOXP3/NFAT Interaction Enhances T Cell Function after TCR Stimulation.Synthesis of fluoroalkylated beta-aminophosphonates and pyridines from primary beta-enaminophosphonates.Two Affinity Sites of the Cannabinoid Subtype 2 Receptor Identified by a Novel Homogeneous Binding Assay.Impact of Scaffold Exploration on Novel Dual-Acting Histone Deacetylases and Phosphodiesterase 5 Inhibitors for the Treatment of Alzheimer's Disease.Decreased levels of guanosine 3', 5'-monophosphate (cGMP) in cerebrospinal fluid (CSF) are associated with cognitive decline and amyloid pathology in Alzheimer's disease.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.Novel approach for chemotype hopping based on annotated databases of chemically feasible fragments and a prospective case study: new melanin concentrating hormone antagonists.Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor.Conformational selection versus induced fit in kinases: the case of PI3K-γ.Zebrafish: Speeding Up the Cancer Drug Discovery Process
P50
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P50
description
hulumtues
@sq
researcher
@en
wetenschapper
@nl
հետազոտող
@hy
name
Julen Oyarzabal
@ast
Julen Oyarzabal
@en
Julen Oyarzabal
@es
Julen Oyarzabal
@nl
Julen Oyarzabal
@sl
type
label
Julen Oyarzabal
@ast
Julen Oyarzabal
@en
Julen Oyarzabal
@es
Julen Oyarzabal
@nl
Julen Oyarzabal
@sl
prefLabel
Julen Oyarzabal
@ast
Julen Oyarzabal
@en
Julen Oyarzabal
@es
Julen Oyarzabal
@nl
Julen Oyarzabal
@sl
P1053
K-7393-2017
P106
P21
P2456
P31
P3829
P496
0000-0003-1941-7255
P569
2000-01-01T00:00:00Z