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Lista de obras de Ajit Jadhav

12-lipoxygenase activity plays an important role in PAR4 and GPVI-mediated platelet reactivity

artículo científico publicado en 2013

3-substituted indole inhibitors against Francisella tularensis FabI identified by structure-based virtual screening

artículo científico publicado en 2013

4-(3-Chloro-5-(trifluoromethyl)pyridin-2-yl)-N-(4-methoxypyridin-2-yl)piperazine-1-carbothioamide (ML267), a potent inhibitor of bacterial phosphopantetheinyl transferase that attenuates secondary metabolism and thwarts bacterial growth

artículo científico publicado en 2014

A 1,536-well-based kinetic HTS assay for inhibitors of Schistosoma mansoni thioredoxin glutathione reductase

artículo científico publicado en 2008

A Comparative Study of Target Engagement Assays for HDAC1 Inhibitor Profiling

scientific article published on 29 October 2019

A High-Content Assay Enables the Automated Screening and Identification of Small Molecules with Specific ALDH1A1-Inhibitory Activity.

artículo científico publicado en 2017

A High-Throughput Screen Identifies 2,9-Diazaspiro[5.5]Undecanes as Inducers of the Endoplasmic Reticulum Stress Response with Cytotoxic Activity in 3D Glioma Cell Models

artículo científico publicado en 2016

A comprehensive strategy to discover inhibitors of the translesion synthesis DNA polymerase κ

artículo científico publicado en 2012

A fluorescence-based high throughput assay for the determination of small molecule-human serum albumin protein binding

artículo científico publicado en 2014

A furoxan-amodiaquine hybrid as a potential therapeutic for three parasitic diseases().

artículo científico publicado en 2012

A grid algorithm for high throughput fitting of dose-response curve data

artículo científico publicado en 2010

A high throughput fluorescence polarization assay for inhibitors of the GoLoco motif/G-alpha interaction

artículo científico publicado en 2008

A high throughput screen identifies potent and selective inhibitors to human epithelial 15-lipoxygenase-2

artículo científico publicado en 2014

A high-throughput approach for identification of novel general anesthetics

artículo científico publicado en 2009

A high-throughput assay for small molecule destabilizers of the KRAS oncoprotein

artículo científico publicado en 2014

A high-throughput screen for aggregation-based inhibition in a large compound library

artículo científico publicado en 2007

A high-throughput small molecule screen identifies synergism between DNA methylation and Aurora kinase pathways for X reactivation

artículo científico publicado en 2016

A highly potent and selective caspase 1 inhibitor that utilizes a key 3-cyanopropanoic acid moiety

artículo científico publicado en 2010

A miniaturized glucocorticoid receptor translocation assay using enzymatic fragment complementation evaluated with qHTS.

artículo científico publicado en 2008

A miniaturized screen for inhibitors of Jumonji histone demethylases

artículo científico publicado en 2009

A novel P300 inhibitor reverses DUX4-mediated global histone H3 hyperacetylation, target gene expression, and cell death

artículo científico publicado en 2019

A potent and selective inhibitor targeting human and murine 12/15-LOX.

artículo científico publicado en 2016

A quantitative high-throughput screen for modulators of IL-6 signaling: a model for interrogating biological networks using chemical libraries

artículo científico publicado en 2009

A quantitative high-throughput screen identifies potential epigenetic modulators of gene expression

artículo científico publicado en 2007

A robotic platform for quantitative high-throughput screening

artículo científico publicado en 2008

A selective USP1-UAF1 inhibitor links deubiquitination to DNA damage responses.

artículo científico publicado en 2014

A small molecule inhibitor of the BLM helicase modulates chromosome stability in human cells

artículo científico publicado en 2013

A strategy to discover inhibitors of Bacillus subtilis surfactin-type phosphopantetheinyl transferase

artículo científico publicado en 2009

Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes

artículo científico publicado en 2015

AlphaScreen-Based Assays: Ultra-High-Throughput Screening for Small-Molecule Inhibitors of Challenging Enzymes and Protein-Protein Interactions

artículo científico publicado en 2016

Anxiolytic Drug FGIN-1-27 Ameliorates Autoimmunity by Metabolic Reprogramming of Pathogenic Th17 Cells

artículo científico publicado en 2020

Are hERG channel blockers also phospholipidosis inducers?

scientific article published on 20 June 2013

Assessing inhibitors of mutant isocitrate dehydrogenase using a suite of pre-clinical discovery assays

artículo científico publicado en 2017

Biochemical and Cellular Characterization and Inhibitor Discovery of Pseudomonas aeruginosa 15-Lipoxygenase

artículo científico publicado en 2016

Biochemical assays for the discovery of TDP1 inhibitors

artículo científico publicado en 2014

Cell Lysate-Based AlphaLISA Deubiquitinase Assay Platform for Identification of Small Molecule Inhibitors

artículo científico publicado en 2017

Characterization of chemical libraries for luciferase inhibitory activity

artículo científico publicado en 2008

Chemical Control of a CRISPR-Cas9 Acetyltransferase.

artículo científico publicado en 2018

Complementarity Between a Docking and a High-Throughput Screen in Discovering New Cruzain Inhibitors

artículo científico publicado en 2010

Compound Management for Quantitative High-Throughput Screening

artículo científico publicado en 2008

Compound cytotoxicity profiling using quantitative high-throughput screening

artículo científico publicado en 2008

Comprehensive Mechanistic Analysis of Hits from High-Throughput and Docking Screens against β-Lactamase

artículo científico publicado en 2008

Connecting Neuronal Cell Protective Pathways and Drug Combinations in a Huntington's Disease Model through the Application of Quantitative Systems Pharmacology.

artículo científico publicado en 2017

Correction: A High-Content Assay Enables the Automated Screening and Identification of Small Molecules with Specific ALDH1A1-Inhibitory Activity

artículo científico publicado en 2018

Covalent small molecule inhibitors of Ca(2+)-bound S100B.

artículo científico publicado en 2014

Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH).

artículo científico publicado en 2017

Discovery and lead identification of quinazoline-based BRD4 inhibitors

scientific article published on 31 August 2018

Discovery of NCT-501, a Potent and Selective Theophylline-Based Inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1)

artículo científico publicado en 2015

Discovery of Orally Bioavailable, Quinoline-based Aldehyde Dehydrogenase 1A1 (ALDH1A1) Inhibitors with Potent Cellular Activity.

artículo científico publicado en 2018

Discovery of a 2,4-Diamino-7-aminoalkoxyquinazoline as a Potent and Selective Inhibitor of Histone Lysine Methyltransferase G9a

artículo científico publicado en 2009

Discovery of a novel dual fungal CYP51/human 5-lipoxygenase inhibitor: implications for anti-fungal therapy

artículo científico publicado en 2013

Discovery of a novel general anesthetic chemotype using high-throughput screening

artículo científico publicado en 2015

Discovery of potent and selective inhibitors of human platelet-type 12- lipoxygenase

artículo científico publicado en 2011

Discovery of potent and selective inhibitors of human reticulocyte 15-lipoxygenase-1.

artículo científico publicado en 2010

Disrupting malaria parasite AMA1-RON2 interaction with a small molecule prevents erythrocyte invasion

artículo científico publicado en 2013

Diverse small molecule inhibitors of human apurinic/apyrimidinic endonuclease APE1 identified from a screen of a large public collection

artículo científico publicado en 2012

Drug-based modulation of endogenous stem cells promotes functional remyelination in vivo

artículo científico publicado en 2015

Dual-fluorophore quantitative high-throughput screen for inhibitors of BRCT-phosphoprotein interaction

artículo científico publicado en 2007

Erratum: Quantitative high throughput screening using a primary human three-dimensional organotypic culture predicts in vivo efficacy

artículo científico publicado en 2016

Exploratory analysis of kinetic solubility measurements of a small molecule library

artículo científico publicado en 2011

First Selective 12-LOX Inhibitor, ML355, Impairs Thrombus Formation and Vessel Occlusion In Vivo With Minimal Effects on Hemostasis

artículo científico

Fluorescence polarization assays in high-throughput screening and drug discovery: a review

artículo científico publicado en 2016

Fluorescence spectroscopic profiling of compound libraries

artículo científico publicado en 2008

Fluorescent protein-based cellular assays analyzed by laser-scanning microplate cytometry in 1536-well plate format

artículo científico publicado en 2006

Fragment-Based Discovery of a Regulatory Site in Thioredoxin Glutathione Reductase Acting as “Doorstop” for NADPH Entry

artículo científico publicado en 2018

Genomic and protein expression analysis reveals flap endonuclease 1 (FEN1) as a key biomarker in breast and ovarian cancer

artículo científico publicado en 2014

High-affinity inhibitors of human NAD-dependent 15-hydroxyprostaglandin dehydrogenase: mechanisms of inhibition and structure-activity relationships

artículo científico publicado en 2010

High-throughput 1,536-well fluorescence polarization assays for α(1)-acid glycoprotein and human serum albumin binding

artículo científico publicado en 2012

High-throughput combinatorial screening identifies drugs that cooperate with ibrutinib to kill activated B-cell-like diffuse large B-cell lymphoma cells

artículo científico publicado en 2014

High-throughput identification of promiscuous inhibitors from screening libraries with the use of a thiol-containing fluorescent probe

artículo científico publicado en 2013

High-throughput screen identifies cyclic nucleotide analogs that inhibit prostatic acid phosphatase

artículo científico publicado en 2012

High-throughput screening with nucleosome substrate identifies small-molecule inhibitors of the human histone lysine methyltransferase NSD2

artículo científico publicado en 2018

Highly predictive and interpretable models for PAMPA permeability

artículo científico publicado en 2016

Identification and Optimization of Inhibitors of Trypanosomal Cysteine Proteases: Cruzain, Rhodesain, and TbCatB

artículo científico publicado en 2010

Identification and characterization of inhibitors of human apurinic/apyrimidinic endonuclease APE1

artículo científico publicado en 2009

Identification of Activators of Human Fumarate Hydratase by Quantitative High-Throughput Screening

scientific article published on 14 September 2019

Identification of novel PARP inhibitors using a cell-based TDP1 inhibitory assay in a quantitative high-throughput screening platform

artículo científico publicado en 2014

Identification of phosphotyrosine mimetic inhibitors of human tyrosyl-DNA phosphodiesterase I by a novel AlphaScreen high-throughput assay

artículo científico publicado en 2009

Inhibition of DNA glycosylases via small molecule purine analogs

artículo científico publicado en 2013

Inhibition of thioredoxin reductase 1 by porphyrins and other small molecules identified by a high-throughput screening assay

artículo científico publicado en 2011

Inhibitors of the Menin-Mixed Lineage Leukemia (MLL) Interaction

artículo científico publicado en 2013

Inhibitors of the apurinic/apyrimidinic endonuclease 1 (APE1)/nucleophosmin (NPM1) interaction that display anti-tumor properties

artículo científico publicado en 2015

Insights into the Action of Inhibitor Enantiomers against Histone Lysine Demethylase 5A.

artículo científico publicado en 2018

Integration of pro-inflammatory cytokines, 12-lipoxygenase and NOX-1 in pancreatic islet beta cell dysfunction

artículo científico publicado en 2012

Irreversible inhibition of cytosolic thioredoxin reductase 1 as a mechanistic basis for anticancer therapy

artículo científico publicado en 2018

KDM4/JMJD2 Histone Demethylase Inhibitors Block Prostate Tumor Growth by Suppressing the Expression of AR and BMYB-Regulated Genes

artículo científico publicado en 2015

KDM5 histone demethylases repress immune response via suppression of STING

artículo científico publicado en 2018

Kinetic, Mutational, and Structural Studies of the Venezuelan Equine Encephalitis Virus Nonstructural Protein 2 Cysteine Protease

artículo científico publicado en 2016

Large-Scale Screening and Identification of Novel Ebola Virus and Marburg Virus Entry Inhibitors

artículo científico publicado en 2016

Lecithin:Cholesterol Acyltransferase Activation by Sulfhydryl-Reactive Small Molecules: Role of Cysteine-31.

artículo científico

Microfluidic Mobility Shift Profiling of Lysine Acetyltransferases Enables Screening and Mechanistic Analysis of Cellular Acetylation Inhibitors.

artículo científico publicado en 2015

Molecular basis for activation of lecithin:cholesterol acyltransferase by a compound that increases HDL cholesterol

artículo científico publicado en 2018

NCATS Inxight Drugs: a comprehensive and curated portal for translational research

artículo científico publicado en 2021

Novel Phenotypic Outcomes Identified for a Public Collection of Approved Drugs from a Publicly Accessible Panel of Assays

artículo científico publicado en 2015

Open Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond

artículo científico publicado en 2016

Optimization and validation of two miniaturized glucocerebrosidase enzyme assays for high throughput screening

artículo científico publicado en 2008

Oxadiazole 2-oxides are toxic to the human hookworm, Ancylostoma ceylanicum, however glutathione reductase is not the primary target

artículo científico publicado en 2012

Parallel Chemistry Approach to Identify Novel Nuclear Receptor Ligands Based on the GW0742 Scaffold

artículo científico publicado en 2017

Peroxisome proliferation-activated receptor δ agonist GW0742 interacts weakly with multiple nuclear receptors, including the vitamin D receptor

scientific article published on 10 June 2013

Pharos: Collating protein information to shed light on the druggable genome

artículo científico publicado en 2016

Platelet 12-LOX is essential for FcγRIIa-mediated platelet activation

artículo científico publicado en 2014

Potent and selective inhibitors of human reticulocyte 12/15-lipoxygenase as anti-stroke therapies

artículo científico publicado en 2014

Preparation of FRET reporters to support chemical probe development

artículo científico publicado en 2010

Protein kinase C regulation of 12-lipoxygenase-mediated human platelet activation

artículo científico publicado en 2011

Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines

artículo científico publicado en 2010

Quantitative High-Throughput Screening Identifies 8-Hydroxyquinolines as Cell-Active Histone Demethylase Inhibitors

artículo científico publicado en 2010

Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol protease

artículo científico publicado en 2010

Quantitative high throughput screening using a primary human three-dimensional organotypic culture predicts in vivo efficacy.

artículo científico publicado en 2015

Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing

artículo científico publicado en 2017

Quantitative high-throughput screen identifies inhibitors of the Schistosoma mansoni redox cascade

artículo científico publicado en 2008

Quantitative high-throughput screening identifies cytoprotective molecules that enhance SUMO conjugation via the inhibition of SUMO-specific protease (SENP)2.

artículo científico publicado en 2017

Quantitative high-throughput screening: a titration-based approach that efficiently identifies biological activities in large chemical libraries

artículo científico publicado en 2006

Selective and cell-active inhibitors of the USP1/ UAF1 deubiquitinase complex reverse cisplatin resistance in non-small cell lung cancer cells

artículo científico publicado en 2011

Selective inhibition of 12-lipoxygenase protects islets and beta cells from inflammatory cytokine-mediated beta cell dysfunction

artículo científico publicado en 2014

Sharing and community curation of mass spectrometry data with Global Natural Products Social Molecular Networking

artículo científico publicado en 2016

Streamlined system for purifying and quantifying a diverse library of compounds and the effect of compound concentration measurements on the accurate interpretation of biological assay results

artículo científico publicado en 2004

Structural Basis for KDM5A Histone Lysine Demethylase Inhibition by Diverse Compounds

artículo científico publicado en 2016

Structural insight into exosite binding and discovery of novel exosite inhibitors of botulinum neurotoxin serotype A through in silico screening

artículo científico publicado en 2014

Structure mechanism insights and the role of nitric oxide donation guide the development of oxadiazole-2-oxides as therapeutic agents against schistosomiasis

artículo científico publicado en 2009

Structure-activity relationship studies and biological characterization of human NAD(+)-dependent 15-hydroxyprostaglandin dehydrogenase inhibitors

artículo científico publicado en 2013

Suppression of the FOXM1 transcriptional programme via novel small molecule inhibition

artículo científico publicado en 2014

Synthesis and SAR studies of 5-(pyridin-4-yl)-1,3,4-thiadiazol-2-amine derivatives as potent inhibitors of Bloom helicase

artículo científico publicado en 2013

Synthesis and structure-activity relationship studies of 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives as potent and selective inhibitors of 12-lipoxygenase

artículo científico publicado en 2014

Synthesis and structure-activity relationship studies of N-benzyl-2-phenylpyrimidin-4-amine derivatives as potent USP1/UAF1 deubiquitinase inhibitors with anticancer activity against nonsmall cell lung cancer

artículo científico publicado en 2014

Synthesis, biological evaluation, and structure-activity relationships of a novel class of apurinic/apyrimidinic endonuclease 1 inhibitors

artículo científico publicado en 2012

Targeting human apurinic/apyrimidinic endonuclease 1 (APE1) in phosphatase and tensin homolog (PTEN) deficient melanoma cells for personalized therapy ⬇️

artículo científico publicado en 2014

Targeting the JMJD2 histone demethylases to epigenetically control herpesvirus infection and reactivation from latency

artículo científico publicado en 2013

The NCATS BioPlanet - An Integrated Platform for Exploring the Universe of Cellular Signaling Pathways for Toxicology, Systems Biology, and Chemical Genomics

The NCGC pharmaceutical collection: a comprehensive resource of clinically approved drugs enabling repurposing and chemical genomics

artículo científico publicado en 2011

The pilot phase of the NIH Chemical Genomics Center

artículo científico publicado en 2009

Three classes of glucocerebrosidase inhibitors identified by quantitative high-throughput screening are chaperone leads for Gaucher disease

artículo científico publicado en 2007

Unexplored therapeutic opportunities in the human genome.

artículo científico publicado en 2018

Varied Role of Ubiquitylation in Generating MHC Class I Peptide Ligands.

artículo científico publicado en 2017

Weighted feature significance: a simple, interpretable model of compound toxicity based on the statistical enrichment of structural features

artículo científico publicado en 2009

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