Cargando…

Substrate-Free High-Throughput Screening Identifies Selective Inhibitors for Uncharacterized Enzymes

Target-based high-throughput screening (HTS) is essential for the discovery of small-molecule modulators of proteins. Typical screening methods for enzymes rely on extensively tailored substrate assays, which are not available for targets of poorly characterized biochemical activity. Here, we report...

Descripción completa

Detalles Bibliográficos
Autores principales:	Bachovchin, Daniel A., Brown, Steven J., Rosen, Hugh, Cravatt, Benjamin F.
Formato:	Texto
Lenguaje:	English
Publicado:	2009
Materias:	Article
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2709489/ https://www.ncbi.nlm.nih.gov/pubmed/19329999 http://dx.doi.org/10.1038/nbt.1531

Ejemplares similares

A high-throughput genetic screen identifies previously uncharacterized Borrelia burgdorferi genes important for resistance against reactive oxygen and nitrogen species
por: Ramsey, Meghan E., et al.
Publicado: (2017)

Mass spectrometry imaging–based assays for aminotransferase activity reveal a broad substrate spectrum for a previously uncharacterized enzyme
por: de Raad, Markus, et al.
Publicado: (2023)

High-throughput gene and SNP discovery in Eucalyptus grandis, an uncharacterized genome
por: Novaes, Evandro, et al.
Publicado: (2008)

Selective Irreversible Inhibitors of the Wnt-Deacylating Enzyme NOTUM Developed by Activity-Based Protein Profiling
por: Suciu, Radu M., et al.
Publicado: (2018)

Multicomponent mapping of boron chemotypes furnishes selective enzyme inhibitors
por: Tan, Joanne, et al.
Publicado: (2017)

Turnover number predictions for kinetically uncharacterized enzymes using machine and deep learning
por: Kroll, Alexander, et al.
Publicado: (2023)

A diversity of uncharacterized reverse transcriptases in bacteria
por: Simon, Dawn M., et al.
Publicado: (2008)

Ultrafast end-to-end protein structure prediction enables high-throughput exploration of uncharacterized proteins
por: Kandathil, Shaun M., et al.
Publicado: (2022)

High Throughput Screening and Selection Methods for Directed Enzyme Evolution
por: Xiao, Han, et al.
Publicado: (2014)

Computational Identification of Uncharacterized Cruzain Binding Sites
por: Durrant, Jacob D., et al.
Publicado: (2010)

High-Throughput Screening Identifies Inhibitors of the SARS Coronavirus Main Proteinase
por: Blanchard, Jan E., et al.
Publicado: (2004)

High-Throughput Functional Screening of Steroid Substrates with Wild-Type and Chimeric P450 Enzymes
por: Urban, Philippe, et al.
Publicado: (2014)

Substrate-selective inhibitors that reprogram the activity of insulin-degrading enzyme
por: Maianti, Juan Pablo, et al.
Publicado: (2019)

Proteomic and evolutionary analyses of sperm activation identify uncharacterized genes in Caenorhabditis nematodes
por: Kasimatis, Katja R., et al.
Publicado: (2018)

A high-throughput, multiplexed assay for superfamily-wide profiling of enzyme activity
por: Bachovchin, Daniel A., et al.
Publicado: (2014)

Classifying the metal dependence of uncharacterized nitrogenases
por: McGlynn, Shawn E., et al.
Publicado: (2013)

Annotation and curation of uncharacterized proteins- challenges
por: Ijaq, Johny, et al.
Publicado: (2015)

Bioactivity descriptors for uncharacterized chemical compounds
por: Bertoni, Martino, et al.
Publicado: (2021)

The extensive and functionally uncharacterized mitochondrial phosphoproteome
por: Niemi, Natalie M., et al.
Publicado: (2021)

Editorial: Characterizing the uncharacterized human proteins
por: Xu, Yan-Ming, et al.
Publicado: (2023)

Click-generated triazole ureas as ultrapotent, in vivo-active serine hydrolase inhibitors
por: Adibekian, Alexander, et al.
Publicado: (2011)

High throughput screening identifies modulators of histone deacetylase inhibitors
por: Gaupel, Ann-Christin, et al.
Publicado: (2014)

High-throughput Screening of Carbohydrate-degrading Enzymes Using Novel Insoluble Chromogenic Substrate Assay Kits
por: Schückel, Julia, et al.
Publicado: (2016)

Discovery of an enzyme and substrate selective inhibitor of ADAM10 using an exosite-binding glycosylated substrate
por: Madoux, Franck, et al.
Publicado: (2016)

Versatile O-GlcNAc Transferase Assay for High-Throughput Identification of Enzyme Variants, Substrates, and Inhibitors
por: Kim, Eun J., et al.
Publicado: (2014)

A High Throughput Screen Identifies Potent and Selective Inhibitors to Human Epithelial 15-Lipoxygenase-2
por: Jameson, J. Brian, et al.
Publicado: (2014)

Droplet Electrospray Ionization Mass Spectrometry for High Throughput Screening for Enzyme Inhibitors
por: Sun, Shuwen, et al.
Publicado: (2014)

Disease gene prediction for molecularly uncharacterized diseases
por: Cáceres, Juan J., et al.
Publicado: (2019)

Bleeding risks for uncharacterized platelet function disorders
por: Brunet, Justin, et al.
Publicado: (2020)

Bacteriophages: Uncharacterized and Dynamic Regulators of the Immune System
por: Sinha, Anshul, et al.
Publicado: (2019)

Evolutional insights on uncharacterized SARS coronavirus genes
por: Inberg, Alex, et al.
Publicado: (2004)

Structure-based substrate screening for an enzyme
por: Xu, Tao, et al.
Publicado: (2009)

High-Throughput Screening Methodology to Identify Alpha-Synuclein Aggregation Inhibitors
por: Pujols, Jordi, et al.
Publicado: (2017)

High-Throughput Screening to Identify Inhibitors of Plasmodium falciparum Importin α
por: Walunj, Sujata B., et al.
Publicado: (2022)

An in silico high-throughput screen identifies potential selective inhibitors for the non-receptor tyrosine kinase Pyk2
por: Meirson, Tomer, et al.
Publicado: (2017)

High-Throughput Virtual Screening, Molecular Dynamics Simulation, and Enzyme Kinetics Identified ZINC84525623 as a Potential Inhibitor of NDM-1
por: Rehman, Md Tabish, et al.
Publicado: (2019)

High throughput screening of hydrolytic enzymes from termites using a natural substrate derived from sugarcane bagasse
por: Lucena, Severino A, et al.
Publicado: (2011)

Identification of Selective CYP3A7 and CYP3A4 Substrates and Inhibitors Using a High-Throughput Screening Platform
por: Kabir, Md, et al.
Publicado: (2022)

Predicted Roles of the Uncharacterized Clustered Genes in Aflatoxin Biosynthesis
por: Ehrlich, Kenneth C.
Publicado: (2009)

Identification and prioritization of novel uncharacterized peptidases for biochemical characterization
por: Rawlings, Neil D.
Publicado: (2013)

Cannot write session to /tmp/vufind_sessions/sess_895qbb276rbptig9tlnhahn7of