Search Results - "KAZLAUSKAS, Egidijus"
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Standard operating procedure for fluorescent thermal shift assay (FTSA) for determination of protein–ligand binding and protein stability
Published in European biophysics journal (01-05-2021)“…A standard operating procedure for a fluorescence-based thermal shift assay (FTSA) is provided describing its typical applications, advantages and limitations…”
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Improving the Hsp90 Inhibitors Containing 4-(2,4-Dihydroxyphenyl)-1,2,3-thiadiazole Scaffold: Synthesis, Affinity and Effect on Cancer Cells
Published in Anti-cancer agents in medicinal chemistry (24-11-2017)“…Human Hsp90 chaperone inhibitors are known to be potential anticancer drugs. Previously we have shown a couple of…”
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Thermodynamics of aryl-dihydroxyphenyl-thiadiazole binding to human Hsp90
Published in PloS one (24-05-2012)“…The design of specific inhibitors against the Hsp90 chaperone and other enzyme relies on the detailed and correct understanding of both the thermodynamics of…”
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Co-crystalization and in vitro biological characterization of 5-aryl-4-(5-substituted-2-4-dihydroxyphenyl)-1,2,3-thiadiazole Hsp90 inhibitors
Published in PloS one (11-09-2012)“…A potential therapeutic strategy for targeting cancer that has gained much interest is the inhibition of the ATP binding and ATPase activity of the molecular…”
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Correction: Thermodynamics of Aryl-Dihydroxyphenyl-Thiadiazole Binding to Human Hsp90
Published in PloS one (07-06-2012)Get full text
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Binding affinity in drug design: experimental and computational techniques
Published in Expert opinion on drug discovery (03-08-2019)“…: In pharmaceutical design where future drugs are developed by targeting a specific chosen protein, the evaluation of ligand affinity is crucial. For this very…”
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Thermott: A comprehensive online tool for protein–ligand binding constant determination
Published in Drug discovery today (01-08-2022)“…[Display omitted] •An online tool for the protein–compound binding constant from thermal shift data.•Provides estimates of the thermodynamic data on target…”
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Thermal shift assay for protein–ligand dissociation constant determination
Published in TrAC, Trends in analytical chemistry (Regular ed.) (01-01-2024)Get full text
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Comprehensive analysis of resorcinyl-imidazole Hsp90 inhibitor design
Published in European journal of medicinal chemistry (05-07-2024)“…Human Hsp90 chaperones are implicated in various aspects of cancer. Due to this, Hsp90 has been explored as potential target in cancer treatment. Initial…”
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Heat Shock Protein 90 Inhibitor Effects on Pancreatic Cancer Cell Cultures
Published in Pancreas (01-04-2021)“…Pancreatic ductal adenocarcinoma is one of the deadliest cancers for which few curative therapies are available to date. Heat shock protein 90 (Hsp90)…”
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Discovery and Characterization of Novel Selective Inhibitors of Carbonic Anhydrase IX
Published in Journal of medicinal chemistry (26-11-2014)“…Human carbonic anhydrase IX (CA IX) is highly expressed in tumor tissues, and its selective inhibition provides a potential target for the treatment of…”
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Interaction of the middle domains stabilizes Hsp90α dimer in a closed conformation with high affinity for p23
Published in Biological chemistry (28-03-2018)“…The human genome encodes two highly similar cytosolic Hsp90 proteins called isoforms Hsp90α and Hsp90β. Of the 300 client proteins for Hsp90 identified so far…”
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5-Aryl-4-(5-substituted-2,4-dihydroxyphenyl)-1,2,3-thiadiazoles as inhibitors of Hsp90 chaperone
Published in Bioorganic & medicinal chemistry letters (15-02-2009)“…The synthesis and in vitro binding of the thiadiazole inhibitors of Hsp90 with K ds up to 5 nM. A series of…”
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PLBD: protein–ligand binding database of thermodynamic and kinetic intrinsic parameters
Published in Database : the journal of biological databases and curation (08-06-2023)“…Abstract We introduce a protein–ligand binding database (PLBD) that presents thermodynamic and kinetic data of reversible protein interactions with small…”
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Co-Crystalization and In Vitro Biological Characterization of 5-Aryl-4
Published in PloS one (11-09-2012)“…A potential therapeutic strategy for targeting cancer that has gained much interest is the inhibition of the ATP binding and ATPase activity of the molecular…”
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Hsp90 stabilizes Cdc25A and counteracts heat shock-mediated Cdc25A degradation and cell-cycle attenuation in pancreatic carcinoma cells
Published in Human molecular genetics (01-11-2012)“…Pancreas cancer cells escape most treatment options. Heat shock protein (Hsp)90 is frequently over-expressed in pancreas carcinomas and protects a number of…”
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