Search Results - "L. M. Viranga Tillekeratne"
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Cofilin Inhibitor Improves Neurological and Cognitive Functions after Intracerebral Hemorrhage by Suppressing Endoplasmic Reticulum Stress Related-Neuroinflammation
Published in Pharmaceuticals (Basel, Switzerland) (01-01-2024)“…Neuroinflammation after intracerebral hemorrhage (ICH) is a crucial factor that determines the extent of the injury. Cofilin is a cytoskeleton-associated…”
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2
Tumor suppressor p53 promotes ferroptosis in oxidative stress conditions independent of modulation of ferroptosis by p21, CDKs, RB, and E2F
Published in The Journal of biological chemistry (01-12-2021)“…p53 is a well-established critical cell cycle regulator. By inducing transcription of the gene encoding p21, p53 inhibits cyclin-dependent kinase…”
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3
Photoaffinity labeling and bioorthogonal ligation: Two critical tools for designing “Fish Hooks” to scout for target proteins
Published in Bioorganic & medicinal chemistry (15-05-2022)“…[Display omitted] Small molecules remain an important category of therapeutic agents. Their binding to different proteins can lead to both desired and…”
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4
Identification and initial characterization of a potent inhibitor of ferroptosis
Published in Journal of cellular biochemistry (01-04-2021)“…Ferroptosis is a form of iron‐dependent cell death characterized by elevated lipid peroxides and reactive oxygen species (ROS). Glutathione (GSH) plays an…”
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Small-Molecule Ferroptotic Agents with Potential to Selectively Target Cancer Stem Cells
Published in Scientific reports (11-04-2019)“…Effective management of advanced cancer requires systemic treatment including small molecules that target unique features of aggressive tumor cells. At the…”
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Rational design of metabolically stable HDAC inhibitors: An overhaul of trifluoromethyl ketones
Published in European journal of medicinal chemistry (15-12-2022)“…Epigenetic regulation of gene expression using histone deacetylase (HDAC) inhibitors is a promising strategy for developing new anticancer agents. The most…”
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7
Mutant p53 reactivators protect breast cancer cells from ferroptosis
Published in Cell biochemistry and function (01-06-2024)“…Ferroptosis is a novel nonapoptotic form of cell death characterized by iron‐dependent reactive oxygen species‐mediated lipid peroxidation. In several…”
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Electrochemical detection of acetylcholine and choline: application to the quantitative nonradiochemical evaluation of choline transport
Published in Analytical and bioanalytical chemistry (01-10-2008)“…The development of analytical methods for determining the cholinergic biomarkers acetylcholine (ACh) and choline (Ch) is important for assessing their role in…”
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Pharmacophore optimization of imidazole chalcones to modulate microtubule dynamics
Published in Bioorganic chemistry (01-05-2022)“…[Display omitted] •Structure-activity relationship of imidazole chalcone mimics.•Cytotoxic with IC50 values in the upper nanomolar to low micromolar…”
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Largazole Analogues Embodying Radical Changes in the Depsipeptide Ring: Development of a More Selective and Highly Potent Analogue
Published in Journal of medicinal chemistry (08-12-2016)“…A number of analogues of the marine-derived histone deacetylase inhibitor largazole incorporating major structural changes in the depsipeptide ring were…”
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A new class of cytotoxic agents targets tubulin and disrupts microtubule dynamics
Published in Bioorganic chemistry (01-11-2021)“…[Display omitted] •Synthesis of chalcone mimics containing an imidazole-based metal-binding group intended for HDAC inhibition.•Compounds showed cytotoxicity…”
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Largazole, a class I histone deacetylase inhibitor, enhances TNF-α-induced ICAM-1 and VCAM-1 expression in rheumatoid arthritis synovial fibroblasts
Published in Toxicology and applied pharmacology (15-07-2013)“…In the present study, we evaluated the effect of largazole (LAR), a marine-derived class I HDAC inhibitor, on tumor necrosis factor-α (TNF-α)-induced…”
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Electrochemical and Electrocatalytic Properties of Imidazole Analogues of the Redox Cofactor Pyrroloquinoline Quinone
Published in Electroanalysis (New York, N.Y.) (01-10-2008)“…The electrochemical and electrocatalytic properties of two synthetic imidazole analogues of the redox cofactor pyrroloquinoline quinone (PQQ) were evaluated…”
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14
Small-molecule anticancer agents kill cancer cells by harnessing reactive oxygen species in an iron-dependent manner
Published in Organic & biomolecular chemistry (28-02-2018)“…In the course of generating a library of open-chain epothilones, we discovered a new class of small molecule anticancer agents that has no effect on tubulin…”
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15
Potential SARS-CoV-2 main protease inhibitors
Published in Drug discovery today (01-03-2021)“…[Display omitted] •The SARS-CoV-2 main protease is a prime drug target.•Coronavirus main proteases share a structurally conserved substrate-binding region.•The…”
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Synthesis and biological evaluation of largazole analogues with modified surface recognition cap groups
Published in European journal of medicinal chemistry (30-10-2014)“…Several largazole analogues with modified surface recognition cap groups were synthesized and their HDAC inhibitory activities were determined. The C7-epimer…”
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17
Inhibition of choline transport by redox-active cholinomimetic bis-catechol reagents
Published in Bioorganic & medicinal chemistry (15-11-2007)“…Two symmetrical bis-catechol substituted hexamethonium and decamethonium analogues were found to inhibit high-affinity choline transport in mouse brain…”
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Tunable Cysteine-Targeting Electrophilic Heteroaromatic Warheads Induce Ferroptosis
Published in Journal of medicinal chemistry (08-09-2022)“…Once considered potential liabilities, the modern era witnesses a renaissance of interest in covalent inhibitors in drug discovery. The available toolbox of…”
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Synthesis and characterization of luminescent cadmium selenide/zinc selenide/zinc sulfide cholinomimetic quantum dots
Published in Nanoscale (07-08-2012)“…Luminescent quantum dots conjugated with highly selective molecular recognition ligands are widely used for targeting and imaging biological structures. In…”
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In Situ Self Assembly of Thiolated ortho-Quinone Capped Electrocatalysts for Bioanalytical Applications
Published in Electroanalysis (New York, N.Y.) (01-10-2011)“…Thiolated o‐quinone‐capped electrocatalysts modeled on the naturally occurring o‐quinone cofactor pyrroloquinoline quinone (PQQ) were designed and synthesized…”
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