Search Results - "Endri, Karaj"

Tunable Cysteine-Targeting Electrophilic Heteroaromatic Warheads Induce Ferroptosis by Karaj, Endri, Sindi, Shaimaa H., Kuganesan, Nishanth, Perera, Lalith, Taylor, William, Tillekeratne, L. M. Viranga

“…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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Tunable Cysteine-Targeting Electrophilic Hetero-Aromatic Warheads Induce Ferroptosis by Karaj, Endri, Sindi, Shaimaa H., Kuganesan, Nishanth, Perera, Lalith, Taylor, William, Viranga Tillekeratne, L. M.

“…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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Medicinal & Chemical Biology Investigation of Ferroptosis Inducers & HDAC Inhibitors by Karaj, Endri

“…According to the Centers for Disease Control and Prevention (CDC), cancer is the second leading cause of death in the United states, where in 2019, 1,752,735…”
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Photoaffinity labeling and bioorthogonal ligation: Two critical tools for designing “Fish Hooks” to scout for target proteins by Karaj, Endri, Sindi, Shaimaa H., Viranga Tillekeratne, L.M.

“…[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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CETZOLE Analogs as Potent Ferroptosis Inducers and Their Target Identification Using Covalent/Affinity Probes by Dlamini, Samkeliso, Mohajeri, Shahrzad, Kuganesan, Nishanth, Sindi, Shaimaa H., Karaj, Endri, Rathnayake, Dewmi S., McDaniel, Jade, Taylor, William R., Tillekeratne, L. M. Viranga

“…Ferroptosis is a recently discovered cell death mechanism triggered by iron-dependent elevation of reactive oxygen species leading to lipid membrane…”
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Leveraging multi-mode microextraction and liquid chromatography stationary phases for quantitative analysis of neurotoxin β-N-methylamino-L-alanine and other non-proteinogenic amino acids by Emmons, Ronald V., Karaj, Endri, Cudjoe, Erasmus, Bell, David S., Tillekeratne, L.M. Viranga, Gionfriddo, Emanuela

“…•Fluorophenyl columns enable separation of underivatized amino acids in as fast as 8 min.•Baseline separation of BMAA and its isomers is achievable without…”
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First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids by Karaj, Endri, Sindi, Shaimaa H., Kuganesan, Nishanth, Koranne, Radhika A., Knoff, Joseph R., James, Antonisamy William, Fu, Yu, Kotsull, Lauren N., Pflum, Mary Kay, Shah, Zahoor, Taylor, William R., Tillekeratne, L. M. Viranga

“…HDAC inhibitors are an attractive class of cytotoxic agents for the design of hybrid molecules. Several HDAC hybrids have emerged over the years, but none…”
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Rational design of metabolically stable HDAC inhibitors: An overhaul of trifluoromethyl ketones by Riddhidev, Banerjee, Endri, Karaj, Sabitri, Lamichhane, Kotsull, Lauren, N., Nishanth, Kuganesan, Dragan, Isailovic, Mary Kay H, Pflum, James, Slama, William, Taylor, L. M. Viranga, Tillekeratne

“…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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The structural simplification of lysergic acid as a natural lead for synthesizing novel anti-Alzheimer agents by Alzweiri, Muhammed, S. Alsegiani, Amsha, Karaj, Endri, A. Almarghalani, Daniyah, Tabaza, Yahia, A. Shah, Zahoor, Tillekeratne, L.M. Viranga

“…[Display omitted] Alzheimer’s disease (AD) is a neurodegenerative disorder, projected to be the second leading cause of mortality by 2040. AD is characterized…”
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Pharmacophore optimization of imidazole chalcones to modulate microtubule dynamics by Karaj, Endri, Dlamini, Samkeliso, Koranne, Radhika, Sindi, Shaimaa H., Perera, Lalith, Taylor, William R., Viranga Tillekeratne, L.M.

“…[Display omitted] •Structure-activity relationship of imidazole chalcone mimics.•Cytotoxic with IC50 values in the upper nanomolar to low micromolar…”
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A new class of cytotoxic agents targets tubulin and disrupts microtubule dynamics by Al-Hamashi, Ayad A., Koranne, Radhika, Dlamini, Samkeliso, Alqahtani, Abdulateef, Karaj, Endri, Rashid, Maisha S., Knoff, Joseph R., Dunworth, Matthew, Pflum, Mary Kay H., Casero, Robert A., Perera, Lalith, Taylor, William R., Tillekeratne, L.M. Viranga

“…[Display omitted] •Synthesis of chalcone mimics containing an imidazole-based metal-binding group intended for HDAC inhibition.•Compounds showed cytotoxicity…”
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