Identification of Ligands for Ion Channels: TRPM2
Sign Up to like & getrecommendations! Published in 2024 at "ChemBioChem"
DOI: 10.1002/cbic.202300790
Abstract: Transient receptor potential melastatin 2 (TRPM2) is a calcium‐permeable, nonselective cation channel with a widespread distribution throughout the body. It is involved in many pathological and physiological processes, making it a potential therapeutic target for… read more here.
Keywords: identification ligands; affinity selection; ion channels; mass ... See more keywords
RNA-ALIS: Methodology for screening soluble RNAs as small molecule targets using ALIS affinity-selection mass spectrometry.
Sign Up to like & getrecommendations! Published in 2019 at "Methods"
DOI: 10.1016/j.ymeth.2019.04.024
Abstract: Recent advances resulting from the completion of the human genome have shown that RNA has the promise to be a target for small molecule drugs, and therefore represents a previously unexploited class of targets for… read more here.
Keywords: affinity selection; methodology; small molecule; selection mass ... See more keywords
Discovery of CD28-Targeted Small Molecule Inhibitors of T Cell Co-Stimulation Using Affinity Selection-Mass Spectrometry (AS-MS) and Ex Vivo Validation.
Sign Up to like & getrecommendations! Published in 2025 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.5c02136
Abstract: CD28 is a key T cell costimulatory receptor implicated in antitumor immunity and immune-related disorders, yet no small molecule modulators of CD28 have reached clinical development. Here, we report the discovery and characterization of small… read more here.
Keywords: cd28; affinity selection; mass spectrometry; small molecule ... See more keywords
Advancing Kir4.2 Channel Ligand Identification through Collision-Induced Affinity Selection Mass Spectrometry
Sign Up to like & getrecommendations! Published in 2024 at "ACS Chemical Biology"
DOI: 10.1021/acschembio.3c00781
Abstract: The inwardly rectifying potassium Kir4.2 channel plays a crucial role in regulating membrane potentials and maintaining potassium homeostasis. Kir4.2 has been implicated in various physiological processes, including insulin secretion, gastric acid regulation, and the pathogenesis… read more here.
Keywords: kir4 channel; affinity selection; collision induced; mass ... See more keywords
Identification of Novel Leishmania donovani Nucleoside Hydrolase Inhibitors from Banisteriopsis laevifolia Using Affinity Selection-Mass Spectrometry
Sign Up to like & getrecommendations! Published in 2025 at "ACS Omega"
DOI: 10.1021/acsomega.5c01613
Abstract: The identification of enzyme inhibitors from natural sources offers a promising pathway for drug discovery. In this study, affinity selection-mass spectrometry (AS-MS) was employed to screen for inhibitors of Leishmania donovani nucleoside hydrolase (LdNH) from… read more here.
Keywords: affinity selection; mass spectrometry; leishmania donovani; nucleoside hydrolase ... See more keywords
Advances in Magnetic Microbead Affinity Selection Screening: Discovery of Natural Ligands to the SARS-CoV-2 Spike Protein.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of the American Society for Mass Spectrometry"
DOI: 10.1021/jasms.1c00318
Abstract: Affinity selection-mass spectrometry, which includes magnetic microbead affinity selection-screening (MagMASS), is ideal for the discovery of ligands in complex mixtures that bind to pharmacological targets. Therapeutic agents are needed to prevent or treat COVID-19, which… read more here.
Keywords: magnetic microbead; protein; sars cov; affinity selection ... See more keywords
Affinity selection–mass spectrometry with linearizable macrocyclic peptide libraries
Sign Up to like & getrecommendations! Published in 2025 at "Science Advances"
DOI: 10.1126/sciadv.adr1018
Abstract: Despite their potential, the preparation of large synthetic macrocyclic libraries for ligand discovery and development has been limited. Here, we produce 100-million-membered macrocyclic libraries containing natural and nonnatural amino acids. Near-quantitative intramolecular disulfide formation is… read more here.
Keywords: macrocyclic libraries; affinity selection; mass spectrometry; affinity ... See more keywords
Robustness of In Vitro Selection Assays of DNA-Encoded Peptidomimetic Ligands to CBX7 and CBX8
Sign Up to like & getrecommendations! Published in 2018 at "SLAS Discovery"
DOI: 10.1177/2472555217750871
Abstract: The identification of protein ligands from a DNA-encoded library is commonly conducted by an affinity selection assay. These assays are often not validated for robustness, raising questions about selections that fail to identify ligands and… read more here.
Keywords: affinity selection; dna encoded; selection assays; selection ... See more keywords
Design and Development of a Technology Platform for DNA-Encoded Library Production and Affinity Selection
Sign Up to like & getrecommendations! Published in 2018 at "SLAS Discovery"
DOI: 10.1177/2472555217752091
Abstract: DNA-encoded libraries (DELs) have emerged as an efficient and cost-effective drug discovery tool for the exploration and screening of very large chemical space using small-molecule collections of unprecedented size. Herein, we report an integrated automation… read more here.
Keywords: affinity selection; production affinity; dna encoded; affinity ... See more keywords
Identification of G-Quadruplex-Binding Inhibitors of Myc Expression through Affinity Selection–Mass Spectrometry
Sign Up to like & getrecommendations! Published in 2019 at "SLAS Discovery"
DOI: 10.1177/2472555218796656
Abstract: The Myc oncogene is overexpressed in many cancers, yet targeting it for cancer therapy has remained elusive. One strategy for inhibition of Myc expression is through stabilization of the G-quadruplex (G4), a G-rich DNA secondary… read more here.
Keywords: affinity selection; selection mass; mass spectrometry; myc expression ... See more keywords