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Fragment Ligands of the m6A-RNA Reader YTHDF2.

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Nai F, Nachawati R, Zálešák F, Wang X, Li Y, Caflisch A
OpenAccess logo ACS Med Chem Lett 13 1500-1509 (2022)
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Cited: 3 times
EuropePMC logo PMID: 36110386

Abstract

We report 17 small-molecule ligands that compete with N6-methyladenosine (m6A) for binding to the m6A-reader domain of YTHDF2 (YT521-B homology domain family 2). We determined their binding mode at high resolution by X-ray crystallography and quantified their affinity by a fluorescence-based binding assay. 6-Cyclopropyluracil and a pyrazolopyrimidine derivative have favorable ligand efficiencies of 0.47 and 0.38 kcal mol-1 per non-hydrogen atom, respectively. They represent useful starting points for hit optimization.

Reviews citing this publication (1)

  1. Characterization of epitranscriptome reader proteins experimentally and in silico: Current knowledge and future perspectives beyond the YTH domain. Miller LG, Demny M, Tamamis P, Contreras LM. Comput Struct Biotechnol J 21 3541-3556 (2023)

Articles citing this publication (2)

  1. Small-Molecule Ebselen Binds to YTHDF Proteins Interfering with the Recognition of N 6-Methyladenosine-Modified RNAs. Micaelli M, Dalle Vedove A, Cerofolini L, Vigna J, Sighel D, Zaccara S, Bonomo I, Poulentzas G, Rosatti EF, Cazzanelli G, Alunno L, Belli R, Peroni D, Dassi E, Murakami S, Jaffrey SR, Fragai M, Mancini I, Lolli G, Quattrone A, Provenzani A. ACS Pharmacol Transl Sci 5 872-891 (2022)
  2. Exploring the brain epitranscriptome: perspectives from the NSAS summit. Lee SM, Koo B, Carré C, Fischer A, He C, Kumar A, Liu K, Meyer KD, Ming GL, Peng J, Roignant JY, Storkebaum E, Sun S, De Pietri Tonelli D, Wang Y, Weng YL, Pulvirenti L, Shi Y, Yoon KJ, Song H. Front Neurosci 17 1291446 (2023)


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